The objective of the investigation was to optimize the iontophoresis process parameters of lisinopril (LSP) by 3 x 3 factorial design, Box-Behnken statistical design. LSP is an ideal candidate for iontophoretic delivery to avoid the... more
The objective of the investigation was to optimize the iontophoresis process parameters of lisinopril (LSP) by 3 x 3 factorial design, Box-Behnken statistical design. LSP is an ideal candidate for iontophoretic delivery to avoid the incomplete absorption problem associated after its oral administration. Independent variables selected were current (X(1)), salt (sodium chloride) concentration (X(2)) and medium/pH (X(3)). The dependent variables studied were amount of LSP permeated in 4 h (Y(1): Q(4)), 24 h (Y(2): Q(24)) and lag time (Y(3)). Mathematical equations and response surface plots were used to relate the dependent and independent variables. The regression equation generated for the iontophoretic permeation was Y(1) = 1.98 + 1.23X(1) - 0.49X(2) + 0.025X(3) - 0.49X(1)X(2) + 0.040X(1)X(3) - 0.010X(2)X(3) + 0.58X(1)(2) - 0.17X(2)(2) - 0.18X(3)(2); Y(2) = 7.28 + 3.32X(1) - 1.52X(2) + 0.22X(3) - 1.30X(1)X(2) + 0.49X(1)X(3) - 0.090X(2)X(3) + 0.79X(1)(2) - 0.62X(2)(2) - 0.33X(3)(2) and Y(3) = 0.60 + 0.0038X(1) + 0.12X(2) - 0.011X(3) + 0.005X(1)X(2) - 0.018X(1)X(3) - 0.015X(2)X(3) - 0.00075X(1)(2) + 0.017X(2)(2) - 0.11X(3)(2). The statistical validity of the polynomials was established and optimized process parameters were selected by feasibility and grid search. Validation of the optimization study with 8 confirmatory runs indicated high degree of prognostic ability of response surface methodology. The use of Box-Behnken design approach helped in identifying the critical process parameters in the iontophoretic delivery of lisinopril.
Research Interests: Chemistry, Design, Response Surface Methodology, Medicine, Optimization, and 15 moreConception, Process, Permeability, Pharmaceutical, Animals, Factorial Design, Regression Analysis, Iontophoresis, Rats, Time Factors, Sodium Chloride, Angiotensin Converting Enzyme Inhibitors, Lisinopril, Skin Absorption, and Pharmacology and pharmaceutical sciences
The aim of the investigation was to develop and evaluate buccoadhesive tablets of diltiazem hydrochloride (DZH) using hydroxypropyl methyl cellulose (HPMC) K4M and Carbopol 934 as mucoadhesive polymers. Formulations A1, A2, A3, A4, and... more
The aim of the investigation was to develop and evaluate buccoadhesive tablets of diltiazem hydrochloride (DZH) using hydroxypropyl methyl cellulose (HPMC) K4M and Carbopol 934 as mucoadhesive polymers. Formulations A1, A2, A3, A4, and B1, B2, and B3, were composed of HPMC K4M and Carbopol 934 at ratios of 1:2, 1:3, 1:4, 1:5, and 1:1, 1:2, 1:3, respectively. The developed formulations were evaluated for physicochemical, in vitro drug release, in vitro adhesion and in vivo studies in healthy human volunteers. The buccal absorption study in healthy volunteers revealed that about 36.86% of the drug was absorbed. Formulation A3 showed maximum release in 8 h. As the concentration of polymer in the formulation increased, the drug release decreased. The bioavailability of diltiazem from buccoadhesive tablets was 1.57-fold higher than oral tablets. The basic pharmacokinetic parameters, C(Max), T(Max), and the area under the curve, were calculated and showed statistically significant difference (P < 0.05) when the drug was given by the buccal route compared to that of oral tablet. The results indicate that suitable bioadhesive buccal tablets with improved bioavailability could be prepared.
Research Interests: Pharmacology, Chemistry, Pharmacokinetics, Medicine, Humans, and 15 morePubmed, Animals, Male, Absorption, Bioavailability, In Vivo, Adult, Mouth mucosa, Drug Carriers, Biological Availability, Area Under Curve, Calcium Channel Blockers, Methylcellulose, Pharmacology and pharmaceutical sciences, and Cmax
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ABSTRACT A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of lacidipine (LCDP) in rabbit serum was developed and validated. LCDP and internal standard (IS), felodipine were extracted into... more
ABSTRACT A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of lacidipine (LCDP) in rabbit serum was developed and validated. LCDP and internal standard (IS), felodipine were extracted into n-hexane and dichloromethane (70:30) solvent system and separated using an isocratic mobile phase, on an Inertsil C18 column. The effluent was monitored by UV detector at 240 nm and at a flow rate of 1.0 mL min(-1). The linearity range of proposed method was 1-500 ng mL(-1). The intra-day and inter-day coefficient of variation and percent error values of the assay method were less than 15% and mean recovery was more than 94 and 95% for LCDP and IS, respectively and the method was found to be precise, accurate, and specific during the study. The method was successfully applied for pharmacokinetic study of lacidipine after application of LCDP microemulsion gel in rabbits.
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Research Interests: Mathematics, Response Surface Methodology, Medicine, Animals, Drug Design, and 15 moreResearch article, Skin, Bioavailability, Hydroxypropyl Methylcellulose, Rats, AAPS PharmSciTech, Drug Carriers, Propylene Glycol, Response surface, Box-Behnken Design, Cumulant, Transdermal, Skin Absorption, buspirone , and Pharmacology and pharmaceutical sciences
... of Physicochemical, in vitro, ex vivo and Mechanical Properties Ramesh Gannu, Adukondalu Devandla, Madhav Burra and Madhusudan Rao Yamsani ... ethyl cellulose and poly vinyl pyorrolidone 30 K were obtained as gift samples from Dr... more
... of Physicochemical, in vitro, ex vivo and Mechanical Properties Ramesh Gannu, Adukondalu Devandla, Madhav Burra and Madhusudan Rao Yamsani ... ethyl cellulose and poly vinyl pyorrolidone 30 K were obtained as gift samples from Dr Reddy&amp;#x27;s Laboratories, Hyderabad ...
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A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of buspirone (BUSP) in rabbit serum was developed and validated. BUSP and internal standard (IS), diltiazem hydrochloride were extracted into... more
A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of buspirone (BUSP) in rabbit serum was developed and validated. BUSP and internal standard (IS), diltiazem hydrochloride were extracted into dichloromethane and separated using an isocratic mobile phase, on a Kromasil C(8) column. The eluent was monitored by UV detector at 235 nm and at a flow rate of 1.0 mL min(-1). The linearity range of proposed method was 1-3000 ng mL(-1). The intra-day and inter-day coefficient of variation and percent error values of the assay method were less than 15% and mean recovery was more than 97 and 96% for BUSP and IS, respectively. The method was found to be precise, accurate, and specific during the study. The method was successfully applied for pharmacokinetic study of buspirone after application of reservoir based transdermal therapeutic system of BUSP to rabbits.
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The current work aims to study the effect of Aloe vera juice on skin permeation of drugs with diverse molecular weight and lipophilicity. Saturated solutions of lisinopril, diclofenac sodium and lacidipine in Aloe vera juice and water or... more
The current work aims to study the effect of Aloe vera juice on skin permeation of drugs with diverse molecular weight and lipophilicity. Saturated solutions of lisinopril, diclofenac sodium and lacidipine in Aloe vera juice and water or water containing 40% v/v polyethylene glycol 400 (control) were used to dose rat abdominal skin mounted in Franz diffusion cells. No significant difference (p>0.05) was observed in solubilities of drugs investigated in aloe juice and control. The Aloe vera juice showed significant (p<0.05) improvement in the permeation of drugs. The flux of lisinopril, diclofenac sodium and lacidipine in Aloe vera juice was increased, respectively, 1.11, 1.11 and 1.93 times than the respective control. The penetration enhancement order was lisinopril < diclofenac sodium < lacidipine. Enhancement potential was dependent upon the molecular weight and lipophilicities of the drug in formulation, with the enhancement effect attributable to as yet unidentified components within the Aloe vera. These results demonstrated that the Aloe vera juice have penetration enhancement effect on skin permeation of drugs studied.
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The main objective of the present research work was to design, optimize and characterize olanzapine loaded nano-emulsion for improved brain transport of the drug. Olanzapine nano-emulsion was formulated using the ultrasonication method.... more
The main objective of the present research work was to design, optimize and characterize olanzapine loaded nano-emulsion for improved brain transport of the drug. Olanzapine nano-emulsion was formulated using the ultrasonication method. The formulation variables (oil and surfactant) and process variables (ultrasonication time) were optimized by Response surface methodology using the Box-Behnken statistical method. Particle size, polydispersity index (PDI) and zeta potential were measured by photon correlation spectroscopy using a Malvern zeta sizer. Morphology of emulsion droplets was examined by transmission electron microscopy (TEM). Release study was performed and drug release was estimated by HPLC method. Stability studies were performed at 4oC-25oC for a period of three months. The optimized nano-emulsion obtained showed a uniform size distribution with an average size in the range of 65.1 nm to 74.21 nm and surface charge in the range of –18.9 mv to – 25.23 mv. The Transmiss...
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Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were... more
Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 ± 0.4%) with the Higuchi model release profile and permeated 21.5 ± 2.9% of the drug (flux 8.35 ± 0.291 µg h1cm2) permeation coefficient 1.34 ± 0.05 cm h1) through porcine buccal membrane. BC3 formulation showed 1.62 ± 0.15 N of peak detachment force and 0.24 ± 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalli...
Monolithic matrix-type transdermal drug delivery systems for carvedilol were prepared using a film casting technique involving hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), Eudragit RS 100 (ERS 100), and Eudragit RL... more
Monolithic matrix-type transdermal drug delivery systems for carvedilol were prepared using a film casting technique involving hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), Eudragit RS 100 (ERS 100), and Eudragit RL 100 (ERL 100) as matrix-forming polymers. The prepared transdermal drug delivery systems were extensively evaluated for in vitro release, ex vivo permeation through rat abdominal skin, moisture absorption, moisture content, water vapor transmission, stability, and mechanical properties. Formulations F2, F3, and F5 were composed of a 4:1 ratio of HPMC, ERS 100; HPMC, HPC; and HPMC, ERL 100, respectively, whereas F4, F6, and F7 were composed of 3:0.5:0.5 of HPMC, ERS 100, HPC; HPMC, HPC, ERL 100; and HPMC, ERS 100, ERL 100. Formulation F1 was composed of HPMC polymer. All formulations carried 8% v/w of d-limonene as a penetration enhancer and 20% v/w of dibutylphthalate as a plasticizer. The physicochemical interaction between carvedilol and polymers...
Research Interests: Materials Science, Medicine, Polymer, Differential scanning calorimetry, Permeability, and 13 moreAnimals, Drug Delivery Systems, Skin, Solubility, Rats, Fourier transform infrared spectroscopy, Plasticizer, Permeation, Tensile Strength, Drug Stability, Volatilization, Transdermal, and Pharmacology and pharmaceutical sciences
Domperidone (DOM) is a dopamine- receptor (D(2)) antagonist, widely used in the treatment of motion-sickness. The pharmacokinetic parameters of DOM make it a suitable candidate for development of Solid Lipid Nanoparticle (SLN) and... more
Domperidone (DOM) is a dopamine- receptor (D(2)) antagonist, widely used in the treatment of motion-sickness. The pharmacokinetic parameters of DOM make it a suitable candidate for development of Solid Lipid Nanoparticle (SLN) and Nanostructured Lipide Carrier (NLC). The purpose of the present investigation was to prepare and evaluate DOM loaded solid lipid nanoparticles (DOM-SLN) and DOM loaded nanostructured lipid carriers (DOM-NLC). DOM loaded SLN and NLC were prepared by hot homogenization followed by ultrasonication technique, using trimyristin as solid lipid, cetyl recinoleate as liquid lipid and a mixture of soy phosphatidylcholine (99%) and tween 80 as surfactant. SLN and NLC were characterized for particle size, polydispersity index (PDI), zeta potential and entrapment efficiency. The effects of composition of lipid materials and surfactant mixture on the particle size, PDI, zeta potential, drug entrapment efficiency, and in vitro drug release behavior were investigated. DS...
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Domperidone (DOM) is a dopamine- receptor (D(2)) antagonist, which is widely used in the treatment of motion-sickness. The pharmacokinetic parameters make DOM a suitable candidate for transdermal delivery. The purpose of the present... more
Domperidone (DOM) is a dopamine- receptor (D(2)) antagonist, which is widely used in the treatment of motion-sickness. The pharmacokinetic parameters make DOM a suitable candidate for transdermal delivery. The purpose of the present investigation was to develop transdermal delivery systems for DOM and to evaluate their physicochemical characteristics, in vitro release an ex vivo permeation through rat abdominal skin and their mechanical properties. Bilayered matrix type transdermal drug delivery systems (TDDS) of DOM were prepared by film casting technique using hydroxypropyl methyl cellulose as primary and Eudragit RL 100 as secondary layers. Brij-35 was incorporated as a solubilizer, d-limonene and propylene glycol were employed as permeation enhancer and plasticizer respectively. The prepared TDDS were extensively evaluated for in vitro release, moisture absorption, moisture content, water vapor transmission, ex vivo permeation through rat abdominal skin, mechanical properties an...
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The purpose of the investigation was to develop and evaluate matrix-type transdermal drug delivery systems (TDDSs) of trandolapril. Matrix-type TDDSs of trandolapril were prepared by solvent evaporation technique. Eight formulations... more
The purpose of the investigation was to develop and evaluate matrix-type transdermal drug delivery systems (TDDSs) of trandolapril. Matrix-type TDDSs of trandolapril were prepared by solvent evaporation technique. Eight formulations (composed of Eudragit RL 100 and Hydroxypropyl methyl cellulose 15 cps at a ratios of 2:8, 4:6, 6:4, 8:2 in formulations A1, A2, A3, A4; and Eudragit RS 100 and Hydroxypropyl methyl cellulose 15 cps in the same ratios in formulations B1, B2, B3, B4, respectively) were prepared. All formulations contained 5% w/w menthol as penetration enhancer and 15% w/w propylene glycol as plasticizer in ethanol as solvent. The prepared TDDSs were evaluated for physicochemical characteristics, in vitro release and ex vivo permeation. The physicochemical interactions between trandolapril and polymers were investigated by Fourier transform infrared spectroscopy. The results suggested that there is no physicochemical interaction between drug and polymers. The maximum drug ...
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The aim of the investigation was to develop and evaluate buccoadhesive tablets of diltiazem hydrochloride (DZH) using hydroxypropyl methyl cellulose (HPMC) K4M and Carbopol 934 as mucoadhesive polymers. Formulations A1, A2, A3, A4, and... more
The aim of the investigation was to develop and evaluate buccoadhesive tablets of diltiazem hydrochloride (DZH) using hydroxypropyl methyl cellulose (HPMC) K4M and Carbopol 934 as mucoadhesive polymers. Formulations A1, A2, A3, A4, and B1, B2, and B3, were composed of HPMC K4M and Carbopol 934 at ratios of 1:2, 1:3, 1:4, 1:5, and 1:1, 1:2, 1:3, respectively. The developed formulations were evaluated for physicochemical, in vitro drug release, in vitro adhesion and in vivo studies in healthy human volunteers. The buccal absorption study in healthy volunteers revealed that about 36.86% of the drug was absorbed. Formulation A3 showed maximum release in 8 h. As the concentration of polymer in the formulation increased, the drug release decreased. The bioavailability of diltiazem from buccoadhesive tablets was 1.57-fold higher than oral tablets. The basic pharmacokinetic parameters, C(Max), T(Max), and the area under the curve, were calculated and showed statistically significant differe...
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This investigation studied the effect of vehicles on the in vitro permeation of carvedilol from saturated solutions across porcine skin and selected appropriate penetration enhancers. Labrasol, Transcutol, polyethylene glycol 400,... more
This investigation studied the effect of vehicles on the in vitro permeation of carvedilol from saturated solutions across porcine skin and selected appropriate penetration enhancers. Labrasol, Transcutol, polyethylene glycol 400, propylene glycol, ethanol, oleic acid, isopropyl myristate, and phosphate buffered saline (pH 7.4) containing 40% v/v polyethylene glycol 400 as control, were used as vehicles; limonene, carvone, camphor, menthol, Transcutol, and Labrasol at 5% w/v concentrations were used as penetration enhancers. Skin permeation studies were conducted in Franz diffusion cells using excised porcine ear skin. Solubility was highest (369.13 mg/mL) in Transcutol, whereas isopropyl myristate showed the lowest solubility (0.79 mg/mL) among all the vehicles. The flux of carvedilol from Transcutol, Labrasol, polyethylene glycol 400, ethanol, and oleic acid was 10.5, 8.6, 4.2, 2.9, and 1.5 times higher, respectively, than that observed with control. The flux obtained using Transc...
Research Interests: Chemistry, Chromatography, Medicine, Pda, Permeability, and 15 moreAnimals, Ethanol, Drug Delivery Systems, Polyethylene Glycol, Fourier transform infrared spectroscopy, Pharmaceutical Formulation Technology, Oleic Acid, Permeation, Camphor, Organic Chemicals, Polyethylene Glycols, Menthol, carvedilol, Pharmacology and pharmaceutical sciences, and In Vitro Techniques
Lercanidipine hydrochloride (LRDP) is used in the treatment of hypertension because of its selectivity and specificity on the smooth vascular cells. The pharmacokinetic parameters make LRDP a suitable candidate for transdermal delivery.... more
Lercanidipine hydrochloride (LRDP) is used in the treatment of hypertension because of its selectivity and specificity on the smooth vascular cells. The pharmacokinetic parameters make LRDP a suitable candidate for transdermal delivery. The purpose of the study was to select a suitable formulation for the development of transdermal drug-delivery system (TDDS) of LRDP and to determine the effect of penetration enhancer, limonene on drug permeation The matrix type TDDS of LRDP were prepared by solvent evaporation technique. Formulations A1, A2, A3, A4, A5 and A6 were composed of Eudragit RL100 (ERL) and hydroxypropyl methyl cellulose (HPMC) in 1.5:8.5, 3:7, 4:6, 6:4, 7:3 and 8.5:1.5 ratios respectively. All the six formulations carried 10 mg of LRDP/patch area, 8% v/w of d-limonene as a penetration enhancer, 20% v/w of propylene glycol as plasticizer in methanol and dichloromethane as solvent system. The prepared TDDS were evaluated for physicochemical characteristics, in-vitro releas...
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BACK GROUND AND THE PURPOSE OF STUDY: Many drug substances and variety of naturally occurring dietary or herbal components are capable of interaction with the CYP enzyme system. The aim of the study was to investigate the effect of... more
BACK GROUND AND THE PURPOSE OF STUDY: Many drug substances and variety of naturally occurring dietary or herbal components are capable of interaction with the CYP enzyme system. The aim of the study was to investigate the effect of pomegranate juice pretreatment on the bioavailability of buspirone in rabbits. White New Zealand rabbits weighing 2.1±0.13 Kg were selected for study. The bioavailability of buspirone after pre-treatment with pomegranate juice (10 ml Kg(-1) for seven days) was compared with an oral solution of 10 mg kg(-1) of buspirone in distilled water. Animals were allowed free access to food and water, until night prior to dosing and were fasted for 10 hrs. In the first phase oral solution (10 mg kg(-1)) was administered through feeding tube followed by rinsing with 10 ml of water. In the second phase, the group was pretreated with pomegranate juice for 7 days and study was conducted after 15 days of washout period. The results showed that there was a significant (p&l...
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Research Interests: Pharmacology, Chemistry, Pharmacokinetics, Medicine, Biological Sciences, and 15 morePhytotherapy, Animals, Male, CHEMICAL SCIENCES, Plant extracts, Rats, Wistar Rats, Nitrendipine, Area Under Curve, Herb Drug Interactions, Small Intestine, Molecular Structure, Punicaceae, Medical and Health Sciences, and first-pass effect
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Research Interests: Pharmacology, Chemistry, Chromatography, Medicine, Pharmaceutics, and 15 moreMicroemulsion, Animals, Phase transition, Bioavailability, Gels, In Vivo, Rats, Emulsions, Rabbits, Permeation, Biological Availability, Organic Chemicals, Dihydropyridines, Calcium Channel Blockers, and Pharmacology and pharmaceutical sciences
The objective of the study was to prepare and characterize the domperidone (DOM) hot-melt extruded (HME) buccal films by both in vitro and in vivo techniques. The HME film formulations contained PEO N10 and/or its combination with HPMC E5... more
The objective of the study was to prepare and characterize the domperidone (DOM) hot-melt extruded (HME) buccal films by both in vitro and in vivo techniques. The HME film formulations contained PEO N10 and/or its combination with HPMC E5 LV or Eudragit RL100 as polymeric carriers, and PEG3350 as a plasticizer. The blends were co-processed at a screw speed of 50 rpm with the barrel temperatures ranging from 120-160°C utilizing a bench top co-rotating twin-screw hot-melt extruder using a transverse-slit die. The HME films were evaluated for drug content, drug excipient interaction, in vitro drug release, mechanical properties, in vivo residence time, in vitro bioadhesion, swelling and erosion, ex vivo permeation from HME films and the selected optimal formulation was subjected for bioavailability studies in healthy human volunteers. The extruded films demonstrated no drug excipient interaction and excellent content uniformity. The selected HME film formulation (DOM2) exhibited a tensile strength (0.72 Kg/mm(2)), elongation at break (28.4% mm(2)), in vivo residence time (120 min), peak detachment force (1.55 N), work of adhesion (1.49 mJ), swelling index (210.2%), erosion (10.5%) and in vitro drug release of 84.8% in 2 h. Bioavailability from the optimized HME buccal films was 1.5 times higher than the oral dosage form and the results showed statistically significant (p &amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;lt; 0.05) difference. The ex vivo-in vivo correlation was found to have biphasic pattern and followed type A correlation. The results indicate that HME is a viable technique for the preparation of DOM buccal-adhesive films with improved bioavailability characteristics.
Research Interests: Materials Science, Polymers, Medicine, Humans, Animals, and 15 moreMale, Drug Delivery Systems, Plasticizers, Bioavailability, Adult, Extrusion, Plasticizer, Domperidone, Drug Carriers, Excipients, Dosage Forms, Drug Compounding, Biological Availability, Dopamine antagonists, and Pharmacology and pharmaceutical sciences
The objective of the present research was two-fold: To characterize the produced inclusion complex of felodipine (FDP)-hydroxypropyl-β-cyclodextrin (HPβCD) utilizing lyophilization, and to develop and characterize a complexed... more
The objective of the present research was two-fold: To characterize the produced inclusion complex of felodipine (FDP)-hydroxypropyl-β-cyclodextrin (HPβCD) utilizing lyophilization, and to develop and characterize a complexed sustained-release polymeric matrix tablets intended for buccal delivery. The phase-solubility diagram suggested an A(L) type system with 1:1 stoichiometry. Solid complexes prepared by physical mixing and lyophilization were characterized by thermal and non-thermal analytical techniques to corroborate the fact of complex formation. The sustained-release FDP tablets were produced by direct compression, and these drug or complex-loaded hydrophilic matrices were assessed for in vitro bioadhesion and release modulation, ex vivo permeation, and in vivo residence time. The in vitro drug release and ex vivo permeation across the porcine buccal membrane demonstrated that the matrix tablets containing FDP-HPβCD (FH5) solid complex exhibited a complete and sustained drug release pattern, and a significantly higher drug permeation (p &amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;lt; 0.05) compared to all of the other formulations tested. This could be attributed to both, the FDP-HPβCD complexation phenomenon, and the presence of hydrophilic polymer in the formulation. All of the formulations tested, demonstrated good stability in human saliva. Additionally, in vivo mucoadhesive behavior of the optimized formulations was studied in healthy human volunteers and subjective parameters were evaluated.
Research Interests: Chemistry, Chromatography, Development, Medicine, Humans, and 15 morePermeability, Pharmaceutical, Animals, Male, Cyclodextrin, Bioavailability, Adult, Mouth mucosa, Freeze Drying, Permeation, Excipients, Drug Stability, Felodipine, Calcium Channel Blockers, and Pharmacology and pharmaceutical sciences
Abstract A simple, specific, precise, sensitive, and rapid high performance liquid chromatographic method with UV detection was developed and validated for quantification of fenoverine in human serum. The developed method employed... more
Abstract A simple, specific, precise, sensitive, and rapid high performance liquid chromatographic method with UV detection was developed and validated for quantification of fenoverine in human serum. The developed method employed liquid-liquid extraction of ...
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Microemulsion based transdermal therapeutic system (TTS) for nitrendipine were developed and evaluated with the aim to improve bioavailability and further therapeutic efficacy. Pseudoternary phase diagrams were constructed for the... more
Microemulsion based transdermal therapeutic system (TTS) for nitrendipine were developed and evaluated with the aim to improve bioavailability and further therapeutic efficacy. Pseudoternary phase diagrams were constructed for the microemulsions composed of isopropyl myristate (IPM), Cremophor and propylene glycol (SMix) as oil, surfactant and co-surfactant respectively. Box–Behnken statistical design was employed to optimize the formulations. IPM, SMix and water; cumulative amount permeated across skin, flux and lag time were selected as independent and dependent variables respectively. The formulations were evaluated for permeation parameters across rat abdominal skin using Franz diffusion cells. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The flux of optimized formulation could meet target flux. The optimized formulation was further formulated as reservoir system (ME-TTS) and evaluated for in vivo bioavailability in rabbits. The bioavailability study reveal that about 3.7 times of improvement (p<0.05) after transdermal administration of ME-TTS compared oral suspension. A new microemulsion system for transdermal delivery of nitrendipine was developed and optimized using Box–Behnken statistical design.
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Research Interests: Chemistry, Medicine, Cellulose, Humans, Animals, and 15 moreMale, Drug Delivery Systems, Bioavailability, Saliva, Adult, Mouth mucosa, Fourier transform infrared spectroscopy, Hypesthesia, Current Drug Delivery, Drug Carriers, Biological Availability, Area Under Curve, Biomechanical Phenomena, Methylcellulose, and Pharmacology and pharmaceutical sciences
... of Physicochemical, in vitro, ex vivo and Mechanical Properties Ramesh Gannu, Adukondalu Devandla, Madhav Burra and Madhusudan Rao Yamsani ... ethyl cellulose and poly vinyl pyorrolidone 30 K were obtained as gift samples from Dr... more
... of Physicochemical, in vitro, ex vivo and Mechanical Properties Ramesh Gannu, Adukondalu Devandla, Madhav Burra and Madhusudan Rao Yamsani ... ethyl cellulose and poly vinyl pyorrolidone 30 K were obtained as gift samples from Dr Reddy&amp;#x27;s Laboratories, Hyderabad ...
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Bilayered buccoadhesive patch for systemic administration of felodipine was developed using hydroxy propyl methyl cellulose as primary layer and Eudragit RLPO as secondary layer. In vitro drug permeation studies through porcine buccal... more
Bilayered buccoadhesive patch for systemic administration of felodipine was developed using hydroxy propyl methyl cellulose as primary layer and Eudragit RLPO as secondary layer. In vitro drug permeation studies through porcine buccal membrane and buccal absorption ...
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Research Interests: Mathematics, Response Surface Methodology, Medicine, Animals, Drug Design, and 15 moreResearch article, Skin, Bioavailability, Hydroxypropyl Methylcellulose, Rats, AAPS PharmSciTech, Drug Carriers, Propylene Glycol, Response surface, Box-Behnken Design, Cumulant, Transdermal, Skin Absorption, buspirone , and Pharmacology and pharmaceutical sciences
A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of lacidipine (LCDP) in rabbit serum was developed and validated. LCDP and internal standard (IS), felodipine were extracted into n-hexane and... more
A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of lacidipine (LCDP) in rabbit serum was developed and validated. LCDP and internal standard (IS), felodipine were extracted into n-hexane and dichloromethane (70:30) solvent system and separated using an isocratic mobile phase, on an Inertsil C18 column. The effluent was monitored by UV detector at 240 nm and at a flow rate of 1.0 mL min(-1). The linearity range of proposed method was 1-500 ng mL(-1). The intra-day and inter-day coefficient of variation and percent error values of the assay method were less than 15% and mean recovery was more than 94 and 95% for LCDP and IS, respectively and the method was found to be precise, accurate, and specific during the study. The method was successfully applied for pharmacokinetic study of lacidipine after application of LCDP microemulsion gel in rabbits.
Research Interests: Chemistry, Analytical Chemistry, Chromatography, Pharmacokinetics, Calibration, and 14 moreAnimals, Temperature, Coefficient of Variation, High Performance Liquid Chromatography, High Pressure Liquid Chromatography, Chemical Precipitation, Time Factors, Rabbits, Flow Rate, Sensitivity and Specificity, Dihydropyridines, Calcium Channel Blockers, Costs and Cost Analysis, and buspirone
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This article describes buccal permeation of chlorpheniramine maleate (CPM) and its transbuccal delivery using mucoadhesive buccal patches. Permeation of CPM was calculated in vitro using porcine buccal membrane and in vivo in healthy... more
This article describes buccal permeation of chlorpheniramine maleate (CPM) and its transbuccal delivery using mucoadhesive buccal patches. Permeation of CPM was calculated in vitro using porcine buccal membrane and in vivo in healthy humans. Buccal formulations were developed with hydroxyethylcellulose (HEC) and evaluated for in vitro release, moisture absorption, mechanical properties, and bioadhesion, and optimized formulation was subjected for bioavailability studies in healthy human volunteers. In vitro flux of CPM was calculated to be 0.14 +/- 0.03 mg.h(-1).cm(-2) and buccal absorption also was demonstrated in vivo in human volunteers. In vitro drug release and moisture absorbed were governed by HEC content and formulations exhibited good tensile and mucoadhesive properties. Bioavailability from optimized buccal patch was 1.46 times higher than the oral dosage form and the results showed statistically significant difference.
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Isradipine (ISDP) is an effective calcium channel blocker used in the treatment of hypertension. It undergoes extensive first pass metabolism and bioavailability through the oral route is only about 15 to 24%. Hence we attempted to... more
Isradipine (ISDP) is an effective calcium channel blocker used in the treatment of hypertension. It undergoes extensive first pass metabolism and bioavailability through the oral route is only about 15 to 24%. Hence we attempted to develop a matrix type controlled transdermal drug delivery system for ISDP. Formulations A1, A2, A3 were composed of Eudragit RL100 and hydroxypropyl methyl cellulose (HPMC) in 1:3, 1:1, 3:1 ratios; A4, A5, A6 were composed of Eudragit RS100 and HPMC in 1:3, 1:1, 3:1 ratios. All six formulations carried 5 mg of ISDP/patch area, 5% v/w of D-limonene, 15 % v/w of propylene glycol in methanol:dichloromethane (1:1). The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy and differential scanning calorimetry. The results suggested no physicochemical incompatibility between the drug and the polymers. The prepared transdermal drug delivery system were evaluated for physicochemical characteristics, mainly in vitro release and ex vivo permeation. The ex vivo permeation studies were carried out across excised rat skin using Franz diffusion cell. All the formulations exhibited satisfactory physicochemical characteristics. Cumulative amount of the drug released in 36 h from the six formulations were 1695.32, 1527.89, 1455.54, 1485.65, 1282.81 and 916.88 μg/cm2 respectively. Corresponding values for the cumulative amounts of drug permeated across the rat skin for the above matrix films were 1456.29, 1284.70, 1182.99, 1212.72, 1046.05, and 782.60 μg/cm2 respectively. By fitting the data into zero order, first order and Higuchi models, it was concluded that drug release from matrix films followed Higuchi model and the mechanism of drug release was diffusion mediated. Based on the physical evaluation, in vitro drug release and ex vivo permeation characteristics, it was concluded that for potential therapeutic use, monolithic drug matrix films A1, may be suitable for the development of a transdermal drug delivery system of ISDP.
Research Interests: Kinetics, Treatment Outcome, Polymers, Pharmaceutical Chemistry, Hypertension, and 14 moreDifferential scanning calorimetry, Infrared spectroscopy, Diffusion, Animals, Male, Drug Delivery Systems, Rats, Wistar Rats, AAPS PharmSciTech, Materials Testing, Drug Compounding, Bandages, Ethyl Cellulose, and Random Allocation
A simple and sensitive high performance liquid chromatographic method for simultaneous quantification of glimepiride (GMP) and atorvastatin (ATN) in human serum was developed and validated. GMP, ATN, and internal standard (IS),... more
A simple and sensitive high performance liquid chromatographic method for simultaneous quantification of glimepiride (GMP) and atorvastatin (ATN) in human serum was developed and validated. GMP, ATN, and internal standard (IS), pioglitazone (PG) were extracted into dichloromethane and methanol solvent system and separated using an isocratic mobile phase on an Inertsil C18 column. The eluent was monitored by UV detector at 230 nm. The linearity range of proposed method was 1–1600 ng mL−1 for each analyte. The retention times for GMP, ATN, and IS were found to be 9.8, 6.92, and 7.96 min, respectively. The intra-day and inter-day coefficient of variation and percentage error values of the assay method were less than 15% and mean recovery was more than 96, 93, and 95% for GMP, ATN, and IS, respectively, and the method was found to be precise, accurate, and specific. The method was successfully applied for pharmacokinetic study of GMP and ATN after oral administration to patients. The CMax, TMax, and AUC0–12 of GMP and ATN were found to be 355.3 ng mL−1, 3.1 hr, 2167.5 ng h mL−l and 12.6 ng mL−1, 2.6 hr, 80.8 ng h mL−l, respectively.
Research Interests:
A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of buspirone (BUSP) in rabbit serum was developed and validated. BUSP and internal standard (IS), diltiazem hydrochloride were extracted into... more
A simple and sensitive high performance liquid chromatographic (HPLC) method for quantification of buspirone (BUSP) in rabbit serum was developed and validated. BUSP and internal standard (IS), diltiazem hydrochloride were extracted into dichloromethane and separated using an ...
Research Interests:
Carvedilol has been used as an antihypertensive drug and also possesses antioxidant and antiproliferative effects. A simple and sensitive analytical method for carvedilol in human serum by using high performance liquid chromatography... more
Carvedilol has been used as an antihypertensive drug and also possesses antioxidant and antiproliferative effects. A simple and sensitive analytical method for carvedilol in human serum by using high performance liquid chromatography (HPLC) was developed. The method employs ...
Research Interests:
A simple and sensitive reverse phase ultra fast liquid chromatographic (UFLC) method for simultaneous determination of nitrendipine and carvone in skin diffusate samples and microemulsions was developed and validated. The separation was... more
A simple and sensitive reverse phase ultra fast liquid chromatographic (UFLC) method for simultaneous determination of nitrendipine and carvone in skin diffusate samples and microemulsions was developed and validated. The separation was achieved using a gradient mobile phase, on an Onyx column. The eluents were monitored by photodiode array detection. The linearity ranges of proposed method were 0.125-50 microg mL(-1) and 0.125-30 microg mL(-1) for nitrendipine and carvone respectively. The intra-day and inter-day coefficient of variation and percent error values of the assay method were less than 10%. The method was found to be precise, accurate, and specific during the study. The method was successfully applied for simultaneous estimation of nitrendipine and carvone in ex vivo skin diffusate samples and microemulsions.
Research Interests: Analytical Chemistry, Pharmaceutical Chemistry, Therapeutic drug monitoring, Microemulsion, Pharmaceutical, and 15 moreCalibration, Animals, Skin, Chemical Analysis, Coefficient of Variation, Microemulsions, High Performance Liquid Chromatography, Rats, Liquid Chromatography, Emulsions, Reproducibility of Results, Monoterpenes, Nitrendipine, Calcium Channel Blockers, and Terpenoid
The aim of this study was to investigate the combined influence of three independent variables on the permeation kinetics of lisinopril from hydrogels for transdermal delivery. A three-factor, three-level Box–Behnken design was used to... more
The aim of this study was to investigate the combined influence of three independent variables on the permeation kinetics of lisinopril from hydrogels for transdermal delivery. A three-factor, three-level Box–Behnken design was used to optimize the independent variables, Carbopol 971 P (X 1), menthol (X 2), and propylene glycol (X 3). Fifteen batches were prepared and evaluated for responses as dependent variables. The dependent variables selected were cumulative amount permeated across rat abdominal skin in 24 h (Q 24; Y 1), flux (Y 2), and lag time (Y 3). Aloe juice has been first time investigated as vehicle for hydrogel preparation. The ex vivo permeation study was conducted using Franz diffusion cells. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The regression equation generated for the cumulative permeation of LSP in 24 h (Q 24) was Y 1 = 1,443.3–602.59X 1 + 93.24X 2 + 91.75X 3 − 18.95X 1X 2 – 140.93X 1X 3 – 4.43X 2X 3 – 152.63X 12 – 150.03X22 − 213.9X 32. The statistical validity of the polynomials was established, and optimized formulation factors were selected by feasibility and grid search. Validation of the optimization study with 15 confirmatory runs indicated high degree of prognostic ability of response surface methodology. The use of Box–Behnken design approach helped in identifying the critical formulation parameters in the transdermal delivery of lisinopril from hydrogels.
Research Interests: Research Design, Kinetics, Response Surface Methodology, Hydrogels, Permeability, and 14 moreVariable Selection, Animals, Factorial Design, Viscosity, Skin, Transdermal Drug Delivery System, Rats, AAPS PharmSciTech, Propylene Glycol, Angiotensin Converting Enzyme Inhibitors, Response surface, Lisinopril, Cumulant, and Regression equation
The objective of the investigation was to optimize the iontophoresis process parameters of lisinopril (LSP) by 3 x 3 factorial design, Box-Behnken statistical design. LSP is an ideal candidate for iontophoretic delivery to avoid the... more
The objective of the investigation was to optimize the iontophoresis process parameters of lisinopril (LSP) by 3 x 3 factorial design, Box-Behnken statistical design. LSP is an ideal candidate for iontophoretic delivery to avoid the incomplete absorption problem associated after its oral administration. Independent variables selected were current (X(1)), salt (sodium chloride) concentration (X(2)) and medium/pH (X(3)). The dependent variables studied were amount of LSP permeated in 4 h (Y(1): Q(4)), 24 h (Y(2): Q(24)) and lag time (Y(3)). Mathematical equations and response surface plots were used to relate the dependent and independent variables. The regression equation generated for the iontophoretic permeation was Y(1) = 1.98 + 1.23X(1) - 0.49X(2) + 0.025X(3) - 0.49X(1)X(2) + 0.040X(1)X(3) - 0.010X(2)X(3) + 0.58X(1)(2) - 0.17X(2)(2) - 0.18X(3)(2); Y(2) = 7.28 + 3.32X(1) - 1.52X(2) + 0.22X(3) - 1.30X(1)X(2) + 0.49X(1)X(3) - 0.090X(2)X(3) + 0.79X(1)(2) - 0.62X(2)(2) - 0.33X(3)(2) and Y(3) = 0.60 + 0.0038X(1) + 0.12X(2) - 0.011X(3) + 0.005X(1)X(2) - 0.018X(1)X(3) - 0.015X(2)X(3) - 0.00075X(1)(2) + 0.017X(2)(2) - 0.11X(3)(2). The statistical validity of the polynomials was established and optimized process parameters were selected by feasibility and grid search. Validation of the optimization study with 8 confirmatory runs indicated high degree of prognostic ability of response surface methodology. The use of Box-Behnken design approach helped in identifying the critical process parameters in the iontophoretic delivery of lisinopril.