International Journal of Pharmaceutical Sciences and Nanotechnology
Self-emulsifying drug delivery systems (SEDDS) are a type of emulsion that have received particul... more Self-emulsifying drug delivery systems (SEDDS) are a type of emulsion that have received particular attention in recent years as a means of enhancing oral bioavailability of poorly absorbed drugs. These systems are ideally isotropic mixture of oil and surfactant (sometimes co-surfactant are added) that form emulsions on mixing with water with little or no energy input. Hydrophobic drugs are dissolved in SEDDS. After administering the drug by this system, emulsion is formed in the GIT by selfemulsification. Generally by this process bioavailability of the drug is increased and quantity required to exert desired effect is decreased. Oil surfactant ratio, amount of surfactant, type of surfactant, nature of oil affect the process of emulsification. In the emulsification process water penetrates into the oil water interface, leading to the formation of liquid crystalline phase, resulting in swelling at the interface. Generally, SEDDS are formed with triglyceride oils and nonionic surfact...
Journal of Drug Delivery Science and Technology, 2015
ABSTRACT The purpose of the present investigation was to improve solubility and dissolution prope... more ABSTRACT The purpose of the present investigation was to improve solubility and dissolution properties of poorly water soluble drug, Embelin, a herbal active ingredient by preparing nanosuspensions. The wet media milling technique was employed for the preparation of nanosuspensions. Further, nanosuspensions were freeze dried to generate nanocrystals. Rotatable central composite design was adopted to study the effects of independent variables viz. amount of stabilizer (Pluronic F68) and amount of milling agents (Zirconium beads) on dependent variables, particle size and % drug release at 30 min. Relationship between dependent and independent variables were further investigated by multiple linear regression analysis. A significant increase was found in the solubility and dissolution rate of the formulations. Differential scanning calorimetry and Powder X-ray diffraction studies confirmed decrease in drug crystallinity. Surface electron microscopy and Transmission electron microscopy revealed plate like morphology. Results suggested remarkable improvement in the dissolution properties of Embelin by preparing nanocrystals.
Abstract Micronisation of simvastatin dissolved in acetone, dimethyl sulfoxide and ethanol with s... more Abstract Micronisation of simvastatin dissolved in acetone, dimethyl sulfoxide and ethanol with supercritical carbon dioxide as antisolvent was successfully performed using a supercritical antisolvent technique. The effect of a few process parameters such as precipitation temperature, the pressure and solute concentration in the liquid solution has been studied to evaluate their influence on morphology and size of particles. The micronised simvastatin were evaluated for drug content, particle size analysis and in vitro dissolution profiles. Fourier transform infrared spectroscopy, differential scanning calorimetry and PXRD patterns was used to study the possible changes after micronisation of simvastatin. The dissolution rate was increased after micronised compared with pure simvastatin in distilled water, pH 1.2 buffer and pH 7.0 buffer. In vivo performance of the optimised formulation was evaluated in rats using pharmacodynamic marker parameters like serum total cholesterol (CH) and triglycerides (TG) for 21 days. Pharmacodynamic studies of micronised simvastatin revealed improved reduction in CH and TG values as compared with pure simvastatin indicating improved bioavailability. In vivo pharmacokinetics in rats showed an increase in bioavailability of micronised simvastatin (3.14 times) compared with plain simvastatin.
ABSTRACT In the present investigation, an attempt was made to improve the dissolution properties ... more ABSTRACT In the present investigation, an attempt was made to improve the dissolution properties of water insoluble herbal active ingredient, Embelin (EBN) by utilizing liquisolid technique, which might offer improved bioavailability. The compacts were prepared using Capryol 90 as non-volatile solvent, Neusilin as carrier and Aerosil 200 as coating material. Mathematical model and 32 factorial design with liquid load factor (X1) and drug concentration (X2) as the independent variables, was utilized to prepare the liquisolid powder systems. The prepared systems were subjected for studying micromeritic properties and possible drug-excipient interactions by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Dissolution studies revealed improvement in the drug release properties. Physicochemical characterization of liquisolid compacts by FTIR, DSC and PXRD techniques suggested reduction in drug crystallinity elaborating for the dissolution enhancement. The study reveals that liquisolid technique is a promising alternative for enhancing dissolution characteristics of EBN.
The aim of the present work was to study the effect of various process parameters on an aqueous-b... more The aim of the present work was to study the effect of various process parameters on an aqueous-based f ilm coating process of tablets performed in a side-vent ed perforated pan-coating apparatus. Results of pre liminary trials indicate that spray rate, inlet air temperature, percentage solid content, atomizing air pressure and speed of rotation affected characteristics of coating. A 3 3 full factorial design was employed to study the ef fect of independent variables; spray rate (X 1), inlet air temperature (X 2) and rotating speed of pan (X 3) on dependent variables: coating uniformity, coati ng process efficiency, surface roughness and percentage loss o n drying. The best batch exhibited spray rate of coa ting solution 8 gm/min, inlet air temperature 55°C and rotating speed of pa n 12 rpm. The surface characteristics of the aqueous -based film-coated tablet were studied under a scanning electron microscope.
The purpose of this research was to formulate and systemically evaluate in vitro and in vivo perf... more The purpose of this research was to formulate and systemically evaluate in vitro and in vivo performances of mucoadhesive amoxicillin microparticles for the potential use in the treatment of gastric and duodenal ulcers, which were associated with Helicobacter pylori. The chitosan/amoxicillin microparticles were successfully prepared in a process of solution-enhanced dispersion by supercritical CO₂ (SEDS). The morphological characteristics of the mucoadhesive microparticles were studied under scanning electron microscope. The resulted microparticles with mean sizes ranged from 1.0 and 2.5 µm had good mucoadhesive properties. In vitro and in vivo mucoadhesive tests showed that chitosan/amoxicillin mucoadhesive microparticles adhered more strongly to gastric mucous layer and could retain in gastrointestinal tract for an extended period of time. The X-Ray Powder Diffractometry and Differential Scanning Calorimetry analysis demonstrated that the SEDS process was a typical physical coating process to produce drug-polymer composite microparticles, which is favourable for drugs since there is no changes in chemistry. In vitro release test showed that amoxicillin released faster in pH 1.0 hydrochloric acid (HCl) than in pH 7.8 phosphate buffer. In vivo H. pylori clearance tests were also carried out by administering amoxicillin powder and mucoadhesive microparticles to H. pylori infectious Wistar rats under fed conditions at single dose or multiple dose(s) in oral administration. The results showed that amoxicillin mucoadhesive microparticles had a better clearance effect than amoxicillin powder. In conclusion, the prolonged gastrointestinal residence time and enhanced amoxicillin stability resulting from the mucoadhesive microparticles of amoxicillin might make a contribution to H. pylori complete eradication.
Cyclosporine A-nanosuspensions were prepared using zirconium oxide beads as a milling media, Polo... more Cyclosporine A-nanosuspensions were prepared using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and distilled water as an aqueous medium using the Pearl Milling technique. The optimized formulation was characterized in terms of particle size ...
ABSTRACT Colon specific drug delivery has gained increased importance not just for the delivery o... more ABSTRACT Colon specific drug delivery has gained increased importance not just for the delivery of drugs in the treatmentassociated with the colon, but also as a potential site for the systemic delivery of therapeutic peptide and proteins. Toachieve successful colon targeted drug delivery, a drug needs to be protected from degradation, release and/orabsorption in the upper portion of the GI tract and then to be ensured abrupt or controlled release in the proximalcolon. The necessity and advantages of colon-specific drug delivery systems have been well recognized anddocumented. The primary approaches to obtain colon-specific delivery are based on prodrugs, pH- and time-dependentsystems or microflora-activated systems and have achieved limited success only. Precise colon drug delivery requiresthat the triggering mechanism in the delivery system only respond to the physiological conditions particular to thecolon. Hence, continuous efforts have been focused on designing colon-specific delivery systems with improved sitespecificity and versatile drug release kinetics to accomplish different therapeutic needs. Among the systems developedmost recently for colon-specific delivery, four systems were unique in terms of achieving in vivo site specificity,design rationale, and feasibility of the manufacturing process (pressure-controlled colon delivery capsules (PCDCs),CODES™, colonic drug delivery system based on pectin and galactomannan coating, and Azo hydrogels). The focusof this review is to provide detailed descriptions of the above mentioned approaches.
International Journal of Pharmaceutical Sciences and Nanotechnology
Self-emulsifying drug delivery systems (SEDDS) are a type of emulsion that have received particul... more Self-emulsifying drug delivery systems (SEDDS) are a type of emulsion that have received particular attention in recent years as a means of enhancing oral bioavailability of poorly absorbed drugs. These systems are ideally isotropic mixture of oil and surfactant (sometimes co-surfactant are added) that form emulsions on mixing with water with little or no energy input. Hydrophobic drugs are dissolved in SEDDS. After administering the drug by this system, emulsion is formed in the GIT by selfemulsification. Generally by this process bioavailability of the drug is increased and quantity required to exert desired effect is decreased. Oil surfactant ratio, amount of surfactant, type of surfactant, nature of oil affect the process of emulsification. In the emulsification process water penetrates into the oil water interface, leading to the formation of liquid crystalline phase, resulting in swelling at the interface. Generally, SEDDS are formed with triglyceride oils and nonionic surfact...
Journal of Drug Delivery Science and Technology, 2015
ABSTRACT The purpose of the present investigation was to improve solubility and dissolution prope... more ABSTRACT The purpose of the present investigation was to improve solubility and dissolution properties of poorly water soluble drug, Embelin, a herbal active ingredient by preparing nanosuspensions. The wet media milling technique was employed for the preparation of nanosuspensions. Further, nanosuspensions were freeze dried to generate nanocrystals. Rotatable central composite design was adopted to study the effects of independent variables viz. amount of stabilizer (Pluronic F68) and amount of milling agents (Zirconium beads) on dependent variables, particle size and % drug release at 30 min. Relationship between dependent and independent variables were further investigated by multiple linear regression analysis. A significant increase was found in the solubility and dissolution rate of the formulations. Differential scanning calorimetry and Powder X-ray diffraction studies confirmed decrease in drug crystallinity. Surface electron microscopy and Transmission electron microscopy revealed plate like morphology. Results suggested remarkable improvement in the dissolution properties of Embelin by preparing nanocrystals.
Abstract Micronisation of simvastatin dissolved in acetone, dimethyl sulfoxide and ethanol with s... more Abstract Micronisation of simvastatin dissolved in acetone, dimethyl sulfoxide and ethanol with supercritical carbon dioxide as antisolvent was successfully performed using a supercritical antisolvent technique. The effect of a few process parameters such as precipitation temperature, the pressure and solute concentration in the liquid solution has been studied to evaluate their influence on morphology and size of particles. The micronised simvastatin were evaluated for drug content, particle size analysis and in vitro dissolution profiles. Fourier transform infrared spectroscopy, differential scanning calorimetry and PXRD patterns was used to study the possible changes after micronisation of simvastatin. The dissolution rate was increased after micronised compared with pure simvastatin in distilled water, pH 1.2 buffer and pH 7.0 buffer. In vivo performance of the optimised formulation was evaluated in rats using pharmacodynamic marker parameters like serum total cholesterol (CH) and triglycerides (TG) for 21 days. Pharmacodynamic studies of micronised simvastatin revealed improved reduction in CH and TG values as compared with pure simvastatin indicating improved bioavailability. In vivo pharmacokinetics in rats showed an increase in bioavailability of micronised simvastatin (3.14 times) compared with plain simvastatin.
ABSTRACT In the present investigation, an attempt was made to improve the dissolution properties ... more ABSTRACT In the present investigation, an attempt was made to improve the dissolution properties of water insoluble herbal active ingredient, Embelin (EBN) by utilizing liquisolid technique, which might offer improved bioavailability. The compacts were prepared using Capryol 90 as non-volatile solvent, Neusilin as carrier and Aerosil 200 as coating material. Mathematical model and 32 factorial design with liquid load factor (X1) and drug concentration (X2) as the independent variables, was utilized to prepare the liquisolid powder systems. The prepared systems were subjected for studying micromeritic properties and possible drug-excipient interactions by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Dissolution studies revealed improvement in the drug release properties. Physicochemical characterization of liquisolid compacts by FTIR, DSC and PXRD techniques suggested reduction in drug crystallinity elaborating for the dissolution enhancement. The study reveals that liquisolid technique is a promising alternative for enhancing dissolution characteristics of EBN.
The aim of the present work was to study the effect of various process parameters on an aqueous-b... more The aim of the present work was to study the effect of various process parameters on an aqueous-based f ilm coating process of tablets performed in a side-vent ed perforated pan-coating apparatus. Results of pre liminary trials indicate that spray rate, inlet air temperature, percentage solid content, atomizing air pressure and speed of rotation affected characteristics of coating. A 3 3 full factorial design was employed to study the ef fect of independent variables; spray rate (X 1), inlet air temperature (X 2) and rotating speed of pan (X 3) on dependent variables: coating uniformity, coati ng process efficiency, surface roughness and percentage loss o n drying. The best batch exhibited spray rate of coa ting solution 8 gm/min, inlet air temperature 55°C and rotating speed of pa n 12 rpm. The surface characteristics of the aqueous -based film-coated tablet were studied under a scanning electron microscope.
The purpose of this research was to formulate and systemically evaluate in vitro and in vivo perf... more The purpose of this research was to formulate and systemically evaluate in vitro and in vivo performances of mucoadhesive amoxicillin microparticles for the potential use in the treatment of gastric and duodenal ulcers, which were associated with Helicobacter pylori. The chitosan/amoxicillin microparticles were successfully prepared in a process of solution-enhanced dispersion by supercritical CO₂ (SEDS). The morphological characteristics of the mucoadhesive microparticles were studied under scanning electron microscope. The resulted microparticles with mean sizes ranged from 1.0 and 2.5 µm had good mucoadhesive properties. In vitro and in vivo mucoadhesive tests showed that chitosan/amoxicillin mucoadhesive microparticles adhered more strongly to gastric mucous layer and could retain in gastrointestinal tract for an extended period of time. The X-Ray Powder Diffractometry and Differential Scanning Calorimetry analysis demonstrated that the SEDS process was a typical physical coating process to produce drug-polymer composite microparticles, which is favourable for drugs since there is no changes in chemistry. In vitro release test showed that amoxicillin released faster in pH 1.0 hydrochloric acid (HCl) than in pH 7.8 phosphate buffer. In vivo H. pylori clearance tests were also carried out by administering amoxicillin powder and mucoadhesive microparticles to H. pylori infectious Wistar rats under fed conditions at single dose or multiple dose(s) in oral administration. The results showed that amoxicillin mucoadhesive microparticles had a better clearance effect than amoxicillin powder. In conclusion, the prolonged gastrointestinal residence time and enhanced amoxicillin stability resulting from the mucoadhesive microparticles of amoxicillin might make a contribution to H. pylori complete eradication.
Cyclosporine A-nanosuspensions were prepared using zirconium oxide beads as a milling media, Polo... more Cyclosporine A-nanosuspensions were prepared using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and distilled water as an aqueous medium using the Pearl Milling technique. The optimized formulation was characterized in terms of particle size ...
ABSTRACT Colon specific drug delivery has gained increased importance not just for the delivery o... more ABSTRACT Colon specific drug delivery has gained increased importance not just for the delivery of drugs in the treatmentassociated with the colon, but also as a potential site for the systemic delivery of therapeutic peptide and proteins. Toachieve successful colon targeted drug delivery, a drug needs to be protected from degradation, release and/orabsorption in the upper portion of the GI tract and then to be ensured abrupt or controlled release in the proximalcolon. The necessity and advantages of colon-specific drug delivery systems have been well recognized anddocumented. The primary approaches to obtain colon-specific delivery are based on prodrugs, pH- and time-dependentsystems or microflora-activated systems and have achieved limited success only. Precise colon drug delivery requiresthat the triggering mechanism in the delivery system only respond to the physiological conditions particular to thecolon. Hence, continuous efforts have been focused on designing colon-specific delivery systems with improved sitespecificity and versatile drug release kinetics to accomplish different therapeutic needs. Among the systems developedmost recently for colon-specific delivery, four systems were unique in terms of achieving in vivo site specificity,design rationale, and feasibility of the manufacturing process (pressure-controlled colon delivery capsules (PCDCs),CODES™, colonic drug delivery system based on pectin and galactomannan coating, and Azo hydrogels). The focusof this review is to provide detailed descriptions of the above mentioned approaches.
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Papers by Jayvadan Patel