Claudio J Salomon
Universidad Nacional de Rosario (UNR) Argentina, Pharmacy, Faculty Member
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Probiotics are live microorganisms that confer beneficial effects on the health of the host if administered in adequate amounts (106 CFU viable microorganisms/g of food). As the most frequent route of administration of these... more
Probiotics are live microorganisms that confer beneficial effects on the health of the host if administered in adequate amounts (106 CFU viable microorganisms/g of food). As the most frequent route of administration of these microorganisms is oral, the number of them that remains viable through the gastrointestinal tract decreases substantially. Thus, in this research work, we developed a series of alginate‐based microparticles using different adjuvants such as methylcellulose, carboxymethylcellulose, chitosan, carbopol, β‐cyclodextrin, starch, carrageenan, and Eudragit® RS 100 as carriers for improving the survival of Lactococcus lactis. The alginate‐based formulations exhibited very good drug encapsulation efficiency, up to 90%. Release studies from selected microparticles revealed that almost 100% of bacteria were in solution at 30 min. By scanning electron microscopy, irregular nonporous particles with a size between 200 and 500 µm were seen. In particular, microparticles formul...
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A stereospecific synthesis of 6,6-dibromo-3α-cyano-2,2-dimethylpenam-(1R)-S-oxide (2) is described. The X-ray single crystal investigation of this compound shows that it crystallizes in the monoclinic system, space group P21, with cell... more
A stereospecific synthesis of 6,6-dibromo-3α-cyano-2,2-dimethylpenam-(1R)-S-oxide (2) is described. The X-ray single crystal investigation of this compound shows that it crystallizes in the monoclinic system, space group P21, with cell parameters a = 6.194(1), b = 9.363(1), c = 9.869(1) Å, β = 96.55(2)°, V = 568(1) Å3, and two molecules per unit cell. Thestructure was solved, from low temperature data, by direct methods, and refined, by least-squares procedures, to a final R = 3.17%, Rw = 3.38%, for 1221 observed independent reflections. The sulfoxide configuration is R. The thiazolidine presents an envelope shape with the C(3) atom 0.56 Å above the other four members of the ring mean plane. Therefore, it exhibits the conformation with α-CH3 pseudoequatorial and β-CH3 and α-CN both pseudoaxial. This conformation is different from the one reported for other penicillin sulfoxide derivatives. The geometry of the β-lactam ring is typical of the fused bicyclic penam nucleus. The ring is non-planar. The N(4) atom displays a pyramidial arrangement. The examination of crystal packing shows that molecules along a are connected by a short C—H … O contactReported single crystal studies showed two dominant conformations for the thiazolidine ring in the fused bicyclic penam nucleus: the C(3) or 2β-3α substituents both pseudoaxial, as found in 2, and the S(1) or 2β-3α substituents both pseudoequatorial, adopted by most sulfoxides. Neither of these conformations can explain the nuclear Overhauser effect data. A conformation with the substituents C2-β-methyl-C3-α-H and C2-α-methyl-C3-α-CN fully eclipsed is in accordance with the experimental results in the solution. The 1H nuclear magnetic resonance data reflect the influence of the magnetic anisotropy of the CN triple bond on the gem-dimethyl groups, particularly in relation with the geometrical features of the molecule. Comparison of 13C nuclear magnetic resonance chemical shifts for 2 and its parent penicillin sulfide (1) indicates configurationally dependent substituent effects, the magnitude of which can be used for the stereochemical assignment of sulfoxide groups in this series. Key words: penicillin sulfoxide derivatives, di-halogen penicillanates, stereospecific synthesis, NMR studies, absolute configuration determination.
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Diclofenac sodium is a non-steroidal anti-inflammatory drug widely used in the treatment of ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. In this context, a rapid onset of action is required. Thus, the aim of this study... more
Diclofenac sodium is a non-steroidal anti-inflammatory drug widely used in the treatment of ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. In this context, a rapid onset of action is required. Thus, the aim of this study was to formulate diclofenac sodium-PVP K-30 fast release tablets from solid dispersions. The physical state and drug:carrier interactions were analyzed by X-ray diffraction and scanning electron microscopy and stability upon storage was also studied. Dissolution rate of diclofenac sodium from solid dispersions was markedly enhanced by increasing the polymer concentration.
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Background Benznidazole and nifurtimox are effective drugs used to treat Chagas’ disease; however, their administration in patients in the chronic phase of the disease is still limited, mainly due to their limited efficacy in the later... more
Background Benznidazole and nifurtimox are effective drugs used to treat Chagas’ disease; however, their administration in patients in the chronic phase of the disease is still limited, mainly due to their limited efficacy in the later chronic stage of the disease and to the adverse effects related to these drugs. Objectives To evaluate the effect of low doses of nanoformulated benznidazole using a chronic model of Trypanosoma cruzi Nicaragua infection in C57BL/6J mice. Methods Nanoformulations were administered in two different schemes: one daily dose for 30 days or one dose every 7 days, 13 times. Results Both treatment schemes showed promising outcomes, such as the elimination of parasitaemia, a reduction in the levels of T. cruzi-specific antibodies and a reduction in T. cruzi-specific IFN-γ-producing cells, as well as an improvement in electrocardiographic alterations and a reduction in inflammation and fibrosis in the heart compared with untreated T. cruzi-infected animals. Th...
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To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is... more
To date, the treatment for cysticercosis and neurocysticercosis consists of a single oral intake of praziquantel (5–10 mg/kg), which since it is only available as tablets, hinders its administration to pediatric patients. Praziquantel is a poorly water-soluble drug which represents a challenge for its formulation in solution, particularly for the pediatric population. Thus, this study aimed to develop a palatable solution for praziquantel using pharmaceutical-accepted co-solvent systems. A design of experiments approach was applied to identify the optimal conditions for achieving a suitable amount of praziquantel in solution using co-solvent mixtures. Thus, praziquantel solubility increased from 0.38 up to 43.50 mg/mL in the optimized system. A taste masking assay in healthy human volunteers confirmed a successful reduction of drug bitterness after the addition of selected flavors and a sweetener. Stability studies were also conducted at different temperatures (4, 25, and 40 °C) for...
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Schistosomiasis is a widely distributed parasitic disease and one of the most important neglected tropical diseases globally, for which Praziquantel® (PZQ) is the only available treatment. In this context, tests with new PZQ formulations... more
Schistosomiasis is a widely distributed parasitic disease and one of the most important neglected tropical diseases globally, for which Praziquantel® (PZQ) is the only available treatment. In this context, tests with new PZQ formulations become relevant for disease control. This study evaluated the effects of PZQ treatment in the prepatent phase of schistosomiasis using two formulations: nanoencapsulated (PZQ-NANO) and active pharmaceutical ingredient (PZQ-API). Five experimental groups were established, for which the following serological parameters were evaluated: ALT, AST, ALP, and TP. Animals treated with PZQ-API at 15 and 30 days post-infection showed decreased eggs per gram of feces (EPG) compared to untreated infected animals. The same animals showed reductions of 63.6 and 65.1%, respectively, at 60 days post-infection. Animals treated with PZQ-NANO experienced no significant changes in EPG at any time of observation. Animals treated with either PZQ-API or PZQ-NANO had higher...
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La microencapsulación es un proceso en el cual sustancias de origen sólido, líquido o compuestos gaseosos son cubiertas o dispersadas en una película de material polimérico. Cuando las dimensiones de las cápsulas obtenidas se encuentran... more
La microencapsulación es un proceso en el cual sustancias de origen sólido, líquido o compuestos gaseosos son cubiertas o dispersadas en una película de material polimérico. Cuando las dimensiones de las cápsulas obtenidas se encuentran entre 1 mm y 1 mm se denomina microencapsulación, mientras que cuando las dimensiones son menores a 1 μm se emplea el término nanoencapsulación.En un sentido amplio, la micro o nanoencapsulación provee un medio de envasar, separar y almacenar materiales en escala micrométrica o nanométrica, según sea el caso, para su posterior liberación bajo condiciones controladas.Fil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaFil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaFil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentin
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Squistosomiasis is a disease caused by trematode parasites of Schistosoma genus. It mainly affects tropical and subtropical areas, remains a major global health problem because of its high incidence in these regions. One of the most... more
Squistosomiasis is a disease caused by trematode parasites of Schistosoma genus. It mainly affects tropical and subtropical areas, remains a major global health problem because of its high incidence in these regions. One of the most important species, because of its prevalence and severity, is Schistosoma mansoni, responsible for intestinal schistosomiasis. The treatment of choice is praziquantel, which exhibit high rates of clinical efficacy. However, this drug doesn’t prevent reinfection and therapeutic failure is frequently observed in endemic areas. Therefore, the search for therapeutic alternatives is urgently required. The objective of this assay was to evaluate in-vitro two types of praziquantel nanoparticles formulations (type A and type S) and, also, an alternative treatment with ivermectin against the adult stage of S. mansoni. The results showed that treatment with such nanoparticles has a similar or better efficiency than the available praziquantel powder. However, treat...
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In this work, chitosan films were prepared by a casting/solvent evaporation methodology using pectin or hydroxypropylmethyl cellulose to form polymeric matrices. Miconazole nitrate, as a model drug, was loaded into such formulations.... more
In this work, chitosan films were prepared by a casting/solvent evaporation methodology using pectin or hydroxypropylmethyl cellulose to form polymeric matrices. Miconazole nitrate, as a model drug, was loaded into such formulations. These polymeric films were characterized in terms of mechanical properties, adhesiveness, and swelling as well as drug release. Besides, the morphology of raw materials and films was investigated by scanning electron microscopy; interactions between polymers were analyzed by infrared spectroscopy and drug crystallinity studied by differential scanning calorimetry and X-ray diffraction. In addition, antifungal activity against cultures of the five most important fungal opportunistic pathogens belonging to Candida genus was investigated. Chitosan:hydroxypropylmethyl cellulose films were found to be the most appropriate formulations in terms of folding endurance, mechanical properties, and adhesiveness. Also, an improvement in the dissolution rate of micon...
Research Interests: Materials Science, Chemistry, Chitosan, Polymers, Medicine, and 15 moreHumans, Differential scanning calorimetry, Candida, Swelling, Drug Delivery Systems, Crystallinity, X ray diffraction, Antifungal Agents, AAPS PharmSciTech, Pectins, Buccal Films, Drug Compounding, Miconazole, Pharmacology and pharmaceutical sciences, and Ciencias Químicas
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Design of Experiments (DoE) techniques were used to identify and optimize the parameters involved in the formulation of triclabendazole pH-sensitive Eudragit® nanoparticles (NPs). Using a Placket Burmann design, Eudragit® E, Eudragit® RS,... more
Design of Experiments (DoE) techniques were used to identify and optimize the parameters involved in the formulation of triclabendazole pH-sensitive Eudragit® nanoparticles (NPs). Using a Placket Burmann design, Eudragit® E, Eudragit® RS, and two stabilizers (PVP and PVA) were evaluated for NPs formulation by nanoprecipitation. Based on the screening results, Eudragit E 100® and PVP were selected as excipients, and their levels were studied and optimized using a central composite design, obtaining an optimum nanoparticulated system with a Size of 240 nm, a PDI of 0.420, and a ZP of 46.3 mV. Finally, a full characterization of the optimum system was carried out by XRD, DSC, equilibrium solubility, and dissolution rate in biorelevant mediums. As observed in XRD and DSC, the nanoencapsulation process produced a remarkable reduction in drug crystallinity that improved drug solubility and dissolution rate. Although more than 90% of TCBZ was dissolved in acidic mediums at 10 minutes, no increase in solubility or dissolution rate was observed in simulated saliva. Consequently, the development of pH-sensitive Eudragit® NPs would be a promising strategy in developing an immediate gastric release TCBZ formulation for oral delivery.
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Raw data in Microsoft Excell format used to create bar and scatter plots
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It is well known that the splitting of tablets can bring serious risks to the health of the treated animals, e.g., the possible adverse reactions caused by overdoses of fenbendazole or aspirin. In this regard, this work aimed to evaluate,... more
It is well known that the splitting of tablets can bring serious risks to the health of the treated animals, e.g., the possible adverse reactions caused by overdoses of fenbendazole or aspirin. In this regard, this work aimed to evaluate, for the first time, the splitting behavior of commercial veterinary tablets and identifying the technological aspects that interfere in this process. Tablets were cut in halves using a tablet splitter and were analyzed regarding mass variation, mass loss, friability, and hardness. Microstructural and morphological evaluations were also performed. For most of the tablets, organic flavor additives provided more uniformity and cohesive matrix, which preserved its hardness after the cut and led to subdivision results within acceptable limits for mass measurements and friability. Apart from the microstructure, the most critical technological aspect for a correct splitting performance in such tablets was the presence of a score. Thus, the results presented here allow us to guide the manufacturing of veterinary drug products in order to produce tablets more adapted to the splitting process.
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PURPOSE The aim of this work was to formulate and characterize surfactant-free glibenclamide nanoparticles using Eudragit RLPO and polyethylene glycol as sole stabilizer. METHODS Glibenclamide nanoparticles were obtained by... more
PURPOSE The aim of this work was to formulate and characterize surfactant-free glibenclamide nanoparticles using Eudragit RLPO and polyethylene glycol as sole stabilizer. METHODS Glibenclamide nanoparticles were obtained by nanoprecipitation and evaluated in terms of drug content, encapsulation efficiency, apparent saturation solubility, drug release profile, solid state and storage stability. The influence of different stirring speed on the particle size, size distribution and zeta potential of the nanoparticles was investigated. The nanoparticle biocompatibility and permeability were analyzed in vitro on Caco-2 cell line (clone HTB-37) and its interaction with mucin was also investigated. RESULTS It was found that increasing the molecular weight of polyethylene glycol from 400 to 6000 decreased drug encapsulation, whereas the aqueous solubility and dissolution rate of the drug increased. Particle size of the nanoformulations, with and without polyethylene glycol, were between 140 and 460 nm. Stability studies confirmed that glibenclamide nanoparticles were stable, in terms of particle size, after 120 days at 4°C. In vitro studies indicated minimal interactions of glibenclamide nanoparticles and mucin glycoproteins suggesting favorable properties to address the intestinal mucus barrier. Cell viability studies confirmed the safety profile of these nanoparticles and showed an increased permeation through epithelial cells. CONCLUSION Taking into consideration these findings, polyethylene glycol is a useful polymer for stabilizing these surfactant-free glibenclamide nanoparticles and represent a promising alternative to improve the treatment of non-insulin dependent diabetes.
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The aim of this work was to develop nanosuspensions of praziquantel (PZQ) and to evaluate their influence on the energetic metabolism of cysticerci inoculated in BALB/c mice. We analyzed metabolic alterations of glycolytic pathways and... more
The aim of this work was to develop nanosuspensions of praziquantel (PZQ) and to evaluate their influence on the energetic metabolism of cysticerci inoculated in BALB/c mice. We analyzed metabolic alterations of glycolytic pathways and the tricarboxylic acid cycle in the parasite. The nanosuspensions were prepared by precipitation and polyvinyl alcohol (PVA), poloxamer 188 (P188) and poloxamer 407 (P407) were used as stabilizers. Nanosuspension prepared with PVA had a particle size of 100nm, while P188- and P407-based nanosuspensions had particle sizes of 74nm and 285nm, respectively. The zeta potential was -8.1, -8.6, and -13.2 for the formulations stabilized with PVA, P188 and P407, respectively. Treatments of T. crassiceps cysticerci-infected mice resulted in an increase in glycolysis organic acids, and enhanced the partial reversion of the tricarboxylic acid cycle, the urea cycle and the production of ketonic bodies in the parasites when compared to the groups treated with conve...
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Benznidazole (BZL) is the drug of choice for the treatment of Chagas' disease, a neglected parasitic infection. It is poorly soluble in water, which may have a direct impact into its bioavailability. Thus, the aim of this... more
Benznidazole (BZL) is the drug of choice for the treatment of Chagas' disease, a neglected parasitic infection. It is poorly soluble in water, which may have a direct impact into its bioavailability. Thus, the aim of this study was to evaluate the impact of stoichiometric and non-stoichiometric BZL-cyclodextrins (CDs) complexes on the bioavailability of BZL. The interaction of BZL with the CDs was investigated using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffractometry (XRD), phase solubility and dissolution studies. The oral bioavailability of BZL from these complexes was examined in rats. Both BZL solubility and dissolution increased by CD complexation. The inclusion complexes were found to improve the dissolution rate of BZL by 4.3-fold in comparison with BZL alone. Complexation of BZL with CDs derivatives increased its plasma concentrations when fed to rats, with AUC0-5 values increasing up to 3.7-fold and Cmax increasing 2.5-fold in comparison with BZL alone. It should be note that a remarkable increase in these parameters was observed in the case of the non-stoichiometric complexes. Thus, these CDs complexes could be used to efficiently deliver BZL in patients suffering from Chagas' disease.
Research Interests: Pharmacology, Chemistry, Kinetics, Pharmacokinetics, Medicine, and 15 moreAnimals, Male, Complexation, Bioavailability, Solubility, Chagas disease, Thermogravimetry, CIENCIAS DE LA SALUD, Rats, X ray diffraction, Cyclodextrins, Biological Macromolecules, Biological Availability, Biochemistry and cell biology, and Dissolution Rate
Research Interests: Organic Chemistry, Scanning Electron Microscopy, Polymers, Atomic Force Microscopy, Infrared spectroscopy, and 11 moreDrug Design, Drug Delivery Systems, Thermogravimetry, Fourier transform infrared spectroscopy, Thermogravimetric Analysis, In vitro models, Antifungal Agents, AAPS PharmSciTech, Enseñanza - Aprendizaje Ciencias Naturales Y Exactas, Pharmacology and pharmaceutical sciences, and Ciencias Químicas
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Chagas disease is a neglected parasitic infection caused by the protozoan Trypanosoma cruzi (T. cruzi) that affects more than 6 million people, mainly in Latin America. Benznidazole is still the drug of choice in many countries to treat... more
Chagas disease is a neglected parasitic infection caused by the protozoan Trypanosoma cruzi (T. cruzi) that affects more than 6 million people, mainly in Latin America. Benznidazole is still the drug of choice in many countries to treat it in spite of its dosage regimen and adverse side effects such as such as allergic dermatitis, peripheral neuropathy and anorexia. Thus, novel, safer, and more efficacious treatments for such neglected infection are urgently required. In this study, the efficacy of orally administered low doses of benznidazole (BNZ) nanoparticles was evaluated during the acute phase in mice infected with T. cruzi Nicaragua (TcN) that were immunosuppressed during the chronic stage of the disease. Moreover, the production of T. cruzi-specific antibodies, cardiac tissue inflammation and reactive oxygen species generation by Vero cells treated with both BNZ nanoparticles (BNZ-nps) and raw BNZ (R-BNZ) were also evaluated. T. cruzi infected mice treated with 10, 25 or 50 ...
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Chagas disease is a serious parasitic infection caused by Trypanosoma cruzi. Unfortunately, the current chemotherapeutic tools are not enough to combat the infection. The aim of this study was to evaluate the trypanocidal activity of... more
Chagas disease is a serious parasitic infection caused by Trypanosoma cruzi. Unfortunately, the current chemotherapeutic tools are not enough to combat the infection. The aim of this study was to evaluate the trypanocidal activity of benznidazole-loaded microparticles during the acute phase of Chagas infection in an experimental murine model. Microparticles were prepared by spray-drying using copolymers derived from esters of acrylic and methacrylic acids as carriers. Dissolution efficiency of the formulations was up to 3.80-fold greater than that of raw benznidazole. Stability assay showed no significant difference (P > 0.05) in the loading capacity of microparticles for 3 years. Cell cultures showed no visible morphological changes or destabilization of the cell membrane nor haemolysis was observed in defibrinated human blood after microparticles treatment. Mice with acute lethal infection survived 100% after 30 days of treatment with benznidazole microparticles (50 mg kg−1 day...
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Aim: To formulate nanocapsules and nanoemulsions of nitazoxanide (NTZ) and evaluate the metabolic effect on Taenia crassiceps cysticerci inoculated intracranially into mice. Materials & methods: NTZ nanosystems were formulated through... more
Aim: To formulate nanocapsules and nanoemulsions of nitazoxanide (NTZ) and evaluate the metabolic effect on Taenia crassiceps cysticerci inoculated intracranially into mice. Materials & methods: NTZ nanosystems were formulated through solvent diffusion methodology. These nanoformulations were administered perorally and their impact on glycolysis, the tricarboxylic acid cycle and fatty acid metabolism in T. crassiceps cysticerci was investigated. Results: Gluconeogenesis and protein catabolism were significantly increased by the nanoformulations when compared with the control group and the NTZ-treated group. All the other metabolic pathways were inhibited by the nanoformulation treatments. Conclusion: The remarkable metabolic modifications that occur in this in vivo model through the application of these developed nanosystems confirm their capability to deliver NTZ into targeted tissues.
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Triclabendazole is the first-line drug of choice to treat and control fasciolasis, a neglected parasitic human disease. It is a class II/IV compound according to the Biopharmaceutics Classification System. Thus, the aim of this study was... more
Triclabendazole is the first-line drug of choice to treat and control fasciolasis, a neglected parasitic human disease. It is a class II/IV compound according to the Biopharmaceutics Classification System. Thus, the aim of this study was to improve aqueous solubility and dissolution rate of triclabendazole complexed with 2-hydroxylpropyl-β-cyclodextrin (HP-β-CD) and methyl-β-cyclodextrin (Me-β-CD) at 1:1 and 1:2 M ratio. The impact of storage on the solubility, dissolution profile, and solid-state properties of such complexes was also investigated. Drug-carrier interactions were characterized by infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry, and scanning electron microscopy. The solubility of triclabendazole improved up to 256- and 341-fold using HP-β-CD and Me-β-CD, respectively. In particular, the drug complexed with Me-β-CD showed a positive deviation from linearity, suggesting that its solubility increases with an increasing concentration of Me-β...
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Praziquantel (PZQ) is the recommended, effective, and safe treatment against all forms of schistosomiasis. Solid dispersions (SDs) in water-soluble polymers have been reported to increase solubility and bioavailability of poorly... more
Praziquantel (PZQ) is the recommended, effective, and safe treatment against all forms of schistosomiasis. Solid dispersions (SDs) in water-soluble polymers have been reported to increase solubility and bioavailability of poorly water-soluble drugs like PZQ, generally due to the amorphous form stabilization. In this work, poloxamer (PLX) 237 and poly(vinylpyrrolidone) (PVP) K30 were evaluated as potential carriers to revert PZQ crystallization. Binary and ternary SDs were prepared by the solvent evaporation method. PZQ solubility increased similarly with PLX either as binary physical mixtures or SDs. Such unpredicted data correlated well with crystalline PZQ and PLX as detected by solid-state NMR (ssNMR) and differential scanning calorimetry in those samples. Ternary PVP/PLX/PZQ SDs showed both ssNMR broad and narrow superimposed signals, thus revealing the presence of amorphous and crystalline PZQ, respectively, and exhibited the highest PZQ dissolution efficiency (up to 82% at 180...
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Sterosomes (STEs), a new and promising non-phospholipidic liposome platform based on palmitic acid (PA) and cholesterol (Chol) mixtures, need to have polyethylene glycol (PEG) chains grafted to their surface in order to obtain... more
Sterosomes (STEs), a new and promising non-phospholipidic liposome platform based on palmitic acid (PA) and cholesterol (Chol) mixtures, need to have polyethylene glycol (PEG) chains grafted to their surface in order to obtain long-circulating nanocarriers in the blood stream. A post-insertion method was chosen to achieve this modification. The post-insertion process of PEG-modified distearoylphosphoethanolamine (DSPE-PEG) was monitored using the zeta potential value of STEs. Various conditions including PEG chain length and the DSPE-PEG/PA-Chol ratio, were explored. Zeta potential of STEs changed from about -40mV for non-modified STEs to values close to 0 mV by the end of the process, i.e. for PEG-modified STEs. The kinetics of DSPE-PEG insertion and the stability of the resulting PEG-modified STEs were not considerably influenced, within the investigated range, by changes in PEG chain lengths and in DSPE-PEG/PA-Chol proportion. The post-insertion of PEG chains reduced in vitro com...