Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis

The purpose of this study was to design a novel vaginal delivery system composed of metronidazole microspheres dispersed within a bioadhesive gel. Microspheres were prepared by solvent evaporation method using Eudragit RS-100 and RL-100 polymers with different drug/polymer ratios. Microspheres were characterized by SEM, DSC, FT-IR and particle size analysis and evaluated for morphology, drug loading and in vitro drug release in simulated vaginal fluid. The % yield, actual drug loading and encapsulation were found to range between 79 ± 0.5 to 94 ± 0.6%, 19.6 ± 0.27 to 35.91 ± 0.66 %, 69.3 ± 0.78 to 81.2 ± 0.36 %, respectively. The FT-IR and DSC spectra revealed that there was no chemical interaction between drug and polymers used. SEM revealed that microspheres were spherical with nearly smooth surface morphology with a mean particle size ranging from 177 ± 0.4 to 456 ± 0.5 µm. The formulation F9 have shown better in vitro release 99 % at 10 h. To achieve bioadhesion to mucosal tissue, formulation F9 was incorporated in the bioadhesive gel made of carbopol 934P. Metronidazole microspheres gel (MTZMG) was characterized by in vitro drug release and antifungal activity. The drug release was controlled up to12 h. Inhibition effect on the C. albicans j1012 growth, suggested their effectiveness in the treatment of vaginal candidiasis. It may be concluded from present study that MTZ-MG can be used as a novel delivery system for local therapy of vaginal candidiasis.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation development and evaluation of thermosensitive gel for vaginal drug delivery

A new reversible thermosensitive drug delivery system was designed and prepared by using chitosan and glycerophosphate with or without poly (ethylene glycol) and used as an a carrier for the Miconazole nitrate, an antifungal agent used in the treatment of vaginal fungal infections. The optimum preparative condition was investigated and it was found that the formulation was solution below or at room temperature with low viscosity, and at 37 ºC, transformed to a non-flowing hydrogel. The formulation was evaluated for gelation temperature, gelation time, drug-polymer compatibility, drug content uniformity, viscosity, in vitro drug release profile and stability studies. The release of loaded Miconazole nitrate from the hydrogel was significantly sustained and the effect of PEG-4000 and Glycerophosphate concentration on release rate was observed. The results showed that the formed hydrogel is a controlled release carrier, which will favour its use as an improved vaginal drug delivery system.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis

The purpose of this study was to design a novel vaginal delivery system composed of metronidazole microspheres dispersed within a bioadhesive gel. Microspheres were prepared by solvent evaporation method using Eudragit RS-100 and RL-100 polymers with different drug/polymer ratios. Microspheres were characterized by SEM, DSC, FT-IR and particle size analysis and evaluated for morphology, drug loading and in vitro drug release in simulated vaginal fluid. The % yield, actual drug loading and encapsulation were found to range between 79 ± 0.5 to 94 ± 0.6%, 19.6 ± 0.27 to 35.91 ± 0.66 %, 69.3 ± 0.78 to 81.2 ± 0.36 %, respectively. The FT-IR and DSC spectra revealed that there was no chemical interaction between drug and polymers used. SEM revealed that microspheres were spherical with nearly smooth surface morphology with a mean particle size ranging from 177 ± 0.4 to 456 ± 0.5 µm. The formulation F9 have shown better in vitro release 99 % at 10 h. To achieve bioadhesion to mucosal tissue, formulation F9 was incorporated in the bioadhesive gel made of carbopol 934P. Metronidazole microspheres gel (MTZMG) was characterized by in vitro drug release and antifungal activity. The drug release was controlled up to12 h. Inhibition effect on the C. albicans j1012 growth, suggested their effectiveness in the treatment of vaginal candidiasis. It may be concluded from present study that MTZ-MG can be used as a novel delivery system for local therapy of vaginal candidiasis.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Porozne nanočestice metoprolol tartarata dobivene pomoću sušenja sprejanjem: Razvoj, karakterizacija i evaluacija in vitro

The present investigation was undertaken to fabricate porous nanoparticles of metoprolol tartrate by spray-drying using ammonium carbonate as pore former. Prepared nanoparticles were coated with Eudragit S100 polymer in order to prevent the release of metoprolol tartrate in the upper GI tract. It was shown that nanoparticles with low size ranges can be obtained with a low feed inlet rate. Micromeritic studies confirmed that nanoparticle batches are discrete and free flowing. Effects of the pore former on drug loading, porosity and in vitro release were studied. It was found that there was an increase in drug loading and porosity with increased the amount of pore former. In vitro drug release studies showed that an increase in pore former made drug release faster. Release kinetics proved that nanoparticles follow a zero-order release mechanism.U radu je opisana priprava poroznih nanočestica metoprolol tartarata pomoću sušenja sprejanjem, koristeći amonijev karbonat za stvaranje pora. Da bi se spriječilo oslobađanje metoprolol tartarata u gornjem dijelu GI trakta, nanočestice su obložene polimerom Eudragit S100. Nanočestice podjednake veličine mogu se dobiti polaganim uklapanjem ljekovite tvari. Mikromeričke studije potvrdile su da su nanočestice zasebne i tečne. Proučavan je utjecaj sredstva za stvaranje pora na količinu uklopljenog lijeka, poroznost i in vitro oslobađanje. Povećanje količine sredstva za stvaranje pora povećava količinu uklopljenog lijeka, poroznost i brzinu oslobađanja ljekovite tvari. Oslobađanje metoprolola slijedi kinetiku nultog reda

Formulation and evaluation of chitosan/chondriotin sulphate complex microcapsules for controlled delivery of water soluble drug

Oral route of drug administration is the most preferred route of drug administration but this route has its own limitations like pH of gastric media and controlling release rate of water soluble drug. To overcome these limitations, formulations containing controlled release matrix need to be developed. Controlled release of drug can be achieved by incorporating the drug into a release rate controlling carriers. Chitosan (CH)/Chondroitin Sulphate (CS) complex microcapsules were prepared to encapsulate the cardio vascular drug Propranolol hydrochloride (PHCl) by emulsion-chemical crosslinking method using sodium tripolyphosphate (STPP) as cross-linking agent. The FT-IR and DSC spectra’s revealed that there is no chemical interaction between drug and polymers used. Encapsulation efficiency and in-vitro drug release was found to be 64-84 % and 55-85 % respectively. Among all the formulations the F4.1 showed controlled drug release. This study revealed that the cross linked microcapsules of chitosan and chondroitin sulphate can be used to control drug release rate of water soluble drug.Colegio de Farmacéuticos de la Provincia de Buenos Aire