A chitosan lactate/poloxamer 407-based matrix containing Eudragit RS microparticles for vaginal delivery of econazole: design and in vitro evaluation
| Autor: | Sara Baldassari, Eleonora Russo, Sergio Cafaggi, Noemi Gaglianone, Brunella Parodi, Gabriele Caviglioli, Anna Maria Schito |
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| Jazyk: | angličtina |
| Rok vydání: | 2013 |
| Předmět: |
Time Factors
Econazole Antifungal Agents Stereochemistry Kinetics Antifungal drug Acrylic Resins Pharmaceutical Science Poloxamer Chitosan chemistry.chemical_compound Drug Delivery Systems Drug Discovery Candida albicans medicine Mucoadhesion Lactic Acid Pharmacology Drug Carriers Calorimetry Differential Scanning Chemistry Organic Chemistry Adhesiveness Controlled release Microspheres Administration Intravaginal Delayed-Action Preparations Poloxamer 407 Emulsions Swelling medicine.symptom medicine.drug Nuclear chemistry |
| Popis: | A matrix based on chitosan lactate and poloxamer 407 was evaluated as a delivery system for the vaginal administration of the antifungal drug econazole. The matrix was investigated both containing the pure drug and after introducing microparticles of Eudragit RS 100 containing econazole. Eudragit RS 100 microparticles were prepared using an emulsion-extraction method and dispersed in a solution containing chitosan lactate (2% w/w) and poloxamer 407 (1.7% w/w). The microparticles, obtained with a yield of 64% w/w and an encapsulation efficiency of 42% w/w, had a diameter of less than 2 μm and a drug loading of 13% w/w. The compressed matrices, characterized by DSC, swelling, erosion, release and mucoadhesion studies, had behaviours dependent on the relative amounts of the contained microparticles. The matrix without microparticles (MECN) showed zero-order release kinetics, with a maximum drug-release of 60% w/w, while those containing 50 or 75% w/w microparticles showed a diffusion controlled release up to 8 and 16 h, respectively, and a linear trend after those time intervals, caused by the erosion process, which allowed reaching a drug-release of approximately 100% w/w at 22 h. In in vitro experiments, the matrices were mucoadhesive and active in inhibiting the growth of Candida albicans 796. |
| Databáze: | OpenAIRE |
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