A chitosan lactate/poloxamer 407-based matrix containing Eudragit RS microparticles for vaginal delivery of econazole: design and in vitro evaluation.
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.
Dipartimento di Chimica e Tecnologie Farmaceutiche ed Alimentari , Genoa , Italy.
Brunella
B
Parodi
Eleonora
E
Russo
Gabriele
G
Caviglioli
Sara
S
Baldassari
Noemi
N
Gaglianone
Anna Maria
AM
Schito
Sergio
S
Cafaggi
D000180:Acrylic Resins / Q000737:chemistry; D000268:Adhesiveness; D000282:Administration, Intravaginal; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002176:Candida albicans / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004464:Econazole / Q000008:administration & dosage* / Q000494:pharmacology; D004655:Emulsions; D019344:Lactic Acid / Q000737:chemistry; D008863:Microspheres; D020442:Poloxamer / Q000737:chemistry; D013997:Time Factors
D000180:Acrylic Resins; D000935:Antifungal Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D020442:Poloxamer; C050528:Eudragit RS; D019344:Lactic Acid; D004464:Econazole; D048271:Chitosan