This research aimed to evaluate a new approach for the preparation of mucoadhesive microparticles and to design an innovative vaginal delivery systems for econazole nitrate (ECN) able to enhance the drug antifungal activity. Different formulations (F1-F7) were prepared by spray-congealing: a lipid-hydrophilic matrix (Gelucire 53/10) was used such as carrier and several mucoadhesive polymers as chitosan, sodium carboxymethylcellulose and poloxamers (Lutrol F68 and F127) were added. All microparticles were characterized and compared for morphology, particle size, drug loading and solubility in simulated vaginal fluid, bioadhesion to mucosal tissue, dissolution behaviour and for their physicochemical properties. The antifungal activity of the microparticles against a strain of Candida albicans was also investigated. Non-aggregated microspheres with prevalent size in the range 100-355 micron were obtained. Both poloxamers significantly (p=0.001) improved the solubility and in vitro bioavailability of the low solubility drug and the mucoadhesive strength. Poloxamers/Gelucire based microparticles exhibited an inhibition effect on the Candida albicans growth, suggesting their use as an affective treatment of vaginal candidiasis, with potential for reduced administration frequency. In conclusion the results demonstrated that spray congealing technology can be considered a novel and solvent free approach for the production of mucoadhesive microparticles for the vaginal delivery of ECN.
Mucoadhesive microspheres prepared by spray-congealing for the vaginal delivery of econazole nitrate / B. Albertini; N. Passerini; M. Di Sabatino; B. Vitali; P. Brigidi; L. Rodriguez. - ELETTRONICO. - (2008). (Intervento presentato al convegno 6th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology tenutosi a Barcelona nel 7-10 April 2008).
Mucoadhesive microspheres prepared by spray-congealing for the vaginal delivery of econazole nitrate.
ALBERTINI, BEATRICE;PASSERINI, NADIA;DI SABATINO, MARCELLO;VITALI, BEATRICE;BRIGIDI, PATRIZIA;RODRIGUEZ, LORENZO
2008
Abstract
This research aimed to evaluate a new approach for the preparation of mucoadhesive microparticles and to design an innovative vaginal delivery systems for econazole nitrate (ECN) able to enhance the drug antifungal activity. Different formulations (F1-F7) were prepared by spray-congealing: a lipid-hydrophilic matrix (Gelucire 53/10) was used such as carrier and several mucoadhesive polymers as chitosan, sodium carboxymethylcellulose and poloxamers (Lutrol F68 and F127) were added. All microparticles were characterized and compared for morphology, particle size, drug loading and solubility in simulated vaginal fluid, bioadhesion to mucosal tissue, dissolution behaviour and for their physicochemical properties. The antifungal activity of the microparticles against a strain of Candida albicans was also investigated. Non-aggregated microspheres with prevalent size in the range 100-355 micron were obtained. Both poloxamers significantly (p=0.001) improved the solubility and in vitro bioavailability of the low solubility drug and the mucoadhesive strength. Poloxamers/Gelucire based microparticles exhibited an inhibition effect on the Candida albicans growth, suggesting their use as an affective treatment of vaginal candidiasis, with potential for reduced administration frequency. In conclusion the results demonstrated that spray congealing technology can be considered a novel and solvent free approach for the production of mucoadhesive microparticles for the vaginal delivery of ECN.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
