Characterisation and in vitro evaluation of bioadhesive liposome gels for local therapy of vaginitis.
The purpose of this study was to design and evaluate a new vaginal delivery system for the local treatment of vaginitis. Liposomes containing two commonly applied drugs in the treatment of vaginal infections, namely clotrimazole and metronidazole, were prepared by the proliposome and the polyol dilution methods. Both types of liposomes were characterised and compared for particle size, polydispersity, entrapment efficiency, and tested for in vitro stability in media that mimic human vaginal conditions (buffer, pH 4.5, and vaginal fluid simulant). To achieve application viscosity and to further improve their stability, liposomes containing drugs were incorporated in a bioadhesive gel made of Carbopol 974P NF resin. In vitro release studies have demonstrated that even after 24 h of incubation in vaginal fluid simulant (at 37 degrees C) more than 30% of the originally entrapped clotrimazole (or 50% of metronidazole) was still retained in the gel. Storage stability studies have proved the ability of Carbopol 974P NF gel to preserve original size distributions of incorporated liposomes. All the performed experiments confirm the applicability of bioadhesive liposome gels as a novel delivery system for local therapy of vaginal infections.
Pavelić
Zeljka
Z
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovacića 1, P.O. Box 156, 10000 Zagreb, Croatia. zpavelic@pharma.hr
Skalko-Basnet
Natasa
N
Jalsenjak
Ivan
I
D000179:Acrylates; D000282:Administration, Intravaginal; D000935:Antifungal Agents / Q000008:administration & dosage; D003022:Clotrimazole / Q000008:administration & dosage; D004339:Drug Compounding; D004355:Drug Stability; D004356:Drug Storage; D005079:Excipients; D005260:Female; D005782:Gels; D006801:Humans; D008081:Liposomes / Q000737:chemistry*; D008795:Metronidazole / Q000008:administration & dosage; D010316:Particle Size; D014014:Tissue Adhesives; D014627:Vaginitis / Q000188:drug therapy*; D014783:Viscosity
D000179:Acrylates; D000935:Antifungal Agents; D005079:Excipients; D005782:Gels; D008081:Liposomes; D014014:Tissue Adhesives; C117167:carbopol 974P NF; D008795:Metronidazole; D003022:Clotrimazole