Liposomal gel with chloramphenicol: characterisation and in vitro release.
The aim of our study was to develop a liposomal carrier system for the local treatment of bacterial vaginosis, capable to efficiently deliver entrapped drug during an extended period of time. Chloramphenicol was entrapped in liposomes composed of egg phosphatidylcholine/egg phosphatidylgycerol-sodium (9:1, molar ratio) and prepared by two different methods, the proliposome method and the polyol dilution method. Both liposome preparations were characterised and compared for particle size, polydispersity, entrapment efficiency and tested for in vitro stability in media that simulate human vaginal conditions (buffer pH 4.5 and vaginal fluid simulant). To achieve application viscosity of liposomes and to further improve their stability, liposomes prepared by the proliposome method were incorporated in the bioadhesive gel made of Carbopol 974P NF resin. In vitro release studies of liposomes incorporated in the gel have shown a prolonged release of entrapped chloramphenicol compared to control gel. Even after 24 hours of incubation in the vaginal fluid simulant, more than 40% of the originally entrapped drug was still retained in the gel. Storage stability studies have proven the ability of the Carbopol 974P NF gel to preserve the original size distribution of incorporated liposomes. All the performed experiments confirm the applicability of liposomes as a novel drug carrier system for the local treatment of bacterial vaginosis.
Pavelić
Zeljka
Z
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, POB 156, 10000 Zagreb, Croatia. zpavelic@pharma.hr
Skalko-Basnet
Natasa
N
Jalsenjak
Ivan
I
D000282:Administration, Intravaginal; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002701:Chloramphenicol / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005260:Female; D005782:Gels / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D008081:Liposomes / Q000737:chemistry* / Q000493:pharmacokinetics; D016585:Vaginosis, Bacterial / Q000188:drug therapy* / Q000378:metabolism
D000900:Anti-Bacterial Agents; D000891:Anti-Infective Agents, Local; D004337:Drug Carriers; D005782:Gels; D008081:Liposomes; D002701:Chloramphenicol