Liposomes containing drugs for treatment of vaginal infections.
To develop a novel vaginal delivery system, able to effectively deliver entrapped drugs during an extended period of time at the site of action, liposomes made of phosphatidylcholine were prepared by two different methods, namely the polyol dilution method and the proliposome method. Liposomes containing three commonly applied drugs in the treatment of vaginal infections: clotrimazole, metronidazole and chloramphenicol were tested for in vitro stability (in buffers at pH 4.5 and 5.9 representing pre- and postmenopausal vaginal pH). In situ stability (in the presence of cow vaginal mucosa) showed that after 6 h incubation (at 37 degrees C), liposomes retained more than 40% of originally entrapped clotrimazole, 28% of entrapped metronidazole or 37% of entrapped chloramphenicol. In vitro and in situ stability studies confirmed the applicability of liposomes as a carrier system for vaginal delivery. Even after 24 h of incubation in the presence of vaginal mucosa liposomes retained sufficient amounts of entrapped drugs.
Pavelić
Z
Z
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.
Skalko-Basnet
N
N
Jalsenjak
I
I
D000282:Administration, Intravaginal; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000737:chemistry; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage* / Q000737:chemistry; D002417:Cattle; D002701:Chloramphenicol / Q000008:administration & dosage* / Q000737:chemistry; D003022:Clotrimazole / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005260:Female; D006863:Hydrogen-Ion Concentration; D008081:Liposomes; D008795:Metronidazole / Q000008:administration & dosage* / Q000737:chemistry; D009175:Mycoplasma Infections / Q000188:drug therapy; D010713:Phosphatidylcholines / Q000008:administration & dosage / Q000737:chemistry; D016585:Vaginosis, Bacterial / Q000188:drug therapy* / Q000378:metabolism
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000891:Anti-Infective Agents, Local; D004337:Drug Carriers; D008081:Liposomes; D010713:Phosphatidylcholines; D008795:Metronidazole; D002701:Chloramphenicol; C010942:1,2-distearoyllecithin; D003022:Clotrimazole