Preparation, in vitro and in vivo evaluation of liposomal/niosomal gel delivery systems for clotrimazole.
Clotrimazole, which is an imidazole derivative antifungal agent, was widely used for the treatment of mycotic infections of the genitourinary tract. To develop alternative formulation for the vaginal administration of clotrimazole to provide sustained and controlled release of appropriate drug for local vaginal therapy, liposomes/niosomes were evaluated as delivery vehicles. To optimize the preparation of liposomes/niosomes with regard to size and entrapment efficiency, multilamellar liposomes/niosomes containing drug were prepared by lipid hydration method. The prepared liposomes/niosomes were incorporated into 2% carbopol gel, and the systems were evaluated for drug stability in phosphate-buffered saline (pH 7.4) and simulated vaginal fluid at 37 +/- 1 degrees C. Further, the vesicle gel system was evaluated by antifungal activity and tolerability on tissue level in rat.
Ning
Meiying
M
Centre of Drug Controlled Release Research, National Research Institute for Family Planning, Da Hui Si Haidian District, Beijing, PR China. mayning999@yahoo.com.cn
Guo
Yingzhi
Y
Pan
Huaizhong
H
Chen
Xianli
X
Gu
Zhongwei
Z
D000180:Acrylic Resins; D000282:Administration, Intravaginal; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D002177:Candidiasis / Q000188:drug therapy; D003022:Clotrimazole / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D004356:Drug Storage / Q000379:methods; D005260:Female; D005782:Gels / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000737:chemistry; D008826:Microbial Sensitivity Tests / Q000379:methods; D010316:Particle Size; D011145:Polyvinyls / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D014621:Vagina / Q000187:drug effects / Q000382:microbiology / Q000473:pathology
D000180:Acrylic Resins; D000935:Antifungal Agents; D004337:Drug Carriers; D005782:Gels; D008081:Liposomes; D011145:Polyvinyls; C006912:carboxypolymethylene; D003022:Clotrimazole