Preparation and in vitro evaluation of liposomal/niosomal delivery systems for antifungal drug clotrimazole.
Clotrimazole, an imidazole derivative antifungal agent is widely used for the treatment of mycotic infections of the genitourinary tract. In order 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 regards to size and entrapment efficiency, multilamellar liposomes/niosomes containing drug were prepared by lipid hydration method. The ability of the systems to deliver clotrimazole into and through the mucosa was evaluated in vitro using rabbit vaginal mucosa with vertical Franz diffusion cells. The in vitro permeation data showed that the liposomes/niosomes system increased the clotrimazole total penetration through the vaginal mucosa by 1.6, 1.5-fold, the accumulation of clotrimazole into the mucosa was increased by 3.1, 2.3-fold, respectively, as compared with control during 24 hr. These results suggest that the studied liposomes/niosomes systems may be appropriate vesicles for the vaginal mucosa delivery of clotrimazole for local vaginal therapy.
Ning
Meiying
M
Beijing Medical University, Beijing, China. mayning999@yahoo.com.cn
Gu
Zhongwei
Z
Pan
Huaizhong
H
Yu
Heming
H
Xiao
Kai
K
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D003022:Clotrimazole / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D004355:Drug Stability; D005260:Female; D066298:In Vitro Techniques; D008081:Liposomes; D009092:Mucous Membrane / Q000378:metabolism; D010316:Particle Size; D010539:Permeability; D011817:Rabbits; D012995:Solubility; D014621:Vagina / Q000378:metabolism*
D000935:Antifungal Agents; D008081:Liposomes; D003022:Clotrimazole