Liposomes/niosomes For Vaginal Drug Delivery

The liposomes/niosomes for vaginal drug delivery system containing two main parts were investigated. The first part studied was mainly on the lipophilic model drug-clotrimazole loaded-liposomes/niosomes preparation, properties and in vitro/in vivo characterization. The second part investigated was on the hydrophilic drug-insulin niosomes preparation and in vitro/in vivo characterization.Firstly, 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, and the accumulation of clotrimazole into the mucosa was increased, as compared with control during 24 h. In addition, the prepared liposomes/niosomes were incorporated into 2 % carbopol gel and the systems were evaluated for drug stability and evaluated by antifungal activity and tolerability on tissue level in rat.Secondly, clotrimazole-containing proliposomes were prepared by penetrating an ethanol solution of CT and Egg phosphatidylcholine (PC) into microporous sorbitol particles, followed by vacuum evaporation of the solvent. The result in scanning electronic micrograph confirmed the formation of liposomes structures from proliposomes. The proliposomes system can provide sustaining release in simulated vaginal fluid at 37±1°C for 24 h. In-vivo performance of blank proliposomes, a physical mixture of sorbitol and drug, clotrimazole proliposomes and commercial ointment formulation were evaluated using antifungal activity test. In addition, CT-proliposomes did not affect the morphology of vaginal tissues. Therefore, the dosage form might be further developed for safe, convenient, and effective treatment of vaginal candidasis with reduced dosing interval.