Abstract

Title : THE ROLE OF CHOLESTEROL AND PENETRATION ENHANCER ON THE PHYSICOCHEMICAL PROPERTIES AND STABILITY OF LIPOSOMES AND TRANSFERSOMES = COMPARATIVE STUDY
By : THANATTHA INTA,PATTARAPORN RUANGKARNJANAPAISARN
Degree : DOCTOR OF PHARMACY
Advisor : ASSIST.PROF.WANDEE RUNGSEEVIJITPRAPA,Ph.D., SUREEWAN DUANGIT, Ph.D.
Keywords : LIPOSOMES, TRANSFERSOMES, CHOLESTEROL, OLAIC ACID, STABILITY
   
For a few decades, the used of liposomes for transdermal drug delivery has evoked considerable interest. Several studies focus on the use of lipoposomes and transfersomes for enhancing transdermal drug delivery. However, the lipid components in vesicles formulation directly affected the physicochemical properties and stability of formulation. The aim of this study was to investigate the effects of cholesterol and penetration enhancer on the physicochemical properties and the stability of liposome and transfersome formulations. The optimal ratio of cholesterol and penetration enhancer was also optimized for the appropriate physicochemical properties and the stability. Different model formulations of liposomes and transfersomes composed of a phosphatidylcholine (as a lipid bilayer forming agent), cholesterol (Chol) (as a membrane stabilizer), oleic acid (OA) (as a penetration enhancer) and ellagic acid (EA) (as a model drug) were experimentally formulated and characterized for size, size distribution, zeta potential and entrapment efficiency. In stability evaluation, all model formulations were incubated under accelerate condition of 45°C for 12 h and then moved to 4°C for 12 h for 3 cycles. The data obtained from this study were analyzed using conventional comparable and computational method. The results indicated that Chol and OA significantly affected the physicochemical properties and the stability of formulation. The computational method showed the relationship between Chol and OA on vesicle was more markedly than the conventional comparable method. The formulation optimization suggested that the optimal vesicle formulation with proper physicochemical properties and stability containing of 4 mM of Chol and 4mM of OA. Moreover, the experimental values were very close to the values predicted by the computer. Thus, our study succeeded in predicting the effects of Chol and OA on physicochemical properties and stability of vesicle formulation. The design of experiment used in this study was useful for the formulations development.
   
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