Effect of Cholesterol and Oleic Acid on Physicochemical Properties and Stability of Liposomes

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Sureewan Duangjit
Thanattha Inta
Pattaraporn Ruangkarnjanapaisarn
Wandee Rungseevijitprapa

Abstract

Introduction: For a few decades, the applications of liposomes to enhance transdermal drug delivery have evoked considerable interest. It has been known that the presence of cholesterol in liposomes is necessary in order to increase membrane rigidity. However, cholesterol could disrupt local packing orders of the fluid bilayers and decrease the skin penetration. The addition of oleic acid as skin penetration enhancer to liposomes is also known as transfersomes, but their effect on physicochemical properties and stability on the system is not yet to be elucidated. The objective 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. Method: Investigated formulations composed of phosphatidylcholine, ellagic acid (as a model drug) and various cholesterol (as a membrane stabilizer) and oleic acid (as a penetration enhancer) at 0-90 %mol were experimentally formulated and characterized for size, size distribution, zeta potential and entrapment efficiency. Physicochemical stability assessment of the tested formulations were subjected to accelerated condition of heating-cooling cycles at 45 °C for 12 h and 4 °C for 12 h, for 3 cycles. The data obtained were analyzed using conventional experimental and computational method. Results: Results indicated that cholesterol and oleic acid significantly affected the physicochemical properties and the stability of the formulations. The computational method showed the relationship between cholesterol and oleic acid on the vesicle characteristics was more markedly than the conventional experimental method. The computational method suggested the optimal formulation with proper physicochemical properties and stability was found out at cholesterol and oleic acid %mol ratio of 40:40 which was comparable to that of the experimental values. Conclusion: The addition of cholesterol and oleic acid affected physicochemical properties as well as stability of liposomes. The design of experiment used in this study was useful and suggestive for further liposome formulations development.

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Pharmaceutical Sciences

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