Fabrication and Characterization of Triterpenoid Oleanolic Acid NIOSOMES

Abstract

Introduction: Phytoconstituents, derived from plants, exhibit diverse pharmacological activities; however, their medical application is frequently impeded by challenges such as poor solubility, limited bioavailability, rapid metabolism, and inadequate targeting to specific sites of action. Oleanolic acid (OA), a natural triterpenoid compound abundant in various plants such as olive oil, garlic, and apples, has emerged as a focal point in cancer research, particularly in the realm of liver cancer therapy. However, its application faces several challenges, including low solubility, limited bioavailability, and the emergence of drug resistance mechanisms. To surmount these hurdles, the formulation of niosomes encapsulating oleanolic acid presents a promising strategy, offering a means to enhance solubility, augment bioavailability, and potentially circumvent issues related to drug resistance.

Objectives: Oleanolic acid has a very low water solubility of about 1 ug/mL and poor permeability which usually results in low oral bioavailability and limited use in clinical treatments. Incorporating OA in niosomal vesicular drug delivery system solubility might be increase which result in increase in bioavailability of OA.

Methods: Niosomes of oleanolic acid was prepared by modified ethanol injection followed by solvent evaporation method. A different combination of span 60 and cholesterol were made to obtained optimized niosomes, span 60, Cholesterol and drug were dissolved separately in ethanol. Cholesterol solution was firstly mixed with span 60. The drug solution was then added to surfactant mixture. The resulting mixture was then added in aqueous phase with help of syringe (flow rate 1.5 mL/min) under constant stirring at 800 rpm on magnetic stirrer. The stirring was continued till 4-6 hours for complete removal of organic phase.

Results: Formulated OA loaded niosmoes were characterized for PDI, average particle size, zeta potential and % entrapment efficiency (%EE). On the basis of these parameter a optimized batch is selected. The optimized batch were further used all other characterization such as, SEM, TEM, invitro drug release etc.

Conclusions: OA loaded niosomes were formulated by modified ethanol injection method. The prepared niosomes were characterized using PDI, average particle size, zeta potential and % entrapment efficiency (%EE), SEM, TEM, invitro drug release techniques. The formulated niosomes of OA shows sustained release of drug from niosomal vesicle.