Efavirenz (EFZ) is a biopharmaceutics classification system (BCS) Class-II, first-line antiretroviral (ARV) drug. However, its utility through the oral route is restricted by its poor solubility. The objective of this study was to formulate EFZ-loaded binary-mixed micelles as a potential carrier for oral administration of EFZ. Rubingh's regular solution theory was used to determine the interaction behavior of the two components (Cremophor RH 40 and Phospholipon 80H) and of the mixed micelles and synergistic behavior was confirmed. The mixed miceller system was formulated using solvent evaporation method and a 3² factorial design was used for the optimization of selected independent variables. Miceller systems were further characterized in terms of morphology, particle size, zeta potential, percent entrapment efficiency, and drug loading. Fourier transform infrared and differential scanning calorimetry measurements confirmed the entrapment of EFZ in the micelles. The optimized formulation presented desirable qualities viz., nanometric size (17.27 ± 0.079), high entrapment efficiency, and good colloidal stability. The prepared optimized micelles can be potential carriers for EFZ in ARV therapies.

中文翻译：

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依法韦仑负载混合聚合物胶束：配方、优化和体外表征

依法韦仑 (EFZ) 是一种生物药剂学分类系统 (BCS) II 类、一线抗逆转录病毒 (ARV) 药物。然而，其通过口服途径的效用受到其较差的溶解性的限制。本研究的目的是制定负载 EFZ 的二元混合胶束作为口服 EFZ 的潜在载体。Rubingh 的正则溶液理论用于确定两种组分（Cremophor RH 40 和 Phospholipon 80H）和混合胶束的相互作用行为，并确认了协同行为。混合胶束系统采用溶剂蒸发法和 3 ²因子设计用于优化选定的自变量。胶束系统在形态、粒径、zeta 电位、截留效率百分比和载药量方面进行了进一步的表征。傅里叶变换红外和差示扫描量热测量证实了 EFZ 在胶束中的截留。优化后的配方呈现出理想的品质，即纳米尺寸 (17.27 ± 0.079)、高包封率和良好的胶体稳定性。制备的优化胶束可以成为抗病毒治疗中 EFZ 的潜在载体。