Pandya Nidhi, Singh Prabha
SVKMs Dr. Bhanuben Nanavati College of Pharmacy, Gate No. 1, Mithibai College Campus, Vaikunthlal Mehta Road, Vile Parle West, Mumbai, 400056, Maharashtra, India.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Mar;398(3):3093-3101. doi: 10.1007/s00210-024-03420-0. Epub 2024 Sep 30.
This study aims to enhance the oral bioavailability of atazanavir sulphate, a human immunodeficiency virus-1 protease inhibitor known for its poor oral absorption, by formulating mixed micelles using Soluplus® and Kolliphor HS 15. Mixed micelles were prepared through the thin film hydration technique. The micelles were characterized for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, drug loading, and confirmed for atazanavir sulphate encapsulation via FTIR studies. In vitro release studies were conducted, and the morphology of the micelles was examined using TEM. Atazanavir sulphate mixed micelles exhibited a particle size of 62.92 nm, PDI of 0.221, zeta potential of - 17.8 mV, high entrapment efficiency (99.76 ± 1.06), and drug loading (14 ± 0.82). In vitro release studies demonstrated sustained release up to 12 h, with maximum solubility observed at 2 h under pH 1.2 conditions. TEM analysis revealed spherical micelle morphology. Oral administration of atazanavir sulphate mixed micelles showed a 1.23-fold increase in relative bioavailability compared to pure drug suspension. The formulation of mixed micelles using Soluplus® and Kolliphor HS 15 offers a promising strategy to improve the oral bioavailability of atazanavir sulphate. These findings suggest the potential utility of mixed micelles as an effective delivery system for atazanavir sulphate, offering enhanced therapeutic outcomes for patients.
本研究旨在通过使用固体分散体辅料（Soluplus®）和聚氧乙烯氢化蓖麻油15（Kolliphor HS 15）制备混合胶束，提高硫酸阿扎那韦的口服生物利用度。硫酸阿扎那韦是一种已知口服吸收较差的人类免疫缺陷病毒1型蛋白酶抑制剂。混合胶束通过薄膜水化技术制备。对胶束进行了粒径、多分散指数（PDI）、zeta电位、包封率、载药量的表征，并通过傅里叶变换红外光谱（FTIR）研究确认了硫酸阿扎那韦的包封情况。进行了体外释放研究，并使用透射电子显微镜（TEM）检查了胶束的形态。硫酸阿扎那韦混合胶束的粒径为62.92 nm，PDI为0.221，zeta电位为 -17.8 mV，包封率高（99.76±1.06），载药量为（14±0.82）。体外释放研究表明，在pH 1.2条件下，可持续释放长达12小时，在2小时时观察到最大溶解度。TEM分析显示为球形胶束形态。与纯药物悬浮液相比，口服硫酸阿扎那韦混合胶束的相对生物利用度提高了1.23倍。使用固体分散体辅料（Soluplus®）和聚氧乙烯氢化蓖麻油15（Kolliphor HS 15）制备混合胶束为提高硫酸阿扎那韦的口服生物利用度提供了一种有前景的策略。这些发现表明混合胶束作为硫酸阿扎那韦有效递送系统的潜在效用，可为患者带来更好的治疗效果。
