Gaur Praveen Kumar, Mishra Shikha, Bajpai Meenakshi, Mishra Anushika
Department of Pharmaceutics, I.T.S. Paramedical College (Pharmacy), Muradnagar, Ghaziabad 201206, India.
Department of Pharmacognosy & Phytochemistry, Jamia Hamdard, New Delhi 110062, India.
Biomed Res Int. 2014;2014:363404. doi: 10.1155/2014/363404. Epub 2014 May 21.
Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of 124.5 ± 3.2 nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6-98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C ± 2°C and 75 ± 5% relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration (C max) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).
固体脂质纳米粒是一种高效的基于脂质的药物递送系统，可提高难溶性药物的生物利用度。依非韦伦是一种来自非核苷抑制剂类别的高度亲脂性药物，用于治疗艾滋病病毒。目前的工作阐述了一种用于依非韦伦的具有提高生物利用度的固体脂质纳米粒制剂的开发。首先，选择了合适的脂质成分和表面活性剂。制备了固体脂质纳米粒并对其物理参数、稳定性和药代动力学特征进行了分析。以单硬脂酸甘油酯为主要脂质、吐温80为表面活性剂制备了载依非韦伦的固体脂质纳米粒。ESLN-3的平均粒径为124.5±3.2纳米，多分散指数值为0.234，zeta电位为负，药物包封率为86%。体外药物释放研究表明，各种固体脂质纳米粒制剂在24小时内的药物释放率为60.6 - 98.22%。优化后的固体脂质纳米粒在40°C±2°C和75±5%相对湿度（RH）条件下180天显示出良好的稳定性。与依非韦伦混悬液（ES）相比，ESLN-3的血浆峰浓度（Cmax）增加了5.32倍，曲线下面积（AUC）增加了10.98倍。
