Rai Nadia, Madni Asadullah, Faisal Amir, Jamshaid Talha, Khan Muhammad Imran, Khan Muhammad Muzamil, Parveen Farzana
Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur 63100, Bahawalpur,Pakistan.
Department of Biology, Lahore University of Management Sciences, Lahore,Pakistan.
Curr Drug Deliv. 2021;18(9):1368-1376. doi: 10.2174/1567201818666210203180153.
Solid lipid nanoparticles (SLNs) is the drug delivery system that has the capability to improve drug release at the desired tumor site. The aim of the present study is to develop glyceryl monostearate (GMS) based SLNs for the controlled delivery of docetaxel.
Hot melt encapsulation (HME) method was employed avoiding the use of organic solvents and, therefore, regarded as green synthesis of SLNs.
Optimized DTX-SLNs showed desirable size (100 nm) with low poly dispersity index and excellent entrapment efficiency. Surface charge confirmed the stability of formulation. transmission electron microscope (TEM) analysis showed spherical shaped particles and fourier transform infrared microscopy (FTIR) revealed compatibility among formulation excipients. Differential scanning calorimeter (DSC) analysis revealed that the melting transition peak of optimized formulation was also greater than 40°C indicating that SLNs would be solid at body temperature. In-vitro release profile (68% in 24 hours) revealed the controlled release profile of DTX-SLNs, indicating lipophilic docetaxel drug was entrapped inside high melting point lipid core. Cytotoxicity study revealed that blank SLNs were found to be biocompatible while dose dependent cytotoxicity was shown by DTX-SLNs.
These studies suggest that DTX-SLNs have the potential for controlled delivery of docetaxel and improved therapeutic outcome.
固体脂质纳米粒(SLNs)是一种能够改善药物在理想肿瘤部位释放的药物递送系统。本研究的目的是开发基于单硬脂酸甘油酯(GMS)的固体脂质纳米粒用于多西他赛的控释。
采用热熔包封(HME)法,避免使用有机溶剂,因此被视为固体脂质纳米粒的绿色合成方法。
优化后的多西他赛固体脂质纳米粒(DTX-SLNs)呈现出理想的粒径(100 nm)、低多分散指数和优异的包封率。表面电荷证实了制剂的稳定性。透射电子显微镜(TEM)分析显示为球形颗粒,傅里叶变换红外显微镜(FTIR)揭示了制剂辅料之间的相容性。差示扫描量热仪(DSC)分析表明,优化制剂的熔融转变峰也大于40°C,表明固体脂质纳米粒在体温下为固体。体外释放曲线(24小时内释放68%)显示了多西他赛固体脂质纳米粒的控释特性,表明亲脂性的多西他赛药物被包裹在高熔点脂质核内。细胞毒性研究表明,空白固体脂质纳米粒具有生物相容性,而多西他赛固体脂质纳米粒表现出剂量依赖性细胞毒性。
这些研究表明,多西他赛固体脂质纳米粒具有多西他赛控释和改善治疗效果的潜力。