Beg Sarwar, Jain Sanyog, Kushwah Varun, Bhatti Gurjit Kaur, Sandhu Premjeet Singh, Katare O P, Singh Bhupinder
University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India.
Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Mohali 160 062, Punjab, India.
Nanomedicine (Lond). 2017 Feb;12(4):333-356. doi: 10.2217/nnm-2016-0336. Epub 2017 Jan 17.
The present studies describe Quality by Design-oriented development and characterization of surface-engineered solid lipid nanoparticles (SLNs) of rosuvastatin calcium for low density lipoprotein-receptor targeting.
MATERIALS & METHODS: SLNs were systematically prepared employing Compritol 888 and Tween-80. Surface modification of SLNs was accomplished with Phospholipon 90G and DSPE-mPEG-2000 as the ligands for specific targeting to the low density lipoprotein-receptors. SLNs were evaluated for size, potential, entrapment, drug release performance and gastric stability. Also, the formulations were evaluated for cellular cytotoxicity, uptake and permeability, pharmacokinetic, pharmacodynamic and biochemical studies.
RESULTS & CONCLUSION: Overall, the studies ratified enhanced biopharmaceutical performance of the surface-engineered SLNs of rosuvastatin as a novel approach for the management of hyperlipidemia-like conditions.
本研究描述了以设计质量为导向开发和表征用于靶向低密度脂蛋白受体的瑞舒伐他汀钙表面工程化固体脂质纳米粒（SLNs）。
采用Compritol 888和吐温80系统地制备SLNs。以磷脂90G和DSPE - mPEG - 2000作为特异性靶向低密度脂蛋白受体的配体对SLNs进行表面修饰。对SLNs的粒径、电位、包封率、药物释放性能和胃稳定性进行评估。此外，还对制剂进行了细胞毒性、摄取和通透性、药代动力学、药效学和生化研究。
总体而言，这些研究证实了瑞舒伐他汀表面工程化SLNs具有增强的生物药剂学性能，是一种治疗高脂血症样病症的新方法。
