Singh Archu, Neupane Yub Raj, Panda Bibhu Prasad, Kohli Kanchan
a Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , New Delhi , India.
b Microbial and Pharmaceutical Biotechnology Laboratory , Centre for Advanced Research in Pharmaceutical Science, Jamia Hamdard , New Delhi , India.
J Microencapsul. 2017 Jun;34(4):416-429. doi: 10.1080/02652048.2017.1340355. Epub 2017 Jun 26.
This study aims at developing an optimised nanostructured lipid carrier (NLC) of lycopene for efficient absorption following oral administration. The optimised formulation showed an average particle size of 121.9 ± 3.66 nm, polydispersity index (PDI) 0.370 ± 0.97 and zeta potential -29.0 ± 0.83 mV. Encapsulation Efficiency (% EE) and drug loading (% DL) was found to be 84.50% ± 4.38 and 9.54% ± 2.65, respectively. In vitro release studies demonstrated the burst release within 4-9 h followed by sustained release over 48 h. The IC value of lycopene extract and optimised NLC for ABTS were found to be 172.37 μg Trolox equivalent and 184.17 μg Trolox equivalent whereas, for DPPH, 117.76 μg Trolox equivalent and 143.08 μg Trolox equivalent respectively. Ex vivo studies and MTT assay revealed that the NLC had better permeation and cause sufficiently more cytotoxicity as compared to drug extract due to higher bioavailability and greater penetration.
本研究旨在开发一种用于口服后高效吸收的番茄红素优化纳米结构脂质载体（NLC）。优化后的制剂平均粒径为121.9±3.66nm，多分散指数（PDI）为0.370±0.97，ζ电位为-29.0±0.83mV。包封率（%EE）和载药量（%DL）分别为84.50%±4.38和9.54%±2.65。体外释放研究表明，在4-9小时内有突发释放，随后在48小时内持续释放。番茄红素提取物和优化后的NLC对ABTS的IC值分别为172.37μg Trolox当量和184.17μg Trolox当量，而对DPPH的IC值分别为117.76μg Trolox当量和143.08μg Trolox当量。体外研究和MTT分析表明，由于生物利用度更高和渗透性更强，与药物提取物相比，NLC具有更好的渗透性并能引起足够多的细胞毒性。
