Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier

Drug Delivery

Dandan Liu¹  Cuiyan Han²  Zhihong Zhu³  Huixin Wang³  Mingshuang Sun³  Xinggang Yang³  Lei Tian³  Weisan Pan³ 

[1] School of Biomedical & Chemical Engineering, Liaoning Institute of Science and Technology, Benxi, Chin;School of Pharmacy, Qiqihar Medical University, Qiqihar, China, an;School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China;

关键词: Poly-arginine;    nanostructured lipid carriers;    surface density;    cellular uptake;    tissue distribution;   

DOI  :  10.1080/10717544.2016.1269849

来源: Taylor & Francis

【 摘 要 】

Poly-arginines are strong tools to elevate the cellular uptake of nanopreparations. To learn the influence of poly-arginine (RRRRRRRR, R8) density on a series of properties of nanostructured lipid carrier (NLC), we build six R8 modified NLCs with different R8 densities (nR-NLC, where n represents the R8 ratio) by fusion–emulsion method with the aid of stearyl-R8. The pharmaceutical characteristics like size, zeta potential and in vitro drug release, cellular uptake, cytotoxicity to A549 cells and tissue distribution in S180 tumor-bearing mice of the six nR-NLCs are all investigated. It turns out that with as little as 2% weight ratio of stearyl-R8 modified on NLC, its pharmaceutical properties, especially zeta potential changes astonishingly; however, the stearyl-R8 ratio should be higher than 4% to upgrade the cellular uptake and cytotoxicity evidently; in the ex vivo tissue distribution assessment, the nR-NLC with less than 8% R8 showed similar tissue accumulation, while NLC with 10% R8 shows obvious acute toxicity to mice. Our study pays attention to the effect of the R8 ratio on the changes of cargo properties, and the results indicate that this topic is essential and worth to be further developed.

【 授权许可】

CC BY