Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier
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 th...
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doaj-dbf67dc1c96d468e823b51a7b1acde912020-11-25T02:53:11ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642017-01-0124151952610.1080/10717544.2016.12698491269849Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrierMingshuang Sun0Zhihong Zhu1Huixin Wang2Cuiyan Han3Dandan Liu4Lei Tian5Xinggang Yang6Weisan Pan7School of Pharmacy, Shenyang Pharmaceutical UniversitySchool of Pharmacy, Shenyang Pharmaceutical UniversitySchool of Pharmacy, Shenyang Pharmaceutical UniversitySchool of Pharmacy, Qiqihar Medical UniversitySchool of Biomedical & Chemical Engineering, Liaoning Institute of Science and TechnologySchool of Pharmacy, Shenyang Pharmaceutical UniversitySchool of Pharmacy, Shenyang Pharmaceutical UniversitySchool of Pharmacy, Shenyang Pharmaceutical UniversityPoly-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.http://dx.doi.org/10.1080/10717544.2016.1269849poly-argininenanostructured lipid carrierssurface densitycellular uptaketissue distribution |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Mingshuang Sun Zhihong Zhu Huixin Wang Cuiyan Han Dandan Liu Lei Tian Xinggang Yang Weisan Pan |
spellingShingle |
Mingshuang Sun Zhihong Zhu Huixin Wang Cuiyan Han Dandan Liu Lei Tian Xinggang Yang Weisan Pan Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier Drug Delivery poly-arginine nanostructured lipid carriers surface density cellular uptake tissue distribution |
author_facet |
Mingshuang Sun Zhihong Zhu Huixin Wang Cuiyan Han Dandan Liu Lei Tian Xinggang Yang Weisan Pan |
author_sort |
Mingshuang Sun |
title |
Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier |
title_short |
Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier |
title_full |
Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier |
title_fullStr |
Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier |
title_full_unstemmed |
Surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier |
title_sort |
surface density of polyarginine influence the size, zeta potential, cellular uptake and tissue distribution of the nanostructured lipid carrier |
publisher |
Taylor & Francis Group |
series |
Drug Delivery |
issn |
1071-7544 1521-0464 |
publishDate |
2017-01-01 |
description |
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. |
topic |
poly-arginine nanostructured lipid carriers surface density cellular uptake tissue distribution |
url |
http://dx.doi.org/10.1080/10717544.2016.1269849 |
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