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A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity

The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier (R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 cells like cellular uptake and cytotoxicity was also appraised using unmodified NLC...

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Detalles Bibliográficos
Autores principales: Sun, Mingshuang, Gao, Yunyun, Zhu, Zhihong, Wang, Huixin, Han, Cuiyan, Yang, Xinggang, Pan, Weisan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shenyang Pharmaceutical University 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032249/
https://www.ncbi.nlm.nih.gov/pubmed/32104313
http://dx.doi.org/10.1016/j.ajps.2016.07.007
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author Sun, Mingshuang
Gao, Yunyun
Zhu, Zhihong
Wang, Huixin
Han, Cuiyan
Yang, Xinggang
Pan, Weisan
author_facet Sun, Mingshuang
Gao, Yunyun
Zhu, Zhihong
Wang, Huixin
Han, Cuiyan
Yang, Xinggang
Pan, Weisan
author_sort Sun, Mingshuang
collection PubMed
description The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier (R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 cells like cellular uptake and cytotoxicity was also appraised using unmodified NLC as the controlled group. As the results revealed, R-NLC had an average diameter of about 40 nm and a positive zeta potential of about +17 mv, the entrapment efficiency decreased apparently, and no significant difference on the in vitro drug release was found after R8-modification. The cellular uptake and cytotoxicity increased obviously compared with unmodified NLC. The cellular uptake mechanisms of R-NLC involved energy, macropinocytosis, clathrin-mediated endocytosis, and caveolin-mediated endocytosis. The outcomes of the present study strongly support the theory that cell penetrating peptides have the ability of enhancing the cellular uptake of nanocarriers.
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spelling pubmed-70322492020-02-26 A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity Sun, Mingshuang Gao, Yunyun Zhu, Zhihong Wang, Huixin Han, Cuiyan Yang, Xinggang Pan, Weisan Asian J Pharm Sci Original Research Article The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier (R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 cells like cellular uptake and cytotoxicity was also appraised using unmodified NLC as the controlled group. As the results revealed, R-NLC had an average diameter of about 40 nm and a positive zeta potential of about +17 mv, the entrapment efficiency decreased apparently, and no significant difference on the in vitro drug release was found after R8-modification. The cellular uptake and cytotoxicity increased obviously compared with unmodified NLC. The cellular uptake mechanisms of R-NLC involved energy, macropinocytosis, clathrin-mediated endocytosis, and caveolin-mediated endocytosis. The outcomes of the present study strongly support the theory that cell penetrating peptides have the ability of enhancing the cellular uptake of nanocarriers. Shenyang Pharmaceutical University 2017-01 2016-08-04 /pmc/articles/PMC7032249/ /pubmed/32104313 http://dx.doi.org/10.1016/j.ajps.2016.07.007 Text en © 2017 Production and hosting by Elsevier B.V. on behalf of Shenyang Pharmaceutical University. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Research Article
Sun, Mingshuang
Gao, Yunyun
Zhu, Zhihong
Wang, Huixin
Han, Cuiyan
Yang, Xinggang
Pan, Weisan
A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
title A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
title_full A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
title_fullStr A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
title_full_unstemmed A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
title_short A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
title_sort systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032249/
https://www.ncbi.nlm.nih.gov/pubmed/32104313
http://dx.doi.org/10.1016/j.ajps.2016.07.007
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