Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin

Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin

Zhen-Hai Zhang,1,2 Yin-Long Zhang,2 Jian-Ping Zhou,2 Hui-Xia Lv21Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China; 2Department of Pharmaceutics, China Pharmaceutical University, Nanjing, ChinaAbstract: The aim of this study was to design and characterize solid lipid nanoparti...

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Autores principales: Zhang ZH, Zhang YL, Zhou JP, Lv HX
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2012
Materias:
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/599ed68ec6bd4d2ebfa9aaa9d6aa4f3b
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spelling oai:doaj.org-article:599ed68ec6bd4d2ebfa9aaa9d6aa4f3b2021-12-02T02:28:08ZSolid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin1176-91141178-2013https://doaj.org/article/599ed68ec6bd4d2ebfa9aaa9d6aa4f3b2012-07-01T00:00:00Zhttp://www.dovepress.com/solid-lipid-nanoparticles-modified-with-stearic-acidndashoctaarginine--a10272https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Zhen-Hai Zhang,1,2 Yin-Long Zhang,2 Jian-Ping Zhou,2 Hui-Xia Lv21Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China; 2Department of Pharmaceutics, China Pharmaceutical University, Nanjing, ChinaAbstract: The aim of this study was to design and characterize solid lipid nanoparticles (SLNs) modified with stearic acid–octaarginine (SA-R8) as carriers for oral administration of insulin (SA-R8-Ins-SLNs). The SLNs were prepared by spontaneous emulsion solvent diffusion methods. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the SA-R8-Ins-SLNs were 162 nm, 29.87 mV, 3.19%, and 76.54%, respectively. The zeta potential of the SLNs changed dramatically, from -32.13 mV to 29.87 mV, by binding the positively charged SA-R8. Morphological studies of SA-R8-Ins-SLNs using transmission electron microscopy showed that they were spherical. In vitro, a degradation experiment by enzymes showed that SLNs and SA-R8 could partially protect insulin from proteolysis. Compared to the insulin solution, the SA-R8-Ins-SLNs increased the Caco-2 cell's internalization by up to 18.44 times. In the in vivo studies, a significant hypoglycemic effect in diabetic rats over controls was obtained, with a SA-R8-Ins-SLN pharmacological availability value of 13.86 ± 0.79. These results demonstrate that SA-R8-modified SLNs promote the oral absorption of insulin.Keywords: solid lipid nanoparticles, cell penetration peptides, stearic acid octaarginine, insulin, oral administration Zhang ZHZhang YLZhou JPLv HXDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 3333-3339 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Zhang ZH
Zhang YL
Zhou JP
Lv HX
Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
description Zhen-Hai Zhang,1,2 Yin-Long Zhang,2 Jian-Ping Zhou,2 Hui-Xia Lv21Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, China; 2Department of Pharmaceutics, China Pharmaceutical University, Nanjing, ChinaAbstract: The aim of this study was to design and characterize solid lipid nanoparticles (SLNs) modified with stearic acid–octaarginine (SA-R8) as carriers for oral administration of insulin (SA-R8-Ins-SLNs). The SLNs were prepared by spontaneous emulsion solvent diffusion methods. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the SA-R8-Ins-SLNs were 162 nm, 29.87 mV, 3.19%, and 76.54%, respectively. The zeta potential of the SLNs changed dramatically, from -32.13 mV to 29.87 mV, by binding the positively charged SA-R8. Morphological studies of SA-R8-Ins-SLNs using transmission electron microscopy showed that they were spherical. In vitro, a degradation experiment by enzymes showed that SLNs and SA-R8 could partially protect insulin from proteolysis. Compared to the insulin solution, the SA-R8-Ins-SLNs increased the Caco-2 cell's internalization by up to 18.44 times. In the in vivo studies, a significant hypoglycemic effect in diabetic rats over controls was obtained, with a SA-R8-Ins-SLN pharmacological availability value of 13.86 ± 0.79. These results demonstrate that SA-R8-modified SLNs promote the oral absorption of insulin.Keywords: solid lipid nanoparticles, cell penetration peptides, stearic acid octaarginine, insulin, oral administration 
format article
author Zhang ZH
Zhang YL
Zhou JP
Lv HX
author_facet Zhang ZH
Zhang YL
Zhou JP
Lv HX
author_sort Zhang ZH
title Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
title_short Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
title_full Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
title_fullStr Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
title_full_unstemmed Solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
title_sort solid lipid nanoparticles modified with stearic acid–octaarginine for oral administration of insulin
publisher Dove Medical Press
publishDate 2012
url https://doaj.org/article/599ed68ec6bd4d2ebfa9aaa9d6aa4f3b
work_keys_str_mv AT zhangzh solidlipidnanoparticlesmodifiedwithstearicacidampndashoctaargininefororaladministrationofinsulin
AT zhangyl solidlipidnanoparticlesmodifiedwithstearicacidampndashoctaargininefororaladministrationofinsulin
AT zhoujp solidlipidnanoparticlesmodifiedwithstearicacidampndashoctaargininefororaladministrationofinsulin
AT lvhx solidlipidnanoparticlesmodifiedwithstearicacidampndashoctaargininefororaladministrationofinsulin
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