Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin

Kunchi Zhang, Shaowa Lv, Xiuyan Li, Yufei Feng, Xin Li, Lu Liu, Shuang Li, Yongji Li School of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin, Heilongjiang Province, People’s Republic of China Background: The purpose of this work was to develop nanostructured lip...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Zhang KC, Lv SW, Li XY, Feng YF, Li X, Liu L, Li S, Li YJ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/d59c9faaccac497688a108983b8f8bc5
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:d59c9faaccac497688a108983b8f8bc5
record_format	dspace
spelling	oai:doaj.org-article:d59c9faaccac497688a108983b8f8bc52021-12-02T07:37:56ZPreparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin1176-91141178-2013https://doaj.org/article/d59c9faaccac497688a108983b8f8bc52013-08-01T00:00:00Zhttp://www.dovepress.com/preparation-characterization-and-in-vivo-pharmacokinetics-of-nanostruc-a14128https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Kunchi Zhang, Shaowa Lv, Xiuyan Li, Yufei Feng, Xin Li, Lu Liu, Shuang Li, Yongji Li School of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin, Heilongjiang Province, People’s Republic of China Background: The purpose of this work was to develop nanostructured lipid carriers (NLCs) loaded simultaneously with oleanolic acid and gentiopicrin. Methods: An aqueous dispersion of NLCs was prepared successfully using a film-ultrasonic method, with glycerin monostearate as the solid lipid and oleic acid as the liquid lipid. Poloxamer 188 was used as the surfactant. A central composite design was used to optimize the technologic parameters. The characteristics of the NLCs were then investigated. Results: The encapsulation efficiency was 48.34% ± 2.76%, drug loading was 8.06% ± 0.42%, particle size was 111.0 ± 1.56 nm, polydispersity index was 0.287 ± 0.01, and zeta potential was –23.8 ± 0.36 mV for the optimized NLCs. The other physicochemical properties were characterized by transmission electron microscopy and differential scanning calorimetry. Drug release followed first-order kinetics and release studies confirmed that oleanolic acid and gentiopicrin fitted a sustained-release model. Compared with NLCs loaded with oleanolic acid or gentiopicrin alone, NLCs loaded with both oleanolic acid and gentiopicrin produced drug concentrations which persisted for a significantly longer time in plasma, with a linear decrement following second-order kinetics. Aspartate and alanine aminotransferase levels were significantly lower on exposure to NLCs loaded with both oleanolic acid and gentiopicrin than in negative controls. Conclusion: The results of this study confirm that oleanolic acid and gentiopicrin can be loaded simultaneously into NLCs. Compared with oleanolic acid and gentiopicrin loaded alone, sustained release and protective effects against hepatic injury were observed using NLCs loaded with both oleanolic acid and gentiopicrin. Keywords: nanostructured lipid carriers, central composite design, in vitro release, pharmacokineticsZhang KCLv SWLi XYFeng YFLi XLiu LLi SLi YJDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 3227-3239 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhang KC Lv SW Li XY Feng YF Li X Liu L Li S Li YJ Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
description	Kunchi Zhang, Shaowa Lv, Xiuyan Li, Yufei Feng, Xin Li, Lu Liu, Shuang Li, Yongji Li School of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin, Heilongjiang Province, People’s Republic of China Background: The purpose of this work was to develop nanostructured lipid carriers (NLCs) loaded simultaneously with oleanolic acid and gentiopicrin. Methods: An aqueous dispersion of NLCs was prepared successfully using a film-ultrasonic method, with glycerin monostearate as the solid lipid and oleic acid as the liquid lipid. Poloxamer 188 was used as the surfactant. A central composite design was used to optimize the technologic parameters. The characteristics of the NLCs were then investigated. Results: The encapsulation efficiency was 48.34% ± 2.76%, drug loading was 8.06% ± 0.42%, particle size was 111.0 ± 1.56 nm, polydispersity index was 0.287 ± 0.01, and zeta potential was –23.8 ± 0.36 mV for the optimized NLCs. The other physicochemical properties were characterized by transmission electron microscopy and differential scanning calorimetry. Drug release followed first-order kinetics and release studies confirmed that oleanolic acid and gentiopicrin fitted a sustained-release model. Compared with NLCs loaded with oleanolic acid or gentiopicrin alone, NLCs loaded with both oleanolic acid and gentiopicrin produced drug concentrations which persisted for a significantly longer time in plasma, with a linear decrement following second-order kinetics. Aspartate and alanine aminotransferase levels were significantly lower on exposure to NLCs loaded with both oleanolic acid and gentiopicrin than in negative controls. Conclusion: The results of this study confirm that oleanolic acid and gentiopicrin can be loaded simultaneously into NLCs. Compared with oleanolic acid and gentiopicrin loaded alone, sustained release and protective effects against hepatic injury were observed using NLCs loaded with both oleanolic acid and gentiopicrin. Keywords: nanostructured lipid carriers, central composite design, in vitro release, pharmacokinetics
format	article
author	Zhang KC Lv SW Li XY Feng YF Li X Liu L Li S Li YJ
author_facet	Zhang KC Lv SW Li XY Feng YF Li X Liu L Li S Li YJ
author_sort	Zhang KC
title	Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
title_short	Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
title_full	Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
title_fullStr	Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
title_full_unstemmed	Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
title_sort	preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/d59c9faaccac497688a108983b8f8bc5
work_keys_str_mv	AT zhangkc preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT lvsw preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT lixy preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT fengyf preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT lix preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT liul preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT lis preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin AT liyj preparationcharacterizationandinvivopharmacokineticsofnanostructuredlipidcarriersloadedwitholeanolicacidandgentiopicrin
_version_	1718399307762106368

Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin

Ejemplares similares