Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations

Xin Jin,1,2 Zhen-hai Zhang,1 E Sun,1 Qian Qian,1 Xiao-bin Tan,1 Xiao-bin Jia11Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 2College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, People&#39;s Republic of...

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Autores principales:	Jin X, Zhang&nbsp; ZH, Sun E, Qian Q, Tan XB, Jia XB
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/c15051d78f0c442b9b72bc0f86daac96
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spelling	oai:doaj.org-article:c15051d78f0c442b9b72bc0f86daac962021-12-02T07:20:24ZPreparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations1176-91141178-2013https://doaj.org/article/c15051d78f0c442b9b72bc0f86daac962012-09-01T00:00:00Zhttp://www.dovepress.com/preparation-of-a-nanoscale-baohuoside-i-phospholipid-complex-and-deter-a10984https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xin Jin,1,2 Zhen-hai Zhang,1 E Sun,1 Qian Qian,1 Xiao-bin Tan,1 Xiao-bin Jia11Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 2College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, People&#39;s Republic of ChinaBackground: Baohuoside I is a potential anticancer drug for a variety of malignancies and has been approved for in vitro use. However, baohuoside I has very poor oral absorption.Methods: In the present study, we prepared baohuoside I-phospholipid complexes of different diameters and determined their physicochemical properties using transmission electron microscopy, ultraviolet spectroscopy, and differential scanning calorimetry. The in vitro absorption of baohuoside I and baohuoside I-phospholipid complexes of different sizes were compared using the Caco-2 cell culture model, and subsequently, the bioavailability of baohuosidel and its complexes were estimated in vivo.Results: Compared with the large-sized phospholipid complexes, a nanoscale phospholipid complex improved the oral bioavailability of baohuoside I. In addition, our results suggest that the smaller the particle size, the faster the complexes crossed the Caco-2 monolayer and the faster they were resorbed after oral administration in rats. The relative oral bioavailability of a nanoscale size 81 &plusmn; 10 nm baohuoside I-phospholipid complex (area under the concentration-time curve [AUC] 0&ndash;&infin;)was 342%, while that of baohuoside I and a 227.3 &plusmn; 65.2 &micro;m baohuoside I-phospholipid complex was 165%.Conclusion: We enhanced the oral bioavailability of baohuoside I by reducing the particle size of the phospholipid complex to the nanometer range, thereby improving its potential for clinical application.Keywords: nanoscale phospholipid complex, Caco-2 cell monolayer, bioavailability, oral absorptionJin XZhang&nbsp; ZHSun EQian QTan XBJia XBDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 4907-4916 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Jin X Zhang&nbsp; ZH Sun E Qian Q Tan XB Jia XB Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
description	Xin Jin,1,2 Zhen-hai Zhang,1 E Sun,1 Qian Qian,1 Xiao-bin Tan,1 Xiao-bin Jia11Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 2College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, People&#39;s Republic of ChinaBackground: Baohuoside I is a potential anticancer drug for a variety of malignancies and has been approved for in vitro use. However, baohuoside I has very poor oral absorption.Methods: In the present study, we prepared baohuoside I-phospholipid complexes of different diameters and determined their physicochemical properties using transmission electron microscopy, ultraviolet spectroscopy, and differential scanning calorimetry. The in vitro absorption of baohuoside I and baohuoside I-phospholipid complexes of different sizes were compared using the Caco-2 cell culture model, and subsequently, the bioavailability of baohuosidel and its complexes were estimated in vivo.Results: Compared with the large-sized phospholipid complexes, a nanoscale phospholipid complex improved the oral bioavailability of baohuoside I. In addition, our results suggest that the smaller the particle size, the faster the complexes crossed the Caco-2 monolayer and the faster they were resorbed after oral administration in rats. The relative oral bioavailability of a nanoscale size 81 &plusmn; 10 nm baohuoside I-phospholipid complex (area under the concentration-time curve [AUC] 0&ndash;&infin;)was 342%, while that of baohuoside I and a 227.3 &plusmn; 65.2 &micro;m baohuoside I-phospholipid complex was 165%.Conclusion: We enhanced the oral bioavailability of baohuoside I by reducing the particle size of the phospholipid complex to the nanometer range, thereby improving its potential for clinical application.Keywords: nanoscale phospholipid complex, Caco-2 cell monolayer, bioavailability, oral absorption
format	article
author	Jin X Zhang&nbsp; ZH Sun E Qian Q Tan XB Jia XB
author_facet	Jin X Zhang&nbsp; ZH Sun E Qian Q Tan XB Jia XB
author_sort	Jin X
title	Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
title_short	Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
title_full	Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
title_fullStr	Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
title_full_unstemmed	Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
title_sort	preparation of a nanoscale baohuoside i-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/c15051d78f0c442b9b72bc0f86daac96
work_keys_str_mv	AT jinx preparationofananoscalebaohuosideiphospholipidcomplexanddeterminationofitsabsorptioninvivoandinvitroevaluations AT zhangampnbspzh preparationofananoscalebaohuosideiphospholipidcomplexanddeterminationofitsabsorptioninvivoandinvitroevaluations AT sune preparationofananoscalebaohuosideiphospholipidcomplexanddeterminationofitsabsorptioninvivoandinvitroevaluations AT qianq preparationofananoscalebaohuosideiphospholipidcomplexanddeterminationofitsabsorptioninvivoandinvitroevaluations AT tanxb preparationofananoscalebaohuosideiphospholipidcomplexanddeterminationofitsabsorptioninvivoandinvitroevaluations AT jiaxb preparationofananoscalebaohuosideiphospholipidcomplexanddeterminationofitsabsorptioninvivoandinvitroevaluations
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Preparation of a nanoscale baohuoside I-phospholipid complex and determination of its absorption: in vivo and in vitro evaluations

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