Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration

Honglin Song1, Shufang Nie1,2, Xinggang Yang1, Ning Li1, Hongtao Xu1, Liangyuan Zheng1, Weisan Pan11Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China; 2Department of Pharmaceutical Engineering, Wuhan Bioengineering Institute, Wuhan, ChinaPurpose: Th...

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Autores principales: Honglin Song, Shufang Nie, Xinggang Yang, et al
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Publicado: Dove Medical Press 2010
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spelling oai:doaj.org-article:eae1d48ca53f4198b9a2f0d2008110202021-12-02T11:07:30ZCharacterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration1176-91141178-2013https://doaj.org/article/eae1d48ca53f4198b9a2f0d2008110202010-11-01T00:00:00Zhttp://www.dovepress.com/characterization-and-in-vivo-evaluation-of-novel-lipidndashchlorambuci-a5613https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Honglin Song1, Shufang Nie1,2, Xinggang Yang1, Ning Li1, Hongtao Xu1, Liangyuan Zheng1, Weisan Pan11Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China; 2Department of Pharmaceutical Engineering, Wuhan Bioengineering Institute, Wuhan, ChinaPurpose: The purpose of the study was to develop and evaluate different lipid-based ­formulations for parenteral administration, as potential novel carrier systems for lipophilic drugs, and to turn an unstable drug such as chlorambucil into a useful one.Methods: A two-stage, high-pressure homogenizer was used to yield a very fine monodispersed lipid nanosphere. The strategy of combining egg yolk phospholipid and nonionic emulsifier (Lutrol F 68 and Tween 80) as an emulsifier mixture was adopted to increase safety and tolerance. The final lipid nanospheres, in a lipophilic mixture consisting of three components, monostearin, medium-chain triglycerides and soya oil, were evaluated for physicochemical properties, such as particle size, surface morphology, drug-entrapment efficiency, drug-loading capacity, lyophilization and in vivo drug-release behavior.Results: A monodispersed lipid nanosphere with a mean particle size ranging from 90 to 150 nm was achieved. The optimized injectable cryoprotectants for lipid nanosphere were sucrose (7.5%) and mannitol (7.5%), which can stabilize the particle size (LD50) at approximately 129 nm after reconstitution. The results show that the formulation can effectively administer anticancer drugs and thus improve patient quality of life.Conclusions: The novel lipid nanosphere complex developed is a useful anticancer drug delivery vehicle for parenteral administration. The formulation strategy has the potential for the development of further methods of drug delivery for a wide variety of anticancer drugs.Keywords: lipid nanosphere, parenteral application, pharmacokinetics, nanotechnology, chlorambucil Honglin SongShufang NieXinggang Yanget alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 933-942 (2010)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Honglin Song
Shufang Nie
Xinggang Yang
et al
Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
description Honglin Song1, Shufang Nie1,2, Xinggang Yang1, Ning Li1, Hongtao Xu1, Liangyuan Zheng1, Weisan Pan11Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China; 2Department of Pharmaceutical Engineering, Wuhan Bioengineering Institute, Wuhan, ChinaPurpose: The purpose of the study was to develop and evaluate different lipid-based ­formulations for parenteral administration, as potential novel carrier systems for lipophilic drugs, and to turn an unstable drug such as chlorambucil into a useful one.Methods: A two-stage, high-pressure homogenizer was used to yield a very fine monodispersed lipid nanosphere. The strategy of combining egg yolk phospholipid and nonionic emulsifier (Lutrol F 68 and Tween 80) as an emulsifier mixture was adopted to increase safety and tolerance. The final lipid nanospheres, in a lipophilic mixture consisting of three components, monostearin, medium-chain triglycerides and soya oil, were evaluated for physicochemical properties, such as particle size, surface morphology, drug-entrapment efficiency, drug-loading capacity, lyophilization and in vivo drug-release behavior.Results: A monodispersed lipid nanosphere with a mean particle size ranging from 90 to 150 nm was achieved. The optimized injectable cryoprotectants for lipid nanosphere were sucrose (7.5%) and mannitol (7.5%), which can stabilize the particle size (LD50) at approximately 129 nm after reconstitution. The results show that the formulation can effectively administer anticancer drugs and thus improve patient quality of life.Conclusions: The novel lipid nanosphere complex developed is a useful anticancer drug delivery vehicle for parenteral administration. The formulation strategy has the potential for the development of further methods of drug delivery for a wide variety of anticancer drugs.Keywords: lipid nanosphere, parenteral application, pharmacokinetics, nanotechnology, chlorambucil
format article
author Honglin Song
Shufang Nie
Xinggang Yang
et al
author_facet Honglin Song
Shufang Nie
Xinggang Yang
et al
author_sort Honglin Song
title Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
title_short Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
title_full Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
title_fullStr Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
title_full_unstemmed Characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
title_sort characterization and in vivo evaluation of novel lipid–chlorambucil nanospheres prepared using a mixture of emulsifiers for parenteral administration
publisher Dove Medical Press
publishDate 2010
url https://doaj.org/article/eae1d48ca53f4198b9a2f0d200811020
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