Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation

Soon-Seok Hong,1 Ju Yeon Choi,2 Jong Oh Kim,2 Mi-Kyung Lee,3 So Hee Kim,4 Soo-Jeong Lim1 1Department of Bioscience and Bioengineering, Sejong University, Seoul, 2College of Pharmacy, Yeungnam University, Gyeongsan, 3College of Pharmacy, Woosuk University, Wanju-gun, Jeollabuk-do, 4College of Pharma...

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Autores principales:	Hong SS, Choi JY, Kim JO, Lee MK, Kim SH, Lim SJ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	paclitaxel triglyceride PEGylation liposome stability formulation Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/25ee7a59499e4e8290f2aa82c11b620d
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spelling	oai:doaj.org-article:25ee7a59499e4e8290f2aa82c11b620d2021-12-02T01:04:02ZDevelopment of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation1178-2013https://doaj.org/article/25ee7a59499e4e8290f2aa82c11b620d2016-09-01T00:00:00Zhttps://www.dovepress.com/development-of-paclitaxel-loaded-liposomal-nanocarrier-stabilized-by-t-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Soon-Seok Hong,1 Ju Yeon Choi,2 Jong Oh Kim,2 Mi-Kyung Lee,3 So Hee Kim,4 Soo-Jeong Lim1 1Department of Bioscience and Bioengineering, Sejong University, Seoul, 2College of Pharmacy, Yeungnam University, Gyeongsan, 3College of Pharmacy, Woosuk University, Wanju-gun, Jeollabuk-do, 4College of Pharmacy and Research Institute of Pharmaceutical Science and Technology, Ajou University, Suwon, Republic of Korea Abstract: Studies have highlighted the challenge of developing injectable liposomes as a paclitaxel (PTX) carrier, a challenge attributable to the limitations in liposomal stability caused by PTX loading. Poor stability of PTX-loaded liposomes is caused by PTX-triggered aggregation or fusion of liposomal membranes and is exacerbated in the presence of PEGylated lipid. In the present study, the effect of triglyceride incorporation on the stability of PTX-loaded/PEGylated liposomes was explored. Incorporation of a medium chain triglyceride Captex 300 into saturated phosphatidylcholine (PC)-based liposomes (1,2-dimyristoyl-sn-glycero-3-phosphocholine [DMPC]:cholesterol [CHOL]:N-(Carbonyl-methoxypolyethyleneglycol 2000)-1, 2-distearoyl-sn-glycero-3-phospho-ethanolamine [PE-PEG]), produced a fine, homogeneous, and membrane-filterable PTX-loaded liposomes fulfilling the requirement of an injectable lipid formulation. Triglyceride incorporation also greatly inhibited the time-dependent leakage of PTX from saturated PC-based liposomes, which appears to be mediated by the inhibition of liposome fusion. In contrast, triglyceride incorporation induced the destabilization and PTX leakage of unsaturated PC-based liposomes, indicating the opposite effect of triglyceride depending on the fluidity status of PC constituting the liposomal membrane. PTX release profile and the in vitro and in vivo anticancer efficacy of triglyceride-incorporated DMPC:CHOL:PE-PEG liposomes were similar to Taxol® while the toxicity of liposomal PTX was significantly lower than that of Taxol. Taken together, triglyceride incorporation provided an injectable PTX formulation by functioning as a formulation stabilizer of PEGylated/saturated PC-based liposomes. Keywords: paclitaxel, triglyceride, PEGylation, liposome, stability, formulationHong SSChoi JYKim JOLee MKKim SHLim SJDove Medical PressarticlepaclitaxeltriglyceridePEGylationliposomestabilityformulationMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 11, Pp 4465-4477 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	paclitaxel triglyceride PEGylation liposome stability formulation Medicine (General) R5-920
spellingShingle	paclitaxel triglyceride PEGylation liposome stability formulation Medicine (General) R5-920 Hong SS Choi JY Kim JO Lee MK Kim SH Lim SJ Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
description	Soon-Seok Hong,1 Ju Yeon Choi,2 Jong Oh Kim,2 Mi-Kyung Lee,3 So Hee Kim,4 Soo-Jeong Lim1 1Department of Bioscience and Bioengineering, Sejong University, Seoul, 2College of Pharmacy, Yeungnam University, Gyeongsan, 3College of Pharmacy, Woosuk University, Wanju-gun, Jeollabuk-do, 4College of Pharmacy and Research Institute of Pharmaceutical Science and Technology, Ajou University, Suwon, Republic of Korea Abstract: Studies have highlighted the challenge of developing injectable liposomes as a paclitaxel (PTX) carrier, a challenge attributable to the limitations in liposomal stability caused by PTX loading. Poor stability of PTX-loaded liposomes is caused by PTX-triggered aggregation or fusion of liposomal membranes and is exacerbated in the presence of PEGylated lipid. In the present study, the effect of triglyceride incorporation on the stability of PTX-loaded/PEGylated liposomes was explored. Incorporation of a medium chain triglyceride Captex 300 into saturated phosphatidylcholine (PC)-based liposomes (1,2-dimyristoyl-sn-glycero-3-phosphocholine [DMPC]:cholesterol [CHOL]:N-(Carbonyl-methoxypolyethyleneglycol 2000)-1, 2-distearoyl-sn-glycero-3-phospho-ethanolamine [PE-PEG]), produced a fine, homogeneous, and membrane-filterable PTX-loaded liposomes fulfilling the requirement of an injectable lipid formulation. Triglyceride incorporation also greatly inhibited the time-dependent leakage of PTX from saturated PC-based liposomes, which appears to be mediated by the inhibition of liposome fusion. In contrast, triglyceride incorporation induced the destabilization and PTX leakage of unsaturated PC-based liposomes, indicating the opposite effect of triglyceride depending on the fluidity status of PC constituting the liposomal membrane. PTX release profile and the in vitro and in vivo anticancer efficacy of triglyceride-incorporated DMPC:CHOL:PE-PEG liposomes were similar to Taxol® while the toxicity of liposomal PTX was significantly lower than that of Taxol. Taken together, triglyceride incorporation provided an injectable PTX formulation by functioning as a formulation stabilizer of PEGylated/saturated PC-based liposomes. Keywords: paclitaxel, triglyceride, PEGylation, liposome, stability, formulation
format	article
author	Hong SS Choi JY Kim JO Lee MK Kim SH Lim SJ
author_facet	Hong SS Choi JY Kim JO Lee MK Kim SH Lim SJ
author_sort	Hong SS
title	Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
title_short	Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
title_full	Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
title_fullStr	Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
title_full_unstemmed	Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
title_sort	development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/25ee7a59499e4e8290f2aa82c11b620d
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_version_	1718403304986247168

Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation

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