Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles

Ying-Chen Chen,* Chia-Yu Su,* Hua-Jun Jhan, Hsiu-O Ho, Ming-Thau Sheu School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan *These authors contributed equally to this work Abstract: To alleviate the inherent problems of amphotericin B (AmB), such as poor water solubil...

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Autores principales:	Chen YC, Su CY, Jhan HJ, Ho HO, Sheu MT
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7beed226c6a347aab5f6e1417f1a53d2
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spelling	oai:doaj.org-article:7beed226c6a347aab5f6e1417f1a53d22021-12-02T00:59:55ZPhysical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles1178-2013https://doaj.org/article/7beed226c6a347aab5f6e1417f1a53d22015-12-01T00:00:00Zhttps://www.dovepress.com/physical-characterization-and-in-vivo-pharmacokinetic-study-of-self-as-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ying-Chen Chen,* Chia-Yu Su,* Hua-Jun Jhan, Hsiu-O Ho, Ming-Thau Sheu School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan *These authors contributed equally to this work Abstract: To alleviate the inherent problems of amphotericin B (AmB), such as poor water solubility and nephrotoxicity, a novel self-assembling mixed polymeric micelle delivery system based on lecithin and combined with amphiphilic polymers, Pluronic®, Kolliphor®, d-alpha tocopheryl polyethylene glycol succinate, and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy(poly(ethylene glycol)-2000 (DSPE-PEG2K) was developed. An optimal formulation (Ambicelles) composed of AmB:lecithin:DSPE-PEG2K in a 1:1:10 weight ratio was obtained. The particle size, polydispersion index, drug encapsulation efficiency, and drug loading were 187.20±10.55 nm, 0.51±0.017, 90.14%, and 7.51%, respectively, and the solubility was increased from 0.001 to 5 mg/mL. Compared with that of Fungizone®, the bioavailability of Ambicelles administered intravenously and orally increased 2.18- and 1.50-fold, respectively. Regarding the in vitro cytotoxicity, Ambicelles had a higher cell viability than free AmB solution or Fungizone® did. With pretreatment of 50 µg/mL ethanolic extract of Taiwanofungus camphoratus followed by AmB to HT29 colon cancer cells, the 50% inhibitory concentration of AmB solution was 12 µg/mL, whereas that of Ambicelles was 1 µg/mL, indicating that Ambicelles exerted a greater synergistic anticancer effect. Keywords: amphotericin B, micelle, amphiphilic polymer, lecithin, DSPE-PEGChen YCSu CYJhan HJHo HOSheu MTDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 7265-7274 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Chen YC Su CY Jhan HJ Ho HO Sheu MT Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles
description	Ying-Chen Chen,* Chia-Yu Su,* Hua-Jun Jhan, Hsiu-O Ho, Ming-Thau Sheu School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan *These authors contributed equally to this work Abstract: To alleviate the inherent problems of amphotericin B (AmB), such as poor water solubility and nephrotoxicity, a novel self-assembling mixed polymeric micelle delivery system based on lecithin and combined with amphiphilic polymers, Pluronic®, Kolliphor®, d-alpha tocopheryl polyethylene glycol succinate, and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy(poly(ethylene glycol)-2000 (DSPE-PEG2K) was developed. An optimal formulation (Ambicelles) composed of AmB:lecithin:DSPE-PEG2K in a 1:1:10 weight ratio was obtained. The particle size, polydispersion index, drug encapsulation efficiency, and drug loading were 187.20±10.55 nm, 0.51±0.017, 90.14%, and 7.51%, respectively, and the solubility was increased from 0.001 to 5 mg/mL. Compared with that of Fungizone®, the bioavailability of Ambicelles administered intravenously and orally increased 2.18- and 1.50-fold, respectively. Regarding the in vitro cytotoxicity, Ambicelles had a higher cell viability than free AmB solution or Fungizone® did. With pretreatment of 50 µg/mL ethanolic extract of Taiwanofungus camphoratus followed by AmB to HT29 colon cancer cells, the 50% inhibitory concentration of AmB solution was 12 µg/mL, whereas that of Ambicelles was 1 µg/mL, indicating that Ambicelles exerted a greater synergistic anticancer effect. Keywords: amphotericin B, micelle, amphiphilic polymer, lecithin, DSPE-PEG
format	article
author	Chen YC Su CY Jhan HJ Ho HO Sheu MT
author_facet	Chen YC Su CY Jhan HJ Ho HO Sheu MT
author_sort	Chen YC
title	Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles
title_short	Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles
title_full	Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles
title_fullStr	Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles
title_full_unstemmed	Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles
title_sort	physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin b-loaded lecithin-based mixed polymeric micelles
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/7beed226c6a347aab5f6e1417f1a53d2
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Physical characterization and in vivo pharmacokinetic study of self-assembling amphotericin B-loaded lecithin-based mixed polymeric micelles

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