The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

Dong Wuk Kim,1,* Thiruganesh Ramasamy,2,* Ju Yeon Choi,2 Jeong Hwan Kim,2 Chul Soon Yong,2 Jong Oh Kim,2 Han-Gon Choi1 1College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, South Korea; 2College of Pharmacy, Yeungnam University, Gyongsan, South Korea...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Kim DW, Ramasamy T, Choi JY, Kim JH, Yong CS, Kim JO, Choi HG
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/4c9ca8cff1214fd8b554367ff8015a54
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:4c9ca8cff1214fd8b554367ff8015a54
record_format	dspace
spelling	oai:doaj.org-article:4c9ca8cff1214fd8b554367ff8015a542021-12-02T00:54:30ZThe influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles1178-2013https://doaj.org/article/4c9ca8cff1214fd8b554367ff8015a542014-08-01T00:00:00Zhttp://www.dovepress.com/the-influence-of-bile-salt-on-the-chemotherapeutic-response-of-docetax-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Dong Wuk Kim,1,* Thiruganesh Ramasamy,2,* Ju Yeon Choi,2 Jeong Hwan Kim,2 Chul Soon Yong,2 Jong Oh Kim,2 Han-Gon Choi1 1College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, South Korea; 2College of Pharmacy, Yeungnam University, Gyongsan, South Korea *These two authors contributed equally to this work Abstract: The primary aim of this work was to investigate the potential of bile salt, sodium taurocholate (NaTC), in improving the bioavailability and anti-tumor efficacy of docetaxel (DCT) upon rectal administration. Poloxamer-based nanomicelles with thermosensitive and mucoadhesive properties were prepared using the cold method. The optimized nanomicellar formulation was evaluated in terms of physicochemical and viscoelastic parameters. Nanomicelles containing bile salt maintained sufficient gelation strength (234×102 mPa·s) and mucoadhesive force (17.3×102 dyne/cm2) to be retained in the upper part of the rectum. They significantly enhanced the DCT internalization across the rectal mucosa and showed a high plasma level during the first 4 hours of the study period, compared to nanomicelles with no bile salt. As a result, a slightly higher rectal bioavailability of ~33% was observed in nanomicelles containing bile salt, compared to ~28% from the latter system. The higher pharmacokinetic parameters for rectally administered DCT/P407/P188/Tween 80/NaTC (0.25%/11%/15%/10%/0.1% by weight, respectively) resulted in significant anti-tumor efficacy. However, the tumor regression rate for the NaTC group was not statistically different from that for nanomicelles without NaTC. Therefore, overall results suggest that thermosensitive nanomicelles could be a potential dosage form for improvement of the bioavailability and chemotherapeutic profile of DCT. Keywords: anti-cancer efficiency, bioavailability, docetaxel, liquid suppository, rectal delivery, thermosensitiveKim DWRamasamy TChoi JYKim JHYong CSKim JOChoi HGDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 3815-3824 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Kim DW Ramasamy T Choi JY Kim JH Yong CS Kim JO Choi HG The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
description	Dong Wuk Kim,1,* Thiruganesh Ramasamy,2,* Ju Yeon Choi,2 Jeong Hwan Kim,2 Chul Soon Yong,2 Jong Oh Kim,2 Han-Gon Choi1 1College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, South Korea; 2College of Pharmacy, Yeungnam University, Gyongsan, South Korea *These two authors contributed equally to this work Abstract: The primary aim of this work was to investigate the potential of bile salt, sodium taurocholate (NaTC), in improving the bioavailability and anti-tumor efficacy of docetaxel (DCT) upon rectal administration. Poloxamer-based nanomicelles with thermosensitive and mucoadhesive properties were prepared using the cold method. The optimized nanomicellar formulation was evaluated in terms of physicochemical and viscoelastic parameters. Nanomicelles containing bile salt maintained sufficient gelation strength (234×102 mPa·s) and mucoadhesive force (17.3×102 dyne/cm2) to be retained in the upper part of the rectum. They significantly enhanced the DCT internalization across the rectal mucosa and showed a high plasma level during the first 4 hours of the study period, compared to nanomicelles with no bile salt. As a result, a slightly higher rectal bioavailability of ~33% was observed in nanomicelles containing bile salt, compared to ~28% from the latter system. The higher pharmacokinetic parameters for rectally administered DCT/P407/P188/Tween 80/NaTC (0.25%/11%/15%/10%/0.1% by weight, respectively) resulted in significant anti-tumor efficacy. However, the tumor regression rate for the NaTC group was not statistically different from that for nanomicelles without NaTC. Therefore, overall results suggest that thermosensitive nanomicelles could be a potential dosage form for improvement of the bioavailability and chemotherapeutic profile of DCT. Keywords: anti-cancer efficiency, bioavailability, docetaxel, liquid suppository, rectal delivery, thermosensitive
format	article
author	Kim DW Ramasamy T Choi JY Kim JH Yong CS Kim JO Choi HG
author_facet	Kim DW Ramasamy T Choi JY Kim JH Yong CS Kim JO Choi HG
author_sort	Kim DW
title	The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
title_short	The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
title_full	The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
title_fullStr	The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
title_full_unstemmed	The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
title_sort	influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/4c9ca8cff1214fd8b554367ff8015a54
work_keys_str_mv	AT kimdw theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT ramasamyt theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT choijy theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT kimjh theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT yongcs theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT kimjo theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT choihg theinfluenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT kimdw influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT ramasamyt influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT choijy influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT kimjh influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT yongcs influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT kimjo influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles AT choihg influenceofbilesaltonthechemotherapeuticresponseofdocetaxelloadedthermosensitivenanomicelles
_version_	1718403436040421376

The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

Ejemplares similares