Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes

Santosh Bashyal,1 Jo-Eun Seo,1 Taekwang Keum,1 Gyubin Noh,1 Young Wook Choi,2 Sangkil Lee1 1College of Pharmacy, Keimyung University, Daegu, Republic of Korea; 2College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea Background: Buccal delivery of insulin is still a challenging issue f...

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Autores principales:	Bashyal S, Seo JE, Keum T, Noh G, Choi YW, Lee S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	insulin permeation TR146 cell cholic acid derivatives elastic bilosomes Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/b6de2fda1ff941248227a62d2c1bfa6d
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spelling	oai:doaj.org-article:b6de2fda1ff941248227a62d2c1bfa6d2021-12-02T04:55:10ZFacilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes1178-2013https://doaj.org/article/b6de2fda1ff941248227a62d2c1bfa6d2018-09-01T00:00:00Zhttps://www.dovepress.com/facilitated-permeation-of-insulin-across-tr146-cells-by-cholic-acid-de-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Santosh Bashyal,1 Jo-Eun Seo,1 Taekwang Keum,1 Gyubin Noh,1 Young Wook Choi,2 Sangkil Lee1 1College of Pharmacy, Keimyung University, Daegu, Republic of Korea; 2College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea Background: Buccal delivery of insulin is still a challenging issue for the researchers due to the presence of permeability barrier (buccal mucosa) in the buccal cavity. The main objective of this study was to investigate the safety, effectiveness, and potential of various liposomes containing different bile salts to improve the permeation of insulin across in vitro TR146 buccal cell layers. Methods: Elastic bilosomes containing soy lecithin and bile salt edge activators (sodium cholate [SC], sodium taurocholate [STC], sodium glycocholate [SGC], sodium deoxyglycocholate [SDGC], or sodium deoxytaurocholate [SDTC]) were fabricated by thin-film hydration method. The prepared liposomes were characterized, and in vitro permeation studies were performed. The fluorescein isothiocyanate-insulin-loaded elastic bilosomes were used to evaluate the quantitative and qualitative cellular uptake studies. Results: The prepared elastic bilosomes had a particle size and an entrapment efficiency of ~140–150 nm and 66%–78%, respectively. SDGC-lipo (SDGC-incorporated liposome) was observed to be the most superior with an enhancement ratio (ER) of 5.24 (P<0.001). The SC-incorporated liposome (SC-lipo) and SDTC-incorporated liposome (SDTC-lipo) also led to a significant enhancement with ERs of 3.20 and 3.10 (P<0.05), respectively, compared with insulin solution. These results were further supported by quantitative and qualitative cellular uptake studies performed employing fluorescence-activated cell sorting analysis and confocal microscopy, respectively. The relative median fluorescence intensity values of elastic bilosomes were counted in the order of SDGC-lipo > SC-lipo > SDTC-lipo > SGC-incorporated liposome > STC-incorporated liposome, and similarity in the permeability profile of the employed elastic bilosomes was noted. Conclusion: This study presents the employment of various derivatives of cholic acid-loaded elastic bilosomes as a promising strategy to enhance the permeation of insulin through buccal route. Keywords: insulin, peptide delivery, bile salts, elastic liposomes, buccal mucosaBashyal SSeo JEKeum TNoh GChoi YWLee SDove Medical PressarticleinsulinpermeationTR146 cellcholic acid derivativeselastic bilosomesMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 5173-5186 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	insulin permeation TR146 cell cholic acid derivatives elastic bilosomes Medicine (General) R5-920
spellingShingle	insulin permeation TR146 cell cholic acid derivatives elastic bilosomes Medicine (General) R5-920 Bashyal S Seo JE Keum T Noh G Choi YW Lee S Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes
description	Santosh Bashyal,1 Jo-Eun Seo,1 Taekwang Keum,1 Gyubin Noh,1 Young Wook Choi,2 Sangkil Lee1 1College of Pharmacy, Keimyung University, Daegu, Republic of Korea; 2College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea Background: Buccal delivery of insulin is still a challenging issue for the researchers due to the presence of permeability barrier (buccal mucosa) in the buccal cavity. The main objective of this study was to investigate the safety, effectiveness, and potential of various liposomes containing different bile salts to improve the permeation of insulin across in vitro TR146 buccal cell layers. Methods: Elastic bilosomes containing soy lecithin and bile salt edge activators (sodium cholate [SC], sodium taurocholate [STC], sodium glycocholate [SGC], sodium deoxyglycocholate [SDGC], or sodium deoxytaurocholate [SDTC]) were fabricated by thin-film hydration method. The prepared liposomes were characterized, and in vitro permeation studies were performed. The fluorescein isothiocyanate-insulin-loaded elastic bilosomes were used to evaluate the quantitative and qualitative cellular uptake studies. Results: The prepared elastic bilosomes had a particle size and an entrapment efficiency of ~140–150 nm and 66%–78%, respectively. SDGC-lipo (SDGC-incorporated liposome) was observed to be the most superior with an enhancement ratio (ER) of 5.24 (P<0.001). The SC-incorporated liposome (SC-lipo) and SDTC-incorporated liposome (SDTC-lipo) also led to a significant enhancement with ERs of 3.20 and 3.10 (P<0.05), respectively, compared with insulin solution. These results were further supported by quantitative and qualitative cellular uptake studies performed employing fluorescence-activated cell sorting analysis and confocal microscopy, respectively. The relative median fluorescence intensity values of elastic bilosomes were counted in the order of SDGC-lipo > SC-lipo > SDTC-lipo > SGC-incorporated liposome > STC-incorporated liposome, and similarity in the permeability profile of the employed elastic bilosomes was noted. Conclusion: This study presents the employment of various derivatives of cholic acid-loaded elastic bilosomes as a promising strategy to enhance the permeation of insulin through buccal route. Keywords: insulin, peptide delivery, bile salts, elastic liposomes, buccal mucosa
format	article
author	Bashyal S Seo JE Keum T Noh G Choi YW Lee S
author_facet	Bashyal S Seo JE Keum T Noh G Choi YW Lee S
author_sort	Bashyal S
title	Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes
title_short	Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes
title_full	Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes
title_fullStr	Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes
title_full_unstemmed	Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes
title_sort	facilitated permeation of insulin across tr146 cells by cholic acid derivatives-modified elastic bilosomes
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/b6de2fda1ff941248227a62d2c1bfa6d
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Facilitated permeation of insulin across TR146 cells by cholic acid derivatives-modified elastic bilosomes

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