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

Authors Bashyal S, Seo JE, Keum T, Noh G, Choi YW, Lee S

Received 15 March 2018

Accepted for publication 3 July 2018

Published 6 September 2018 Volume 2018:13 Pages 5173—5186

DOI https://doi.org/10.2147/IJN.S168310

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Justinn Cochran

Peer reviewer comments 2

Editor who approved publication: Dr Thomas Webster


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

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