Back to Journals » International Journal of Nanomedicine » Volume 14

Preparation, intestinal segment stability, and mucoadhesion properties of novel thymopentin-loaded chitosan derivatives coated with poly (n-butyl) cyanoacrylate nanoparticles

Authors Xu Y, Lu S, Liu Q, Hong Y, Xu B, Ping Q, Jin X, Shen Y, Webster TJ, Rao Y

Received 14 November 2018

Accepted for publication 31 January 2019

Published 4 March 2019 Volume 2019:14 Pages 1659—1668

DOI https://doi.org/10.2147/IJN.S194529

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Govarthanan Muthusamy

Peer reviewer comments 2

Editor who approved publication: Prof. Dr. Anderson Oliveira Lobo


Ying Xu,1 Shengzhe Lu,1 Qi Liu,2 Yun Hong,3 Bohui Xu,4 Qineng Ping,5 Xuefeng Jin,5 Yan Shen,5 Thomas J Webster,6 Yuefeng Rao3,7

1Department of Pharmaceutics, School of Pharmacy, Jiangsu University, Zhenjiang, 212013, China; 2Department of Dermatology, Johns Hopkins University School of Medicine, Baltimore, MD 21231, USA; 3Department of Pharmacy, School of Medicine, The First Affiliated Hospital, Zhejiang University, Hangzhou 310003, China; 4Department of Pharmacy, School of Pharmacy, Nantong University, Nantong 226001, China; 5Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China; 6Department of Chemical Engineering, Northeastern University, Boston, MA 02115, USA; 7Department of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China

Background: In order to develop a promising carrier for the oral delivery of proteins and peptide drugs, a novel bioadhesive nanocarrier of chitosan (CTS) derivatives coated with poly (n-butyl) cyanoacrylate nanoparticles (PBCA-NPs) was prepared in this study.
Methods: Three different thymopentin (TP5)-loaded nanoparticles were prepared in the present study. TP5-PBCA-NPs were developed by modifying an emulsion polymerization method, and CTS and chitosan–glutathione (CG) derivative-coated PBCA nanoparticles were obtained from the electrostatic interactions between CTS or CG with negatively charged PBCA nanoparticles.
Results: The particle sizes of TP5-PBCA-NPs, TP5-CTS-PBCA-NPs, and TP5-CG-PBCA-NPs were 212.3±6.9, 274.6±8.2, and 310.4±7.5 nm, respectively, while the respective zeta potentials were –22.6±0.76, 23.3±1.2, and 34.6±1.6 mV with encapsulation efficiencies of 79.37%±2.15%, 74.21%±2.13%, and 72.65%±1.48%, respectively. An everted intestinal ring method indicated that drug stability was remarkably improved after incorporation into the nanoparticles, especially the CG-coated nanoparticles. The mucus layer retention rates for CTS- and CG-coated nanoparticles were 1.43 and 1.83 times that of the uncoated nanoparticles, respectively, using ex vivo mucosa. The in vivo mucoadhesion study illustrated that the transfer of uncoated PBCA-NPs from the stomach to the intestine was faster than that of CTS-PBCA-NPs and CG-PBCA-NPs, while the CG-PBCA-NPs presented the best intestinal retentive characteristic.
Conclusion: In summary, this study demonstrated the feasibility and benefit of orally delivering peptide drugs using novel CTS derivative-coated nanoparticles with optimal stability and bioadhesive properties.

Keywords: chitosan derivatives, PBCA nanoparticles, thymopentin, stability, bioadhesive
 

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]