Next Article in Journal
Targeting Notch3 in Hepatocellular Carcinoma: Molecular Mechanisms and Therapeutic Perspectives
Next Article in Special Issue
The Role of Reactive Oxygen Species (ROS) in the Biological Activities of Metallic Nanoparticles
Previous Article in Journal
Immuno-PET for Clinical Theranostic Approaches
Previous Article in Special Issue
Differential Cytotoxic Potential of Silver Nanoparticles in Human Ovarian Cancer Cells and Ovarian Cancer Stem Cells
Article Menu
Issue 1 (January) cover image

Export Article

Open AccessArticle
Int. J. Mol. Sci. 2017, 18(1), 54;

Multifunctional Composite Microcapsules for Oral Delivery of Insulin

Key Laboratory of Chemical Engineering Process and Technology for High-Efficiency Conversion, School of Chemistry and Material Science, College of Heilongjiang Province (Heilongjiang University), Heilongjiang University, Harbin 150080, China
College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin 150025, China
Institute of Tumor Research, Harbin Medical University, Harbin 150080, China
School of Pharmaceutical Science, Aichi Gakuin University, Nagoya 470-0195, Japan
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China
Authors to whom correspondence should be addressed.
Academic Editor: Bing Yan
Received: 7 November 2016 / Revised: 11 December 2016 / Accepted: 21 December 2016 / Published: 28 December 2016
(This article belongs to the Collection Bioactive Nanoparticles)
Full-Text   |   PDF [2815 KB, uploaded 28 December 2016]   |  


In this study, we designed and developed a new drug delivery system of multifunctional composite microcapsules for oral administration of insulin. Firstly, in order to enhance the encapsulation efficiency, insulin was complexed with functional sodium deoxycholate to form insulin-sodium deoxycholate complex using hydrophobic ion pairing method. Then the complex was encapsulated into poly(lactide-co-glycolide) (PLGA) nanoparticles by emulsion solvent diffusion method. The PLGA nanoparticles have a mean size of 168 nm and a zeta potential of −29.2 mV. The encapsulation efficiency was increased to 94.2% for the complex. In order to deliver insulin to specific gastrointestinal regions and reduce the burst release of insulin from PLGA nanoparticles, hence enhancing the bioavailability of insulin, enteric targeting multifunctional composite microcapsules were further prepared by encapsulating PLGA nanoparticles into pH-sensitive hydroxypropyl methyl cellulose phthalate (HP55) using organic spray-drying method. A pH-dependent insulin release profile was observed for this drug delivery system in vitro. All these strategies help to enhance the encapsulation efficiency, control the drug release, and protect insulin from degradation. In diabetic fasted rats, administration of the composite microcapsules produced a great enhancement in the relative bioavailability, which illustrated that this formulation was an effective candidate for oral insulin delivery. View Full-Text
Keywords: insulin; sodium deoxycholate; HP55; PLGA nanoparticles; microcapsules insulin; sodium deoxycholate; HP55; PLGA nanoparticles; microcapsules

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Sun, S.; Liang, N.; Gong, X.; An, W.; Kawashima, Y.; Cui, F.; Yan, P. Multifunctional Composite Microcapsules for Oral Delivery of Insulin. Int. J. Mol. Sci. 2017, 18, 54.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top