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Pharmaceutics 2016, 8(4), 30; doi:10.3390/pharmaceutics8040030

Cross-Linked Dependency of Boronic Acid-Conjugated Chitosan Nanoparticles by Diols for Sustained Insulin Release

1
School of Pharmacy, University of Nottingham Malaysia Campus, Jalan Broga, Semenyih 43500, Selangor Darul Ehsan, Malaysia
2
School of Pharmacy, University of Nottingham, University Park, Nottingham, NG7 2RD, UK
3
Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana
*
Author to whom correspondence should be addressed.
Academic Editor: Roderick B. Walker
Received: 17 August 2016 / Revised: 13 September 2016 / Accepted: 15 September 2016 / Published: 8 October 2016
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Abstract

Boronic acids have been widely investigated for their potential use as glucose sensors in glucose responsive polymeric insulin delivery systems. Interactions between cyclic diols and boronic acids, anchored to polymeric delivery systems, may result in swelling of the delivery system, releasing the drug. In this study, 4-formylphenylboronic acid conjugated chitosan was formulated into insulin containing nanoparticles via polyelectrolyte complexation. The nanoparticles had an average diameter of 140 ± 12.8 nm, polydispersity index of 0.17 ± 0.1, zeta potential of +19.1 ± 0.69 mV, encapsulation efficiency of 81% ± 1.2%, and an insulin loading capacity of 46% ± 1.8% w/w. Changes in size of the nanoparticles and release of insulin were type of sugar- and concentration-dependent. High concentration of diols resulted in a sustained release of insulin due to crosslink formation with boronic acid moieties within the nanoparticles. The formulation has potential to be developed into a self-regulated insulin delivery system for the treatment of diabetes. View Full-Text
Keywords: stimuli-responsive; glucose; fructose; drug delivery; nanoparticles stimuli-responsive; glucose; fructose; drug delivery; nanoparticles
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MDPI and ACS Style

Siddiqui, N.A.; Billa, N.; Roberts, C.J.; Asantewaa Osei, Y. Cross-Linked Dependency of Boronic Acid-Conjugated Chitosan Nanoparticles by Diols for Sustained Insulin Release. Pharmaceutics 2016, 8, 30.

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