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Molecules 2017, 22(10), 1707;

Electrostatic Self-Assembled Chitosan-Pectin Nano- and Microparticles for Insulin Delivery

Faculty of Animal Science and Food Engineering, USP—University of São Paulo, Av. Duque de Caxias Norte, 225, Pirassununga CEP 13635-900, São Paulo, Brazil
Department of Exact and Earth Science, UNIFESP—Federal University of São Paulo, Rua São Nicolau, 210, Diadema CEP 09913-030, São Paulo, Brazil
Institut für Biologie und Biotechnologie der Pflanzen, Westfälische Wilhelms—Universität Münster, Schlossgarten 3, 48149 Münster, Germany
School of Food Science and Nutrition, University of Leeds, Leeds LS2 9JT, UK
School of Chemical Engineering, UNICAMP—State University of Campinas, Av. Albert Einstein, 500, Campinas CEP 13083-852, São Paulo, Brazil
Authors to whom correspondence should be addressed.
Received: 14 July 2017 / Revised: 29 September 2017 / Accepted: 4 October 2017 / Published: 12 October 2017
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A polyelectrolyte complex system of chitosan-pectin nano- and microparticles was developed to encapsulate the hormone insulin. The aim of this work was to obtain small particles for oral insulin delivery without chemical crosslinkers based on natural and biodegradable polysaccharides. The nano- and microparticles were developed using chitosans (with different degrees of acetylation: 15.0% and 28.8%) and pectin solutions at various charge ratios (n+/n given by the chitosan/pectin mass ratio) and total charge. Nano- and microparticles were characterized regarding particle size, zeta potential, production yield, encapsulation efficiency, stability in different media, transmission electron microscopy and cytotoxicity assays using Caco-2 cells. The insulin release was evaluated in vitro in simulated gastric and intestinal media. Small-sized particles (~240–~1900 nm) with a maximum production yield of ~34.0% were obtained. The highest encapsulation efficiency (~62.0%) of the system was observed at a charge ratio (n+/n) 5.00. The system was stable in various media, particularly in simulated gastric fluid (pH 1.2). Transmission electron microscopy (TEM) analysis showed spherical shape particles when insulin was added to the system. In simulated intestinal fluid (pH 6.8), controlled insulin release occurred over 2 h. In vitro tests indicated that the proposed system presents potential as a drug delivery for oral administration of bioactive peptides. View Full-Text
Keywords: chitosan; pectin; microparticles; nanoparticles; insulin; Caco-2 cells chitosan; pectin; microparticles; nanoparticles; insulin; Caco-2 cells

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Maciel, V.B.V.; Yoshida, C.M.P.; Pereira, S.M.S.S.; Goycoolea, F.M.; Franco, T.T. Electrostatic Self-Assembled Chitosan-Pectin Nano- and Microparticles for Insulin Delivery. Molecules 2017, 22, 1707.

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