Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin

The design of nanoparticle formulations composed of biopolymers, that govern the physicochemical properties of orally delivered insulin, relies on improving insulin stability and absorption through the intestinal mucosa while protecting it from harsh conditions in the gastrointestinal (GI) tract. Ch...

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Main Authors: Bruno Pessoa, Mar Collado-Gonzalez, Giuseppina Sandri, António Ribeiro
Format: Article
Language:English
Published: MDPI AG 2023-03-01
Series:Marine Drugs
Subjects:
Online Access:https://www.mdpi.com/1660-3397/21/3/179
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author Bruno Pessoa
Mar Collado-Gonzalez
Giuseppina Sandri
António Ribeiro
author_facet Bruno Pessoa
Mar Collado-Gonzalez
Giuseppina Sandri
António Ribeiro
author_sort Bruno Pessoa
collection DOAJ
description The design of nanoparticle formulations composed of biopolymers, that govern the physicochemical properties of orally delivered insulin, relies on improving insulin stability and absorption through the intestinal mucosa while protecting it from harsh conditions in the gastrointestinal (GI) tract. Chitosan/polyethylene glycol (PEG) and albumin coating of alginate/dextran sulfate hydrogel cores are presented as a multilayer complex protecting insulin within the nanoparticle. This study aims to optimize a nanoparticle formulation by assessing the relationship between design parameters and experimental data using response surface methodology through a 3-factor 3-level optimization Box–Behnken design. While the selected independent variables were the concentrations of PEG, chitosan and albumin, the dependent variables were particle size, polydispersity index (PDI), zeta potential, and insulin release. Experimental results showed a nanoparticle size ranging from 313 to 585 nm, with PDI from 0.17 to 0.39 and zeta potential ranging from −29 to −44 mV. Insulin bioactivity was maintained in simulated GI media with over 45% cumulative release after 180 min in a simulated intestinal medium. Based on the experimental responses and according to the criteria of desirability on the experimental region’s constraints, solutions of 0.03% PEG, 0.047% chitosan and 1.20% albumin provide an optimum nanoparticle formulation for insulin oral delivery.
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spelling doaj.art-d79259e5fea6483d80a7ff6ceb431ce32023-11-17T12:17:39ZengMDPI AGMarine Drugs1660-33972023-03-0121317910.3390/md21030179Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of InsulinBruno Pessoa0Mar Collado-Gonzalez1Giuseppina Sandri2António Ribeiro3Faculty of Pharmacy, University of Coimbra, 3000-048 Coimbra, PortugalFaculty of Pharmacy, University of Coimbra, 3000-048 Coimbra, PortugalDepartment of Drug Sciences, University of Pavia, Viale Taramelli, 12, 27100 Pavia, ItalyFaculty of Pharmacy, University of Coimbra, 3000-048 Coimbra, PortugalThe design of nanoparticle formulations composed of biopolymers, that govern the physicochemical properties of orally delivered insulin, relies on improving insulin stability and absorption through the intestinal mucosa while protecting it from harsh conditions in the gastrointestinal (GI) tract. Chitosan/polyethylene glycol (PEG) and albumin coating of alginate/dextran sulfate hydrogel cores are presented as a multilayer complex protecting insulin within the nanoparticle. This study aims to optimize a nanoparticle formulation by assessing the relationship between design parameters and experimental data using response surface methodology through a 3-factor 3-level optimization Box–Behnken design. While the selected independent variables were the concentrations of PEG, chitosan and albumin, the dependent variables were particle size, polydispersity index (PDI), zeta potential, and insulin release. Experimental results showed a nanoparticle size ranging from 313 to 585 nm, with PDI from 0.17 to 0.39 and zeta potential ranging from −29 to −44 mV. Insulin bioactivity was maintained in simulated GI media with over 45% cumulative release after 180 min in a simulated intestinal medium. Based on the experimental responses and according to the criteria of desirability on the experimental region’s constraints, solutions of 0.03% PEG, 0.047% chitosan and 1.20% albumin provide an optimum nanoparticle formulation for insulin oral delivery.https://www.mdpi.com/1660-3397/21/3/179biopolymersBox–Behnkenfactorial optimizationinsulin deliveryionotropic gelationnanoparticles
spellingShingle Bruno Pessoa
Mar Collado-Gonzalez
Giuseppina Sandri
António Ribeiro
Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin
Marine Drugs
biopolymers
Box–Behnken
factorial optimization
insulin delivery
ionotropic gelation
nanoparticles
title Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin
title_full Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin
title_fullStr Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin
title_full_unstemmed Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin
title_short Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin
title_sort chitosan albumin coating factorial optimization of alginate dextran sulfate cores for oral delivery of insulin
topic biopolymers
Box–Behnken
factorial optimization
insulin delivery
ionotropic gelation
nanoparticles
url https://www.mdpi.com/1660-3397/21/3/179
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AT giuseppinasandri chitosanalbumincoatingfactorialoptimizationofalginatedextransulfatecoresfororaldeliveryofinsulin
AT antonioribeiro chitosanalbumincoatingfactorialoptimizationofalginatedextransulfatecoresfororaldeliveryofinsulin