Increasing the Bile Acid Sequestration Performance of Cationic Hydrogels by Using an Advanced/Controlled Polymerization Technique
authors Mendonca, PV; Matos, A; Sousa, AF; Serra, AC; Simoes, S; Coelho, JFJ
nationality International
journal PHARMACEUTICAL RESEARCH
author keywords bile acid sequestrants (BAS); cationic hydrogel; free radical polymerization (FRP); supplemental activator and reducing agent atom transfer radical polymerization (SARA ATRP)
keywords CONTROLLED/LIVING RADICAL POLYMERIZATION; IN-VITRO; HYPOCHOLESTEROLEMIC CAPACITY; BINDING; POLYMERS; CHITOSAN; STATINS
abstract Purpose To investigate the influence of the polymerization technique and the content of hydroxyl groups on the performance of new bile acid sequestrants based on PAMPMTA-co-PHEA (PAMPTMA: poly((3-acrylamidopropyl)trimethylammonium chloride); PHEA: poly(2-hydroxyethyl acrylate)) hydrogels. Methods PAMPMTA-co-PHEA hydrogels were prepared using either free radical polymerization or supplemental activator and reducing agent atom transfer radical polymerization. The chemical structure and composition of the hydrogels was confirmed by both FTIR and ssNMR. The binding of sodium cholate as the model bile salt was evaluated in simulated intestinal fluid using HPLC. The degradation of the polymers was evaluated in vitro in solutions mimicking the gastrointestinal tract environment. Results The binding showed that an increase of the amount of HEA in the hydrogel lead to a decrease of the binding capacity. In addition, it was demonstrated for the first time that the hydrogels produced by SARA ATRP presented a higher binding capacity than similar ones produced by FRP. Finally, it was observed that copolymers of PAMPTMA-co-PHEA showed no sign of degradation in solutions mimicking both the stomach and the intestine environment. Conclusion The use of an advanced polymerization technique, such as the SARA ATRP, could be beneficial for the preparation of BAS with enhanced performance.
publisher SPRINGER/PLENUM PUBLISHERS
issn 0724-8741
year published 2017
volume 34
issue 9
beginning page 1934
ending page 1943
digital object identifier (doi) 10.1007/s11095-017-2204-5
web of science category Chemistry, Multidisciplinary; Pharmacology & Pharmacy
subject category Chemistry; Pharmacology & Pharmacy
unique article identifier WOS:000406495100017
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journal analysis (jcr 2017):
journal impact factor 3.335
5 year journal impact factor 3.513
category normalized journal impact factor percentile 68.229
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