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Please use this identifier to cite or link to this item: http://hdl.handle.net/10481/36490

Title: In Vitro and in Vivo Evaluation of Novel Cross-Linked Saccharide Based Polymers as Bile Acid Sequestrants
Authors: López Jaramillo, Francisco Javier
Girón González, María Dolores
Salto González, Rafael
Hernández Mateo, Fernando
Santoyo González, Francisco
Issue Date: 2015
Abstract: Bile acid sequestrants (BAS) represent a therapeutic approach for the management of hypercholesterolemia that relies on the cationic polymeric nature of BAS to selectively bind negatively charged bile acids. We hypothesized that the cross-linking of β-cyclodextrin (β-CD) and saccharides such as starch or dextrin with divinyl sulfone (DVS) yields homo- and hetero-polymeric materials with the ability to trap sterols. Our hypothesis was put to test by synthesizing a library of 22 polymers that were screened to evaluate their capability to sequester both cholesterol (CHOL) and cholic and deoxycholic acids (CA and DCA). Three polymers synthesized in high yield were identified as promising. Two were neutral hetero-polymers of β-CD and starch or dextrin and the third was a weakly cationic homo-polymer of starch, highlighting the importance of the cavity effect. They were tested in hypercholesterolemic male Wistar rats and their ability to regulate hypercholesterolemia was similar to that for the reference BAS cholestyramine, but with two additional advantages: (i) they normalized the TG level and (ii) they did not increase the creatinine level. Neither hepatotoxicity nor kidney injury was detected, further supporting them as therapeutical candidates to manage hypercholesterolemia.
Sponsorship: Financial Support was provided by Universidad de Granada in the frame of the Granada Research of Excellence Initiative on BioHealth (GREIB).
Publisher: MDPI
Keywords: Cross-linked saccharides
Hypercholesterolemia
Bile acid sequestrants
Cyclodextrin
Dextrin
Starch
Divinyl sulfone
URI: http://hdl.handle.net/10481/36490
ISSN: 1420-3049
Rights : Creative Commons Attribution-NonCommercial-NoDerivs 3.0 License
Citation: López Jaramillo, F.J.; et al. In Vitro and in Vivo Evaluation of Novel Cross-Linked Saccharide Based Polymers as Bile Acid Sequestrants. Molecules, 20(3): 3716-3729 (2015). [http://hdl.handle.net/10481/36490]
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