TY - JOUR
T1 - Alginate modified with maleimide-terminated PEG as drug carriers with enhanced mucoadhesion
AU - Shtenberg, Yarden
AU - Goldfeder, Mor
AU - Schroeder, Avi
AU - Bianco-Peled, Havazelet
N1 - Publisher Copyright:
© 2017 Elsevier Ltd
PY - 2017/11/1
Y1 - 2017/11/1
N2 - The goal of this study was to generate a new mucoadhesive carbohydrate-based delivery system composed of alginate (Alg) backbone covalently attached to polyethylene glycol (PEG) modified with a unique functional end-group (maleimide). The immobilization of PEG-maleimide chains significantly improved the mucoadhesion properties attributed to thioether bonds creation via Michael-type addition and hydrogen bonding with the mucus glycoproteins. Mucoadhesion studies using tensile and rotating cylinder assays revealed a 3.6-fold enhanced detachment force and a 2.8-fold enhanced retention time compared to the unmodified polymer, respectively. Additional indirect studies confirmed the presence of polymer-mucus glycoproteins interactions. Drug release experiments were used to evaluate the release profiles from Alg-PEG-maleimide tablets in comparison to Alg and Alg-SH tablets. Viability studies of normal human dermal fibroblasts cells depicted the non-toxic nature of Alg-PEG-maleimide. Overall, our studies disclose that PEG-maleimide substitutions on other biocompatible polymers can lead to the development of useful biomaterials for diverse biomedical applications.
AB - The goal of this study was to generate a new mucoadhesive carbohydrate-based delivery system composed of alginate (Alg) backbone covalently attached to polyethylene glycol (PEG) modified with a unique functional end-group (maleimide). The immobilization of PEG-maleimide chains significantly improved the mucoadhesion properties attributed to thioether bonds creation via Michael-type addition and hydrogen bonding with the mucus glycoproteins. Mucoadhesion studies using tensile and rotating cylinder assays revealed a 3.6-fold enhanced detachment force and a 2.8-fold enhanced retention time compared to the unmodified polymer, respectively. Additional indirect studies confirmed the presence of polymer-mucus glycoproteins interactions. Drug release experiments were used to evaluate the release profiles from Alg-PEG-maleimide tablets in comparison to Alg and Alg-SH tablets. Viability studies of normal human dermal fibroblasts cells depicted the non-toxic nature of Alg-PEG-maleimide. Overall, our studies disclose that PEG-maleimide substitutions on other biocompatible polymers can lead to the development of useful biomaterials for diverse biomedical applications.
KW - PEG
KW - alginate
KW - carbohydrate polymer
KW - drug delivery
KW - maleimide
KW - mucoadhesion
UR - http://www.scopus.com/inward/record.url?scp=85026899915&partnerID=8YFLogxK
U2 - 10.1016/j.carbpol.2017.07.076
DO - 10.1016/j.carbpol.2017.07.076
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AN - SCOPUS:85026899915
SN - 0144-8617
VL - 175
SP - 337
EP - 346
JO - Carbohydrate Polymers
JF - Carbohydrate Polymers
ER -