Dendritic Boronic Acids for the Delivery of Diol-containing Drugs

This thesis outlines the preparation of polymeric micelles between boronic acid-functionalized PEG-dendritic block copolymers and diol-containing drugs, as a promising strategy in drug delivery. Taking advantage of terminal azide groups for functionalization, PEG-GATG dendritic block copolymers with...

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Detalhes bibliográficos
Autor: Al-Ni'mat, Muna Ahmad Hwaimel
Tipo de documento: tese
Data de publicação:2020
País:España
Recursos:Universidad de Santiago de Compostela (USC)
Repositório:Minerva. Repositorio Institucional de la Universidad de Santiago de Compostela
Idioma:inglês
OAI Identifier:oai:minerva.usc.gal:10347/24412
Acesso em linha:http://hdl.handle.net/10347/24412
Access Level:Acceso aberto
Palavra-chave:Materias::Investigación::23 Química::2304 Química macromolecular::230409 Modificación de macromoléculas
Materias::Investigación::23 Química::2304 Química macromolecular::230423 Síntesis de macromoléculas
Materias::Investigación::23 Química::2390 Química farmacéutica::239001 Diseño. Síntesis y estudio nuevos fármacos
Descrição
Resumo:This thesis outlines the preparation of polymeric micelles between boronic acid-functionalized PEG-dendritic block copolymers and diol-containing drugs, as a promising strategy in drug delivery. Taking advantage of terminal azide groups for functionalization, PEG-GATG dendritic block copolymers with peripheral boronic acids were obtained via reductive amination with 2-formylphenylboronic. The ability of the resulting boronic acid-functionalized copolymers (PEG-[G3]-BO2H2) to encapsulate drugs incorporating 1,2- and 1,3-diols into micelles, via selective boronic ester formation, was assessed in aqueous media at pH 7.4. Gemcitabine, an anticancer drug was selected for a deeper study. After incorporation into micelles in the presence of catechol, the encapsulation efficiency and stability of the micelles were determined, and their toxicity profile studied.