Polymeric nanostructures with pH-labile core for controlled drug release

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• 作者：Rakesh Banerjee ; Saikat Maiti ; Debabrata Dey ; Dibakar Dhara ; ^{dibakar@chem.iitkgp.ernet.in" class="auth_mail" title="E-mail the corresponding author} ; ^{dibakar@live.in" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Polymer colloids ; Thiol&ndash ; acrylate Michael addition ; RAFT polymers ; Block copolymers ; pH-triggered degradation ; Thermosensitive release ; Prednisolone
• 刊名：Journal of Colloid and Interface Science
• 出版年：2016
• 出版时间：15 January 2016
• 年：2016
• 卷：462
• 期：Complete
• 页码：176-182
• 全文大小：1491 K

文摘

Efficient and stimuli-triggered controlled delivery of therapeutics is one of the important issues in modern advanced therapy. In the present work, a versatile route for the synthesis of core cross-linked polymeric nanostructures (CLPN) through thiol–acrylate Michael addition reaction via the formation of β-thiopropionate has been described. The acid groups of the poly(acrylic acid) block of poly(ethylene glycol)-b-poly(N-isopropylacrylamide)-b-poly(acrylic acid) triblock copolymer were reacted with 2-hydroxyethyl acrylate (HEA) to yield the corresponding acrylate-functionalized copolymer (P1). Following this, P1 was reacted with a thiol functionalized cross-linker (CL) resulting in the formation of core cross-linked polymeric nanoparticles through acrylate–thiol Michael reaction. The ability of these nanoparticles to encapsulate drug molecules inside their core and their effective release following a pH-triggered controlled degradation of the core were demonstrated. The temperature sensitive release behaviour of the system was also studied. The non-toxic nature of the precursor polymers and the core cross-linked polymeric nanoparticles was also established, that further substantiated their potential as carriers for controlled release of drugs.