Abstract
A novel polyrotaxane (PR)-based triblock copolymer was exploited as polymeric carrier for doxorubicin (DOX). A sample holding a feed molar ratio of Pluronic F127 to β-CD to poly(ethylene glycol) methyl ether methacrylate (PEGMA) equal to 1:30:20 was synthesized via the in situ atom transfer radical polymerization (ATRP) and then conjugated with DOX using pH sensitive hydrazone linker. The resulting PR-DOX conjugates enabled to self-assemble into nano-particles of about 70 nm in diameter in aqueous solution as evidenced by TEM. The release of DOX was varied from 10 % to 37 % over 72 h at physiological and acidic pH, respectively. The PR-based triblock copolymer without DOX conjugation showed almost non toxicity, while these nano-particles with DOX conjugation presented increased toxicity.
Highlights
During the past decade there has been a growing interest in the investigation of polymeric conjugates or polymer-drug conjugates as potential drug delivery systems [1]
3 Results and discussion 3.1 Synthesis and characterization of PR-DOX According to our previous report [12 a], a PR-based triblock copolymer sample F-30-20 was synthesized via the in situ atom transfer free radical polymerization (ATRP) of poly(ethylene glycol) methyl ether methacrylate (PEGMA) initiated with a PPR made from a distal 2-bromopropionyl end-capped Pluronic F127 with β-CDs at 25 °C
A substantially higher number of PEGMA was incorporated to attach to two ends of the PPR most likely due to the fact that the resulting PPR is insoluble in aqueous solution and the end-capping ATRP was carried out heterogeneously
Summary
During the past decade there has been a growing interest in the investigation of polymeric conjugates or polymer-drug conjugates as potential drug delivery systems [1]. When poorly water- soluble drugs are covalently linked to water-soluble polymers or amphiphlic block copolymers to give rise to the polymeric conjugates, they generally enable to self-assemble into nano-sized polymeric micelles with a size of about 50-150 nm in diameter in aqueous solution. We prepared a pH-triggered target delivery system of DOX conjugated to β-CDs entrapped on the Pluronic F127 block of a PR-based triblock copolymer via acid-labile hydrazone linkage.
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
