Elsevier

Journal of Controlled Release

Volume 32, Issue 3, 1 December 1994, Pages 269-277
Journal of Controlled Release

Improved synthesis of adriamycin-conjugated poly (ethylene oxide)-poly (aspartic acid) block copolymer and formation of unimodal micellar structure with controlled amount of physically entrapped adriamycin

https://doi.org/10.1016/0168-3659(94)90237-2Get rights and content

Abstract

The conjugation reaction of adriamycin (ADR) to poly (ethylene oxide)-poly (aspartic acid) block copolymer (PEO-P(Asp)) was optimized in order to inhibit side reactions, which damage the ADR residues. By diminishing alkaline components and lowering temperature, ADR was successfully conjugated to PEO-P(Asp) without side reactions. The obtained ADR-conjugated poly(ethylene oxide)-poly(aspartic acid) block copolymer [PEO-P(Asp(ADR))] was observed to form a micellar structure with a narrower distribution in size than the PEO-P(Asp(ADR)) synthesized by the previously reported method. Unconjugated ADR remained in the inner core of the PEO-P(Asp(ADR)) micelles was removed by dialysis in organic solvents to obtain the micelle without free ADR. Regulated amount of free ADR was then successfully entrapped into the inner core of these purified micelles. In vitro cytotoxicity against P388D1 cells of PEO-P(Asp(ADR)) micelle without free ADR was assayed to estimate the contribution of physically entrapped ADR on anti-tumor activity of the micelle-forming polymeric drug, PEO-P(Asp(ADR)).

References (19)

There are more references available in the full text version of this article.

Cited by (147)

  • Self-assembled polymeric nanostructures: a promising platform for bioimaging and therapeutic applications

    2022, Engineered Nanostructures for Therapeutics and Biomedical Applications
  • Applications of Polymers in Parenteral Drug Delivery

    2020, Applications of Polymers in Drug Delivery
  • Polymeric micelles in biomedical science

    2019, Nanoparticles in Pharmacotherapy
View all citing articles on Scopus
View full text