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Exploiting ionizable nature of PEtOx- co -PEI to prepare pH sensitive, doxorubicin loaded micelles.

Research paper by Naile N Ozturk, Asli A Kara, Sevgi S Gulyuz, Umut Ugur UU Ozkose, Mehmet Atilla MA Tasdelen, Asuman A Bozkir, Ozgur O Yilmaz, Imran I Vural

Indexed on: 07 Jul '20Published on: 07 Jul '20Published in: Journal of microencapsulation



Abstract

This study was conducted to evaluate block copolymers containing two different poly(ethyleneimine) (PEI) amounts, as new pH-sensitive micellar delivery systems for doxorubicin. Micelles were prepared with block copolymers consisting of poly(2-ethyl-2-oxazoline)--poly(ethyleneimine) (PEtOx--PEI) and poly(ε-caprolactone) (PCL) as hydrophilic and hydrophobic blocks, respectively. Doxorubicin loading, micelle size, pH-dependent drug release, and in vitro cytotoxicity on MCF-7 cells were investigated. The average size of drug-loaded micelles, was under 100 nm and drug loading was between 10.7-48.3% (w/w). pH-sensitive drug release was more pronounced (84.7% and 68.9% (w/w) of drug was released at pH 5.0 and pH 7.4, respectively) for the micelles of the copolymer with the lowest PEI amount. Cell viability of doxorubicin-loaded micelles which were prepared by the copolymer with the lowest PEI amount was 28-33% at 72 h. PEtOx--PEI--PCL micelles of this copolymer were found to be stable and effective pH-sensitive nano-sized carriers for doxorubicin delivery.