Enhanced pharmacokinetic and therapeutic of GSH-responsive mPEG-<i>b</i>-P(HPMA)-SGI1776 conjugate for osteosarcoma.

ABSTRACT:

Introduction

SGI-1776 represents the first serine/threonine kinase inhibitor to be utilized in the treatment of osteosarcoma. It is severely restricted by poor aqueous solubility, short degradation half-life and severe side effect.

Methods

A polymeric prodrug is prepared by covalently embedding SGI-1776 into mPEG-b-P(N-(2-hydroxypropyl) methylacrylamide) carrier via GSH-responsive disulfide bond. The chemical composition and assembly properties of the conjugate are characterized.

Results

The loading capacity of SGI1776 in the conjugate is 22%. The conjugate displays a typical spherical nanoparticle with diameters around 150-260 nm. Cumulative release amounts of SGI1776 can be detected to be 52.9% at the concentration dithiothreitol of 20 mM at 24 h. The hemolys

SUBMITTER: Shi X 

PROVIDER: S-EPMC12588892 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature