Multifunctional titanium phosphate carriers for enhancing drug delivery and evaluating real-time therapeutic efficacy of a hydrophobic drug component in Euphorbia kansui

Abstract

Nanoparticles are often used to serve as drug delivery systems to improve the therapeutic efficacy of some hydrophobic drugs. In this work, PEG and peptide-modified titanium phosphate nanoparticles (TiP–PEG/peptide) were synthesized to enhance the drug delivery efficacy of tirucalla-8,24-diene-3β,11β-diol-7-one (KS-01), a major bioactive and hydrophobic component extracted from Euphorbia kansui. This drug delivery system with a loading efficiency of about 29.8 mg KS-01/1 g TiP–PEG/peptide exerted a significantly lower cell viability rate of MCF-7 than free KS-01, indicating that these carriers can effectively increase the therapeutic efficacy by improving its water solubility. Moreover, according to the fluorescence intensity of FAM which can be generated by caspase-3 cleaving DEVD-embedded peptide, the caspase-3 level could be determined and the therapeutic efficacy could be visualized in real time.