4.6 Article

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

Journal

ANALYST
Volume 146, Issue 5, Pages 1620-1625

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d1an00163a

Keywords

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Funding

  1. National Natural Science Foundation of China [21705081]
  2. Natural Science Foundation of Jiangsu Province [BK20161037, BK20201232]
  3. Natural Science Foundation of Nanjing University of Chinese Medicine [NZY21705081]
  4. 333 High-level Talents Training Project Funded by Jiangsu Province [BRA2020071]

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Synthesis of PEG and peptide-modified titanium phosphate nanoparticles improved the drug delivery efficacy of the hydrophobic drug KS-01, leading to increased therapeutic efficacy as demonstrated by lower cell viability rate and real-time visualization of therapeutic effects.
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-3 beta,11 beta-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.

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