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Updated: Feb 12, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
09:56

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles

Published on: August 2, 2016

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Self-assembled and pH-sensitive mixed micelles as an intracellular doxorubicin delivery system

Samira Jafarzadeh-Holagh1, Sameereh Hashemi-Najafabadi1, Hossein Shaki1

  • 1Biomedical Engineering Division, Chemical Engineering Faculty, Tarbiat Modares University, P.O. Box: 14115-143, Tehran, Iran.

Journal of Colloid and Interface Science
|April 6, 2018
PubMed

Insights

This study developed a pH-sensitive nanocarrier for doxorubicin delivery, showing enhanced drug release in acidic tumor environments. The nanocarrier demonstrated improved anti-cancer effects and cellular uptake compared to free doxorubicin.

Area of Science:

  • Biomedical Engineering
  • Materials Science
  • Oncology

Background:

  • Nanocarrier systems are crucial for targeted cancer therapy.
  • Intelligent drug delivery systems respond to specific stimuli for enhanced efficacy.
  • The acidic tumor microenvironment presents a target for pH-sensitive drug release.

Purpose of the Study:

  • To develop a pH-sensitive mixed micellar system for doxorubicin delivery.
  • To investigate the drug release profile of the nanocarrier at different pH levels.
  • To evaluate the in vitro cytotoxicity and cellular uptake of the doxorubicin-loaded micelles.

Main Methods:

  • Conjugation of Dextran-Stearic Acid (Dex-SA) and Dextran-Histidine (Dex-His) polymers to form mixed micelles.
  • Encapsulation of doxorubicin (DOX) into the micellar system.
  • In vitro drug release studies at neutral (pH 7.4) and acidic pH.
  • Cytotoxicity and cell uptake assays using U87 MG cell line.

Main Results:

  • The Dex-SA/Dex-His mixed micellar system effectively encapsulated doxorubicin.
  • Drug release was significantly higher under acidic conditions (76%) compared to neutral conditions (56%).
  • DOX-loaded micelles exhibited superior anti-proliferation effects and cellular uptake in U87 MG cells versus free DOX.

Conclusions:

  • The developed pH-sensitive mixed micellar system is a promising nanocarrier for targeted doxorubicin delivery in cancer therapy.
  • The system's ability to release drugs in response to acidic pH enhances its therapeutic potential.
  • The enhanced cytotoxicity and cellular uptake suggest improved efficacy for cancer treatment.
Keywords:
DextranHistidineMixed micelleStearic acidpH sensitive

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