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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
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Multifunctional Mixed Micelles for Efficient Docetaxol Delivery for Cancer Therapy
Pei Zhang1, Wenxiu He1, Huiyuan Zhang1
1School of Pharmaceutical Science, Shandong University, 44 West Wenhua Road, Jinan, Shandong Province, 250012, P. R. China.
Chempluschem
|January 23, 2020
Summary
This study developed redox-sensitive mixed micelles for docetaxel (DTX) delivery, utilizing folic acid (FA) for targeted cancer therapy. These targeted micelles show enhanced cellular uptake and potent anticancer activity in folate receptor-positive cells.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery
Background:
- Docetaxel (DTX) is a potent anticancer drug with limitations in specificity and efficacy.
- Developing targeted drug delivery systems can improve cancer chemotherapy outcomes.
- Functional co-polymers offer versatile platforms for creating advanced nanocarriers.
Purpose of the Study:
- To construct redox-sensitive mixed micelles co-assembled from PEG-PBLG-SS-DTX and PEG-FA.
- To enhance the target specificity and anticancer efficiency of docetaxel (DTX).
- To evaluate the drug release, cellular uptake, and cytotoxicity of the developed mixed micelles.
Main Methods:
- Preparation of mixed micelles using the dialysis method.
- Characterization of micelle size, polydispersity, and critical micelle concentration.
- In vitro drug release studies in the presence and absence of a reducing agent (DTT).
- In vitro cytotoxicity, cellular uptake, and apoptosis assays using MTT, fluorescence microscopy, and flow cytometry on FR-positive and FR-negative cell lines.
Main Results:
- Spherical mixed micelles with a size of 129.7±2.1 nm and low polydispersity (0.10±0.02) were successfully prepared.
- The mixed micelles exhibited excellent self-assembly and stability, with a critical micelle concentration of 5.08 μg/mL.
- DTX release was significantly accelerated in the presence of DTT, indicating redox-sensitivity.
- Folic acid (FA)-targeted micelles showed enhanced cellular uptake and cytotoxicity in folate receptor (FR)-positive MCF-7 cells compared to non-targeted micelles.
Conclusions:
- Redox-sensitive PEG-PBLG-SS-DTX/PEG-FA mixed micelles demonstrate efficient DTX release in response to reducing environments.
- FA-mediated targeting significantly improves cellular uptake and antitumor efficacy in FR-positive cancer cells.
- These targeted mixed micelles represent a promising drug delivery system for enhanced cancer chemotherapy.
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