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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
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Redox-Responsive Polymersomes as Smart Doxorubicin Delivery Systems
Carmen Ferrero1, Marta Casas1, Isidoro Caraballo1
1Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/Prof. García González No. 2, 41012 Sevilla, Spain.
Pharmaceutics
|August 26, 2022
Summary
Redox-responsive polymersomes efficiently encapsulate doxorubicin hydrochloride (Dox·HCl) for controlled anticancer drug delivery. These smart nanocarriers release drugs selectively in the tumor microenvironment, enhancing therapeutic efficacy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery
Background:
- Stimuli-responsive polymersomes offer programmed release of cytotoxic anticancer agents like doxorubicin hydrochloride (Dox·HCl).
- A novel biodegradable, redox-responsive triblock copolymer (mPEG-PDH-mPEG) with disulfide linkages was developed.
Purpose of the Study:
- To develop and characterize polymersomes for simultaneous formation and doxorubicin hydrochloride loading using a solvent-exchange method.
- To evaluate the drug encapsulation efficiency and in vitro release profile of the designed polymersomes.
Main Methods:
- Synthesis of mPEG-PDH-mPEG triblock copolymer.
- Solvent-exchange method for polymersome formation and doxorubicin hydrochloride loading.
- Characterization of polymersome morphology, size, zeta potential, encapsulation efficiency, and drug release kinetics.
Main Results:
- Uniform spherical polymersomes (120-190 nm) with negative zeta potentials were successfully prepared.
- High encapsulation efficiency of doxorubicin hydrochloride (up to 98 wt.%) was achieved.
- Prolonged, diffusion-driven drug release (~34% in 48 h) at physiological conditions was observed, with enhanced release (~77%) in the presence of glutathione (GSH) due to disulfide bond cleavage.
Conclusions:
- The designed redox-responsive polymersomes demonstrate excellent potential for controlled and selective delivery of doxorubicin hydrochloride.
- These smart nanocarriers are promising for targeted drug release in the reductive environment characteristic of cancer cells.
Keywords:
doxorubicin hydrochloridedrug release kineticspolymersomeredox-responsivesmart drug delivery systemstriblock copolymer mPEG–PDH–mPEG
