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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Doxycycline delivery from PLGA microspheres prepared by a modified solvent removal method.
Roshni S Patel1, Daniel Y Cho, Cheng Tian
1Department of Molecular Pharmacology, Physiology, and Biotechnology, Center for Biomedical Engineering, Center for Biomedical Engineering, Brown University, Providence, RI 02912, USA.
Journal of Microencapsulation
|January 24, 2012
Summary
Researchers developed a new method for encapsulating hydrophilic drugs in poly(lactic-co-glycolic acid) (PLGA) microspheres. This technique achieves high drug loading and sustained release over 85 days.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Encapsulating hydrophilic drugs in biodegradable polymers like poly(lactic-co-glycolic acid) (PLGA) is challenging due to drug solubility issues.
- Existing methods often result in low encapsulation efficiencies and burst release, limiting therapeutic efficacy.
- Developing robust methods for hydrophilic drug encapsulation in PLGA is crucial for advanced drug delivery applications.
Purpose of the Study:
- To develop and optimize a modified solvent removal method for encapsulating hydrophilic drugs within PLGA.
- To characterize the resulting PLGA microspheres and evaluate their drug loading, particle size, and release kinetics.
- To investigate the effect of salt addition on drug release profiles.
Main Methods:
- Utilized a water/oil/oil double emulsion technique for encapsulating hydrophilic doxycycline within PLGA.
- Characterized microsphere particle size distribution, ranging from approximately 600 nm to 19 µm.
- Employed Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction for material analysis.
Main Results:
- Achieved high encapsulation efficiencies of up to 74% for doxycycline loadings from 1% to 10% (w/w).
- Demonstrated biphasic drug release over 85 days, with nearly complete release by the study's end.
- Observed that salt addition increased initial drug release magnitude but did not alter release kinetics; material analysis suggested amorphous drug dispersion within PLGA.
Conclusions:
- The modified solvent removal method is effective for encapsulating hydrophilic drugs in PLGA, yielding high efficiencies and controlled release.
- The amorphous state of doxycycline within PLGA spheres likely contributes to the observed slow and prolonged drug release.
- This approach offers a promising strategy for developing sustained-release formulations of hydrophilic drugs.
