Doxycycline delivery from PLGA microspheres prepared by a modified solvent removal method

We report on the development of a modified solvent removal method for the encapsulation of hydrophilic drugs within poly(lactic-co-glycolic acid) (PLGA). Using a water/oil/oil double emulsion, hydrophilic doxycycline was encapsulated within PLGA spheres with particle diameters ranging from approxima...

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Bibliographic Details
Published in:Journal of microencapsulation 2012-06, Vol.29 (4), p.344-352
Main Authors: Patel, Roshni S., Cho, Daniel Y., Tian, Cheng, Chang, Amy, Estrellas, Kenneth M., Lavin, Danya, Furtado, Stacia, Mathiowitz, Edith
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - administration & dosage
biodegradable polymers
Biological and medical sciences
Calorimetry, Differential Scanning
Crystallography, X-Ray
Delayed-Action Preparations
Doxycycline - administration & dosage
Drug Compounding - methods
drug delivery
Drug Delivery Systems
Emulsions
General pharmacology
Hydrophobic and Hydrophilic Interactions
Lactic Acid
Medical sciences
microencapsulation
Microscopy, Electron, Scanning
Microspheres
Nanospheres - chemistry
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyglycolic Acid
Solvents
Spectroscopy, Fourier Transform Infrared
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Summary:We report on the development of a modified solvent removal method for the encapsulation of hydrophilic drugs within poly(lactic-co-glycolic acid) (PLGA). Using a water/oil/oil double emulsion, hydrophilic doxycycline was encapsulated within PLGA spheres with particle diameters ranging from approximately 600 nm to 19 µm. Encapsulation efficiencies of up to 74% were achieved for theoretical loadings from 1% to 10% (w/w), with biphasic release over 85 days with nearly complete release at the end of this time course. About 1% salt was added to the formulations to examine its effects on doxycycline release; salt modulated release only by increasing the magnitude of initial release without altering kinetics. Fourier transform infrared spectroscopy indicated no characteristic differences between doxycycline-loaded and control spheres. Differential scanning calorimetry and X-ray diffraction suggest that there may be a molecular dispersion of the doxycycline within the spheres and the doxycycline may be in an amorphous state, which could explain the slow, prolonged release of the drug.
ISSN:0265-2048
1464-5246
DOI:10.3109/02652048.2011.651499