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Methods Development for Blood Borne Macrophage Carriage of Nanoformulated Antiretroviral Drugs
Published on: December 9, 2010
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Electrosprayed core-shell solid dispersions of acyclovir fabricated using an epoxy-coated concentric spray head.
Zhe-Peng Liu1, Lei Cui2, Deng-Guang Yu3
1School of Medical Instrument and Food Engineering, Shanghai, People's Republic of China.
International Journal of Nanomedicine
|May 3, 2014
Summary
This study introduces novel core-shell microparticle solid dispersions for poorly soluble drugs. These microparticles significantly enhance drug dissolution and sublingual permeation, offering a promising delivery system.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Poorly water-soluble drugs present significant bioavailability challenges.
- Conventional solid dispersions (SDs) have limitations in drug stabilization and release.
- Novel structural designs are needed to improve drug solubility and permeability.
Purpose of the Study:
- To develop and characterize a novel core-shell microparticle solid dispersion (SD) system.
- To enhance the dissolution and sublingual permeation of poorly water-soluble drugs.
- To investigate the amorphous state and distribution of active ingredients within the SD.
Main Methods:
- Fabrication of core-shell microparticles using coaxial electrospraying with polyvinylpyrrolidone (PVP) matrix.
- Characterization of microparticle size, drug content, and morphology.
- Analysis of drug-solubilizer distribution using differential scanning calorimetry (DSC) and X-ray diffraction (XRD).
- In vitro dissolution and sublingual mucosa permeation studies.
Main Results:
- Successfully prepared core-shell microparticle SDs with tunable drug content and average diameters of 1.36±0.67 and 1.74±0.58 μm.
- Acyclovir (ACY), sodium dodecyl sulfate, and sucralose were found in an amorphous state within the PVP matrix.
- Rapid ACY release within 1 minute and an approximately eightfold increase in sublingual permeation rate compared to raw ACY.
- Demonstrated favorable second-order interactions contributing to the amorphous state.
Conclusions:
- The novel core-shell microparticle SD system effectively improves the dissolution and sublingual permeation of poorly water-soluble drugs like acyclovir.
- Coaxial electrospraying is a viable method for fabricating complex SD structures.
- The developed system holds potential for enhanced oral and transmucosal drug delivery applications.
Keywords:
coaxial electrosprayingcore–shell microparticleepoxy-coated spray headpoorly water-soluble drugsolid dispersionMore Related Videos
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