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Comparison of electrospun and extruded Soluplus®-based solid dosage forms of improved dissolution.
Zsombor K Nagy1, Attila Balogh, Balázs Vajna
1Organic Chemistry and Technology Department, Budapest University of Technology and Economics, H-1111 Budapest, Hungary. nagyzsomborkristof@gmail.com
Journal of Pharmaceutical Sciences
|September 16, 2011
Summary
Electrospinning and extrusion of spironolactone using Soluplus® improved drug dissolution. Electrospun fibers showed superior dissolution enhancement due to solid solutions and increased surface area.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Poor water solubility of active pharmaceutical ingredients (APIs) presents a significant challenge in drug formulation.
- Improving drug dissolution is crucial for enhancing bioavailability and therapeutic efficacy.
Purpose of the Study:
- To enhance the dissolution of a poorly water-soluble drug, spironolactone, using electrospinning (ES) and extrusion.
- To compare the effectiveness of ES and extrusion in forming solid solutions and improving drug dissolution.
Main Methods:
- Spironolactone was formulated with Soluplus® (a polyvinyl caprolactame-polyvinyl acetate-polyethylene glycol graft copolymer) as a carrier matrix.
- Electrospinning and extrusion techniques were employed to create drug-loaded fibers and extrudates.
- Characterization was performed using Raman microscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM), and energy-dispersive spectrometry (EDS).
Main Results:
- Electrospinning resulted in a true solid solution of spironolactone, achieving significant amorphization.
- Extrusion yielded a low amount of crystalline spironolactone, as detected by Raman microscopy, XRD, SEM, and EDS.
- Raman microspectrometry demonstrated the lowest detection limit for spironolactone crystals.
- Both ES and extrusion significantly improved drug dissolution rates.
Conclusions:
- Electrospun ultrafine fibers containing spironolactone solid solutions exhibited more effective dissolution enhancement compared to extrudates.
- These continuous manufacturing technologies show promise for addressing the poor dissolution of poorly water-soluble drugs.
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