Background: Chili peppers are widely used in many cuisines as a spice, and capsaicin is
the main component. It has been reported that capsaicin acts as an antihyperglycemic agent. However,
it shows poor aqueous solubility and bioavailability.
Objective: The is to enhance the aqueous solubility and antihyperglycemic activity of capsaicin
through solid dispersion formulation.
Methods: Solid dispersions were prepared by the solvent evaporation method using polyethylene
glycol 6000 (PEG 6000) as a hydrophilic carrier. Polymer-drug miscibility and drug crystallinity
were characterized through the differential thermal analysis and X-ray powder patterns analysis.
Solid dispersions were evaluated for solubility, in vitro drug dissolution and in vivo animal study in
Results: Results of x-ray powder patterns analysis showed a considerable reduction of drug crystallinity
in solid dispersion. Differential thermal analysis result revealed a complete disappearance of
capsaicin melting onset temperature in solid dispersion. From the phase solubility data, it was observed
that the aqueous solubility of capsaicin was increased with increasing concentration of PEG
6000. Solid dispersion formulation showed considerable enhancement of in vitro release of drugs in
comparison to pure capsaicin. In vivo animal study in rats shows that the solid dispersion containing
capsaicin significantly reduced the blood glucose level in comparison to the free capsaicin.
Conclusion: Higher anti-hyperglycemic effect of capsaicin loaded solid dispersion in comparison to
the pure drug may be due to the enhancement of aqueous solubility of capsaicin. Thus, the solid
dispersion of capsaicin showed a simple approach for capsaicin delivery with improved antidiabetic
Keywords: Solid dispersion, capsaicin, in vitro dissolution rate, phase solubility, solubility enhancement, diabetes.
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