Abstract
Objective: Observations from traditional medicine and findings of modern science recommend use of curcuminoids and piperine in inflammatory ailments such as rheumatoid arthritis. Therapeutic potential of these phytoconstituents cannot be exploited to the maximum extent because of poor solubility and low bioavailability. The objective of this study was to overcome these challenges and harness the potential of these phytoconstituents by developing lipid and surfactant-based formulations. Methods: A microemulsion was prepared by selecting lipids, surfactants and cosurfactants on the basis of the solubility and stability of phytoconstituents. It was further converted into a transparent gel for topical application. The phytoformulation was characterized by physicochemical tests. Its hemocompatibility and irritation potential was determined. Further phytoformulation was studied in RAW 264.7 cells for cell internalization and antiarthritic potential was investigated in Complete Freund’s Adjuvant (CFA) induced arthritic rats. The disease progression was recorded. At the end of the study hematological, biochemical and oxidative stress parameters were measured. Results: A stable phytoformulation containing 0.75% w/w curcuminoids and 0.25% w/w piperine was developed. At the end of 24 hours, the amount of curcuminoids and piperine permeated through the skin from phytoformulation was 4.38 and 1.38 times that of the oil. It had good hemocompatibility and poor irritation potential. Internalization of phytoformulation in RAW 264.7 cells was concentration dependent. There were significant changes in rats due to disease induction by CFA and results indicated regression of the disease progress due to phytoformulation. Conclusion: Lipid and surfactant-based formulation improved solubility and permeability of phytoconstituents. The developed phytoformulation could recover inflammatory changes in rats and it can be further studied in human beings.
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