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Research Article

Mechanochemical preparation of kaempferol intermolecular complexes for enhancing the solubility and bioavailability

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Pages 1924-1932 | Received 28 Nov 2017, Accepted 12 Jul 2018, Published online: 11 Sep 2018
 

Abstract

In this study, complexes of kaempferol (KF) with polysaccharide arabinogalactan (AG) and disodium glycyrrhizinate (Na2GA) were prepared through mechanochemical technique to improve the solubility and bioavailability of KF. The physicochemical properties and the interactions of KF with AG/Na2GA were investigated through dissolution, SEM, XRD, and DSC studies. The reduction of particle sizes and destruction of crystal forms revealed the formation of solid dispersion which may have assisted the dissolution of the drug. The accelerated stability study showed higher stability for KF–Na2GA complex. In vivo pharmacokinetic study was performed to observe the plasma drug concentrations for KF complexes. Mechanochemical complexation of KF with AG/Na2GA improved the pharmacological activity as evident by the inhibitory potential of the complexes towards carbohydrate metabolic enzymes. In vivo studies were performed in STZ-induced diabetic mice, where the group treated with KF–AG complex showed better liver and kidney function and lower blood glucose levels than pure KF. Therefore, mechanochemical complexes of KF with polysaccharide or glycyrrhizate may serve as a promising formulation for the treatment of diabetes.

Acknowledgements

The authors appreciate diploma students Shiping Jiang and Xiang Zheng (School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China) for their technical assistance in blood specimen collection.

Disclosure statement

No potential conflict of interest was reported by the authors.

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