Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood

Adehin, Ayorinde; Tan, Keai Sinn; Tan, Wen

doi:10.1016/j.curtheres.2019.06.003

Cited by 1 publication

(1 citation statement)

References 13 publications

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“…STV exhibited a wide range of biological activities and pharmacological effects, including anti-fungal 2 , anti-neoplastic 3 , 4 , 5 , anti-viral 6 , 7 , improving insulin sensitivity, reducing plasma triglycerides 8 , 9 . It also reduces vasoconstriction by the regulation of the ion channels and has cardioprotective effect against coronary reperfusion damage with little toxicity 10 , 11 , 12 . However, one drawback of STV's application as medicine could be its low solubility and low bioavailability 13 .…”

Section: Introductionmentioning

confidence: 99%

Simultaneous improvement to solubility and bioavailability of active natural compound isosteviol using cyclodextrin metal-organic frameworks

Chen

Guo

Zhang

et al. 2021

Acta Pharmaceutica Sinica B

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Cyclodextrin metal-organic framework (CD-MOF) as a highly porous supramolecular carrier could be one of the solutions to the insolubility of isosteviol (STV). The solubility of STV was lower than 20.00 ng/mL at pH 1.0 and pH 4.5, whilst its solubility increased to 20,074.30 ng/mL at pH 6.8 and 129.58 ng/mL in water with a significant pH-dependence. The in vitro release profiles of STV from STV@CD-MOF (0.5:1) were pH-independent in distinct pH media and closed to be thoroughly released but no such release profiles were observed for STV@CD-MOF (1:1) owing to nanoclusters formation. The bioavailability of STV@CD-MOF (1:1) in rats was 8.67-fold higher than that of STV, and was 1.32- and 1.27-fold higher than that of STV@CD and STV@CD-MOF (0.5:1). Our results indicated that the inclusion mechanism played a primary role when STV in CD-MOF was at a low loading ratio, while the increasement in bioavailability at a high loading ratio, which was attributed to the nanocluster mechanism. This was confirmed by molecular simulation. In conclusion, CD-MOF is a promising system for STV loading, overcoming the insolubility and to improve the bioavailability of this natural compound.

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