Pharmacokinetic studies of hyperoside-2-hydroxypropyl-β-cyclodextrin inclusion complex and ameliorated DSS-induced colitis in mice

An inclusion complex formation with cyclodextrin is a promising method to improve the bioavailability of water-insoluble drugs. The pharmacokinetic characteristics of Hypero-side-2-hydroxypropyl-beta-cyclodextrin inclusion complex in rats were evaluated. Compared with Hyperoside, the results showed that maximum plasma concentration and AUC0-t in-dexes of Hyperoside inclusion complex in rat plasma were increased, the value of half-life time was prolonged, and the value of apparent clearance was decreased, which proved that Hyperoside complexed with 2-hydroxypropyl-beta-cyclodextrin could improve its bioavail-ability and increase its blood concentration. Secondly, the therapeutic effect of Hyper-oside before and after complexing was further compared through the dextran sodium sulfate-induced colitis in mice. The experimental results showed that under the same dose, the Hyperoside inclusion complex had a better therapeutic effect, which could significantly increase the body weight of mice, improve the disease activity index, alleviate colon shorten-ing, improve pathological colon changes, and have a better protective effect on colitis mice. According to 16S rDNA sequencing analyses, Hyperoside-2-hydroxypropyl-beta-cyclodextrin may have an anti-inflammatory effect by increasing the abundance of beneficial bacteria (e.g. Firmicuria) and decreasing the proportion of harmful bacteria (e.g. Bacteroidetes) to balance the colon's microbiota.

Automated summary

An inclusion complex formed with cyclodextrin can improve the bioavailability of water-insoluble drugs. The pharmacokinetic characteristics of Hyperoside-2-hydroxypropyl-beta-cyclodextrin inclusion complex were evaluated in rats, showing increased plasma concentration and AUC0-t indexes, prolonged half-life time, and decreased apparent clearance. In addition, the Hyperoside inclusion complex demonstrated a superior therapeutic effect in a colitis mice model, increasing body weight, improving disease activity index, alleviating colon shortening, and showing a protective effect. This may be attributed to the complex's anti-inflammatory effect by balancing the colon's microbiota.