pharmacokinetics and in vivo chemosuppressive activity studies on cryptolepine hydrochloride and cryptolepine hydrochloride-loaded gelatine nanoformulation designed for parenteral administration for the treatment of malaria

Respuesta :

The primary goal of this study was to compare the pharmacokinetics profile of the medication free in solution with that of the parenterally administered, gelatine nanoparticles (CHN) containing cryptolepine hydrochloride for the treatment of malaria (CHS).

Via giving CHN or CHS (equal to 10 mg/kg of medication) by IV bolus injection into the lateral tail vein, single-dose pharmacokinetics was studied in Wistar rats. After delivery, the drug's plasma concentration was observed for 24 hours. In Wistar rats given a P.

berghei parasite challenge, chemopresor activity was examined. The intraperitoneal injection of either CHN or CHS at a dosage of 2.5–100 mg/kg/day was administered to the animals.

Giemsa-stained thin blood smears obtained on day four of infection were examined by light microscopy to gauge the amount of parasitaemia. It was discovered that CHN achieved a greater area under the curve (AUC (0-24)) compared to H CHS (by 4.5-folds).owever, CHS created a greater amount of dispersion (4-folds).

CHS had a lower (11.7 h) elimination half-life than CHN because of increased distribution and elimination rates (21.85 h). In comparison to CHS, CHN had greater chemosuppressive efficacy at all dosage levels due to its improved pharmacokinetic profile.

The molecule with the greatest chemosuppression (97.89 3.10) generated by 100 mg/kg of cryptolepine hydrochloride was loaded into gelatine nanoparticles, which enhanced both pharmacokinetics and in vivo antiplasmodial efficacy.

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