Dasatinib (DST) is a Biopharmaceutics Classification System Class II medication with a high permeability and very low solubility. DST's low water solubility and poor dissolution result in low bioavailability. As a result, restricted aqueous solubility represents a bottleneck for DST's therapeutic success. Due to a large first-pass effect, animal research suggests that DST has an absolute bioavailability of 14–34 percent. Lipid-based drug delivery technologies, such as solid lipid nanoparticles (SLNs), can be utilised to circumvent hepatic first-pass metabolism and improve oral bioavailability. Methods: Submicron colloidal carriers with a size range of 50–1000 nm are known as SLNs. These are made from physiological lipids that have been distributed in water or an aqueous surfactant solution. By utilising intestinal lymphatic transport, DST can be easily loaded into SLNs to boost oral bioavailability. In a bioavailability research in rats, an ideal system was compared to that of DST suspension (SUS). Results: ATCC cell lines were used in an in vitro cytotoxicity research using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay technique, the percent inhibition was higher in SLN than in SUS. The pharmacokinetics of DST-SLNs in male Wistar rats following oral administration were investigated. When compared to a DST SUS, DST's bioavailability was improved by 2.28 times. Conclusion: The findings suggest that SLNs are a good lipid-based carrier system for increasing DST oral bioavailability.
Author(s)
Details
A. A. Mohamed Yasir Arafath
Department of Pharmacy Practice, Vinayaka Mission’s College
of Pharmacy, Salem, Tamil Nadu, India.
B.
Jaykar
Vinayaka Mission’s Research Foundation (Deemed to be
University), Salem, Tamil Nadu, India.
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