Enhancement of oral bioavailability via solid lipid nanoparticles of anticancer drug dasatinib - An in vitro cytotoxicity and pharmacokinetic study
Journal Title: Asian Journal of Pharamceutical and Clinical Research - Year 2019, Vol 12, Issue 6
Abstract
Objective: Dasatinib (DST) is a BCS Class II drug having very low solubility and high permeability. Low aqueous solubility and poor dissolution of DST leads to poor bioavailability, Thus, limited aqueous solubility is the bottleneck for the therapeutic outcome of DST. Animal data suggests that the absolute bioavailability of DST is about 14 to 34% due to an extensive first-pass effect. To overcome hepatic first-pass metabolism and to enhance oral bioavailability, lipid–based drug delivery systems like solid lipid nanoparticles can be used. Methods: Solid lipid nanoparticles (SLNs) are sub-micron colloidal carriers having a size range of 50–1000 nm. These are prepared with physiological lipid and dispersed in water or aqueous surfactant solution. Dasatinib can be conveniently loaded into solid lipid nanoparticles to improve the oral bioavailability by exploiting the intestinal lymphatic transport. An optimal system was evaluated for bioavailability study in rats compared with that of dasatinib suspension. Results: In vitro cytotoxicity study were done by MTT assay method through ATCC cell lines, the percent inhibition was more in SLN when compared with Suspension. The Pharmacokinetics of dasatinib-SLNs after oral administration in male wistar rats was studied. The bioavailability of dasatinib was increased by 2.28 fold when compared with that of a dasatinib suspension. Conclusion: The results are indicative of SLNs as suitable lipid based carrier system for improving the oral bioavailability of dasatinib.
Authors and Affiliations
mohamed yasir arafath Aasiyar Abdul Rahman
Keywords
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