Pyrimethamine nanosuspension with improved bioavailability: in vivo pharmacokinetic studies

Drug Delivery and Translational Research
Vividha DhapteVarsha Pokharkar

Abstract

Pyrimethamine is a standard antiprotozoal drug recommended for prophylaxis and treatment of malarial infections. Limited bioavailability, slow onset of action, and life-threatening side effects restrict its use. Hence, in the present study, pyrimethamine nanosuspension was prepared with the objective to improve its dissolution rate and pharmacokinetic profile. Stable pyrimethamine nanosuspension with submicron particle size was prepared by nanoprecipitation and high-pressure homogenization techniques. Nanosizing and stabilizers modified the surface characteristics of drug particles resulting in considerable increase in the dissolution rate. The in vivo pharmacokinetic studies of the prepared nanosuspension were carried out and compared with plain pyrimethamine suspension and marketed pyrimethamine suspension. The in vivo pharmacokinetic profiling of pyrimethamine nanosuspension in rats showed higher AUC0-24 h and C max compared to the plain and marketed pyrimethamine suspensions. In contrast to its plain and marketed formulation, pyrimethamine nanosuspension showed rapid onset of action (T max 0.5 h vs. 2 h). Also, the low volume of distribution and reduced elimination half-life of the developed nanosuspension can lead to reduc...Continue Reading

References

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Apr 14, 2011·Journal of Biomedical Nanotechnology·Vividha Dhapte, Varsha Pokharkar

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Citations

Dec 21, 2019·Drug Delivery and Translational Research·Varsha PokharkarVividha Dhapte-Pawar

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