thienopyrimidine and Pancreatic-Neoplasms

This research aimed to improve water solubility and oral bioavailability of a newly synthesized thienopyrimidine derivative (TPD) with anti-pancreatic cancer activity by loading on starch nanoparticles (SNPs).. TPD was synthesized, purified and its ADME behavior was predicted using Swiss ADME software. A UV spectroscopy method was developed and validated to measure TPD concentration at various dosage forms. SNPs loaded with TPD (SNPs-TPD) were prepared, characterized for particle size, polydispersity index, zeta potential, transmission electron microscopy, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), entrapment efficiency, in-vitro release, and in-vivo animal study.. The Swiss ADME results showed that TPD can be administered orally; however, it has low oral bioavailability (0.55) and poor water solubility. The significant regression coefficient of the calibration curve (r. SNPs-TPD were superior in drug solubility and oral bioavailability than those obtained from TPD suspension.

Topics: Animals; Antineoplastic Agents; Biological Availability; Drug Liberation; Female; Mice; Nanoparticles; Pancreatic Neoplasms; Pyrimidines; Solubility; Starch