Tacrolimus loaded lipid-polymer hybrid nanoparticles incorporated thermosensitive gel as intravesical drug delivery system

Abstract

A drug that is administered through a catheter into the bladder is referred to as an intravesical drug delivery system. The aim of this work is to improvise intravesical drug delivery of Tacrolimus loaded lipid polymer hybrid nanoparticles thermosensitive gel for bladder wall to provide control release, increase intravesical residence time and avoid fast removal by urination. The Tacrolimus loaded lipid polymer hybrid nanoparticles mimic cell membrane and enhance cellular uptakes. Our data reveals nanocarrier formation with a mean particle size, zeta potential and entrapment efficiency of optimal formula was found to be 124±0.01 nm,-27.5±0.102mv and 72% ± 0.15% respectively. In situ gelling formulations containing TAC-CS-LPHNs can adhere to the mucosal layer of the bladder and help in the diffusion of therapeutic agent across the bladder wall. To impart mechanical strength and mucoadhesive properties, the chitosan concentration was adjusted to 0.5% and 0.25%.The image of field emission scanning electron microscope shows an irregular surface with filled pores with nanoparticles. The gel was syringeable and had reasonable viscosity within room temperature. A Tissue uptake study reveals that Tacrolimus loaded lipid polymer hybrid nanoparticles have been penetrating bladder tissues and accumulated inside the cytoplasm and nucleus of urothelium epithelial cells. In addition, the bioimaging study shows that the gel resided inside the bladder for up to 2 hrs and completely urinated out of the bladder with negligible distribution to other tissues.