Ursodiol Loaded Polymeric Nanoparticle: Formulation, Optimization And Invitro – Invivo Pharmacodynamic Evaluation

Abstract

The present research is to formulate and evaluate the in-vivo pharmacokinetic studies on Ursodiol polymeric
nanoparticle. The polymeric nanoparticles were optimized by 23
factorial design and the best formulation will
be selected based on the effect of independent variable on dependent variable. The optimized polymeric
nanoparticle will be subjected to in-vivo pharmacokinetic and pharmacodynamics studies. The Ursodiol
polymeric nanoparticle was formulated by homogenization cum ultra-sonication method by investigating the
effect of variables like polymer concentration (HPMC), homogenization time (min) and ultra sonication time
(min) using a factorial design. The formulated Ursodiol polymeric nanoparticle was evaluated for particle size
(nm), zeta potential (mV), polydispersity index, entrapment efficiency (%), drug content, in-vitro drug release,
in-vitro release kinetic studies and stability studies as per ICH guidelines criteria. The optimized polymeric
nanoparticle will be subjected to in-vivo pharmacokinetic and Pharmacodynamic studies. From the derived data
U4 formulation showed predicted particle size (168.0 ± 3.24 nm), maximum zeta potential (-34.1 ± 2.34mV), less
polydispersity index (0.320 ± 0.24), increased entrapment efficiency (98.62 ± 3.68%), and good release
properties (92.22 ± 3.14 at 24h) among the eight formulations tested. From the in-vivo pharmacokinetic
evidence, it was concluded that the polymeric nanoparticle with Ursodiol showed improved bioavailability than
the marketed dosage form Ursocol SR®, by enhancing the plasma drug concentration profile like AUC and Cmax.
The findings suggest that PNs have controlled drug release and can be used as a drug delivery carrier for Ursodiol
to improve bioavailability