DESIGN, EVALUATION, AND PHARMACOKINETIC STUDIES OF PALIPERIDONE SOLID LIPID NANOPARTICLES FOR BIOAVAILABILITY ENHANCEMENT

Cheekati Reshma and Pasham Venkanna*

ABSTRACT

The purpose of the study was to develop and assess paliperidone (PPD) loaded solid lipid nanoparticles (SLNs) for the treatment of schizophrenia. SLNs use solid lipids such as glyceryl tristearate, tripalmitin, and glyceryl stearate citrate, followed by hot homogenization and ultrasonication. Particle size (P.S.), zeta-potential (Z.P.), polydispersity index (PDI), entrapment efficiency (E.E.), drug content, and in vitro release studies were conducted on all produced formulations. The optimized formulation (PDP 4) containing tripalmitin has been observed. In this instance, low lipid concentration has been associated with higher drug release percentages (86.51%), lower P.S. (210.68 nm), higher E.E. (74.65%), low PDI (0.208), and good Z.P. (-28.97), all of which point to a stable formulation. Pharmacokinetic studies show that the formulation (PDP 4) has an improved relative bioavailability that is 2.26 times higher than the coarse suspension of pure drug. It was concluded that the tripalmitin-containing formulation SLN-PDP (4) exhibits significant results.

Keywords: Solid lipid nanoparticles, Paliperidone, Hot homogenization & ultrasonication, and Pharmacokinetic studies.