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DESIGN, DEVELOPMENT AND IN VIVO PHARMACOKINETIC EVALUATION OF ZOTEPINE LOADED SOLID LIPID NANOPARTICLES FOR ENHANCED ORAL BIOAVAILABILITY

NAGARAJ BANALA, TİRUMALESH C, DİNESH SURAM, NARENDAR DUDHIPALA

Acta Pharmaceutica Sciencia - 2021;59(3):385-404

Nanotechnology and Novel Drug Delivery Laboratory, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana, India

 

The purpose of this work was to prepare and evaluate the zotepine (ZT) loaded solid lipid nanoparticles (SLNs) that might improve the oral bioavailability. ZT-SLNs were developed using homogenization method and characterized for optimal system based on physicochemical characteristics and in-vitro release. Optimized ZT-SLNs were evaluated for permeation, crystalline nature using DSC and XRD, surface morphology using SEM and physical stability. Further, pharmacokinetic (PK) studies of ZT-SLN were conducted in Wistar rats comparison with ZT-coarse suspension (ZT-CS). Optimized formulation showed Z-avg, PDI, ZP of 138.1±3.2, 0.23±0.02 and -26.4±1.5 mV, respectively. In-vitro release studies showed prolonged release, DSC and XRD studies revealed the conversion of ZT to amorphous form. SEM studies showed spherical shape. Permeability and PK studies showed 1.4-folds and 2.0-folds improvement in oral bioavailability, respectively in comparison with ZTCS formulation. Therefore, the results concluded that SLNs could be considered as a new alternative delivery system for the enhancement of oral bioavailability of ZT.