ACTA Pharmaceutica Sciencia 2021 , Vol 59 , Num 3
Design, development and in vivo pharmacokinetic evaluation of zotepine loaded solid lipid nanoparticles for enhanced oral bioavailability
Nagaraj BANALA 1 Tirumalesh C 1 Dinesh SURAM 1 Narendar DUDHIPALA 1
1 Nanotechnology and Novel Drug Delivery Laboratory, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana-506009, India
DOI : 10.23893/1307-2080.APS.05923 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. Keywords : Zotepine, solid lipid nanoparticles, crystallinity, in vitro release, ex vivo permeation, oral bioavailability

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