Yogeeta O Agrawal, Tulshidas S Patil, Kiran D Patil, Nayan A Gujarathi, Amit Gangwal, Sameer N Goyal
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In-vivo Pharmacokinetic Assessment and In-vitro Characterization of Strategically Optimized Perphenazine-loaded Nanostructured Lipid Carriers for Nose-to-brain Targeting.
Background: Perphenazine (PPZ) is a prevalent antipsychotic medication used to treat schizophrenia. After oral treatment, however, it shows substantial first-pass metabolism and decreased bioavailability.
Objective: The goal of this research was to incorporate PPZ into nanostructured lipid carriers and thereby improve its bioavailability and brain targeting (PPZ-NLCs).
Methods: PPZ-NLCs were formulated by a high-pressure homogenization methodology under heated conditions and optimized by applying a 23-full factorial design.
Results: The optimized PPZ-NLCs showed particle size 167.5 nm, PDI 0.277, Zeta Potential of -28.8 mV, and 98.6% EE. The drug release during In-vitro experiments of PPZ-NLCs exhibited a prolonged release profile of the drug best fitted into the Higuchi kinetic model. PPZ-NLCs when examined In-vivo pharmacokinetically a significant increase in t1/2, AUC0-∞, and Cmax was observed which indicates a greater bioavailability and a lesser elimination (Kel).
Conclusion: These results suggested the superiority of NLCs in enhancing the bioavailability of PPZ drug and their suitability for successful brain targeting, which could be subject to a patent application to protect the novel formulation.
期刊介绍:
Recent Patents on Nanotechnology publishes full-length/mini reviews and research articles that reflect or deal with studies in relation to a patent, application of reported patents in a study, discussion of comparison of results regarding application of a given patent, etc., and also guest edited thematic issues on recent patents in the field of nanotechnology. A selection of important and recent patents on nanotechnology is also included in the journal. The journal is essential reading for all researchers involved in nanotechnology.