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Quetiapine Fumarate Loaded Nanostructured Lipid Carrier for Enhancing Oral Bioavailability: Design, Development and Pharmacokinetic Assessment

Author(s):

Shweta Agarwal*, S.L HariKumar, Poonam Negi, Navneet Upadhyay and Rajeev Garg   Pages 1 - 15 ( 15 )

Abstract:


Aim: The study aimed at developing and characterizing nanostructure lipid carriers (NLC) of Quetiapine fumarate (QF) by Design of Experiment (DoE) for enhancement of bioavailability. Background:QF, an anti-psychotic drug, has oral bioavailability of 9% due to hepatic first pass metabolism necessitating use of high doses. Its side effects are dose related and enhancement in bioavailability would result in minimization of side effects.

Objective: The objective of the study was enhancement of bioavailability of NLC of QF by preferential lymphatic uptake.

Methods: Hot emulsification-ultrasonication was the method of formulation using PrecirolATO5 and Oleic acid as solid and liquid lipid respectively. Poloxamer188 and Phospholipon90G were used as surfactant and stabilizer respectively. Solid:liquid lipid ratio and Phospholipon90G amount were independent variables and percent entrapment efficiency (%EE), particle size (PS) dependent variables during optimization by Central Composite Design.

Results: The optimized formulation showed %EE of 77.21%, PS of 140.2nm and surface charge of -19.9mV. Higuchi kinetic model was followed during in-vitro release. TEM revealed spherical, smooth nanoparticles. X-ray diffraction study con-firmed presence of drug in amorphous state in NLC. Pharmacokinetic study in rats showed AUC0-∞ of QF-NLC to be 3.93 times that of QF in suspension suggesting significant enhancement in bioavailability. An increase in AUC0-∞ in cyclo-heximide untreated rats group of QF loaded NLC by 2.43 times ascompared to cycloheximide treated group, confirmed lymphatic absorption of QF-NLC.

Conclusion: The results validated DoE as an appropriate tool for developing QF loaded NLC and proved NLC to be a promising delivery system for enhancement of oral bioavailability of QF.

Keywords:

Quetiapine fumarate, nanostructure lipid carrier, Phospholipon90G, pharmacokinetic, bioavailability

Affiliation:

Research Scholar, IKG Punjab Technical University,Kapurthala, Punjab, Registrar, CUJ, Ranchi, School of Pharmaceutical Sciences, Shoolini University,Solan, H.P, School of Pharmaceutical Sciences, Shoolini University,Solan, H.P, Department of Pharmaceutics, Amar Shaheed Baba AjitSingh JujharSingh Memorial, College of Pharmacy, Bela, Ropar, Punjab



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