Formulation and evaluation of olanzapine loaded chitosan nanoparticles for nose to brain targeting an in vitro and ex vivo toxicity study

J Ruby,V Pandey

doi:10.7324/japs.2016.60905

Abstract

Statistical Optimization of Olanzapine Ternary Solid Dispersions with Pvp K 30 and Peg 20,000 by Response Surface MethodologyAnil Katharia, Ratendra Kumar, Rajiv Sharma, Yogendra Singh, Uday Veer Singh Teotia

Highlights

IntroductionOLA has poor bioavailability (40%), due to hepatic first pass metabolism and low permeability due to efflux by Pglycoprotein
Olanzapine (OLA) is a thioenobenzodiazepine class psychotropic agent used for the treatment of schizophrenia and bipolar disorders (Fig.1.) (Bhana and Perry, 2001).OLA has poor bioavailability (40%), due to hepatic first pass metabolism and low permeability due to efflux by Pglycoprotein
The olanzapine loaded chitosan nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate anions

Summary

Introduction

OLA has poor bioavailability (40%), due to hepatic first pass metabolism and low permeability due to efflux by Pglycoprotein. OLA is associated with numerous dose related side effects due to non targeted dosage forms (Mattiuz et al, 1997). OLA is available as tablet, an orally-disintegrating tablet, which rapidly dissolves in saliva and as 10 mg vial of intramuscular injection. All above dosage forms show low bioavailability due to extensive first pass metabolism and consequences in numerous side effects due to non targeted delivery system. Brain targeting of OLA requires a desirable formulation strategy to overcome its first pass metabolism and restrict the barrier from transport of drugs from systemic circulation into the central nervous system thereby reducing the dose related side effects (Sahni et al, 2011, Haque et al, 2012)

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