Abstract
Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain.
Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia.
Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out.
Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460, respectively. The encapsulation efficiency of formulation S6 was found to be 87.25%. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96%, respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%.
Conclusion: These results reveal the potential application of novel olanzapine-NLC in intranasal drug delivery system for the treatment of Schizophrenia.
Keywords: Olanzapine, schizophrenia, nanostructured lipid carriers, taguchi experimental design, X-ray diffraction, ciliotoxicity.
Graphical Abstract
[http://dx.doi.org/10.1016/j.ijpharm.2020.119569] [PMID: 32592899]
[http://dx.doi.org/10.1016/j.molliq.2020.113734]
[http://dx.doi.org/10.1016/j.carbpol.2019.115826] [PMID: 31952620]
[http://dx.doi.org/10.1016/j.jddst.2019.02.017]
[http://dx.doi.org/10.1016/j.ijpharm.2008.01.045] [PMID: 18343059]
[http://dx.doi.org/10.4103/0250-474X.57282] [PMID: 20502539]
[http://dx.doi.org/10.2174/157488511798109637]
[http://dx.doi.org/10.1080/02652040500435295] [PMID: 16854814]
[http://dx.doi.org/10.1016/S0378-5173(02)00180-1] [PMID: 12176234]
[http://dx.doi.org/10.2165/00023210-200115110-00005] [PMID: 11700151]
[http://dx.doi.org/10.1016/j.eswa.2010.02.023]
[http://dx.doi.org/10.1016/j.jddst.2020.101731]
[http://dx.doi.org/10.1016/j.ejps.2020.105533] [PMID: 32871214]
[http://dx.doi.org/10.1016/j.colsurfa.2020.125396]
[http://dx.doi.org/10.2174/1567201053586047] [PMID: 16305417]
[http://dx.doi.org/10.2174/1573413711107061014]
[http://dx.doi.org/10.1016/j.colsurfb.2014.06.037] [PMID: 25033434]
[PMID: 20524422]
[http://dx.doi.org/10.3109/10717544.2014.885999] [PMID: 24512368]
[http://dx.doi.org/10.1002/jps.20480] [PMID: 16419051]
[http://dx.doi.org/10.1016/j.apsusc.2006.05.023]
[http://dx.doi.org/10.1007/s12272-001-2136-8] [PMID: 19023548]
[http://dx.doi.org/10.1016/S0378-5173(02)00267-3] [PMID: 12176298]
[http://dx.doi.org/10.1016/j.ejpb.2019.03.017] [PMID: 30905779]
[http://dx.doi.org/10.1007/s13201-019-0912-1]