Development of Olanzapine Nano-Emulsion for Enhanced Brain Delivery

DOI:

https://doi.org/10.37285/ijpsn.2012.5.1.9

Authors

  • Madhusudan Rao Y
  • Shailaja M
  • Ramakrishna S
  • Ramesh G
  • K H Reddy
  • Diwan P V

Abstract

The main objective of the present research work was to design, optimize and characterize olanzapine loaded nano-emulsion for improved brain transport of the drug.   Olanzapine nano-emulsion was formulated using the ultrasonication method. The formulation variables (oil and surfactant) and process variables (ultrasonication time) were optimized by Response surface methodology using the Box-Behnken statistical method. Particle size, polydispersity index (PDI) and zeta potential were measured by photon correlation spectroscopy using a Malvern zeta sizer. Morphology of emulsion droplets was examined by transmission electron microscopy (TEM). Release study was performed and drug release was estimated by HPLC method. Stability studies were performed at 4oC-25oC for a period of three months. The optimized nano-emulsion obtained showed a uniform size distribution with an average size in the range of 65.1 nm to 74.21 nm and surface charge in the range of –18.9 mv to – 25.23 mv. The Transmission electron microscopy studies on olanzapine nano-emulsion revealed a spherical morphology of globules. An average of 91.91% of drug was released from the optimized formulation over a period of 24 hours. The particle size analysis after three months showed no significant change implying that the nano-emulsion was quite stable when stored at room temperature. Stable olanzapine nano-emulsion was formulated. The novel nanoformulation was found to be a potential vehicle for delivery of olanzapine to the brain.

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Keywords:

Olanzapine, Nanoemulsion, Optimization, Box-Behnken statistical design, Transmission electron microscope, Stability studies

Published

2012-05-31

How to Cite

1.
Y MR, M S, S R, G R, Reddy KH, P V D. Development of Olanzapine Nano-Emulsion for Enhanced Brain Delivery. Scopus Indexed [Internet]. 2012 May 31 [cited 2024 Dec. 30];5(1):1648-59. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/568

Issue

Vol. 5 No. 1 (2012): April-June 2012

Section

Research Articles
Crossref
Scopus
Google Scholar
Europe PMC

References

Boulton D.W., DeVane C.L., and Liston H.L. (2002). In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci 71:163-169.

Box G.E.P. and Behnken D.W. (1960). Some new three level designs for the study of quantitative variables. Technometrics 2: 455–75.

Jafari S.M., He Y, and Bhandari B. (2007). Production of sub-micron emulsions by ultrasound and microfluidization techniques. J Food Engineering 82(4): 478-88.

Kreuter J (2001). Nanoparticulate systems for brain delivery of drugs. Adv Drug Deliv Rev 47: 65−81.

Lieberman H. A., Rieger M.M. and Banker G.S. (1988). Pharmaceutical Dosage Forms: Disperse Systems. Marcel Dekker, Inc.: New York, Vol. 1.

Mou D. (2008). Hydrogel-thickened nano-emulsion system for topical delivery of lipophilic drugs. Int J Pharmaceutics 353: 270–276.

Prostaglandin E1 across the blood–brain barrier in rats. J Pharm Pharmacol 57: 61–66.

Riehm H. and Biedler J.L. (1972). Potentiation of drug effect by Tween 80 in Chinese hamster cells resistant to actinomycin D and daunomycin. Cancer Res 32(6): 1195-1200.

Sarker. D.K. (2005). Engineering of Nano-emulsions for drug delivery. Curr Drug Deliv 2: 297-310.

Seelig A. and Gerebtzoff G. (2006). Enhancement of drug absorption by noncharged detergents through membrane and P-glycoprotein binding. Expert Opin Drug Metab Toxicol 2(5): 733-752.

Shafiq S., Shakeel F., Talegaonkar S., Ahmad K.J., Khar R.K. and Ali M. (2007). Development and bioavailability assessment of ramipril nano-emulsion formulation. Eur J Pharm Biopharm 66: 227-43.

Taogoshi T., Nomura A., Murakami T., Nagai J., and Takano M. (2005). Transport of prostaglandin E1 across the blood–brain barrier in rats. J Pharm Pharmacol 57: 61–66.

Temsamani J., Scherrmann J.M., Rees A.R., and Kaczorek M. (2000). Brain drug delivery technologies: novel approaches for transporting therapeutics. Pharm Sci Technol Today 2: 49–59.

Vyas T.K., Shahiwala A. and Amiji M.M., (2008). Improved oral bioavailability and brain transport of saquinavir upon Administration in novel nano-emulsion formulations. Int J Pharm 347(1-2): 93–101.

Wang J.S., Taylor R., Ruan Y., Donovan J.L., Markowitz J.S., and Lindsay De Vane C. (2004). Olanzapine penetration into brain is greater in transgenic Abcb1a P-glycoprotein-deficient mice than FVB1 (wild-type) animals. Neuropsychopharmacology 29(3): 551-557.

Zhang M.Y., Morrison R.A., and Chong S. (2003). Commonly used surfactant, Tween 80, improves absorption of P-glycoprotein substrate digoxin, in rats. Arch Pharm Res 26: 768–772.