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Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

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2015
j.ijpharm.2015.07.007.pdf (4.771Mb)
Authors
Dordevic, Sanela M
Cekic, Nebojsa
Savić, Miroslav M.
Isailovic, Tanja M
Ranđelović, Danijela
Marković, Bojan D.
Savić, Saša R.
Stamenic, Tamara Timic
Daniels, Rolf
Savić, Snežana D.
Article (Accepted Version)
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Abstract
This paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, surface charge, morphology, drug-vehicle interactions, and physical stability. To estimate the simultaneous influence of nanoemulsion formulation and preparation parameters-co-emulsifier type, aqueous phase type, homogenization temperature-on the critical quality attributes of developed nanoemulsions, a general factorial experimental design was applied. From the established design space and stability data, promising risperidone-loaded nanoemulsions (mean size about 160 nm, size distribution LT 0.15, zeta potential around -50 mV), containing sodium oleate in the aqueous phase and polysorbate 80, poloxamer 188 or Solutol (R) HS15 as co-emulsifier, were produced by hot homogen...ization and their ability to improve risperidone delivery to the brain was assessed in rats. Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer). Namely, polysorbate 80-costabilized nanoemulsion showed increased (1.4-7.4-fold higher) risperidone brain availability compared to other nanoemulsions and drug solution, suggesting this nanoemulsion as a promising carrier worth exploring further for brain targeting.

Keywords:
Parenteral nanoemulsions / Brain targeting / Poorly water-soluble drugs / General factorial design / Physical stability / Pharmacokinetics
Source:
International Journal of Pharmaceutics, 2015, 493, 1-2, 40-54
Publisher:
  • Elsevier Science Bv, Amsterdam
Projects:
  • Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)
  • Behavioral ?ffects following repeated administration of newly synthesized ligands selective for distinct subtypes of GABAA receptor benzodiazepine binding site: comparison with standard psychopharmacologic drugs (RS-175076)
  • Micro- Nanosystems and Sensors for Electric Power and Process Industry and Environmental Protection (RS-32008)
Note:
  • This is peer-reviewed version of the artcle: S.M. Đorđević, N.D. Cekić, M.M. Savić, T.M. Isailović, D. V Ranđelović, B.D. Marković, S.R. Savić, T.T. Stamenić, R. Daniels, S.D. Savić, Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation, Int. J. Pharm. 493 (2015) 40–54. https://doi.org/10.1016/j.ijpharm.2015.07.007
  • Published version: http://cer.ihtm.bg.ac.rs/handle/123456789/1697

DOI: 10.1016/j.ijpharm.2015.07.007

ISSN: 0378-5173

PubMed: 26209070

WoS: 000360492000005

Scopus: 2-s2.0-84938080952
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/3201
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