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

• Published in: International journal of pharmaceutics 2015-09, Vol.493 (1-2), p.40-54
• Main Authors: Đorđević, Sanela M., Cekić, Nebojša D., Savić, Miroslav M., Isailović, Tanja M., Ranđelović, Danijela V., Marković, Bojan D., Savić, Saša R., Stamenić, Tamara Timić, Daniels, Rolf, Savić, Snežana D.
• Format: Article
• Language: English
• Subjects: Animals; Brain - metabolism; Brain targeting; Chemistry, Pharmaceutical; Drug Delivery Systems; Drug Stability; Emulsifying Agents; Emulsions - chemistry; General factorial design; Lecithins - chemistry; Male; Nanoparticles - chemistry; Parenteral nanoemulsions; Particle Size; Pharmacokinetics; Physical stability; Poloxamer - chemistry; Polyethylene Glycols - chemistry; Polysorbates - chemistry; Poorly water-soluble drugs; Rats; Rats, Wistar; Risperidone - administration & dosage; Risperidone - pharmacokinetics; Solubility; Stearic Acids - chemistry; Technology, Pharmaceutical
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2015.07.007

[Display omitted] 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 160nm, size distribution