Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation
Authorized Users Only
2015
Authors
Đorđević, SanelaCekić, Nebojša

Savić, Miroslav

Isailović, Tanja
Ranđelović, Danijela

Marković, Bojan

Savić, Saša R.

Timić-Stamenić, Tamara

Daniels, Rolf
Savić, Snežana

Article (Published version)

Metadata
Show full item recordAbstract
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.
Source:
International Journal of Pharmaceutics, 2015, 493, 1-2, 40-54Publisher:
- Elsevier Science BV, Amsterdam
Funding / projects:
DOI: 10.1016/j.ijpharm.2015.07.007
ISSN: 0378-5173
PubMed: 26209070
WoS: 000360492000005
Scopus: 2-s2.0-84938080952
Collections
Institution/Community
PharmacyTY - JOUR AU - Đorđević, Sanela AU - Cekić, Nebojša AU - Savić, Miroslav AU - Isailović, Tanja AU - Ranđelović, Danijela AU - Marković, Bojan AU - Savić, Saša R. AU - Timić-Stamenić, Tamara AU - Daniels, Rolf AU - Savić, Snežana PY - 2015 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2346 AB - 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 homogenization 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. PB - Elsevier Science BV, Amsterdam T2 - International Journal of Pharmaceutics T1 - Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation VL - 493 IS - 1-2 SP - 40 EP - 54 DO - 10.1016/j.ijpharm.2015.07.007 ER -
@article{ author = "Đorđević, Sanela and Cekić, Nebojša and Savić, Miroslav and Isailović, Tanja and Ranđelović, Danijela and Marković, Bojan and Savić, Saša R. and Timić-Stamenić, Tamara and Daniels, Rolf and Savić, Snežana", year = "2015", 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 homogenization 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.", publisher = "Elsevier Science BV, Amsterdam", journal = "International Journal of Pharmaceutics", title = "Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation", volume = "493", number = "1-2", pages = "40-54", doi = "10.1016/j.ijpharm.2015.07.007" }
Đorđević, S., Cekić, N., Savić, M., Isailović, T., Ranđelović, D., Marković, B., Savić, S. R., Timić-Stamenić, T., Daniels, R.,& Savić, S.. (2015). Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation. in International Journal of Pharmaceutics Elsevier Science BV, Amsterdam., 493(1-2), 40-54. https://doi.org/10.1016/j.ijpharm.2015.07.007
Đorđević S, Cekić N, Savić M, Isailović T, Ranđelović D, Marković B, Savić SR, Timić-Stamenić T, Daniels R, Savić S. Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation. in International Journal of Pharmaceutics. 2015;493(1-2):40-54. doi:10.1016/j.ijpharm.2015.07.007 .
Đorđević, Sanela, Cekić, Nebojša, Savić, Miroslav, Isailović, Tanja, Ranđelović, Danijela, Marković, Bojan, Savić, Saša R., Timić-Stamenić, Tamara, Daniels, Rolf, Savić, Snežana, "Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation" in International Journal of Pharmaceutics, 493, no. 1-2 (2015):40-54, https://doi.org/10.1016/j.ijpharm.2015.07.007 . .