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

Samo za registrovane korisnike
2015
Autori
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.
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentu
Apstrakt
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.

Ključne reči:
Parenteral nanoemulsions / Brain targeting / Poorly water-soluble drugs / General factorial design / Physical stability / Pharmacokinetics
Izvor:
International Journal of Pharmaceutics, 2015, 493, 1-2, 40-54
Izdavač:
  • Elsevier Science Bv, Amsterdam
Projekti:
  • Razvoj mikro- i nanosistema kao nosača za lekove sa antiinflamatornim delovanjem i metoda za njihovu karakterizaciju (RS-34031)
  • Bihejvioralni efekti ponavljane primene novosintetisanih supstanci selektivnih za pojedine podtipove benzodiazepinskog mesta vezivanja GABA A receptora: poređenje sa standardnim psihofarmakološkim lekovima (RS-175076)
  • Mikro, nano-sistemi i senzori za primenu u elektroprivredi, procesnoj industriji i zaštiti životne sredine (RS-32008)
Napomena:
  • Accepted version: http://cer.ihtm.bg.ac.rs/handle/123456789/3201

DOI: 10.1016/j.ijpharm.2015.07.007

ISSN: 0378-5173

PubMed: 26209070

WoS: 000360492000005

Scopus: 2-s2.0-84938080952
[ Google Scholar ]
34
26
URI
http://cer.ihtm.bg.ac.rs/handle/123456789/1697
Kolekcije
  • Radovi istraživača / Researchers' publications
Institucija
IHTM
TY  - JOUR
AU  - Dordevic, Sanela M
AU  - Cekic, Nebojsa
AU  - Savić, Miroslav M.
AU  - Isailovic, Tanja M
AU  - Ranđelović, Danijela
AU  - Marković, Bojan D.
AU  - Savić, Saša R.
AU  - Stamenic, Tamara Timic
AU  - Daniels, Rolf
AU  - Savić, Snežana D.
PY  - 2015
UR  - http://cer.ihtm.bg.ac.rs/handle/123456789/1697
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 = "Dordevic, Sanela M and Cekic, Nebojsa and Savić, Miroslav M. and Isailovic, Tanja M and Ranđelović, Danijela and Marković, Bojan D. and Savić, Saša R. and Stamenic, Tamara Timic and Daniels, Rolf and Savić, Snežana D.",
year = "2015",
url = "http://cer.ihtm.bg.ac.rs/handle/123456789/1697",
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"
}
Dordevic SM, Cekic N, Savić MM, Isailovic TM, Ranđelović D, Marković BD, Savić SR, Stamenic TT, Daniels R, Savić SD. Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation. International Journal of Pharmaceutics. 2015;493(1-2):40-54
Dordevic, S. M., Cekic, N., Savić, M. M., Isailovic, T. M., Ranđelović, D., Marković, B. D., Savić, S. R., Stamenic, T. T., Daniels, R.,& Savić, S. D. (2015). Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation.
International Journal of PharmaceuticsElsevier Science Bv, Amsterdam., 493(1-2), 40-54.
https://doi.org/10.1016/j.ijpharm.2015.07.007
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., "Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation" 493, no. 1-2 (2015):40-54,
https://doi.org/10.1016/j.ijpharm.2015.07.007 .

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