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Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances

Authorized Users Only
2017
Authors
Đorđević, Sanela
Santrač, Anja
Cekić, Nebojša
Marković, Bojan
Divović, Branka
Ilić, Tanja
Savić, Miroslav
Savić, Snežana
Article (Published version)
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Abstract
This work aimed to deepen the lately acquired knowledge about parenteral nanoemulsions as carriers for brain delivery of risperidone, a poorly water-soluble antipsychotic drug, through establishing the prospective relationship between their physicochemical, pharmacokinetic, biodistribution, and behavioral performances. For this purpose, two optimized risperidone-loaded nanoemulsions, stabilized by lecithin or lecithin/polysorbate 80 mixture, and costabilized by sodium oleate, were produced by high-pressure homogenization. The characterization revealed the favorable droplet size, narrow size distribution, high surface charge, with proven stability to autoclaving and long-term stability for at least one year at 25 +/- 2 degrees C. Pharmacokinetic and tissue distribution results demonstrated improved plasma, liver, and brain pharmacokinetic parameters, resulting in 1.2-1.5-fold increased relative bioavailability, 1.1-1.8-fold decreased liver distribution, and about 1.3-fold improved brain... uptake of risperidone active moiety following intraperitoneal administration of nanoemulsions relative to solution in rats. In behavioral study, investigated nanoemulsions showed pronounced reduction in basal and, more pertinently, amphetamine-induced locomotor activity in rats, with an early onset of antipsychotic action, and this effect lasted at least 90 min after drug injection. Together, these findings corroborate the applicability of parenteral nanoemulsions as carriers for enhanced brain delivery of risperidone, further suggesting their promise in acute psychosis treatment or other emergency situations.

Keywords:
Parenteral nanoemulsion / Poorly water-soluble drug / Long-term stability / Pharmacokinetics / Tissue distribution / Antipsychotic efficiency
Source:
International Journal of Pharmaceutics, 2017, 533, 2, 421-430
Publisher:
  • Elsevier Science BV, Amsterdam
Funding / projects:
  • Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)

DOI: 10.1016/j.ijpharm.2017.05.051

ISSN: 0378-5173

PubMed: 28552767

WoS: 000414188500013

Scopus: 2-s2.0-85020132880
[ Google Scholar ]
21
21
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2883
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Đorđević, Sanela
AU  - Santrač, Anja
AU  - Cekić, Nebojša
AU  - Marković, Bojan
AU  - Divović, Branka
AU  - Ilić, Tanja
AU  - Savić, Miroslav
AU  - Savić, Snežana
PY  - 2017
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2883
AB  - This work aimed to deepen the lately acquired knowledge about parenteral nanoemulsions as carriers for brain delivery of risperidone, a poorly water-soluble antipsychotic drug, through establishing the prospective relationship between their physicochemical, pharmacokinetic, biodistribution, and behavioral performances. For this purpose, two optimized risperidone-loaded nanoemulsions, stabilized by lecithin or lecithin/polysorbate 80 mixture, and costabilized by sodium oleate, were produced by high-pressure homogenization. The characterization revealed the favorable droplet size, narrow size distribution, high surface charge, with proven stability to autoclaving and long-term stability for at least one year at 25 +/- 2 degrees C. Pharmacokinetic and tissue distribution results demonstrated improved plasma, liver, and brain pharmacokinetic parameters, resulting in 1.2-1.5-fold increased relative bioavailability, 1.1-1.8-fold decreased liver distribution, and about 1.3-fold improved brain uptake of risperidone active moiety following intraperitoneal administration of nanoemulsions relative to solution in rats. In behavioral study, investigated nanoemulsions showed pronounced reduction in basal and, more pertinently, amphetamine-induced locomotor activity in rats, with an early onset of antipsychotic action, and this effect lasted at least 90 min after drug injection. Together, these findings corroborate the applicability of parenteral nanoemulsions as carriers for enhanced brain delivery of risperidone, further suggesting their promise in acute psychosis treatment or other emergency situations.
PB  - Elsevier Science BV, Amsterdam
T2  - International Journal of Pharmaceutics
T1  - Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances
VL  - 533
IS  - 2
SP  - 421
EP  - 430
DO  - 10.1016/j.ijpharm.2017.05.051
UR  - conv_3981
ER  - 
@article{
author = "Đorđević, Sanela and Santrač, Anja and Cekić, Nebojša and Marković, Bojan and Divović, Branka and Ilić, Tanja and Savić, Miroslav and Savić, Snežana",
year = "2017",
abstract = "This work aimed to deepen the lately acquired knowledge about parenteral nanoemulsions as carriers for brain delivery of risperidone, a poorly water-soluble antipsychotic drug, through establishing the prospective relationship between their physicochemical, pharmacokinetic, biodistribution, and behavioral performances. For this purpose, two optimized risperidone-loaded nanoemulsions, stabilized by lecithin or lecithin/polysorbate 80 mixture, and costabilized by sodium oleate, were produced by high-pressure homogenization. The characterization revealed the favorable droplet size, narrow size distribution, high surface charge, with proven stability to autoclaving and long-term stability for at least one year at 25 +/- 2 degrees C. Pharmacokinetic and tissue distribution results demonstrated improved plasma, liver, and brain pharmacokinetic parameters, resulting in 1.2-1.5-fold increased relative bioavailability, 1.1-1.8-fold decreased liver distribution, and about 1.3-fold improved brain uptake of risperidone active moiety following intraperitoneal administration of nanoemulsions relative to solution in rats. In behavioral study, investigated nanoemulsions showed pronounced reduction in basal and, more pertinently, amphetamine-induced locomotor activity in rats, with an early onset of antipsychotic action, and this effect lasted at least 90 min after drug injection. Together, these findings corroborate the applicability of parenteral nanoemulsions as carriers for enhanced brain delivery of risperidone, further suggesting their promise in acute psychosis treatment or other emergency situations.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "International Journal of Pharmaceutics",
title = "Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances",
volume = "533",
number = "2",
pages = "421-430",
doi = "10.1016/j.ijpharm.2017.05.051",
url = "conv_3981"
}
Đorđević, S., Santrač, A., Cekić, N., Marković, B., Divović, B., Ilić, T., Savić, M.,& Savić, S.. (2017). Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances. in International Journal of Pharmaceutics
Elsevier Science BV, Amsterdam., 533(2), 421-430.
https://doi.org/10.1016/j.ijpharm.2017.05.051
conv_3981
Đorđević S, Santrač A, Cekić N, Marković B, Divović B, Ilić T, Savić M, Savić S. Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances. in International Journal of Pharmaceutics. 2017;533(2):421-430.
doi:10.1016/j.ijpharm.2017.05.051
conv_3981 .
Đorđević, Sanela, Santrač, Anja, Cekić, Nebojša, Marković, Bojan, Divović, Branka, Ilić, Tanja, Savić, Miroslav, Savić, Snežana, "Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances" in International Journal of Pharmaceutics, 533, no. 2 (2017):421-430,
https://doi.org/10.1016/j.ijpharm.2017.05.051 .,
conv_3981 .

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