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Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances

Authorized Users Only
2013
Authors
Dordevic, Sanela M.
Radulovic, Tamara S.
Cekic, Nebojsa
Randjelović, Danijela
Savić, Miroslav M.
Krajisnik, Danina R.
Milic, Jela R.
Savić, Snežana D.
Article (Published version)
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Abstract
With the aid of experimental design, we developed and characterized nanoemulsions for parenteral drug delivery. Formulations containing a mixture of medium-chain triglycerides and soybean oil as oil phase, lecithin (soybean/egg) and polysorbate 80 as emulsifiers, and 0.1M phosphate buffer solution (pH 8) as aqueous phase were prepared by cold high-pressure homogenization. To study the effects of the oil content, lecithin type, and the presence of diazepam as a model drug and their interactions on physicochemical characteristics of nanoemulsions, a three factor two-level full factorial design was applied. The nanoemulsions were evaluated concerning droplet size and size distribution, surface charge, viscosity, morphology, drug-excipient interactions, and physical stability. The characterization revealed the small spherical droplets in the range 195-220nm with polydispersity index below 0.15 and zeta potential between -30 and -60mV. Interactions among the investigated factors, rather tha...n factors alone, were shown to more profoundly affect nanoemulsion characteristics. In vivo pharmacokinetic study of selected diazepam nanoemulsions with different oil content (20%, 30%, and 40%, w/w) demonstrated fast and intense initial distribution into rat brain of diazepam from nanoemulsions with 20% and 30% (w/w) oil content, suggesting their applicability in urgent situations.

Keywords:
nanoemulsion / diazepam / full factorial design / particle size / atomic force microscopy / FTIR / drug-excipient interaction / stability / pharmacokinetics
Source:
Journal of Pharmaceutical Sciences, 2013, 102, 11, 4159-4172
Publisher:
  • Wiley-Blackwell, Hoboken
Funding / 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)

DOI: 10.1002/jps.23734

ISSN: 0022-3549

PubMed: 24114833

WoS: 000325550400032

Scopus: 2-s2.0-84885846550
[ Google Scholar ]
38
31
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/1194
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - JOUR
AU  - Dordevic, Sanela M.
AU  - Radulovic, Tamara S.
AU  - Cekic, Nebojsa
AU  - Randjelović, Danijela
AU  - Savić, Miroslav M.
AU  - Krajisnik, Danina R.
AU  - Milic, Jela R.
AU  - Savić, Snežana D.
PY  - 2013
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/1194
AB  - With the aid of experimental design, we developed and characterized nanoemulsions for parenteral drug delivery. Formulations containing a mixture of medium-chain triglycerides and soybean oil as oil phase, lecithin (soybean/egg) and polysorbate 80 as emulsifiers, and 0.1M phosphate buffer solution (pH 8) as aqueous phase were prepared by cold high-pressure homogenization. To study the effects of the oil content, lecithin type, and the presence of diazepam as a model drug and their interactions on physicochemical characteristics of nanoemulsions, a three factor two-level full factorial design was applied. The nanoemulsions were evaluated concerning droplet size and size distribution, surface charge, viscosity, morphology, drug-excipient interactions, and physical stability. The characterization revealed the small spherical droplets in the range 195-220nm with polydispersity index below 0.15 and zeta potential between -30 and -60mV. Interactions among the investigated factors, rather than factors alone, were shown to more profoundly affect nanoemulsion characteristics. In vivo pharmacokinetic study of selected diazepam nanoemulsions with different oil content (20%, 30%, and 40%, w/w) demonstrated fast and intense initial distribution into rat brain of diazepam from nanoemulsions with 20% and 30% (w/w) oil content, suggesting their applicability in urgent situations.
PB  - Wiley-Blackwell, Hoboken
T2  - Journal of Pharmaceutical Sciences
T1  - Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances
VL  - 102
IS  - 11
SP  - 4159
EP  - 4172
DO  - 10.1002/jps.23734
ER  - 
@article{
author = "Dordevic, Sanela M. and Radulovic, Tamara S. and Cekic, Nebojsa and Randjelović, Danijela and Savić, Miroslav M. and Krajisnik, Danina R. and Milic, Jela R. and Savić, Snežana D.",
year = "2013",
abstract = "With the aid of experimental design, we developed and characterized nanoemulsions for parenteral drug delivery. Formulations containing a mixture of medium-chain triglycerides and soybean oil as oil phase, lecithin (soybean/egg) and polysorbate 80 as emulsifiers, and 0.1M phosphate buffer solution (pH 8) as aqueous phase were prepared by cold high-pressure homogenization. To study the effects of the oil content, lecithin type, and the presence of diazepam as a model drug and their interactions on physicochemical characteristics of nanoemulsions, a three factor two-level full factorial design was applied. The nanoemulsions were evaluated concerning droplet size and size distribution, surface charge, viscosity, morphology, drug-excipient interactions, and physical stability. The characterization revealed the small spherical droplets in the range 195-220nm with polydispersity index below 0.15 and zeta potential between -30 and -60mV. Interactions among the investigated factors, rather than factors alone, were shown to more profoundly affect nanoemulsion characteristics. In vivo pharmacokinetic study of selected diazepam nanoemulsions with different oil content (20%, 30%, and 40%, w/w) demonstrated fast and intense initial distribution into rat brain of diazepam from nanoemulsions with 20% and 30% (w/w) oil content, suggesting their applicability in urgent situations.",
publisher = "Wiley-Blackwell, Hoboken",
journal = "Journal of Pharmaceutical Sciences",
title = "Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances",
volume = "102",
number = "11",
pages = "4159-4172",
doi = "10.1002/jps.23734"
}
Dordevic, S. M., Radulovic, T. S., Cekic, N., Randjelović, D., Savić, M. M., Krajisnik, D. R., Milic, J. R.,& Savić, S. D.. (2013). Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances. in Journal of Pharmaceutical Sciences
Wiley-Blackwell, Hoboken., 102(11), 4159-4172.
https://doi.org/10.1002/jps.23734
Dordevic SM, Radulovic TS, Cekic N, Randjelović D, Savić MM, Krajisnik DR, Milic JR, Savić SD. Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances. in Journal of Pharmaceutical Sciences. 2013;102(11):4159-4172.
doi:10.1002/jps.23734 .
Dordevic, Sanela M., Radulovic, Tamara S., Cekic, Nebojsa, Randjelović, Danijela, Savić, Miroslav M., Krajisnik, Danina R., Milic, Jela R., Savić, Snežana D., "Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances" in Journal of Pharmaceutical Sciences, 102, no. 11 (2013):4159-4172,
https://doi.org/10.1002/jps.23734 . .

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