Experimental Design in Formulation of Diazepam Nanoemulsions: Physicochemical and Pharmacokinetic Performances
Само за регистроване кориснике
2013
Аутори
Đorđević, SanelaRadulović, Tamara
Cekić, Nebojša
Ranđelović, Danijela
Savić, Miroslav
Krajišnik, Danina
Milić, Jela
Savić, Snežana
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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.
Кључне речи:
nanoemulsion / diazepam / full factorial design / particle size / atomic force microscopy / FTIR / drug-excipient interaction / stability / pharmacokineticsИзвор:
Journal of Pharmaceutical Sciences, 2013, 102, 11, 4159-4172Издавач:
- Wiley-Blackwell, Hoboken
Финансирање / пројекти:
DOI: 10.1002/jps.23734
ISSN: 0022-3549
PubMed: 24114833
WoS: 000325550400032
Scopus: 2-s2.0-84885846550
Институција/група
PharmacyTY - JOUR AU - Đorđević, Sanela AU - Radulović, Tamara AU - Cekić, Nebojša AU - Ranđelović, Danijela AU - Savić, Miroslav AU - Krajišnik, Danina AU - Milić, Jela AU - Savić, Snežana PY - 2013 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1873 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 = "Đorđević, Sanela and Radulović, Tamara and Cekić, Nebojša and Ranđelović, Danijela and Savić, Miroslav and Krajišnik, Danina and Milić, Jela and Savić, Snežana", 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" }
Đorđević, S., Radulović, T., Cekić, N., Ranđelović, D., Savić, M., Krajišnik, D., Milić, J.,& Savić, S.. (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
Đorđević S, Radulović T, Cekić N, Ranđelović D, Savić M, Krajišnik D, Milić J, Savić S. 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 .
Đorđević, Sanela, Radulović, Tamara, Cekić, Nebojša, Ranđelović, Danijela, Savić, Miroslav, Krajišnik, Danina, Milić, Jela, Savić, Snežana, "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 . .