TY  - JOUR
AU  - Todosijević, Marija N.
AU  - Savić, Miroslav
AU  - Batinić, Bojan
AU  - Marković, Bojan
AU  - Gasperlin, Mirjana
AU  - Ranđelović, Danijela
AU  - Lukić, Milica
AU  - Savić, Snežana
PY  - 2015
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2362
AB  - To elaborate the decisive role of surfactants in promotion of aceclofenac' skin absorption, potentially avoiding irritation, we developed non-ionic microemulsions varying natural or synthetic surfactants: sucrose esters (laurate or myristate) vs. polysorbate 80. A comprehensive physicochemical characterization indicated no significant influence of the solubilized nonsteroidal anti-inflammatory drug on the bicontinuous structure of blank formulations. To evaluate skin tolerability of isopropyl alcohol, a sucrose ester-based microemulsion containing transcutol P as a cosurfactant was also developed. The measured skin parameters strongly depended on the (co)surfactant type, showing higher compatibility of the microemulsions containing sucrose ester and isopropyl alcohol. In vitro release results, in vivo tape stripping and pharmacokinetics in rats confirmed superiority of the sucrose ester-over polysorbate-based microemulsions (total amounts of aceclofenac penetrated 60.81 +/- 5.97 and 60.86 +/- 3.67 vs. 27.00 +/- 5.09 mu g/cm(2), and its maximum plasma concentrations 275.57 +/- 109.49 and 281.31 +/- 76.76 vs. 150.23 +/- 69.74 ng/ml for sucrose laurate- and myristate- vs. polysorbate 80-based microemulsions, respectively). Hence, sugar-based excipients increased delivery of aceclofenac through stratum corneum by increasing its fluidity, showing overall more satisfying safety profiles. In conclusion, sucrose ester-based microemulsions proved to be promising carriers for dermal/transdermal aceclofenac delivery.
PB  - Elsevier Science BV, Amsterdam
T2  - International Journal of Pharmaceutics
T1  - Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance
VL  - 496
IS  - 2
SP  - 931
EP  - 941
DO  - 10.1016/j.ijpharm.2015.10.048
ER  - 

@article{
author = "Todosijević, Marija N. and Savić, Miroslav and Batinić, Bojan and Marković, Bojan and Gasperlin, Mirjana and Ranđelović, Danijela and Lukić, Milica and Savić, Snežana",
year = "2015",
abstract = "To elaborate the decisive role of surfactants in promotion of aceclofenac' skin absorption, potentially avoiding irritation, we developed non-ionic microemulsions varying natural or synthetic surfactants: sucrose esters (laurate or myristate) vs. polysorbate 80. A comprehensive physicochemical characterization indicated no significant influence of the solubilized nonsteroidal anti-inflammatory drug on the bicontinuous structure of blank formulations. To evaluate skin tolerability of isopropyl alcohol, a sucrose ester-based microemulsion containing transcutol P as a cosurfactant was also developed. The measured skin parameters strongly depended on the (co)surfactant type, showing higher compatibility of the microemulsions containing sucrose ester and isopropyl alcohol. In vitro release results, in vivo tape stripping and pharmacokinetics in rats confirmed superiority of the sucrose ester-over polysorbate-based microemulsions (total amounts of aceclofenac penetrated 60.81 +/- 5.97 and 60.86 +/- 3.67 vs. 27.00 +/- 5.09 mu g/cm(2), and its maximum plasma concentrations 275.57 +/- 109.49 and 281.31 +/- 76.76 vs. 150.23 +/- 69.74 ng/ml for sucrose laurate- and myristate- vs. polysorbate 80-based microemulsions, respectively). Hence, sugar-based excipients increased delivery of aceclofenac through stratum corneum by increasing its fluidity, showing overall more satisfying safety profiles. In conclusion, sucrose ester-based microemulsions proved to be promising carriers for dermal/transdermal aceclofenac delivery.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "International Journal of Pharmaceutics",
title = "Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance",
volume = "496",
number = "2",
pages = "931-941",
doi = "10.1016/j.ijpharm.2015.10.048"
}

Todosijević, M. N., Savić, M., Batinić, B., Marković, B., Gasperlin, M., Ranđelović, D., Lukić, M.,& Savić, S.. (2015). Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance. in International Journal of Pharmaceutics
Elsevier Science BV, Amsterdam., 496(2), 931-941.
https://doi.org/10.1016/j.ijpharm.2015.10.048

Todosijević MN, Savić M, Batinić B, Marković B, Gasperlin M, Ranđelović D, Lukić M, Savić S. Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance. in International Journal of Pharmaceutics. 2015;496(2):931-941.
doi:10.1016/j.ijpharm.2015.10.048 .

Todosijević, Marija N., Savić, Miroslav, Batinić, Bojan, Marković, Bojan, Gasperlin, Mirjana, Ranđelović, Danijela, Lukić, Milica, Savić, Snežana, "Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance" in International Journal of Pharmaceutics, 496, no. 2 (2015):931-941,
https://doi.org/10.1016/j.ijpharm.2015.10.048 . .

TY  - JOUR
AU  - Todosijević, Marija N.
AU  - Cekić, Nebojša
AU  - Savić, Miroslav
AU  - Gasperlin, Mirjana
AU  - Ranđelović, Danijela
AU  - Savić, Snežana
PY  - 2014
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2125
AB  - We assessed the functionality of sucrose esters (sucrose laurate, myristate, palmitate, and stearate), relatively innocuous nonionic surfactants, in formulation of biocompatible microemulsions. The putative influence of surfactant structure on the extension of microemulsion region was explored through the construction of the pseudo-ternary phase diagrams for the isopropyl myristate/sucrose ester-isopropyl alcohol/water system, using the titration method and mixture experimental approach. Minor changes in surfactant tail length strongly affected the microemulsion area boundaries. D-optimal mixture design proved to be highly applicable in detecting the microemulsion regions. Examination of conductivity, rheology, and thermal behavior of the selected sucrose laurate and sucrose myristate-based microemulsions, upon dilution with water, indicated existence of percolation threshold and suggested the phase inversion from water-in-oil to oil-in-water via a bicontinuous structure. Atomic force micrographs confirmed the suggested type of microemulsions and were valuable in further exploring their inner structure. The solubilization capacity of aceclofenac as a model drug has decreased as the water volume fraction in microemulsion increased. High surfactant concentration and the measured solubility of aceclofenac in microemulsion components suggested that the interfacial film may mostly contribute to aceclofenac solubilization.
PB  - Springer, New York
T2  - Colloid and Polymer Science
T1  - Sucrose ester-based biocompatible microemulsions as vehicles for aceclofenac as a model drug: formulation approach using D-optimal mixture design
VL  - 292
IS  - 12
SP  - 3061
EP  - 3076
DO  - 10.1007/s00396-014-3351-4
ER  - 

@article{
author = "Todosijević, Marija N. and Cekić, Nebojša and Savić, Miroslav and Gasperlin, Mirjana and Ranđelović, Danijela and Savić, Snežana",
year = "2014",
abstract = "We assessed the functionality of sucrose esters (sucrose laurate, myristate, palmitate, and stearate), relatively innocuous nonionic surfactants, in formulation of biocompatible microemulsions. The putative influence of surfactant structure on the extension of microemulsion region was explored through the construction of the pseudo-ternary phase diagrams for the isopropyl myristate/sucrose ester-isopropyl alcohol/water system, using the titration method and mixture experimental approach. Minor changes in surfactant tail length strongly affected the microemulsion area boundaries. D-optimal mixture design proved to be highly applicable in detecting the microemulsion regions. Examination of conductivity, rheology, and thermal behavior of the selected sucrose laurate and sucrose myristate-based microemulsions, upon dilution with water, indicated existence of percolation threshold and suggested the phase inversion from water-in-oil to oil-in-water via a bicontinuous structure. Atomic force micrographs confirmed the suggested type of microemulsions and were valuable in further exploring their inner structure. The solubilization capacity of aceclofenac as a model drug has decreased as the water volume fraction in microemulsion increased. High surfactant concentration and the measured solubility of aceclofenac in microemulsion components suggested that the interfacial film may mostly contribute to aceclofenac solubilization.",
publisher = "Springer, New York",
journal = "Colloid and Polymer Science",
title = "Sucrose ester-based biocompatible microemulsions as vehicles for aceclofenac as a model drug: formulation approach using D-optimal mixture design",
volume = "292",
number = "12",
pages = "3061-3076",
doi = "10.1007/s00396-014-3351-4"
}

Todosijević, M. N., Cekić, N., Savić, M., Gasperlin, M., Ranđelović, D.,& Savić, S.. (2014). Sucrose ester-based biocompatible microemulsions as vehicles for aceclofenac as a model drug: formulation approach using D-optimal mixture design. in Colloid and Polymer Science
Springer, New York., 292(12), 3061-3076.
https://doi.org/10.1007/s00396-014-3351-4

Todosijević MN, Cekić N, Savić M, Gasperlin M, Ranđelović D, Savić S. Sucrose ester-based biocompatible microemulsions as vehicles for aceclofenac as a model drug: formulation approach using D-optimal mixture design. in Colloid and Polymer Science. 2014;292(12):3061-3076.
doi:10.1007/s00396-014-3351-4 .

Todosijević, Marija N., Cekić, Nebojša, Savić, Miroslav, Gasperlin, Mirjana, Ranđelović, Danijela, Savić, Snežana, "Sucrose ester-based biocompatible microemulsions as vehicles for aceclofenac as a model drug: formulation approach using D-optimal mixture design" in Colloid and Polymer Science, 292, no. 12 (2014):3061-3076,
https://doi.org/10.1007/s00396-014-3351-4 . .