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Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances
In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the size of microemulsion region in pseudo-ternary phase diagrams and their ability to form different types of microemulsions was evaluated. The comprehensive physicochemical characterization of microemulsions and the evaluation of their structure was performed, while the localization of tacrolimus in microemulsions was further investigated using electron paramagnetic resonance spectroscopy. Moreover, stability studies proved no change in tacrolimus content during one year of storage at room temperature. In addition, in vivo skin performance indicated no skin irritation potential of blank microemulsions, whereas in vitro release testing using Franz diffusion cells showed s...uperior release rate of tacrolimus from microemulsions (0.98 +/- 0.10 and 0.92 +/- 0.11 mu g/cm(2)/h for two bicontinuous and 1.00 +/- 0.24 mu g/cm(2)/h for oil-in-water microemulsion) compared to referent Protopic ointment (0.15 +/- 0.08 mu g/cm(2)/h). Furthermore, ex vivo penetration assessed through porcine ear skin using tape stripping, confirmed superiority of two microemulsions related to the reference, implying developed microemulsions as promising carriers for dermal delivery of tacrolimus.
TY - JOUR
AU - Savić, Vedrana
AU - Todosijević, Marija N.
AU - Ilić, Tanja
AU - Lukić, Milica
AU - Mitsou, Evgenia
AU - Papadimitriou, Vassiliki
AU - Avramiotis, Spyridon
AU - Marković, Bojan
AU - Cekić, Nebojša
AU - Savić, Snežana
PY - 2017
UR - http://farfar.pharmacy.bg.ac.rs/handle/123456789/2823
AB - In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the size of microemulsion region in pseudo-ternary phase diagrams and their ability to form different types of microemulsions was evaluated. The comprehensive physicochemical characterization of microemulsions and the evaluation of their structure was performed, while the localization of tacrolimus in microemulsions was further investigated using electron paramagnetic resonance spectroscopy. Moreover, stability studies proved no change in tacrolimus content during one year of storage at room temperature. In addition, in vivo skin performance indicated no skin irritation potential of blank microemulsions, whereas in vitro release testing using Franz diffusion cells showed superior release rate of tacrolimus from microemulsions (0.98 +/- 0.10 and 0.92 +/- 0.11 mu g/cm(2)/h for two bicontinuous and 1.00 +/- 0.24 mu g/cm(2)/h for oil-in-water microemulsion) compared to referent Protopic ointment (0.15 +/- 0.08 mu g/cm(2)/h). Furthermore, ex vivo penetration assessed through porcine ear skin using tape stripping, confirmed superiority of two microemulsions related to the reference, implying developed microemulsions as promising carriers for dermal delivery of tacrolimus.
PB - Elsevier Science BV, Amsterdam
T2 - International Journal of Pharmaceutics
T1 - Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances
VL - 529
IS - 1-2
SP - 491
EP - 505
DO - 10.1016/j.ijpharm.2017.07.036
UR - conv_3925
ER -
@article{
author = "Savić, Vedrana and Todosijević, Marija N. and Ilić, Tanja and Lukić, Milica and Mitsou, Evgenia and Papadimitriou, Vassiliki and Avramiotis, Spyridon and Marković, Bojan and Cekić, Nebojša and Savić, Snežana",
year = "2017",
abstract = "In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the size of microemulsion region in pseudo-ternary phase diagrams and their ability to form different types of microemulsions was evaluated. The comprehensive physicochemical characterization of microemulsions and the evaluation of their structure was performed, while the localization of tacrolimus in microemulsions was further investigated using electron paramagnetic resonance spectroscopy. Moreover, stability studies proved no change in tacrolimus content during one year of storage at room temperature. In addition, in vivo skin performance indicated no skin irritation potential of blank microemulsions, whereas in vitro release testing using Franz diffusion cells showed superior release rate of tacrolimus from microemulsions (0.98 +/- 0.10 and 0.92 +/- 0.11 mu g/cm(2)/h for two bicontinuous and 1.00 +/- 0.24 mu g/cm(2)/h for oil-in-water microemulsion) compared to referent Protopic ointment (0.15 +/- 0.08 mu g/cm(2)/h). Furthermore, ex vivo penetration assessed through porcine ear skin using tape stripping, confirmed superiority of two microemulsions related to the reference, implying developed microemulsions as promising carriers for dermal delivery of tacrolimus.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "International Journal of Pharmaceutics",
title = "Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances",
volume = "529",
number = "1-2",
pages = "491-505",
doi = "10.1016/j.ijpharm.2017.07.036",
url = "conv_3925"
}
Savić, V., Todosijević, M. N., Ilić, T., Lukić, M., Mitsou, E., Papadimitriou, V., Avramiotis, S., Marković, B., Cekić, N.,& Savić, S.. (2017). Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances. in International Journal of Pharmaceutics
Elsevier Science BV, Amsterdam., 529(1-2), 491-505.
https://doi.org/10.1016/j.ijpharm.2017.07.036
conv_3925
Savić V, Todosijević MN, Ilić T, Lukić M, Mitsou E, Papadimitriou V, Avramiotis S, Marković B, Cekić N, Savić S. Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances. in International Journal of Pharmaceutics. 2017;529(1-2):491-505.
doi:10.1016/j.ijpharm.2017.07.036
conv_3925 .
Savić, Vedrana, Todosijević, Marija N., Ilić, Tanja, Lukić, Milica, Mitsou, Evgenia, Papadimitriou, Vassiliki, Avramiotis, Spyridon, Marković, Bojan, Cekić, Nebojša, Savić, Snežana, "Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances" in International Journal of Pharmaceutics, 529, no. 1-2 (2017):491-505,
https://doi.org/10.1016/j.ijpharm.2017.07.036 .,
conv_3925 .
