Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances
Само за регистроване кориснике
2017
Аутори
Savić, VedranaTodosijević, Marija N.
Ilić, Tanja
Lukić, Milica
Mitsou, Evgenia
Papadimitriou, Vassiliki
Avramiotis, Spyridon
Marković, Bojan
Cekić, Nebojša
Savić, Snežana
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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.
Кључне речи:
Lecithin-based microemulsions / Tacrolimus / Propylene glycol monocaprylate / Skin irritation potential / Electron paramagnetic resonance spectroscopy / In vitro release / Tape strippingИзвор:
International Journal of Pharmaceutics, 2017, 529, 1-2, 491-505Издавач:
- Elsevier Science BV, Amsterdam
Финансирање / пројекти:
- Развој микро- и наносистема као носача за лекове са антиинфламаторним деловањем и метода за њихову карактеризацију (RS-MESTD-Technological Development (TD or TR)-34031)
DOI: 10.1016/j.ijpharm.2017.07.036
ISSN: 0378-5173
PubMed: 28711641
WoS: 000408009200046
Scopus: 2-s2.0-85024906743
Институција/група
PharmacyTY - 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 - https://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 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" }
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
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 .
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 . .