Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance
Само за регистроване кориснике
2015
Аутори
Todosijević, MarijaSavić, Miroslav M.
Batinić, Bojan B.
Marković, Bojan D.
Gasperlin, Mirjana
Randjelović, Danijela
Lukić, Milica
Savić, Snežana D.
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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.
Кључне речи:
Bicontinuous microemulsion / Sucrose ester / Aceclofenac / Skin irritation potential / Tape stripping / PharmacokineticsИзвор:
International Journal of Pharmaceutics, 2015, 496, 2, 931-941Издавач:
- Elsevier
Финансирање / пројекти:
- Развој микро- и наносистема као носача за лекове са антиинфламаторним деловањем и метода за њихову карактеризацију (RS-34031)
- Бихејвиорални ефекти понављане примене новосинтетисаних супстанци селективних за поједине подтипове бензодиазепинског места везивања ГАБА А рецептора: поређење са стандардним психофармаколошким лековима (RS-175076)
- Микро, нано-системи и сензори за примену у електропривреди, процесној индустрији и заштити животне средине (RS-32008)
Напомена:
- Accepted version: http://cer.ihtm.bg.ac.rs/handle/123456789/3202
DOI: 10.1016/j.ijpharm.2015.10.048
ISSN: 0378-5173
PubMed: 26497615
WoS: 000367384700079
Scopus: 2-s2.0-84949571214
Институција/група
IHTMTY - JOUR AU - Todosijević, Marija AU - Savić, Miroslav M. AU - Batinić, Bojan B. AU - Marković, Bojan D. AU - Gasperlin, Mirjana AU - Randjelović, Danijela AU - Lukić, Milica AU - Savić, Snežana D. PY - 2015 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/1805 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 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 and Savić, Miroslav M. and Batinić, Bojan B. and Marković, Bojan D. and Gasperlin, Mirjana and Randjelović, Danijela and Lukić, Milica and Savić, Snežana D.", 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", 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., Savić, M. M., Batinić, B. B., Marković, B. D., Gasperlin, M., Randjelović, D., Lukić, M.,& Savić, S. D.. (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., 496(2), 931-941. https://doi.org/10.1016/j.ijpharm.2015.10.048
Todosijević M, Savić MM, Batinić BB, Marković BD, Gasperlin M, Randjelović D, Lukić M, Savić SD. 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, Savić, Miroslav M., Batinić, Bojan B., Marković, Bojan D., Gasperlin, Mirjana, Randjelović, Danijela, Lukić, Milica, Savić, Snežana D., "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 . .