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, Marija N.Savić, Miroslav
Batinić, Bojan
Marković, Bojan
Gasperlin, Mirjana
Ranđelović, Danijela
Lukić, Milica
Savić, Snežana
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.
Извор:
International Journal of Pharmaceutics, 2015, 496, 2, 931-941Издавач:
- 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.2015.10.048
ISSN: 0378-5173
PubMed: 26497615
WoS: 000367384700079
Scopus: 2-s2.0-84949571214
Институција/група
PharmacyTY - 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 . .