Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance
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2015
Authors
Todosijević, MarijaSavić, Miroslav M.

Batinić, Bojan B.

Marković, Bojan D.

Gasperlin, Mirjana
Randjelović, Danijela

Lukić, Milica
Savić, Snežana D.

Article (Published version)

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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.
Keywords:
Bicontinuous microemulsion / Sucrose ester / Aceclofenac / Skin irritation potential / Tape stripping / PharmacokineticsSource:
International Journal of Pharmaceutics, 2015, 496, 2, 931-941Publisher:
- Elsevier
Funding / projects:
- Development of micro- and nanosystems as carriers for drugs with anti-inflammatory effect and methods for their characterization (RS-34031)
- Behavioral ?ffects following repeated administration of newly synthesized ligands selective for distinct subtypes of GABAA receptor benzodiazepine binding site: comparison with standard psychopharmacologic drugs (RS-175076)
- Micro- Nanosystems and Sensors for Electric Power and Process Industry and Environmental Protection (RS-32008)
Note:
- 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
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Institution/Community
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 . .