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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
j.ijpharm.2015.10.048.pdf (826.9Kb)
Authors
Todosijević, Marija
Savić, Miroslav M.
Batinić, Bojan B.
Marković, Bojan D.
Gasperlin, Mirjana
Randjelović, Danijela
Lukić, Milica
Savić, Snežana D.
Article (Accepted Version)
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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.

Keywords:
Bicontinuous microemulsion / Sucrose ester / Aceclofenac / Skin irritation potential / Tape stripping / Pharmacokinetics
Source:
International Journal of Pharmaceutics, 2015, 496, 2, 931-941
Publisher:
  • 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:
  • This is peer-reviewed version of the artcle: M.N. Todosijević, M.M. Savić, B.B. Batinić, B.D. Marković, M. Gašperlin, D. V Ranđelović, M.Ž. Lukić, S.D. Savić, Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance, Int. J. Pharm. 496 (2015) 931–941. https://doi.org/10.1016/j.ijpharm.2015.10.048
  • Published version: http://cer.ihtm.bg.ac.rs/handle/123456789/1805

DOI: 10.1016/j.ijpharm.2015.10.048

ISSN: 0378-5173

PubMed: 26497615

WoS: 000367384700079

Scopus: 2-s2.0-84949571214
[ Google Scholar ]
38
33
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/3202
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - 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/123456789/3202
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 . .

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