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Percutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization

Authorized Users Only
2020
Authors
Đekić, Ljiljana
Marković, Bojan
Micov, Ana
Tomić, Maja
Pecikoza, Uroš
Stepanović-Petrović, Radica
Article (Published version)
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Abstract
The study focused on formulation of carmellose sodium hydrogels and nonionic microemulsions with 5% and 10% of levetiracetam and investigation of drug concentration influence on their physicochemical characteristics and in-use stability as well as influence of drug concentration and carrier type on in vitro drug release and in vivo antihyperalgesic/antiedematous activity in a rat model of localized (intraplantar) carrageenan-induced inflammation. Hydrogels were pseudoplastic semisolids with thixotropy and pH 7.37–7.58. Microemulsions were low viscous Newtonian nanodispersions of oil droplets (13.11–15.11 nm) in water, with pH 4.01–4.64. Physical stability of the investigated systems was preserved over the 3-month storage under ambient conditions. Levetiracetam release followed zero order and Korsmeyer-Peppas models (R2 ≥ 0.99) reflecting the combined effects of drug concentration and carrier viscosity. All levetiracetam-loaded formulations produced significant reduction of hyperalgesia... and paw swelling induced by carrageenan (p < 0.001). Their efficacy in exerting antihyperalgesic activity was significantly higher than that observed with the reference 5% ibuprofen hydrogel preparation (up to 6 h) (p < 0.001), while antiedematous activity was comparable with the reference product. No erythema and visible blood vessels were observed in a rat ear test. The study demonstrated percutaneous delivery of levetiracetam as useful and safe therapeutic option for localized inflammatory pain with potential to overcome the insufficient efficacy of topically applied nonsteroidal anti-inflammatory drugs in the form of a hydrogel. [Figure not available: see fulltext.]. © 2020, Controlled Release Society.

Keywords:
Antihyperalgesic/antiedematous efficacy / Hydrogel / Levetiracetam / Microemulsion / Percutaneous delivery / Antihyperalgesic/antiedematous efficacy / Hydrogel / Levetiracetam / Microemulsion / Percutaneous delivery
Source:
Drug Delivery and Translational Research, 2020
Publisher:
  • Springer
Funding / projects:
  • Geosistemske osnove prostorno-funkcionalne organizacije Republike Srbije (RS-146010)
  • Examination of mechanisms of action, toxicity and interactions of adjuvant analgesics (RS-175045)

DOI: 10.1007/s13346-020-00787-4

ISSN: 2190-393X

WoS: 000535379400001

Scopus: 2-s2.0-85085338096
[ Google Scholar ]
2
1
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/3589
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Đekić, Ljiljana
AU  - Marković, Bojan
AU  - Micov, Ana
AU  - Tomić, Maja
AU  - Pecikoza, Uroš
AU  - Stepanović-Petrović, Radica
PY  - 2020
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3589
AB  - The study focused on formulation of carmellose sodium hydrogels and nonionic microemulsions with 5% and 10% of levetiracetam and investigation of drug concentration influence on their physicochemical characteristics and in-use stability as well as influence of drug concentration and carrier type on in vitro drug release and in vivo antihyperalgesic/antiedematous activity in a rat model of localized (intraplantar) carrageenan-induced inflammation. Hydrogels were pseudoplastic semisolids with thixotropy and pH 7.37–7.58. Microemulsions were low viscous Newtonian nanodispersions of oil droplets (13.11–15.11 nm) in water, with pH 4.01–4.64. Physical stability of the investigated systems was preserved over the 3-month storage under ambient conditions. Levetiracetam release followed zero order and Korsmeyer-Peppas models (R2 ≥ 0.99) reflecting the combined effects of drug concentration and carrier viscosity. All levetiracetam-loaded formulations produced significant reduction of hyperalgesia and paw swelling induced by carrageenan (p < 0.001). Their efficacy in exerting antihyperalgesic activity was significantly higher than that observed with the reference 5% ibuprofen hydrogel preparation (up to 6 h) (p < 0.001), while antiedematous activity was comparable with the reference product. No erythema and visible blood vessels were observed in a rat ear test. The study demonstrated percutaneous delivery of levetiracetam as useful and safe therapeutic option for localized inflammatory pain with potential to overcome the insufficient efficacy of topically applied nonsteroidal anti-inflammatory drugs in the form of a hydrogel. [Figure not available: see fulltext.]. © 2020, Controlled Release Society.
PB  - Springer
T2  - Drug Delivery and Translational Research
T1  - Percutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization
DO  - 10.1007/s13346-020-00787-4
ER  - 
@article{
author = "Đekić, Ljiljana and Marković, Bojan and Micov, Ana and Tomić, Maja and Pecikoza, Uroš and Stepanović-Petrović, Radica",
year = "2020",
abstract = "The study focused on formulation of carmellose sodium hydrogels and nonionic microemulsions with 5% and 10% of levetiracetam and investigation of drug concentration influence on their physicochemical characteristics and in-use stability as well as influence of drug concentration and carrier type on in vitro drug release and in vivo antihyperalgesic/antiedematous activity in a rat model of localized (intraplantar) carrageenan-induced inflammation. Hydrogels were pseudoplastic semisolids with thixotropy and pH 7.37–7.58. Microemulsions were low viscous Newtonian nanodispersions of oil droplets (13.11–15.11 nm) in water, with pH 4.01–4.64. Physical stability of the investigated systems was preserved over the 3-month storage under ambient conditions. Levetiracetam release followed zero order and Korsmeyer-Peppas models (R2 ≥ 0.99) reflecting the combined effects of drug concentration and carrier viscosity. All levetiracetam-loaded formulations produced significant reduction of hyperalgesia and paw swelling induced by carrageenan (p < 0.001). Their efficacy in exerting antihyperalgesic activity was significantly higher than that observed with the reference 5% ibuprofen hydrogel preparation (up to 6 h) (p < 0.001), while antiedematous activity was comparable with the reference product. No erythema and visible blood vessels were observed in a rat ear test. The study demonstrated percutaneous delivery of levetiracetam as useful and safe therapeutic option for localized inflammatory pain with potential to overcome the insufficient efficacy of topically applied nonsteroidal anti-inflammatory drugs in the form of a hydrogel. [Figure not available: see fulltext.]. © 2020, Controlled Release Society.",
publisher = "Springer",
journal = "Drug Delivery and Translational Research",
title = "Percutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization",
doi = "10.1007/s13346-020-00787-4"
}
Đekić, L., Marković, B., Micov, A., Tomić, M., Pecikoza, U.,& Stepanović-Petrović, R.. (2020). Percutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization. in Drug Delivery and Translational Research
Springer..
https://doi.org/10.1007/s13346-020-00787-4
Đekić L, Marković B, Micov A, Tomić M, Pecikoza U, Stepanović-Petrović R. Percutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization. in Drug Delivery and Translational Research. 2020;.
doi:10.1007/s13346-020-00787-4 .
Đekić, Ljiljana, Marković, Bojan, Micov, Ana, Tomić, Maja, Pecikoza, Uroš, Stepanović-Petrović, Radica, "Percutaneous delivery of levetiracetam as an alternative to topical nonsteroidal anti-inflammatory drugs: formulation development, in vitro and in vivo characterization" in Drug Delivery and Translational Research (2020),
https://doi.org/10.1007/s13346-020-00787-4 . .

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