Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats
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2016
Authors
Đekić, LjiljanaMartinović, Martina
Stepanović-Petrović, Radica
Micov, Ana
Tomić, Maja
Primorac, Marija
Article (Published version)
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The study investigated usage of hydrogel of an anionic polymer xanthan gum for design of ibuprofen-loaded hydrogel-thickened microemulsions (HTMs) from the nonionic oil-in-water microemulsion (M). Xanthan gum demonstrated the performances of a thickening agent in physically stable HTMs at 5 +/- 3 degrees C, 20 +/- 3 degrees C, and 40 +/- 1 degrees C during 6 months. The results of physicochemical characterization (pH, conductivity, rheological behaviour, spreadability) indicated that HTMs containing 0.25-1.00% of the polymer had colloidal structure with oil nanodroplets of 1434 +/- 0.98 nm (PdI 0220 +/- 0.075) dispersed in aqueous phase thickened with the polymer gel network which strength depended on the polymer concentration. HTMs with ibuprofen (5%) were evaluated as percutaneous drug delivery carriers. In vitro ibuprofen release from HTMs followed zero order kinetic (r > 0.995) for 12 h, while the referent hydrogel was described by Higuchi model. The HTM with optimized drug release... rate and spreadability (HTM1) and the polymer-free microemulsion (M) were assessed and compared with the referent hydrogel in in vivo studies in rats. HTM1 and M were significantly more efficacious than reference hydrogel in producing antihyperalgesic and at lower extent antiedematous activity in prophylactic topical treatment protocol, whilst they were comparable in producing antihyperalgesic/antiedematous effects in therapeutic protocol. Topical treatments produced no obvious skin irritation.
Source:
European Journal of Pharmaceutical Sciences, 2016, 92, 255-265Publisher:
- Elsevier Science BV, Amsterdam
Funding / projects:
- Novel encapsulation and enzyme technologies for designing of new biocatalysts and biologically active compounds targeting enhancement of food quality, safety and competitiveness (RS-MESTD-Integrated and Interdisciplinary Research (IIR or III)-46010)
DOI: 10.1016/j.ejps.2016.05.005
ISSN: 0928-0987
PubMed: 27157041
WoS: 000381833900028
Scopus: 2-s2.0-84971591986
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Institution/Community
PharmacyTY - JOUR AU - Đekić, Ljiljana AU - Martinović, Martina AU - Stepanović-Petrović, Radica AU - Micov, Ana AU - Tomić, Maja AU - Primorac, Marija PY - 2016 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2714 AB - The study investigated usage of hydrogel of an anionic polymer xanthan gum for design of ibuprofen-loaded hydrogel-thickened microemulsions (HTMs) from the nonionic oil-in-water microemulsion (M). Xanthan gum demonstrated the performances of a thickening agent in physically stable HTMs at 5 +/- 3 degrees C, 20 +/- 3 degrees C, and 40 +/- 1 degrees C during 6 months. The results of physicochemical characterization (pH, conductivity, rheological behaviour, spreadability) indicated that HTMs containing 0.25-1.00% of the polymer had colloidal structure with oil nanodroplets of 1434 +/- 0.98 nm (PdI 0220 +/- 0.075) dispersed in aqueous phase thickened with the polymer gel network which strength depended on the polymer concentration. HTMs with ibuprofen (5%) were evaluated as percutaneous drug delivery carriers. In vitro ibuprofen release from HTMs followed zero order kinetic (r > 0.995) for 12 h, while the referent hydrogel was described by Higuchi model. The HTM with optimized drug release rate and spreadability (HTM1) and the polymer-free microemulsion (M) were assessed and compared with the referent hydrogel in in vivo studies in rats. HTM1 and M were significantly more efficacious than reference hydrogel in producing antihyperalgesic and at lower extent antiedematous activity in prophylactic topical treatment protocol, whilst they were comparable in producing antihyperalgesic/antiedematous effects in therapeutic protocol. Topical treatments produced no obvious skin irritation. PB - Elsevier Science BV, Amsterdam T2 - European Journal of Pharmaceutical Sciences T1 - Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats VL - 92 SP - 255 EP - 265 DO - 10.1016/j.ejps.2016.05.005 ER -
@article{ author = "Đekić, Ljiljana and Martinović, Martina and Stepanović-Petrović, Radica and Micov, Ana and Tomić, Maja and Primorac, Marija", year = "2016", abstract = "The study investigated usage of hydrogel of an anionic polymer xanthan gum for design of ibuprofen-loaded hydrogel-thickened microemulsions (HTMs) from the nonionic oil-in-water microemulsion (M). Xanthan gum demonstrated the performances of a thickening agent in physically stable HTMs at 5 +/- 3 degrees C, 20 +/- 3 degrees C, and 40 +/- 1 degrees C during 6 months. The results of physicochemical characterization (pH, conductivity, rheological behaviour, spreadability) indicated that HTMs containing 0.25-1.00% of the polymer had colloidal structure with oil nanodroplets of 1434 +/- 0.98 nm (PdI 0220 +/- 0.075) dispersed in aqueous phase thickened with the polymer gel network which strength depended on the polymer concentration. HTMs with ibuprofen (5%) were evaluated as percutaneous drug delivery carriers. In vitro ibuprofen release from HTMs followed zero order kinetic (r > 0.995) for 12 h, while the referent hydrogel was described by Higuchi model. The HTM with optimized drug release rate and spreadability (HTM1) and the polymer-free microemulsion (M) were assessed and compared with the referent hydrogel in in vivo studies in rats. HTM1 and M were significantly more efficacious than reference hydrogel in producing antihyperalgesic and at lower extent antiedematous activity in prophylactic topical treatment protocol, whilst they were comparable in producing antihyperalgesic/antiedematous effects in therapeutic protocol. Topical treatments produced no obvious skin irritation.", publisher = "Elsevier Science BV, Amsterdam", journal = "European Journal of Pharmaceutical Sciences", title = "Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats", volume = "92", pages = "255-265", doi = "10.1016/j.ejps.2016.05.005" }
Đekić, L., Martinović, M., Stepanović-Petrović, R., Micov, A., Tomić, M.,& Primorac, M.. (2016). Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats. in European Journal of Pharmaceutical Sciences Elsevier Science BV, Amsterdam., 92, 255-265. https://doi.org/10.1016/j.ejps.2016.05.005
Đekić L, Martinović M, Stepanović-Petrović R, Micov A, Tomić M, Primorac M. Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats. in European Journal of Pharmaceutical Sciences. 2016;92:255-265. doi:10.1016/j.ejps.2016.05.005 .
Đekić, Ljiljana, Martinović, Martina, Stepanović-Petrović, Radica, Micov, Ana, Tomić, Maja, Primorac, Marija, "Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats" in European Journal of Pharmaceutical Sciences, 92 (2016):255-265, https://doi.org/10.1016/j.ejps.2016.05.005 . .