Formulation of hydrogel-thickened nonionic microemulsions with enhanced percutaneous delivery of ibuprofen assessed in vivo in rats
Copyright © 2016 Elsevier B.V. All rights reserved..
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°C, 20±3°C, and 40±1°C during 6months. 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 14.34±0.98nm (PdI 0.220±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 12h, 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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2016 |
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| Erschienen: |
2016 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:92 |
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| Enthalten in: |
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences - 92(2016) vom: 20. Sept., Seite 255-65 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Djekic, Ljiljana [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 06.04.2017 Date Revised 06.04.2017 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejps.2016.05.005 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM260138967 |
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| 520 | |a Copyright © 2016 Elsevier B.V. All rights reserved. | ||
| 520 | |a 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°C, 20±3°C, and 40±1°C during 6months. 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 14.34±0.98nm (PdI 0.220±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 12h, 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Analgesic effect | |
| 650 | 4 | |a Antiinflammatory activity | |
| 650 | 4 | |a Hydrogel-thickened microemulsions | |
| 650 | 4 | |a Ibuprofen | |
| 650 | 4 | |a In vitro drug release | |
| 650 | 4 | |a Xanthan gum | |
| 650 | 7 | |a Analgesics |2 NLM | |
| 650 | 7 | |a Anti-Inflammatory Agents, Non-Steroidal |2 NLM | |
| 650 | 7 | |a Emulsions |2 NLM | |
| 650 | 7 | |a Hydrogels |2 NLM | |
| 650 | 7 | |a Carrageenan |2 NLM | |
| 650 | 7 | |a 9000-07-1 |2 NLM | |
| 650 | 7 | |a Ibuprofen |2 NLM | |
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| 700 | 1 | |a Martinovic, Martina |e verfasserin |4 aut | |
| 700 | 1 | |a Stepanović-Petrović, Radica |e verfasserin |4 aut | |
| 700 | 1 | |a Micov, Ana |e verfasserin |4 aut | |
| 700 | 1 | |a Tomić, Maja |e verfasserin |4 aut | |
| 700 | 1 | |a Primorac, Marija |e verfasserin |4 aut | |
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