Topical hydrogels with escin β-sitosterol phytosome and escin: Formulation development and in vivo assessment of antihyperalgesic activity
Samo za registrovane korisnike
2019
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
The physicochemical properties, stability, in vivo antihyperalgesic activity, and skin irritation potential of the carbomer hydrogels with the new chemical entity escin β-sitosterol (ES) phytosome were characterized and compared with those containing escin. Physicochemical characterization of the hydrogels (performed 48 hr after preparation) included organoleptic examination, pH measurement, light microscopy, differential scanning calorimetry analysis and rheological tests. The obtained results showed that increasing concentration of the active substances within 1–5% affected the appearance (color and transparency) of the hydrogels, their pH, consistency, and rheological behavior. Unlike acidic escin, which was dissolved in the liquid phase of the pseudoplastic hydrogels E1–E5 and reduced their maximal apparent viscosity (ηmax), minimal apparent viscosity (ηmin), and hysteresis area (H) in comparison to the plain carbomer hydrogel, amphiphilic ES-enhanced ηmax, ηmin, and thixotropy of ...the hydrogels ES1–ES5, which is favorable for prolonged retention at skin surface. Evaluation of in-use stability of the hydrogels showed that organoleptic characteristics, flow behavior, and pH values could be preserved for 3 months under ambient conditions. The rat ear test results suggested that the hydrogels are safe to be used on human skin. Both escin and ES-loaded hydrogels exerted significant, concentration-dependent antihyperalgesic effect in inflammatory pain model in rats. ES-loaded hydrogels were significantly more effective than those loaded with escin. This is a first report on the antihyperalgesic effect of topically applied escin as well as ES in a model of inflammatory pain.
Ključne reči:
analgesia / escin / hydrogel / inflammation / pain / Wistar ratsIzvor:
Drug Development Research, 2019Izdavač:
- Wiley-Liss Inc.
Finansiranje / projekti:
- Razvoj novih inkapsulacionih i enzimskih tehnologija za proizvodnju biokatalizatora i biološki aktivnih komponenata hrane u cilju povećanja njene konkurentnosti, kvaliteta i bezbednosti (RS-MESTD-Integrated and Interdisciplinary Research (IIR or III)-46010)
- Ispitivanje mehanizma dejstva, interakcija i toksičnih efekata adjuvantnih analgetika (RS-MESTD-Basic Research (BR or ON)-175045)
DOI: 10.1002/ddr.21572
ISSN: 0272-4391
WoS: 000478505200001
Scopus: 2-s2.0-85068899272
Institucija/grupa
PharmacyTY - JOUR AU - Đekić, Ljiljana AU - Čalija, Bojan AU - Micov, Ana AU - Tomić, Maja AU - Stepanović-Petrović, Radica PY - 2019 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3268 AB - The physicochemical properties, stability, in vivo antihyperalgesic activity, and skin irritation potential of the carbomer hydrogels with the new chemical entity escin β-sitosterol (ES) phytosome were characterized and compared with those containing escin. Physicochemical characterization of the hydrogels (performed 48 hr after preparation) included organoleptic examination, pH measurement, light microscopy, differential scanning calorimetry analysis and rheological tests. The obtained results showed that increasing concentration of the active substances within 1–5% affected the appearance (color and transparency) of the hydrogels, their pH, consistency, and rheological behavior. Unlike acidic escin, which was dissolved in the liquid phase of the pseudoplastic hydrogels E1–E5 and reduced their maximal apparent viscosity (ηmax), minimal apparent viscosity (ηmin), and hysteresis area (H) in comparison to the plain carbomer hydrogel, amphiphilic ES-enhanced ηmax, ηmin, and thixotropy of the hydrogels ES1–ES5, which is favorable for prolonged retention at skin surface. Evaluation of in-use stability of the hydrogels showed that organoleptic characteristics, flow behavior, and pH values could be preserved for 3 months under ambient conditions. The rat ear test results suggested that the hydrogels are safe to be used on human skin. Both escin and ES-loaded hydrogels exerted significant, concentration-dependent antihyperalgesic effect in inflammatory pain model in rats. ES-loaded hydrogels were significantly more effective than those loaded with escin. This is a first report on the antihyperalgesic effect of topically applied escin as well as ES in a model of inflammatory pain. PB - Wiley-Liss Inc. T2 - Drug Development Research T1 - Topical hydrogels with escin β-sitosterol phytosome and escin: Formulation development and in vivo assessment of antihyperalgesic activity DO - 10.1002/ddr.21572 ER -
@article{ author = "Đekić, Ljiljana and Čalija, Bojan and Micov, Ana and Tomić, Maja and Stepanović-Petrović, Radica", year = "2019", abstract = "The physicochemical properties, stability, in vivo antihyperalgesic activity, and skin irritation potential of the carbomer hydrogels with the new chemical entity escin β-sitosterol (ES) phytosome were characterized and compared with those containing escin. Physicochemical characterization of the hydrogels (performed 48 hr after preparation) included organoleptic examination, pH measurement, light microscopy, differential scanning calorimetry analysis and rheological tests. The obtained results showed that increasing concentration of the active substances within 1–5% affected the appearance (color and transparency) of the hydrogels, their pH, consistency, and rheological behavior. Unlike acidic escin, which was dissolved in the liquid phase of the pseudoplastic hydrogels E1–E5 and reduced their maximal apparent viscosity (ηmax), minimal apparent viscosity (ηmin), and hysteresis area (H) in comparison to the plain carbomer hydrogel, amphiphilic ES-enhanced ηmax, ηmin, and thixotropy of the hydrogels ES1–ES5, which is favorable for prolonged retention at skin surface. Evaluation of in-use stability of the hydrogels showed that organoleptic characteristics, flow behavior, and pH values could be preserved for 3 months under ambient conditions. The rat ear test results suggested that the hydrogels are safe to be used on human skin. Both escin and ES-loaded hydrogels exerted significant, concentration-dependent antihyperalgesic effect in inflammatory pain model in rats. ES-loaded hydrogels were significantly more effective than those loaded with escin. This is a first report on the antihyperalgesic effect of topically applied escin as well as ES in a model of inflammatory pain.", publisher = "Wiley-Liss Inc.", journal = "Drug Development Research", title = "Topical hydrogels with escin β-sitosterol phytosome and escin: Formulation development and in vivo assessment of antihyperalgesic activity", doi = "10.1002/ddr.21572" }
Đekić, L., Čalija, B., Micov, A., Tomić, M.,& Stepanović-Petrović, R.. (2019). Topical hydrogels with escin β-sitosterol phytosome and escin: Formulation development and in vivo assessment of antihyperalgesic activity. in Drug Development Research Wiley-Liss Inc... https://doi.org/10.1002/ddr.21572
Đekić L, Čalija B, Micov A, Tomić M, Stepanović-Petrović R. Topical hydrogels with escin β-sitosterol phytosome and escin: Formulation development and in vivo assessment of antihyperalgesic activity. in Drug Development Research. 2019;. doi:10.1002/ddr.21572 .
Đekić, Ljiljana, Čalija, Bojan, Micov, Ana, Tomić, Maja, Stepanović-Petrović, Radica, "Topical hydrogels with escin β-sitosterol phytosome and escin: Formulation development and in vivo assessment of antihyperalgesic activity" in Drug Development Research (2019), https://doi.org/10.1002/ddr.21572 . .