Evaluation of percutaneous absorption of 4-nerolidylcathecol from four topical formulations

Röpke, Cristina Dislich; Kaneko, Telma Mary; Rodrigues, Reinaldo; Silva, Vanessa V. da; Barros, Sônia; Sawada, Tânia Cristina Higashi; Kato, Massuo Jorge; Barros, S. B. M.

doi:10.1016/s0378-5173(02)00477-5

Cited by 48 publications

(32 citation statements)

References 17 publications

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“…Release may be improved by selecting the appropriate vehicle. The in vitro release studies which measure drug/vehicle interactions are considered to be useful and crucial in pre-formulation step to choose an appropriate vehicle (40,41). The release of antioxidant compounds of the PPE from different emulsion systems (F1 and F2) through nitrocellulose membrane was examined and the values found were very close to both formulations, showing that the difference in lipid content did not affect the release of these components of the extract.…”

Section: In Vivo Studiesmentioning

confidence: 99%

Topical Formulations Containing Pimenta pseudocaryophyllus Extract: In Vitro Antioxidant Activity and In Vivo Efficacy Against UV-B-Induced Oxidative Stress

et al. 2013

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Abstract. Pimenta pseudocaryophyllus is a Brazilian native plant that presents high concentrations of flavonoids and other polyphenolic compounds. Herein, we evaluated: (1) the chemical properties of P. pseudocaryophyllus ethanolic extract (PPE), (2) the in vitro antioxidant activity (AA) of PPE and of two different topical formulations (F1 and F2) containing PPE, (3) physico-chemical and functional stability, (4) in vitro release of PPE, and (5) in vivo capacity of formulations to prevent UV-B irradiation-induced skin damage. Results show that the polyphenol and flavonoid contents in PPE were 199.33 and 28.32 mg/g, respectively, and HPLC results show the presence of eugenol, tannic acid, and rutin. Evaluation of the in vitro AA of PPE demonstrated a dose-dependent effect and an IC 50 of 4.75 μg/mL in 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 3.0 μg/mL in 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The ferric-reducing antioxidant power (FRAP assay) was 0.046 μmol/L trolox equivalent/ μg/mL of extract. Among the AA, only the capacity to scavenge DPPH radical of PPE was maintained in F1 and F2. In addition, both formulations satisfactorily released the extract. The evaluation of the functional stability of F1 and F2 did not demonstrate loss of activity by storage at room temperature and at 4°C/6 months. In irradiated mice, treatment with F1 and F2 added with PPE significantly increased the capacity to scavenge ABTS radical and the FRAP of skin compared to vehicle-treated mice. In conclusion, the present results suggest that formulations containing PPE may be a topical source of antioxidant compounds to decrease oxidative damages of the skin.

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Section: In Vivo Studiesmentioning

confidence: 99%

Topical Formulations Containing Pimenta pseudocaryophyllus Extract: In Vitro Antioxidant Activity and In Vivo Efficacy Against UV-B-Induced Oxidative Stress

et al. 2013

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“…Each MMP band was quantified densitometrically by computer imaging analysis with a GS-700 densitometer and molecular analysis software, version 1.4 (Bio-Rad, Hercules, CA, USA) (7). P. umbellata crude extract was prepared as previously described (8). Briefly, plant material of P. umbellata was obtained from the medicinal herb garden of the Faculdade de Ciências Farmacêu-ticas, Universidade de São Paulo, and a sample was deposited in the Herbarium of the Instituto de Biociências, Universidade de São Paulo (Silva/Ropke 01) and identified by Prof. José Rubens Pirani (Institute of Biology, University of São Paulo).…”

Section: Dose-dependent In Vitro Inhibition Of Rabbit Corneal Matrix mentioning

confidence: 99%

“…The recovered filtrate was freeze-dried. The final concentration of 4-NC, a catechol derivative, in the crude extract was 7.09% (w/ w), as evaluated by HPLC with electrochemical detection (8).…”

Section: Dose-dependent In Vitro Inhibition Of Rabbit Corneal Matrix mentioning

confidence: 99%

Dose-dependent in vitro inhibition of rabbit corneal matrix metalloproteinases by an extract of Pothomorphe umbellata after alkali injury

Barros

Röpke

et al. 2007

Braz J Med Biol Res

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The in vitro ability of Pothomorphe umbellata ethanolic crude extract to inhibit matrix metalloproteinase (MMP) in normal cornea and in cornea after alkali injury was demonstrated. Corneas of albino rabbits were injured with 1 N NaOH for 20 s. After 48 h the corneas were excised, homogenized and analyzed for MMP-9 (92 kDa), pro-MMP-2 (72 kDa) and MMP-2 (67 kDa) activity by gelatin zymography. The activity was also measured in untreated corneas. After electrophoresis of 20 µg protein, gels were incubated with 50, 100, or 250 µg/mL lyophilized hydroethanolic (1:1) root crude extract of P. umbellata standardized for 4-nerolidylcatechol (7.09%). The activity of the enzymes was compared with that of untreated gel. At 48 h after injury, the activity of all MMPs was increased compared with untreated eyes. When the gels were incubated with P. umbellata extract the activity of MMP-2, pro-MMP-2 and MMP-9 decreased in a dose-dependent manner. MMP-9 activity decreased by approximately 50% after incubation with 50 µg/mL and was completely abolished at 100 and 250 µg/mL of the extract. After incubation with 50 µg/mL the activity of pro-MMP-2 and MMP-2 also decreased by 50%. The activity of pro-MMP-2 was almost completely abolished after incubation with 250 µg/mL of the extract. For MMP-2 the incubation with 100 or 250 µg/ mL of the extract of P. umbellata promoted a 10-fold decrease in activity. In conclusion, P. umbellata root crude extract can be useful as an alternative therapy to control MMP activity after corneal injury.

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“…However, for appropriate skin protection, it is necessary that they exhibit permeation capacity, since the skin serves as a penetration barrier (Masaki, 2010;Pinnell, 2003;Röpke et al, 2002).…”

Section: Introductionmentioning

confidence: 99%

Employing photoacoustic spectroscopy in the evaluation of the skin permeation profile of emulsion containing antioxidant phenolic-rich extract ofMelochia arenosa

Tunin¹,

Borghi²,

Nogueira

et al. 2015

Pharmaceutical Biology

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Context: Oxidative stress is an important factor modulating skin alterations. Melochia arenosa Benth. (Malvaceae) is a Brazilian plant with antimicrobial activity and antioxidant potential. Objective: The objective of this study is to develop a topical formulation containing antioxidant phenolic-rich extract of M. arenosa and to evaluate its skin permeation profile. Materials and methods: Response surface methodology was used to maximize the total phenolic (TP) content of the extract and its antioxidant activity was evaluated by 2,2-diphenyl-1-picryl-hydrazyl (DPPH), 2,2 0 -azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and respiratory burst methods. An emulsion containing 1% optimized extract (OE) was developed and employed photoacoustic spectroscopy (PAS) for the determination of its skin permeation profile. The morphology of the skin was studied in histological sections stained with hematoxylin-eosin. Results and discussion: The optimum conditions predicted for the major extractive efficiency of the phenolics with 100% ethanol led extraction time 101 h and plant:solvent proportion 1:13.5 (w/v). OE presented TP ¼ 724.6 ± 8.2 mg GAE/g extract and scavenging capacity of DPPH (IC 50 value ¼ 11.43 ± 0.14 mg/mL) and ABTS radicals (IC 50 value ¼ 35.42 ± 0.48 mg/mL). The production of ROS by neutrophils after stimulation with phorbol miristate acetate was lower when the OE was present in the reaction medium, endorsing its high antioxidant capacity. The data obtained by PAS indicated that the OE present in the emulsion has permeated and was distributed in the whole skin. No histopathological alterations were observed in the histological analysis. Conclusion: The formulation developed is a promising tool for skin care and could prevent the damage caused by oxidative stress.

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Evaluation of percutaneous absorption of 4-nerolidylcathecol from four topical formulations

Cited by 48 publications

References 17 publications

Topical Formulations Containing Pimenta pseudocaryophyllus Extract: In Vitro Antioxidant Activity and In Vivo Efficacy Against UV-B-Induced Oxidative Stress

Topical Formulations Containing Pimenta pseudocaryophyllus Extract: In Vitro Antioxidant Activity and In Vivo Efficacy Against UV-B-Induced Oxidative Stress

Dose-dependent in vitro inhibition of rabbit corneal matrix metalloproteinases by an extract of Pothomorphe umbellata after alkali injury

Employing photoacoustic spectroscopy in the evaluation of the skin permeation profile of emulsion containing antioxidant phenolic-rich extract ofMelochia arenosa

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