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Background: Topical adapalene and tretinoin, are comedolytic, anti-comedogenic and anti-inflammatory, on RAR (?, ?, ?) receptors binding. Adapalene enables quicker follicular penetration, by lesser anti-AP-1 (c-Jun, c-Fos) and no CRBPII mRNA actions, causing chemical stability, lipophilicity and less photo-lability, producing lesser photosensitivity and no skin irritation, unlike tretinoin; wherein reducible by overnight application and combination therapy, slow-release polymers or emollients, respectively. Topical nadifloxacin is bactericidal, anti-inflammatory and comedolytic, with inhibitory effect on DNA gyrase, DNA topoisomerase IV and IL-1?, IL-6, IL-8. The Global Alliance to Improve Outcomes in Acne Guidelines recommend synergistic and additive combination therapies, which enhance therapeutic efficacy and reduce adverse effects. Due to inadequacy of data, this study was conducted, to compare the safety among topical anti-acne monotherapies and combination therapies, and to easily detect any adverse effect producing component in the topical combination therapy.Methods: In this multi-centre, prospective, randomised, open-labelled, comparative study, groups A, B, C, D and E (20 patients each), applied topical 1% nadifloxacin monotherapy, 0.1% adapalene monotherapy, 0.025% tretinoin monotherapy, 1% nadifloxacin and 0.1% adapalene combination therapy and 1% nadifloxacin and 0.025% tretinoin combination therapy, respectively, over their facial mild to moderate acne lesions, once daily overnight; and adverse effects, like erythema, scaling, dryness, prutitus, burning, or stinging, were assessed on 0, 15, 30, 60, 90 days and follow-ups, by Local Irritation Scale.Results: In all 5 groups, no adverse effects were observed, with no statistically significant difference among the observations.Conclusions: The therapies were well tolerated and safe among all 5 groups.
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BACKGROUND: Although Eriobotrya japonica leaves have been studied as a raw material for various cosmetic products, little is known about the anti-oxidant, anti-inflammatory, and anti-melanogenic activities of Eriobotrya japonica leaf ethanol extract (EJEE). METHODS: This study was conducted to evaluate the anti-oxidant, anti-inflammatory, and anti-melanogenic activities of EJEE using different in vitro models. In addition, we investigated the potential irritation of EJEE to skin and eye using animal alternative tests. RESULTS: The total content of polyphenols, one of the active constituents of EJEE, was analyzed by high-performance liquid chromatography and found to contain 88.68 mg tannic acid equivalent/g. EJEE showed a concentration-dependent 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging activity, and a superoxide dismutase-like activity. The anti-inflammatory effect of 0.5% (w/v) EJEE was demonstrated by a reduction in lipopolysaccharide-induced nitric oxide and tumor necrosis factor-alpha levels in RAW 264.7 cells. EJEE also significantly inhibited melanogenesis in melanocyte stimulating hormone-induced B16F1 cells. EJEE did not show any irritation in skin and eye in animal alternative test. CONCLUSIONS: These results indicate that the EJEE possesses anti-oxidant, anti-inflammatory, and anti-melanogenic activities, while it did not induce toxicity or irritation in neither skin nor eye. Therefore, EJEE can be used as a cosmetic ingredient for skin improvement.
Subject(s)
Animals , Chromatography, Liquid , Eriobotrya , Ethanol , In Vitro Techniques , Melanocytes , Nitric Oxide , Polyphenols , Skin , Superoxides , Tannins , Tumor Necrosis Factor-alphaABSTRACT
OBJECTIVE: To study the local irritative response and cytotoxicity of glycerol in vivo and in vitro, and evaluate the safety of glycerol as an excipient in inhaled preparations preliminarily. METHODS: Local irritation test: rats were divided into two groups, the glycerol group received 20% glycerol by intratracheal atomization once a day, followed by 5 d, the control group was given the equal volume of 0.9% sodium chloride solutions in the same way. After administration, the throat, trachea and lung were taken for histopathological examination, and bronchoalveolar lavage was performed in each group, total protein (TP) content (BCA method) and alkaline phosphatase (ALP), lactate dehydrogenase (LDH) activity in the lavage fluid were detected (biochemical instrument). Cytotoxicity test: the toxic effects of glycerol on adenocarcinoma human alveolar epithelial-like cells (A549), human bronchial epithelial cells (16HBE) and rat tracheal epithelial cells (RTE) were studied by MTT assay. RESULTS: Local irritation test:the control group showed mild infiltration of inflammatory cells in the alveolar (1/8), glycerol group showed perivascular inflammation (2/8) and moderate mild to mild infiltration of inflammatory cells in the alveolar (6/8); bronchoalveolar lavage fluid test showed that, compared with the control group, the level of ALP in the glycerol group was elevated significantly (P<0.05). There was a dose-effect relationship between the cytotoxicity on A549, 16HBE and RTE cells with varying volume fraction of glycerol content in the range of 0.25%-10%, r2 values were 0.989, 0.981, 0.964, and IC50 were 4.28%, 4.40%, 4.31% respectively. CONCLUSION: The 20% glycerol has slight irritation to the lung in vivo, and in vitro glycerol has obvious toxic effect on A549 and 16HBE cells when the volume fraction reached 2.0%, when it reached 4.0%, it has significant toxic effect on RTE cells, suggesting that large dose of glycerol may cause mild irritation and toxicity to the lungs.
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Objective To study the local irritation of repeated intrathecal injection of Ziconotide Acetate,and to provide reference for irritancy evaluation ofintrathecal injection.Methods Sixteen New Zealand rabbits were assigned into two groupsat random:Control group and Ziconotide Acetate group,eight animals each group.Totally 50 μL saline or Ziconotide Acetate (100 μg/mL) were administrated by repeated lumbar intrathecal injection once daily for 7 d.Animal behavior was observed every day,and four animals in each group were sacrificed 2 d later after the last injection,the lumbar spinal cord was removed for histopathological examination and irritancy evaluation.The remaining animals were sacrificed for initancy evaluation 14 d later after the last injection.Results Only one animal died after anesthesia on day three in saline group,while no obvious adverse reactions were observed in other rabbits during the entire study,and no intrathecal irritant reactions of histopathological examination were found in both groups.The reversible minor mechanical damage was observed at the injection point,2 d after the last administration.Conclusion For 7 d repeated lumbar intrathecal injection in rabbits,no intrathecal irritant reactions observed in Ziconotide group,and the New Zealand rabbit could be used as a local irritation evaluation model.
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This study aimed to assess the attraction effect against Lycorma delicatula and antioxidant activity of hexane, chloroform, butanol and water fraction obtained from Ailanthus altissima methanol extract. The attraction effect of chloroform fraction showed the highest activity (47%) as compared to that of other fractions. In the DPPH radical scavenging activity, methanol and butanol fraction showed higher antioxidant activity than other solvent fractions. From the above results, the potential chloroform fraction was further performed by local irritation test in New Zealand white rabbits. In eye irritation test, chloroform fraction showed moderate irritant at high concentration 0.5 g/site/mL, but there was no eye irritation at low concentration (0.05 g/site/mL). In accordance with the Draize evaluation of skin irritation, the primary irritation index was calculated to 3.3 and 0.68 at high (0.5 g/site/mL) and low concentration (0.05 g/site/mL) causing moderate and mild irritation, respectively. On the basis of this study, Ailanthus altissima chloroform fraction could be safely considered to be a candidate of attractant against Lycorma delicatula.
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Rabbits , Ailanthus , Chloroform , Methanol , Skin , WaterABSTRACT
Objective To establish a rat model of ulcerative colitis by immunological sensitization combined with local acetic acid irritation.Methods Thirty healthy 2-3-month-old Wistar rats were randomly divided into 3 groups:normal control group,model group and SASP-treated model group(n=10 rats per group).The ulcerative colitis in the model group and positive group was developed by immunological sensitization with rabbit colon mucosal proteins and local irritation with 5%acetic acid.The rats of the model and positive groups were fed with sulfasalazine,and rats of the control group fed with normal saline.The rats of positive control group were treated with sulfasalazine.Two weeks later,all rats were killed and colon mucosal and blood samples were collected.The concentrations of NO,NOS,MDA,SOD and GSH-Px in the colonic mucosal homogenate were measured by biochemistry,the contents of IL-4 and TNF-α were measured by RIA,and the serum concentration of IFN-γ was measured by ELISA.Results Compared with the normal control group,the concentration of MDA,NO,NOS in the colonic mucosa was increased,and SOD and GSH-Px levels significantly decreased in the model group.Compared with the model group,the concentrations of MDA,NO,and NOS in the colonic mucosal tissue were decreased,and the levels of SOD and GSH-Px decreased in the SASP-treated model group.The contents of IL-4 in the serum and colonic mucosal homogenate of model group were significantly lower, and the contents of TNF-α in the serum and colonic mucosal homogenate were significantly increased than those of the normal control group. The IL-4 levels in the serum and colonic mucosal homogenate was increased, and that of TNF and IFN-γ significantly decreased in the SASP-treated model group, compared with those of the normal control group.Conclusion The rat model of ulcerative colitis established by immunological sensitization combined with local acetic acid irritation, as described in the present study, can better simulate the characteristic chronic alterations in human ulcerative colitis,and may better serve studies and evaluation of treatment of this disease.