没食子酸(GA)具有抗氧化,抗炎和抗菌特性,虽然鞣花酸(EA)具有抗癌作用,抗病毒和光保护活性。在这项研究中,测试了掺入泊洛沙姆凝胶中的这些物质的组合,以验证这些物质的单独作用,除了利用可能的互补效应,旨在提供额外的治疗益处。由于成立,含有GA的配方,获得EA和GA+EA,对冻融循环对pH值的影响进行了评估,这表明在大多数样品中显著下降(p<0.05),包括载体(不含药物)和含有两种药物的凝胶。没有样品显示出超出皮肤正常pH范围的变化,值范围从4.8到6.0。关于电导率,GA,EA和GA+EA制剂在冻融循环后显示减少(p<0.05)。制剂中的药物含量范围从最初的95.86%至101.35%到冻融循环后的91.30%至101.51%。关于药物释放,结果显示以下累积百分比:1.5h后GA-3%-92.58%;6h后AE-3%-51.60%;2h后GA+EA(1.5%=1.5%)-99.91%;GA+EA-(1.5%=1.5%)释放57.06%,6小时后。关于毒性,观察到用GA处理的组显示在制剂中剂量为3000mg/Kg的幼虫的较低存活率(40%)。遵循同样的趋势,在使用Zophobasmorio幼虫进行的急性致死浓度(ALC50)测试中,在48小时时观察到GA的ALC50为2191.51mg/Kg。黑色素分析显示GA组中浓度降低了30mg/Kg,3mg/Kg的EA和3,300,3000mg/Kg的GA+EA,纯药物。在将药物掺入凝胶中的组中,溶媒(凝胶)中黑色素有显著下降(P<0.05),浓度为300和3000mg/Kg的GA和EA。另一方面,在GA+EA的组合中,当与对照组相比时,在3和30mg/Kg的浓度下观察到降低。因此,该凝胶作为局部使用的药物制剂显示出良好的质量和低毒性,使其有希望用于皮肤疗法。
Gallic acid (GA) has antioxidant, anti-inflammatory and antimicrobial properties, while ellagic acid (EA) demonstrates anticancer, antiviral and photoprotective activity. In this study, the combination of these substances incorporated into a poloxamer gel was tested to verify the individual effect of the substances, in addition to taking advantage of a probable complementary effect, aiming to provide additional therapeutic benefits. As a result of the incorporation, formulations containing GA, EA and GA + EA were obtained, which were evaluated for the effects of the Freeze-thaw cycle on pH, which revealed a significant decrease (p < 0.05) in most samples, including the vehicle (without drug) and the gel containing both drugs. No sample showed variation outside the normal pH range for the skin, with values ranging from 4.8 to 6.0. Regarding conductivity, the GA, EA and GA + EA formulations showed a reduction (p < 0.05) after the freeze-thaw cycle. The drug content in the formulations ranged from 95.86% to 101.35% initially to 91.30% to 101.51% after the freeze-thaw cycle. Regarding the drug release, the results revealed the following cumulative percentages: GA-3% - 92.58% after 1.5 h; AE-3% - 51.60% after 6 h; GA + EA (1.5% = 1.5%) - 99.91% after 2 h; GA + EA- (1.5% = 1.5%) released 57.06%, after 6 h. Regarding toxicity, it was observed that the group treated with GA showed a lower survival rate of the larvae (40%) at the dose 3000 mg/Kg in the formulation. Following the same trend, in the acute lethal concentration (ALC50) test performed using Zophobas morio larvae, an ALC50 of 2191.51 mg/Kg was observed for GA at 48 h. Melanin analysis showed a decrease in concentrations of 30 mg/Kg in the GA group, 3 mg/Kg of EA and 3, 300, 3000 mg/Kg of GA + EA, of the pure drugs. In the groups with the drugs incorporated into the gel, there was a significant decrease (P < 0.05) in melanin in the vehicle (gel), at concentrations of 300 and 3000 mg/Kg of GA and EA. On the other hand, in the combination of GA + EA, a reduction was observed at concentrations of 3 and 30 mg/Kg when compared to the control group. Thus, the gel showed good quality as a pharmaceutical formulation for topical use and low toxicity, making it promising for use in skin therapies.