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含鼠李糖脂的生物粘附性聚合物薄膜,一种创新的局部抗菌制剂。

Bioadhesive Polymeric Films Containing Rhamnolipids, An Innovative Antimicrobial Topical Formulation.

机构信息

Departamento de Química, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid, PR-445, Km 380 - Campus Universitário, Londrina, Paraná, 86057-970, Brazil.

Departamento de Bioquímica E Biotecnologia, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid, PR-445, Km 380 - Campus Universitário, Londrina, Paraná, 86057-970, Brazil.

出版信息

AAPS PharmSciTech. 2024 Jul 31;25(6):177. doi: 10.1208/s12249-024-02895-7.

Abstract

Acne affects most of the world's population, causing an impact on the self-esteem of adolescents and young adults. One of the causes is the presence of the bacteria Cutibacterium acnes which are part of the natural microbiota of the skin. Topical treatments consist of anti-inflammatory and antibiotics, which could select resistant strains. Alternatives to the antibiotic are biocomposites that have antimicrobial activity like biosurfactants which are produced by bacteria. An innovative way of applying these compounds is bioadhesive polymeric films that adhere to the skin and release the active principle topically. Rhamnolipids have great potential to be used in the treatment of acne because they present antimicrobial activity against C. acnes in low and safe concentrations (MIC of 15.62 µg/mL, CBM of 31.25 µg/mL and CC50 of 181.93 µg/mL). Four films with different rhamnolipids concentrations (0.0; 0.1; 0.2; and 0.3%, w/w) were obtained as to visual appearance, mass variation, thickness, density, solubility, pH, water vapor transmission, mechanical properties (folding endurance, bioadhesion strength, tensile strength, elongation at break and Young's modulus), scanning electron microscopy and infrared. The results show that these formulations had a homogeneous appearance; elastic mechanical properties; pH similar to human skin and bioadhesive. The polymeric films containing rhamnolipids were effective against C. acnes, in the in vitro test, at the three concentrations tested, the film with the highest concentration (0.3%, w/w) being the most promising for presenting the highest antimicrobial activity. Thus, the polymeric film containing rhamnolipids has the potential to be used in the treatment of acne.

摘要

痤疮影响了世界上大多数人口,对青少年和年轻人的自尊心造成了影响。其原因之一是痤疮丙酸杆菌的存在,它是皮肤天然微生物群的一部分。局部治疗包括抗炎和抗生素,这可能会选择出耐药菌株。抗生素的替代品是具有抗菌活性的生物复合材料,如由细菌产生的生物表面活性剂。一种创新的应用这些化合物的方法是生物粘附聚合物薄膜,它可以粘附在皮肤上并局部释放活性物质。鼠李糖脂由于具有针对痤疮丙酸杆菌的低浓度和安全的抗菌活性(MIC 为 15.62µg/mL、CBM 为 31.25µg/mL 和 CC50 为 181.93µg/mL),因此在治疗痤疮方面具有很大的潜力。为了观察外观、质量变化、厚度、密度、溶解度、pH 值、水蒸气传输、机械性能(耐折性、生物粘附强度、拉伸强度、断裂伸长率和杨氏模量)、扫描电子显微镜和红外光谱,获得了四种不同鼠李糖脂浓度(0.0;0.1;0.2;和 0.3%,w/w)的薄膜。结果表明,这些配方具有均匀的外观;弹性机械性能;与人体皮肤相似的 pH 值和生物粘附性。含有鼠李糖脂的聚合物薄膜对痤疮丙酸杆菌有效,在体外试验中,在测试的三个浓度下,浓度最高的薄膜(0.3%,w/w)最有希望表现出最高的抗菌活性。因此,含有鼠李糖脂的聚合物薄膜具有治疗痤疮的潜力。

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