Abstract Acne vulgaris is a chronic skin disease of the pilosebaceous unit. Several pathophysiological associations have been identified in which Propionibacterium acnes plays a major role. Although there are a number of antibiotic therapies suggested for acne, many of them have limitations in their safety and efficacy. Therefore, there is a high demand to develop a safe alternative therapy for acne. Fullerene is an emerging nanomaterial believed to be a potential candidate for the treatment of acne due to its antibacterial and antioxidant activities. The low water solubility of fullerene limits its application in the cosmeceutical products. In the present study, a water soluble derivative of fullerene, glycine-fullerene conjugate (Gly-Ful), was developed and optimized using Design expert® software. As the positively charged molecules could act directly on the negatively charged bacterial cellular membranes, chitosan surface modified glycine-fullerene conjugate nanoparticles (Chi-Gly-Ful NPs) were prepared and Chi-Gly-Ful NPs gel was formulated for topical use in acne treatment. In vitro susceptibility of Propionibacterium acnes to Chi-Gly-Ful NPs formulation and comparator drug (streptomycin) was evaluated. The results showed that Chi-Gly-Ful NPs formulation inhibited effectively the growth of P. acnes and showed comparable antibacterial activity to streptomycin. The minimum bactericidal concentration (MIC) for Chi-Gly-Ful NPs was 8 µg/ml. Chi-Gly-Ful NPs at the concentrations of 25–400 µM showed no cytotoxicity on L929 fibroblast cells. Conclusively, our present work showed for the first time that Chi-Gly-Ful NPs has antimicrobial effects against P. acnes with no cytotoxic effect, suggesting Chi-Gly-Ful NPs as a promising novel therapeutic agent for the treatment of acne.

中文翻译：

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富勒烯新型外用剂型的开发，对痤疮丙酸杆菌具有抗菌活性

摘要 寻常痤疮是毛囊皮脂腺单位的一种慢性皮肤病。已经确定了几种病理生理学关联，其中痤疮丙酸杆菌起主要作用。尽管建议使用多种抗生素治疗痤疮，但其中许多在安全性和有效性方面存在局限性。因此，迫切需要开发一种安全的痤疮替代疗法。富勒烯是一种新兴的纳米材料，由于其抗菌和抗氧化活性，被认为是治疗痤疮的潜在候选材料。富勒烯的低水溶性限制了其在药妆产品中的应用。在本研究中，使用 Design Expert® 软件开发和优化了富勒烯的水溶性衍生物甘氨酸-富勒烯结合物 (Gly-Ful)。由于带正电荷的分子可以直接作用于带负电荷的细菌细胞膜，因此制备了壳聚糖表面修饰的甘氨酸-富勒烯共轭纳米粒子（Chi-Gly-Ful NPs），并配制了 Chi-Gly-Ful NPs 凝胶用于局部治疗痤疮. 评估了痤疮丙酸杆菌对 Chi-Gly-Ful NPs 制剂和比较药物（链霉素）的体外敏感性。结果表明，Chi-Gly-Ful NPs 制剂可有效抑制痤疮丙酸杆菌的生长，并显示出与链霉素相当的抗菌活性。Chi-Gly-Ful NPs 的最低杀菌浓度 (MIC) 为 8 µg/ml。浓度为 25–400 µM 的 Chi-Gly-Ful NPs 对 L929 成纤维细胞没有细胞毒性。最后，