Department of Medicine, Infectious Diseases & Immunity, Hammersmith Hospital, Faculty of Medicine, Imperial College London, London W12 0NN, UK.
Biomaterials. 2011 Nov;32(31):8029-39. doi: 10.1016/j.biomaterials.2011.07.021. Epub 2011 Jul 31.
Cutaneous leishmaniasis (CL) is a neglected tropical disease that causes prominent skin scaring. No water soluble, non-toxic, short course and low cost treatment exists. We developed a new water soluble amphotericin B-polymethacrylic acid (AmB-PMA) using established and scalable chemistries. AmB-PMA was stable for 9 months during storage. In vitro, it was effective against Leishmania spp. promastigotes and amastigote infected macrophages. It was also less toxic and more effective than deoxycholate-AmB, and similar to liposomal AmB. Its in vivo activity was determined in both early and established CL lesion models of Leishmania major infection in genetically susceptible non-healing BALB/c mice. Intradermal AmB-PMA at a total dose of 18 mg of AmB/kg body weight led to rapid parasite killing and lesion healing. No toxicity was seen. No parasite relapse occurred after 80 days follow-up. Histological studies confirmed rapid parasite clearance from macrophages followed by accelerated fibroblast mediated tissue repair, regeneration and cure of the infection. Quantitative mRNA studies of the CL lesions showed that accelerated healing was associated with increased Tumour Necrosis Factor-α and Interferon-γ, and reduced Interleukin-10. These results suggest that a cost-effective AmB-PMA could be used to pharmacologically treat and immuno-therapeutically accelerate the healing of CL lesions.
皮肤利什曼病(CL)是一种被忽视的热带病,会导致明显的皮肤疤痕。目前尚无水溶性、无毒、疗程短且成本低的治疗方法。我们使用已建立且可扩展的化学方法开发了一种新的水溶性两性霉素 B-聚甲基丙烯酸(AmB-PMA)。AmB-PMA 在储存期间稳定 9 个月。在体外,它对利什曼原虫的前鞭毛体和感染的巨噬细胞内阿米巴原虫有效。它的毒性比去氧胆酸两性霉素 B 低,疗效比两性霉素 B 脂质体好。其体内活性在易感非愈合 BALB/c 小鼠的利什曼原虫感染早期和已建立的 CL 病变模型中得到了确定。皮内给予 18mg/kg 体重的 AmB-PMA 总剂量可迅速杀死寄生虫并治愈病变。未见毒性。80 天后随访无寄生虫复发。组织学研究证实,巨噬细胞内的寄生虫迅速清除,随后成纤维细胞介导的组织修复、再生和感染治愈加速。CL 病变的定量 mRNA 研究表明,加速愈合与增加肿瘤坏死因子-α和干扰素-γ以及减少白细胞介素-10 有关。这些结果表明,一种具有成本效益的 AmB-PMA 可用于治疗皮肤利什曼病并免疫治疗加速 CL 病变的愈合。