Psoriasis is a chronic, immune-mediated skin disease with no cure. Intravenous arsenic trioxide (ATO) has been used to treat psoriasis in animal studies. However, the high toxicity of ATO limits its application to clinics for systemic administration. The aim of this study was to fabricate sustained-release ATO liposome gels (ATO-Lip-Gels) to be used for the treatment of psoriasis. The ATO Liposomes were prepared using a zinc acetate gradient method. ATO concentrations were analyzed by HPLC-HG-AFS. The ATO-Lip-Gels were characterized with respect to size, zeta potential, and entrapment efficiency. Stability, in vitro drug release, and in vivo efficacy were also evaluated. The optimal formulation of ATO-Lip was ATO (0.45%), S100 (9%), and cholesterol (1.5%) (W/V) in 0.3 mol/L zinc acetate and incubated for 10 min. In the in vitro drug release study, ATO-Lip-Gels exhibited a slower release profile of ATO than that from Gels only. Compared with the model group, ATO-Lip-Gels-H significantly reduced PASI scores after psoriasis in mice and was superior to tacrolimus at day 5. HE staining showed that the pathological changes caused by psoriasis in mice were significantly improved in the treatment groups, and ATO-Lip-Gels-H had the best effect among the treatment groups. ATO-Lip-Gels applied topologically to imiquimote-induced psoriatic plaque models significantly reduced the levels of key psoriatic cytokines such as IL-6 and TNF-alpha. We have developed ATO-Lip-Gels for the treatment of psoriasis, which demonstrated higher efficacy with the benchmark, Tacrolimus, and can be an alternative to the conventional treatment with Tacrolimus.

Photodynamic therapy (PDT) is a novel therapy that achieves therapeutic effects by exciting photosensitizers accumulated in tumour tissues with specific wavelengths of light. Among the various photosensitizers, 5-aminoketovaleric acid (5-ALA) has been used in the treatment of basal cell carcinoma, glioma, bladder cancer, and other tumours owing to its safety and economy. However, the efficacy of PDT is limited by the poor permeability and targeting of 5-ALA, and favourable nano-delivery systems would provide ideal platforms to solve this problem. Researchers have developed a variety of 5-ALA nano-delivery systems, such as nanoparticles, liposomes, and gels, and have achieved good efficacy in the treatment of various tumours. In this review, we present the progress of 5-ALA nano-delivery systems in different oncology fields and discuss the current challenges and future research prospects.

目的 研究口服纳米药物递送系统的体外吸收模型及内吞机制,为其吸收效果评价与开发应用提供参考.方法 利用中国知网、万方数据、维普、PubMed等数据库查询2006年1月-2021年4月发表的相关文献,对纳米药物递送系统的口服吸收模型与内吞机制研究进行总结归纳.结果 随着纳米药物递送系统的研究进展,口服吸收模型从Caco-2细胞模型和MDCK细胞模型等单一细胞模型,逐渐发展到应用Caco-2/HT29细胞模型、Caco-2/M细胞模型和Caco-2/HT29/Raji B细胞模型等共培养模型进行体外研究.目前,纳米药物递送系统的机制研究仍是以Caco-2细胞模型和MDCK细胞模型为基础进行考察,主要表现为网格蛋白、小窝蛋白、巨胞饮等多种途径共存的内吞机制.结论 为了更好地构建口服纳米药物递送系统,细胞吸收及机制研究具有重要的意义.因此,模拟小肠吸收的细胞模型及内吞机制的深入研究都将促进口服纳米药物的合理构建与安全应用.