Departamento de Fisiologia e Biofísica, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Av. Antônio Carlos 6627, Pampulha, 31270-901 Belo Horizonte, MG, Brazil.
Expert Opin Drug Deliv. 2010 Dec;7(12):1343-58. doi: 10.1517/17425247.2010.529897. Epub 2010 Oct 28.
Pentavalent antimonials are the first-line drugs for treatment of the major tropical disease leishmaniasis. However, their use is limited by the need for daily parenteral administration, their severe side effects and treatment failures. As leishmaniasis belongs to the group of neglected diseases, the improvement of old drugs through new delivery approaches has more support than the development of new chemical entities.
The review covers, from 1977 to the present, the progress achieved towards pharmaceutically acceptable liposome-based formulations of antimonials, identification of specific ligands for improved targeting of infected macrophages and new approaches for oral and topical delivery of antimonial drugs.
Insights into the most promising delivery strategies to improve antimonial therapy and the chemical basis and future directions for achieving innovative orally and topically effective formulations.
The development of drug delivery strategies for the old pentavalent antimonials is a still growing and promising field, with expected innovations in the near future from improved knowledge of antimony chemistry.
五价锑剂是治疗主要热带病利什曼病的一线药物。然而，由于需要每日进行肠胃外给药、严重的副作用和治疗失败，其应用受到限制。由于利什曼病属于被忽视的疾病之一，通过新的给药途径改进旧药物比开发新的化学实体更受支持。
从 1977 年至今，综述了在药学上可接受的基于脂质体的锑制剂方面取得的进展，确定了用于改善感染巨噬细胞靶向的特定配体，以及用于口服和局部递送锑药物的新方法。
深入了解最有前途的药物传递策略，以改善锑剂治疗效果，以及实现创新的口服和局部有效制剂的化学基础和未来方向。
五价锑药物传递策略的发展仍然是一个充满希望的领域，随着对锑化学的认识不断提高，预计在不久的将来会有创新。
