莫匹罗星剂型改造研究进展

Progress on Formulation Modification of Mupirocin

莫匹罗星(Mupirocin,MPC)是一种广泛使用的外用抗生素,其抑制细菌异亮氨酰-tRNA的形成使其抑菌效果独特,但常规使用的MPC软膏有一定毒副作用,如其对创伤部位正常成纤维细胞的毒性作用及软膏基质的毒副作用等。同时,随着细菌对MPC的耐药性逐渐提高,MPC的抑菌效果也受到影响。近年来针对MPC的特点,已经发展出多种更加方便患者使用的新剂型。更重要的是,新剂型可以减少MPC的毒副作用、控制药物释放速度、延长血清半衰期等,在增进疗效的同时,一定程度上减少了耐药菌的筛选。本文主要综述莫匹罗星喷雾剂、贴剂、水凝胶和纳米等新制剂的研究进展。

Mupirocin(MPC) is a widely used topical antibiotic, its mechanism of inhibiting the formation of bacterial isoleucyl-tRNA makes its antibacterial effect unique and safe to use. The conventionally used MPC ointment has certain toxic and side effects, such as its toxic effect on normal fibroblasts at the wound site and the toxic and side effects of the ointment matrix. In addition, as the tolerance of bacteria to MPC gradually increased, the bacteriostatic effect of MPC was also affected. In recent years, according to the characteristics of MPC, a variety of new formulation that are more convenient for patients have been developed. More importantly, the new formulation can reduce the toxic and side effects of MPC, control the drug release rate, prolong the serum half-life, etc., while improving the curative effect and reducing the screening of drug-resistant bacteria to a certain extent. This paper mainly reviews the research progress of mupirocin sprays, patches, hydrogels and nano-formulations.