皮肤疾病治疗的酶激活前药的新药研究进展

Research development of new prodrugs triggered by dermatological enzymes of treating dermatological diseases

多数传统的经皮给药系统(traditional transdermal drug delivery system,TDDS)药物,由于化学稳定性差、油水分配系数不理想等,并不适合作为TDDS药物局部给药。而前体药物可以在皮肤组织经酶激活,代谢释放出具有活性物质的化合物。该文对目前最新的酶激活前体药物包括解热镇痛抗炎药、抗菌药、抗组胺药、抗肿瘤药、阿片受体拮抗剂、激素等前体药物及其新技术协同给药模式的制备原理、释药机制、存在问题、研究动态等进行归纳总结,并展望未来前体药物开发应用的趋势。酶激活前体药物在经皮给药系统应用中具有特异性、选择性、高透过率等释药特点,其不仅可以增加皮肤对药物的选择性,还能提高药物皮肤透过率,降低药物不良反应,具有良好的应用前景。

Due to their poor chemical stability,poor oil-water partition coefficient and other factors,most of the traditional transdermal drug delivery system(TDDS)drugs,are not conducive to local skin.Prodrugs can release compounds with active substances through enzyme catalysis in skin tissue.The enzyme activation of prodrugs for antipyretic analgesic anti-inflammatory drugs,antimicrobials,antihistamines,antineoplastic drugs,opioid receptor antagonists,hormones and their new collaborative drug delivery mode of the preparation principle of release mechanism of drug,problems,research trends,etc.were summarized,and the latest research and prospects for the future trend of the enzyme activation of prodrug development and application were introduced.Enzyme activation type prodrugs exhibited specificity,selectivity,high transmittance release characteristics of the drug.Enzyme activation of prodrugs can increase the selectivity of drugs through the skin,improve drug skin permeation rate and reduce adverse drug reactions and has good application prospects.