A prodrug strategy to deliver cisplatin(IV) and paclitaxel in nanomicelles to improve efficacy and tolerance

详细信息    查看全文

• 作者：Haihua Xiao ; Haiqin Song ; Qiang Yang ; Haidong Cai ; Ruogu Qi ; Lesan Yan ; Shi Liu ; Yonghui Zheng ; Yubin Huang ; Tongjun Liu ; Xiabin Jing
• 关键词：Platinum drugs ; Paclitaxel ; Combination therapy ; Drug delivery ; Micelles
• 刊名：Biomaterials
• 出版年：2012
• 出版时间：September, 2012
• 年：2012
• 卷：33
• 期：27
• 页码：6507-6519
• 全文大小：925 K

文摘

A strategy of preparing composite micelles containing both cisplatin(IV) prodrug and paclitaxel was developed, i.e., synthesizing a cisplatin(IV) conjugate and a paclitaxel conjugate starting with the same biodegradable and amphiphilic block copolymer, and co-assembling the two conjugates. The composite micelles could release effective anticancer drug cisplatin(II) upon cellular reduction and PTX via acid hydrolysis once they came into the cancerous cells. Moreover, the composite micelles displayed synergistic effect in?vitro and the combination therapy in micellar dosage-form led to reduced systematic toxicity and enhanced antitumor efficacy in?vivo.