Liang Yanchao, Su Zhihui, Yao Yao, Zhang Na
School of Pharmaceutical Science, Shandong University, 44 Wenhua Xi Road, Ji'nan 250012, Shandong, China.
Materials (Basel). 2015 Jan 23;8(2):379-391. doi: 10.3390/ma8020379.
A novel polymer-drug conjugate was prepared by the chemical reaction between the copolymer Pluronic P123 and the docetaxel via a pH sensitive hydrazone bond. These pluronic P123-docetaxel (DTX) conjugates (P123-DTX) could form the stable drug-loaded materials that can self-assemble into the defined nano-micelles in aqueous solution because of their obvious amphiphilic property and low critical micelle concentration. The spherical morphology and particle size of the prepared nano-micelles were characterized by transmission electron microscopy and dynamic light scattering, respectively. Moreover, after the introduction of pH sensitive hydrazone bond, P123-DTX micelle showed a pH dependent drug release behavior. At pH 5.0 (in 48 h), the cumulative release amount of DTX were ~84.9%, which is about six times higher than that at pH 7.4. The prepared novel p123-DTX conjugates may offer a great benefit for drug delivery and controlling the drug release.
通过共聚物普朗尼克P123与多西他赛之间经由pH敏感腙键的化学反应制备了一种新型聚合物-药物偶联物。这些普朗尼克P123-多西他赛（DTX）偶联物（P123-DTX）能够形成稳定的载药材料，由于其明显的两亲性和低临界胶束浓度，它们在水溶液中能自组装成特定的纳米胶束。分别通过透射电子显微镜和动态光散射对制备的纳米胶束的球形形态和粒径进行了表征。此外，引入pH敏感腙键后，P123-DTX胶束表现出pH依赖性药物释放行为。在pH 5.0时（48小时内），DTX的累积释放量约为84.9%，这比在pH 7.4时高出约六倍。制备的新型P123-DTX偶联物可能对药物递送和控制药物释放有很大益处。
