Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.
Department of Chemical Engineering, National Taiwan University of Science and Technology, 43 Section 4, Keelung Road, Taipei 10607, Taiwan; Graduate Institute of Applied Science and Technology, National Taiwan University of Science and Technology, 43 Section 4, Keelung Road, Taipei 10607, Taiwan.
Int J Pharm. 2017 Dec 20;534(1-2):136-143. doi: 10.1016/j.ijpharm.2017.10.023. Epub 2017 Oct 12.
Previously reported amphiphilic diblock copolymer with pendant dendron moieties (PD) has been further evaluated in tumor-bearing mice as a potential drug carrier. This PD-based micelle of an average diameter of 100nm was found to be biocompatible, non-toxic and physically stable in colloidal system up to 15days. It enhanced the in vitro potency of doxorubicin (DOX) in 4T1 breast tumor cells by increasing its uptake, by 3-fold, compared to free DOX. In 4T1 tumor-bearing mice, the tumor growth rate of PD/DOX (2mg/kg DOX equivalent) treated group was significantly delayed and their tumor volume was significantly reduced by 1.5-fold compared to those treated with free DOX. The biodistribution studies indicated that PD/DOX enhanced accumulation of DOX in tumor by 5- and 2-fold higher than free DOX treated mice at 15min and 1h post-administration, respectively. These results suggest that PD micelle is a promising nanocarrier for chemotherapeutic agents.
先前报道的具有支化树状大分子侧基的两亲性嵌段共聚物（PD）已进一步在荷瘤小鼠中进行评估，作为一种潜在的药物载体。这种平均直径为 100nm 的 PD 基胶束在胶体系统中具有生物相容性、无毒和物理稳定性，可稳定 15 天。与游离 DOX 相比，它将 DOX（DOX）的体外效力提高了 3 倍，增加了 DOX 的摄取。在 4T1 荷瘤小鼠中，与游离 DOX 治疗组相比，PD/DOX（2mg/kg DOX 当量）治疗组的肿瘤生长速度明显延迟，肿瘤体积明显减少了 1.5 倍。生物分布研究表明，与游离 DOX 治疗的小鼠相比，PD/DOX 在给药后 15min 和 1h 时，分别将 DOX 在肿瘤中的蓄积增加了 5 倍和 2 倍。这些结果表明 PD 胶束是一种有前途的化疗药物纳米载体。
