Stepwise encapsulation and controlled two-stage release system for cis-Diamminediiodoplatinum.
Stepwise encapsulation and controlled two-stage release system for cis-Diamminediiodoplatinum.
复制标题
顺式二氨二碘铂的逐步封装和受控两阶段释放系统。
DOI：
10.2147/ijn.s61570
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发表时间：
2014
影响因子：
8
通讯作者：
Wu Q
中科院分区：
文献类型：
--
作者：
Chen Y;Li Q;Wu Q
顺式二碘二氨铂（cis-DIDP）是一种具有较高抗癌活性的顺铂类抗癌药物，但其稳定性和价格均低于顺铂。在这项研究中，通过乳化溶剂蒸发法制备了基于微米硬脂酸的顺式DIDP载体系统。顺式DIDP固体脂质纳米粒的最大载药量为22.03%，包封率为97.24%。在37.5°C的磷酸盐缓冲盐水（pH =7.4）中的体外药物释放表现出独特的两阶段过程，这可以证明对患有肿瘤和恶性肿瘤的患者有益。MTT（3-[4，5-dimethylthiazol-2-yl]-2，5-diphenyltetrazolium bromide）法结果表明，负载cis-DIDP的固体脂质纳米粒释放的cis-DIDP比未负载的cis-DIDP具有更好的抑制活性。
cis-Diamminediiodoplatinum (cis-DIDP) is a cisplatin-like anticancer drug with higher anticancer activity, but lower stability and price than cisplatin. In this study, a cis-DIDP carrier system based on micro-sized stearic acid was prepared by an emulsion solvent evaporation method. The maximum drug loading capacity of cis-DIDP-loaded solid lipid nanoparticles was 22.03%, and their encapsulation efficiency was 97.24%. In vitro drug release in phosphate-buffered saline (pH =7.4) at 37.5°C exhibited a unique two-stage process, which could prove beneficial for patients with tumors and malignancies. MTT (3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide) assay results showed that cis-DIDP released from cis-DIDP-loaded solid lipid nanoparticles had better inhibition activity than cis-DIDP that had not been loaded.