Stepwise encapsulation and controlled two-stage release system for cis-Diamminediiodoplatinum

Yun Chen,^1,* Qian Li,^1,2,* Qingsheng Wu<sup>1

1</sup>Department of Chemistry, Key Laboratory of Yangtze River Water Environment, Ministry of Education, Tongji University, Shanghai; ²Shanghai Institute of Quality Inspection and Technical Research, Shanghai, People’s Republic of China

^*These authors contributed equally to this work

Abstract: 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.

Keywords: stearic acid, emulsion solvent evaporation method, drug delivery, cis-DIDP, in vitro

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