Encapsulation of cisplatin in a pegylated calcium phosphate nanoparticle (CPNP) for enhanced cytotoxicity to cancerous cells

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• 作者：Yang Ding^a ; Kang Zhai^a ; Pei Pei^a ; Yue Lin^b ; Yinchu Ma^a ; Huixia Zhu^a ; Mingfeng Shao^c ; ^{sssmmmfff@126.com} ; Xianzhu Yang^a ; ^{yangxz@hfut.edu.cn} ; Wei Tao^a ; ^{taow@hfut.edu.cn}
• 关键词：Calcium phosphate nanoparticle (CPNP) ; Cisplatin ; Drug delivery ; Encapsulation ; Premature release ; Cisplatin resistance
• 刊名：Journal of Colloid and Interface Science
• 出版年：2017
• 出版时间：1 May 2017
• 年：2017
• 卷：493
• 期：Complete
• 页码：181-189
• 全文大小：1714 K
• 卷排序：493

文摘

Exchange of the chloride ion (Cl−) ligands of cisplatin with carboxylates is widely used in fabricating cisplatin loaded nanoparticles for improved cancer therapy. However, the dynamic exchange may cause premature cisplatin release and even disintegration of the nanoparticles in Cl−-containing medium such as in plasma. Molecules bearing carboxylates are capable of mediating the mineralization process of calcium phosphate; therefore, it is possible to overcome the disadvantage by sequestering cisplatin in a calcium phosphate nanoparticle (CPNP).ExperimentsWith the hypothesis, precipitation reaction of calcium nitrate and disodium hydrogen phosphate was performed in a solution of poly(ethylene glycol)-poly(acrylic acid) block copolymers with their carboxylates partly conjugated with cisplatin. Then, structure, physicochemical properties, and bioactivity of the product were carefully investigated with multiple characterization methods.FindingsIt was revealed a pegylated, cisplatin encapsulated CPNP was prepared; and with appropriate mole ratio of cisplatin to carboxylates, the nanoparticle encapsulated cisplatin efficiently (>90%), was stable and almost entirely prevented the cisplatin release in Cl−-containing medium at pH 7.4 but released them in an acidic condition, and showed moderately and greatly enhanced cytotoxicities to the lung cancer cell line A549 and its cisplatin resistance form A549R respectively in comparison with the free cisplatin.