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A pH responsive complexation-based drug delivery system for oxaliplatin


A responsive drug delivery system (DDS) for oxaliplatin (OX) has been designed with a view to overcoming several common drawbacks associated with this widely used anticancer agent, including fast degradation/deactivation in the blood stream, lack of tumor selectivity, and low bioavailability. The present approach is based on the direct host‒guest encapsulation of OX by a pH-responsive receptor, carboxylatopillar[6]arene (CP6A). The binding affinities of CP6A for OX were found to be pH-sensitive at biologically relevant pH. For example, the association constant (Ka) at pH 7.4 [Ka = (1.02 ± 0.05) × 104 M–1] is 24 times larger than that at pH 5.4 [Ka = (4.21 ± 0.06) × 102 M–1]. Encapsulation of OX within the CP6A cavity did not affect its in vitro cytotoxicity as inferred from comparison studies carried out in several cancer cells (e.g., the HepG-2, MCF-7, and A549 cell lines). On the other hand, complexation by CP6A serves to increase the inherent stability of OX in plasma by 2.8-fold over a 24 h incubation period. The formation of a CP6A⊃OX host–guest complex served to enhance in a statistically significant way the ability of OX to inhibit the regrowth of sarcoma 180 (S180) tumors in Kunming (KM) mice xenografts. The improved anticancer activity observed in vivo for CP6A⊃OX is attributed to the combined effects of enhanced stability of the host–guest complex and the pH-responsive release of OX. Specifically, it is proposed that OX is protected as the result of complex formation and then released effectively in the acidic tumor environment.

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Publication details

The article was received on 31 Mar 2017, accepted on 18 Apr 2017 and first published on 19 Apr 2017

Article type: Edge Article
DOI: 10.1039/C7SC01438D
Citation: Chem. Sci., 2017, Accepted Manuscript
  • Open access: Creative Commons BY-NC license
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    A pH responsive complexation-based drug delivery system for oxaliplatin

    B. Li, Z. Meng, Q. Li, X. Huang, Z. Kang, H. Dong, J. Chen, J. Sun, Y. dong, J. Li, X. Jia, J. L. Sessler, Q. Meng and C. Li, Chem. Sci., 2017, Accepted Manuscript , DOI: 10.1039/C7SC01438D

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