Tripeptide-Stabilized Oil-in-Water Nanoemulsion of an Oleic Acids–Platinum(II) Conjugate as an Anticancer Nanomedicine,Bioconjugate Chemistry

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Tripeptide-Stabilized Oil-in-Water Nanoemulsion of an Oleic Acids–Platinum(II) Conjugate as an Anticancer Nanomedicine
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2018-07-12 00:00:00 , DOI: 10.1021/acs.bioconjchem.8b00409
Sylwia A. Dragulska ₁ , Ying Chen , Marek T. Wlodarczyk _{1,

2} , Mina Poursharifi _{1,

2} , Peter Dottino , Rein V. Ulijn _{2,

3,

4} , John A. Martignetti ₅ , Aneta J. Mieszawska _{1,

2}

Affiliation

We report a nanoemulsion (NE) which is stabilized by self-assembling tripeptide lysine-tyrosine-phenylalanine (KYF) and encapsulates an oleic acids–platinum conjugate formed using simple Pt (II) coordination chemistry. The KYF-Pt-NE is evaluated both in cultured ovarian cancer cells and in an in vivo preclinical cancer model and shows pH dependent Pt (II) release, which is low at physiological pH and enhanced at tumoral pH. The biological activity of KYF-Pt-NE, evaluated in multiple ovarian cancer cell lines, is significantly higher when compared to the analogous Pt (II) complex used in the clinic. Concurrently, the KYF-Pt-NE platform shows good compatibility with the immune system. Preliminary in vivo testing of KYF-Pt-NE with tumor bearing mice indicates efficient Pt (II) delivery to the tumor. Together, these results demonstrate the potential of peptide-stabilized nanoemulsions, specifically KYF-Pt-NE as an effective nanomedicine against cancer.

中文翻译：

三肽稳定的油酸-铂（II）缀合物水包油纳米乳剂作为抗癌纳米药物。

我们报告了一种纳米乳液（NE），其通过三肽赖氨酸-酪氨酸-苯丙氨酸的自组装而稳定，并封装了使用简单的Pt（II）配位化学形成的油酸-铂共轭物。在培养的卵巢癌细胞和体内临床前癌症模型中均对KYF-Pt-NE进行了评估，并显示了pH依赖性Pt（II）的释放，该释放在生理pH值较低而在肿瘤pH值较高。与临床中使用的类似的Pt（II）复合物相比，在多种卵巢癌细胞系中评估的KYF-Pt-NE的生物学活性明显更高。同时，KYF-Pt-NE平台与免疫系统显示出良好的兼容性。用荷瘤小鼠对KYF-Pt-NE进行的初步体内测试表明，Pt（II）可以有效地递送至肿瘤。一起，

更新日期：2018-07-12

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