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首页> 美国卫生研究院文献>Oncotarget >Oral nano-delivery of anticancer ginsenoside 25-OCH3-PPD a natural inhibitor of the MDM2 oncogene: Nanoparticle preparation characterization in vitro and in vivo anti-prostate cancer activity and mechanisms of action
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Oral nano-delivery of anticancer ginsenoside 25-OCH3-PPD a natural inhibitor of the MDM2 oncogene: Nanoparticle preparation characterization in vitro and in vivo anti-prostate cancer activity and mechanisms of action

机译：人参皂甙25-OCH3-PPD（MDM2癌基因的天然抑制剂）的口服纳米递送：纳米颗粒的制备表征体外和体内抗前列腺癌活性及其作用机制

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The Mouse Double Minute 2 (MDM2) oncogene plays a critical role in cancer development and progression through p53-dependent and p53-independent mechanisms. Both natural and synthetic MDM2 inhibitors have been shown anticancer activity against several human cancers. We have recently identified a novel ginsenoside, 25-OCH3-PPD (GS25), one of the most active anticancer ginsenosides discovered thus far, and have demonstrated its MDM2 inhibition and anticancer activity in various human cancer models, including prostate cancer. However, the oral bioavailability of GS25 is limited, which hampers its further development as an oral anticancer agent. The present study was designed to develop a novel nanoparticle formulation for oral delivery of GS25. After GS25 was successfully encapsulated into PEG-PLGA nanoparticles (GS25NP) and its physicochemical properties were characterized, the efficiency of MDM2 targeting, anticancer efficacy, pharmacokinetics, and safety were evaluated in in vitro and in vivo models of human prostate cancer. Our results indicated that, compared with the unencapsulated GS25, GS25NP demonstrated better MDM2 inhibition, improved oral bioavailability and enhanced in vitro and in vivo activities. In conclusion, the validated nano-formulation for GS25 oral delivery improves its molecular targeting, oral bioavailability and anticancer efficacy, providing a basis for further development of GS25 as a novel agent for cancer therapy and prevention.
机译：小鼠Double Minute 2（MDM2）癌基因通过依赖p53和不依赖p53的机制在癌症的发展和进程中起着至关重要的作用。天然和合成MDM2抑制剂均已显示出对几种人类癌症的抗癌活性。我们最近鉴定了一种新型人参皂甙25-OCH3-PPD（GS25），这是迄今为止发现的最活跃的抗癌人参皂甙之一，并且已在包括前列腺癌在内的各种人类癌症模型中证明了其对MDM2的抑制作用和抗癌活性。但是，GS25的口服生物利用度有限，阻碍了其作为口服抗癌药的进一步发展。本研究旨在开发一种用于口服GS25的新型纳米颗粒制剂。将GS25成功封装到PEG-PLGA纳米颗粒（GS25NP）中并对其理化性质进行表征后，在人前列腺癌的体内和体外模型中评估了MDM2靶向的效率，抗癌功效，药代动力学和安全性。我们的结果表明，与未封装的GS25相比，GS25NP表现出更好的MDM2抑制作用，改善的口服生物利用度并增强了体内和体外活性。总之，经验证的用于GS25口服递送的纳米制剂改善了其分子靶向性，口服生物利用度和抗癌功效，为进一步开发GS25作为癌症治疗和预防的新型药物提供了基础。

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