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首页> 外文期刊>Drug Design, Development and Therapy >Enhancement of Antitumor Efficacy of Paclitaxel-Loaded PEGylated Liposomes by N,N-Dimethyl Tertiary Amino Moiety in Pancreatic Cancer
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Enhancement of Antitumor Efficacy of Paclitaxel-Loaded PEGylated Liposomes by N,N-Dimethyl Tertiary Amino Moiety in Pancreatic Cancer

机译：胰腺癌中N，N-二甲基叔氨基部分在胰腺癌中提高紫杉醇加载的聚乙二醇化脂质体的抗肿瘤效果

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Introduction: Pancreatic cancer, or pancreatic duct adenocarcinoma (PDAC), remains one of the most lethal cancers and features insidious onset, highly aggressive behavior and early distant metastasis. The dense fibrotic stroma surrounding tumor cells is thought to be a shield to resist the permeation of chemotherapy drugs in the treatment of PDAC. Thus, we synthesized a pancreas-targeting paclitaxel-loaded PEGylated liposome and investigated its antitumor efficacy in the patient-derived orthotopic xenograft (PDOX) nude mouse models of PDAC. Methods: The PTX-loaded PEGylated liposomes were prepared by film dispersion-ultrasonic method and modified by an N,N-dimethyl tertiary amino residue. Morphology characteristics of the PTX-loaded liposomes were observed by transmission electron microscope (TEM). The PDOX models of PDAC were established by orthotopic implantation and imaged by a micro positron emission tomography/computed tomography (PET/CT) imaging system. The in vivo distribution and antitumor study were then carried out to observe the pancreas-targeting accumulation and the antitumor efficacy of the proposed PTX liposomes. Results: PTX loaded well into both modified (PTX-Lip2N) and unmodified (PTX-Lip) PEGylated liposomes with spherical shapes and suitable parameters for the endocytosis process. The PDOX nude mouse models were successfully created in which high 18F-FDG intaking regions were observed by micro-PET/CT. In addition to higher cellular uptakes of PTX-Lip2N by the BxPC-3 cells, the proposed nanoparticle had a notable penetrating ability towards PDAC tumor tissues, and consequently, the antitumor ability of PTX-Lip2N was significantly superior to the unmodified PTX-Lip in vivo PDOX models and even more effective than nab-PTX in restraining tumor growth. Conclusion: The modified pancreas-targeting PTX-loaded PEGylated liposomes provide a promising platform for the treatment of pancreatic cancer.
机译：简介：胰腺癌或胰腺导管腺癌（PDAC）仍然是最致命的癌症之一，具有阴险发作，高度侵略性的行为和早期的转移。围绕肿瘤细胞的致密纤维化基质被认为是抵抗PDAC治疗中化疗药物渗透的盾牌。因此，我们合成了一种胰腺靶向紫杉醇负载的聚乙二醇化脂质体，并在患者衍生的原位异种移植物（PDOX）裸鼠裸鼠模型中研究其抗肿瘤功效。方法：通过薄膜分散超声波方法制备PTX加载的聚乙二醇化脂质体，并通过N，N-二甲基叔氨基残基改性。通过透射电子显微镜（TEM）观察PTX负载脂质体的形态特征。 PDAC的PDOX模型由原位植入和通过微正电子发射断层扫描/计算机断层扫描（PET / CT）成像系统成像。然后进行体内分布和抗肿瘤研究以观察所提出的PTX脂质体的胰腺靶向积累和抗肿瘤效果。结果：PTX加入到改性（PTX-LIP2N）和未改性（PTX-唇）Pegymated脂质体中，具有球形形状和用于内吞作用的合适参数。成功地创建了PDOX裸鼠模型，其中通过微pET / CT观察到高18F-FDG接种区域。除了通过BxPC-3细胞进行PTX-LIP2N的较高细胞摄取之外，所提出的纳米颗粒对PDAC肿瘤组织具有显着的渗透能力，因此，PTX-LIP2N的抗肿瘤能力显着优于未修饰的PTX - 唇体内PDOX模型比抑制肿瘤生长的NAB-PTX更有效。结论：改性胰腺靶向PTX的PEG化脂质体提供了一种用于治疗胰腺癌的有希望的平台。

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