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首页> 外文期刊>The Open Drug Delivery Journal >In Vitro Evaluation of the Activity of Gemcitabine-Loaded Pegylated Unilamellar Liposomes Against Papillary Thyroid Cancer Cells
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In Vitro Evaluation of the Activity of Gemcitabine-Loaded Pegylated Unilamellar Liposomes Against Papillary Thyroid Cancer Cells

机译：吉西他滨负载的聚乙二醇化单层脂质体对乳头状甲状腺癌细胞的活性的体外评估

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摘要

Papillary carcinoma is the most common form of malignant thyroid tumor. At present, a subset of these tumors are poorly responsive to the current treatment. Gemcitabine is a pyrimidine analog active against different types of solid tumors, but its use is limited by its short half-life. To improve the therapeutic effectiveness of this drug, gemcitabine-loaded unilamellar pegylated liposomes were prepared and investigated against two human papillary thyroid carcinoma cell lines, i.e. TPC-1 and B-CPAP cells. The pH gradient drug encapsulation followed by the membrane extrusion technique were used to achieve unilamellar liposomes characterized by a mean size of ~200 nm, a polydispersity index of 0.02 and a zeta potential of -1.7 mV. The gemcitabine was released from liposomes following a biphasic profile. The liposomal encapsulated gemcitabine showed an increased cytotoxic activity compared to the free drug against both thyroid carcinoma cell lines, as a consequence of the better drug internalization favored by the vesicular device. These findings demonstrate the advantage of channeling gemcitabine by liposomes suggesting a promising role for such a pharmaceutical formulation in the treatment of refractory papillary thyroid carcinoma.
机译：乳头状癌是甲状腺恶性肿瘤的最常见形式。目前，这些肿瘤的一部分对当前的治疗反应较差。吉西他滨是一种对不同类型实体瘤具有活性的嘧啶类似物，但其使用受到半衰期短的限制。为了提高该药物的治疗效果，制备了装载吉西他滨的单层聚乙二醇化脂质体，并针对两种人乳头状甲状腺癌细胞系TPC-1和B-CPAP细胞进行了研究。使用pH梯度药物封装和随后的膜挤出技术来获得单层脂质体，其特征是平均粒径约为200 nm，多分散指数为0.02，ζ电位为-1.7 mV。吉西他滨以两相曲线从脂质体释放。与游离药物相比，脂质体包封的吉西他滨对两种甲状腺癌细胞系均表现出更高的细胞毒活性，这是由于囊泡装置有利于更好的药物内在化。这些发现证明了通过脂质体引导吉西他滨的优点，表明这种药物制剂在难治性甲状腺乳头状癌的治疗中具有有希望的作用。

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