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首页> 外文期刊>Journal of dermatological science >Effect of liposome encapsulation of tea catechins on their accumulation in basal cell carcinomas.
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Effect of liposome encapsulation of tea catechins on their accumulation in basal cell carcinomas.

机译:茶儿茶素脂质体包封对其在基底细胞癌中积累的影响。

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BACKGROUND: (-)-Epigallocatechin gallate (EGCG), the main active polyphenol in green tea, is associated with antioxidant and anticancer activities. OBJECTIVE: The aim of this study was to evaluate the feasibility of using liposomes for intratumor distribution of EGCG and its derivative, (+)-catechin. METHOD: Liposomes containing egg phosphatidylcholine, cholesterol, or anionic surfactant in the presence of 15% ethanol were prepared. The physicochemical characteristics including vesicle size, zeta potential, drug entrapment, and drug release of liposomal formulations were determined. The liposomes containing EGCG were injected into basal cell carcinomas (BCCs), melanomas, and colon tumors to examine the tumor uptake of the drug. Liposomes were also incubated with a given number of BCC cells, and the cell viability was estimated. RESULT: Almost no drug molecules were observed when free EGCG was administered to BCCs. EGCG encapsulated in liposomes with deoxycholic acid (DA) and ethanol increased drug deposition by 20-fold as compared to the free form. The larger vesicle size of this formulation was suggested to be the predominant factor governing this enhancement. The liposomes without ethanol showed low or negligible enhancement on EGCG uptake in BCCs. Liposomes protected EGCG from degradation, resulting in the induction of greater BCC death compared to that by free EGCG at lower concentrations. CONCLUSION: These results suggest that the intratumor injection of liposomes containing EGCG with moderate modification is an effective approach for increasing EGCG deposition in BCCs.
机译:背景:(-)-表没食子儿茶素没食子酸酯(EGCG)是绿茶中的主要活性多酚,与抗氧化剂和抗癌活性有关。目的:本研究的目的是评估使用脂质体进行EGCG及其衍生物(+)-儿茶素在肿瘤内分布的可行性。方法:在15%乙醇存在下,制备含有卵磷脂,胆甾醇或阴离子表面活性剂的脂质体。确定了脂质体制剂的物理化学特征,包括囊泡大小,ζ电位,药物截留和药物释放。将含有EGCG的脂质体注射到基底细胞癌(BCC),黑色素瘤和结肠肿瘤中,以检查药物对肿瘤的吸收情况。脂质体也与给定数量的BCC细胞一起孵育,并评估了细胞活力。结果:将游离EGCG应用于BCC时几乎未观察到药物分子。与游离形式相比,用脱氧胆酸(DA)和乙醇包裹在脂质体中的EGCG使药物沉积增加了20倍。提示该制剂较大的囊泡大小是控制这种增强作用的主要因素。没有乙醇的脂质体对BCC中EGCG摄取的增强作用很小或可忽略不计。与较低浓度的游离EGCG相比,脂质体可保护EGCG免受降解,从而导致更大的BCC死亡。结论:这些结果表明,在肿瘤内注射含有适度修饰的EGCG的脂质体是增加BCC中EGCG沉积的有效方法。

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