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载紫杉醇、叶酸靶向和 TAT 肽偶联的聚合物脂质体:体外和体内评价。

Paclitaxel-loaded, folic-acid-targeted and TAT-peptide-conjugated polymeric liposomes: in vitro and in vivo evaluation.

机构信息

The Key Laboratory of Breast Cancer Prevention and Therapy Ministry of Education, Tianjin Medical University Cancer Institute and Hospital, Tianjin 300060, China.

出版信息

Pharm Res. 2010 Sep;27(9):1914-26. doi: 10.1007/s11095-010-0196-5. Epub 2010 Jun 26.

Abstract

OBJECTIVE

Folic acid and TAT peptide were conjugated on the octadecyl-quaternized, lysine-modified chitosan-cholesterol polymeric liposomes (FA-TATp-PLs) to investigate their potential feasibility for tumor-targeted drug delivery.

METHODS

FA-TATp-PLs encapsulating paclitaxel or calcein were synthesized and characterized. Cellular uptake of PLs, FA-PLs, TATp-PLs and FA-TATp-PLs was studied by confocal laser scanning microscopy (CLSM) in folate receptor (FR)-positive KB nasopharyngeal epidermal carcinoma cells and FR-deficient A549 lung cancer cells. In vitro and in vivo antitumor activity of paclitaxel-loaded FA-TATp-PLs were also evaluated in KB and A549 cells as well as in a murine KB xenograft model.

RESULTS

Our data showed that 80% paclitaxel released from FA-TATp-PLs in 2 weeks. Different from other various PLs, CLSM analyses showed that FA-TATp-PLs had a significantly high efficient intracellular uptake in both KB and A549 cells. These data revealed the targeting effects of folate decoration, the transmembrane ability of TAT peptide as well as a synergistic interaction between them. In addition, paclitaxel-loaded FA-TATp-PLs exhibited a more superior antitumor effect in vitro and in vivo as compared to that with Taxol.

CONCLUSIONS

FA-TATp-PLs possessing both targeting effect and transmembrane ability may serve as a promising carrier for the intracellular delivery of therapeutic agents.

摘要

目的

将叶酸和 TAT 肽偶联到十八烷基季铵化、赖氨酸修饰的壳聚糖-胆固醇聚合物脂质体(FA-TATp-PLs)上,以研究其用于肿瘤靶向药物传递的潜在可行性。

方法

合成并表征了包载紫杉醇或钙黄绿素的 FA-TATp-PLs。通过共聚焦激光扫描显微镜(CLSM)研究了 FA-TATp-PLs、FA-PLs、TATp-PLs 和 FA-TATp-PLs 在叶酸受体(FR)阳性 KB 鼻咽表皮癌细胞和 FR 缺失的 A549 肺癌细胞中的细胞摄取情况。还在 KB 和 A549 细胞以及小鼠 KB 异种移植模型中评估了载紫杉醇的 FA-TATp-PLs 的体外和体内抗肿瘤活性。

结果

我们的数据表明,FA-TATp-PLs 在 2 周内释放了 80%的紫杉醇。与其他各种 PLs 不同,CLSM 分析表明,FA-TATp-PLs 在 KB 和 A549 细胞中均具有高效的细胞内摄取。这些数据揭示了叶酸修饰的靶向作用、TAT 肽的跨膜能力以及它们之间的协同相互作用。此外,与 Taxol 相比,载紫杉醇的 FA-TATp-PLs 在体外和体内均表现出更优异的抗肿瘤效果。

结论

具有靶向作用和跨膜能力的 FA-TATp-PLs 可能成为治疗剂细胞内递药的有前途的载体。

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