Abstract

A deliver system based on a PZLL and PAMAM block copolymer (PZLL-D3) with TAT modified on the surface has been developed. It is designed to perform highly efficient nucleus-targeted gene and drug co-delivery. Confocal laser scanning microscopy (CLSM) revealed that more TAT-PZLL-D3 entered the nucleus than does PZLL-D3 alone. The TAT-modified vector serves as a gene and drug co-delivery system to achieve high gene transfection efficiency, high apoptosis and low viability in A549 cells.

Highlights

  • Small cell lung cancer (SCLC) originated from bronchial neuroendocrine cells and belongs to a special type of bronchogenic carcinoma

  • In this study, based on transactivator of transcription (TAT)’s active transport property to the nucleus, we developed a high-efficiency nucleus-targeted co-delivery vector that delivers genes and drugs directly into the nucleus of A549 cells

  • It is possible to solve the problem of drug resistance of SCLC if DOX can be directly transferred into the nucleus by vector

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Summary

Introduction

Small cell lung cancer (SCLC) originated from bronchial neuroendocrine cells and belongs to a special type of bronchogenic carcinoma. Breaking through the barriers of chemotherapy resistance of SCLC patients and improving the effect of chemotherapy is a common concern in the field of treatment at this stage. It can be detected in SCLC tissues and SCLC cell lines cultured in vitro that the high expression of P-glycoprotein. It is well known that TAT peptides, derived from the transactivator of transcription of human immunodeficiency virus type 1 (HIV-1), are the most frequently used cell nucleus-targeting peptides [6] Because it can be recognized by the nuclear pore complex, the carrier modified by Tat can transport all kinds of goods to the nucleus accurately [7,8,9,10,11,12,13].

Materials
Synthesis
Drug loading and release
In vitro DOX transfer efficiency
Apoptosis and MTT assay
Results And Discussion
Conclusion
Full Text
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