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通过X射线光刻技术制备的用于靶向和持续给药系统的载拉帕替尼粉末的可生物降解聚合物微结构的评估。

Evaluation of Lapatinib Powder-Entrapped Biodegradable Polymeric Microstructures Fabricated by X-Ray Lithography for a Targeted and Sustained Drug Delivery System.

作者信息

Jeong Eun-Goo, Yoo Hyung Jung, Song Byeonghwa, Kim Hwang-Phill, Han Sae-Won, Kim Tae-You, Cho Dong-Il Dan

机构信息

Cancer Research Institute, Seoul National University College of Medicine, Seoul 110-799, Korea.

Inter-university Semiconductor Research Center, Automation System Research Institute, School of Electrical Engineering and Computer Science, Seoul National University, Seoul 151-744, Korea.

出版信息

Materials (Basel). 2015 Feb 5;8(2):519-534. doi: 10.3390/ma8020519.

Abstract

An oral medication of a molecular targeted drug, lapatinib, is taken regularly to maintain the drug concentration within the desired therapeutic levels. To alleviate the need for such cumbersome administration schedules in several drugs, advanced drug delivery systems (DDSs), which can provide time-controlled and sustained drug release, have recently received significant attention. A biodegradable synthetic polymer, such as polycaprolactone (PCL), is usually used as a carrier material for DDSs. In this paper, lapatinib powder-entrapped, PCL microstructures were fabricated with a precise X-ray lithography-based method. experiments on HER2 positive-human gastric cancer derived NCI-N87 cells were performed to appraise the drug release characteristics of the fabricated DDSs. The results indicate that after the X-ray lithography process, the lapatinib powder is still working well and show time- and dose- dependent drug release efficiencies. The cell growth inhibition characteristics of one hundred 40-μm sized microstructures were similar to those of a 1 μM lapatinib solution for over 144 h. In conclusion, the developed lapatinib-entrapped PCL microstructures can be used in molecular targeted delivery and sustained release as effective cancer-targeted DDSs.

摘要

一种分子靶向药物拉帕替尼的口服制剂需定期服用,以将药物浓度维持在所需的治疗水平内。为了减轻几种药物这种繁琐给药方案的需求,能够实现时间控制和持续药物释放的先进药物递送系统(DDS)最近受到了广泛关注。一种可生物降解的合成聚合物,如聚己内酯(PCL),通常用作DDS的载体材料。在本文中,采用基于精确X射线光刻的方法制备了包裹拉帕替尼粉末的PCL微结构。对HER2阳性人胃癌来源的NCI-N87细胞进行实验,以评估所制备DDS的药物释放特性。结果表明,经过X射线光刻过程后,拉帕替尼粉末仍能良好发挥作用,并呈现出时间和剂量依赖性的药物释放效率。100个40μm大小的微结构的细胞生长抑制特性与1μM拉帕替尼溶液在144小时以上的特性相似。总之,所开发的包裹拉帕替尼的PCL微结构可作为有效的癌症靶向DDS用于分子靶向递送和持续释放。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6bf8/5455267/7616970e815e/materials-08-00519-g001.jpg

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