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

机译:靶向和持续药物输送系统的X射线光刻技术制备的包裹有Lapatinib粉末的生物可降解聚合物微结构的评价

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摘要

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. In vitro experiments on HER2 positive-human gastric cancer derived NCI-N87 cells were performed to appraise the drug release characteristics of the fabricated DDSs. The in vitro 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.
机译:定期服用分子靶向药物拉帕替尼的口服药物,以将药物浓度维持在所需的治疗水平内。为了减轻几种药物中此类繁琐的给药计划的需要,可以提供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。可生物降解的合成聚合物,例如聚己内酯(PCL),通常用作DDS的载体材料。在本文中,采用精确的X射线光刻技术制备了包裹有拉帕替尼粉末的PCL微结构。对HER2阳性的人胃癌衍生的NCI-N87细胞进行了体外实验,以评估所制备DDS的药物释放特性。体外结果表明,在X射线光刻工艺之后,拉帕替尼粉末仍能正常工作,并显示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拉帕替尼溶液持续144 h的相似。总之,已开发的拉帕替尼包裹的PCL微结构可作为有效的针对癌症的DDS用于分子靶向递送和持续释放。

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