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中国生物工程杂志

CHINA BIOTECHNOLOGY
中国生物工程杂志
中国生物工程杂志  2018, Vol. 38 Issue (9): 65-73    DOI: 10.13523/j.cb.20180910
综述     
口服抗癌药物纳米载体的研究进展 *
潘晓倩1,熊向源1,2,**(),龚妍春2,李资玲2,李玉萍2
1 江西科技师范大学药学院 南昌 330013
2 江西科技师范大学生命科学学院 南昌 330013
Advances in Research of Oral Anticancer Drug Nanocarrier
Xiao-qian PAN1,Xiang-yuan XIONG1,2,**(),Yan-chun GONG2,Zi-ling LI2,Yu-ping LI2
1 School of Pharmaceutical Sciences, Jiangxi Science and Technology Normal University,Nanchang 330013,China
2 School of Life Sciences, Jiangxi Science and Technology Normal University,Nanchang 330013,China
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摘要：

实现抗癌药物的口服给药,对于癌症的化疗及患者的生活会有很大的方便性。但大多数抗癌药物直接口服给药时,由于受到胃肠道的屏蔽作用导致生物利用度降低,所以寻找一种有效的药物载体,对于实现抗癌药物的口服给药是至关重要的。纳米技术的出现,带动了纳米药物载体的发展,使得抗癌药物的口服给药有了很大的突破。对不同材料,主要包括合成高分子材料、天然高分子材料作为口服抗癌药物载体的特点以及体内体外的研究结果进行回顾和综述。
关键词： 药物载体;  口服给药;  高分子共聚物;  纳米粒子    
Abstract:

Cancer chemotherapy and the patient’s life will be very convenient if oral administration of anti-cancer drugs can be achieved. For most anti-cancer drugs, their bioavailability and treatment efficiency will be decreased by oral administration, due to the gastrointestinal barrier. So it is important to find an effective drug carrier for oral administration of anticancer drugs. The emergence of nanotechnology, led to the development of nano-drugs. Therefor a great breakthrough has been achieved for oral administration of anti-cancer drugs. The research progress of different materials, including synthetic polymer materials, natural macromolecular materials and liposomes as oral anticancer drug carriers, including their in vivo or in vitro studies has been reviewed.
Key words: Drug carriers    Oral administration    Anticancer drugs    Nano particles
收稿日期: 2018-04-22 出版日期: 2018-10-12
基金资助: * 国家自然科学基金(21664007);江西省主要学科学术和技术带头人培养计划(20153BCB22009);江西省高等学校科技落地计划(KJLD13071)
通讯作者: 熊向源     E-mail: xyxiong@gmail.com
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潘晓倩
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引用本文:

潘晓倩,熊向源,龚妍春,李资玲,李玉萍. 口服抗癌药物纳米载体的研究进展 *[J]. 中国生物工程杂志, 2018, 38(9): 65-73.

Xiao-qian PAN,Xiang-yuan XIONG,Yan-chun GONG,Zi-ling LI,Yu-ping LI. Advances in Research of Oral Anticancer Drug Nanocarrier. China Biotechnology, 2018, 38(9): 65-73.

链接本文:

https://manu60.magtech.com.cn/biotech/CN/10.13523/j.cb.20180910    或    https://manu60.magtech.com.cn/biotech/CN/Y2018/V38/I9/65

图1  纳米粒子在上皮细胞的摄取[14]
Material Modified group Modification purpose Model drug Key finding Ref
PLGA TPGS/PVA 减小纳米粒子的粒径,提高药物包埋 紫杉醇 TPGS对聚合物的修饰有利于提高细胞对纳米粒子的吸收 [17-18]
TPGS 改善药物在剂型中的溶解性 紫衫醇 为药物的口服输送提供了实验依据 [9,19-20]
FA 增加纳米载体的靶向性 紫杉醇 叶酸功能化的纳米粒子具有提高药物的口服生物利用度的潜力 [21]
PLA 无 三苯氧胺 该药物的纳米剂型能够降低药物的毒副作用 [22]
TPGS/MMT 提高药物的包埋,增加纳米粒子的黏膜黏附性 紫杉醇 TPGS/MMT对聚合物的修饰作为药物的纳米载体,提高了药物在体内的生物利用度 [4,23]
PEG 提高PLA纳米粒子在胃肠道中的稳定性 放射性标记的破伤风类毒素 增加了纳米粒子在肠道中的吸收,提高了药物的血浆浓度 [24]
Material Modified group Modification purpose Model drug Key finding Ref
PCL共聚物 DDAB 增加纳米粒子在细胞表面的保留时间 多烯紫杉醇 修饰后的纳米载体提高了药物的摄取率,以及细胞毒性 [25]
聚酸酐 环糊精 提高药物的包埋,调节药物从纳米载体中的释放 喜树碱/紫杉醇 通过环糊精对纳米载体的修饰,在一定程度上可以提高药物在体内的口服生物利用度 [16,26]
PEG 抑制P-gp及细胞色素P450的活性 紫杉醇 改善了药物载体在体内的生物黏附性 [27-28]
壳聚糖 单油酸甘油酯 提高药物载体在体内的生物黏附性 紫杉醇 使PTX在低剂量下达到治疗浓度,减少药物的不良作用 [29]
羧甲基壳聚糖 增加上皮细胞的通透性,维持纳米粒子在胃肠道中的稳定性 盐酸阿霉素 证明了该剂型是盐酸阿霉素,一种安全有效的口服给药载体 [30]
硫酸基,辛基 抑制P-gp的外排 紫杉醇 潜在的能够增强P-gp底物口服吸收 [31-32]
透明质酸 壳聚糖 能够保护HA-PTX的脂键不被破坏 紫杉醇 提高药物的靶向性,保护药物的稳定性 [33]
磷脂双分子 无 阿霉素 该剂型能够提高药物在肿瘤细胞中的摄取 [34]
N-三甲基壳聚糖氯化物 增加粒子的稳定性及在肠道中的吸收 姜黄素 较小粒径的脂质体有利于提高药物的血浆浓度 [35]
表1  不同材料作为药物口服输送载体
图2  Docetaxel-loaded M-PLGA-TPGS 纳米粒子制备示意图 (a)docetaxel-loaded M-PLGA-TPGS 纳米粒子DLS粒径分布 (b)docetaxel-loaded M-PLGA-TPGS 纳米粒子的FESEM图像 (c)docetaxel-loaded M-PLGA-TPGS 纳米粒子的TEM图像(d)[18]
图3  NOSC胶束对PTX口服吸收的影响[31]
图4  CS/HA-PTX CNPs的制备与应用原理[33]
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