摘要
主要研究吸附安丝菌素P3(AP3)的纳米炭(CNP)混悬注射液(AP3-CNP)的粒径、吸附率、体外释放等相关指标,以及淋巴示踪性和体外抗肿瘤活性。采用超滤离心法分离AP3-CNP中游离的AP3、透析法测定体外释放度、HPLC法检测药物浓度并计算吸附率,CCK8法检测AP3-CNP对人源肿瘤细胞株HepG-2、Bel-7402、HeLa、SiHa、A549和SKOV3的抑制作用。结果表明吸附AP3前后,纳米炭的粒径、淋巴示踪性未发生明显改变;随AP3浓度的增加,吸附率呈下降趋势。体外释放结果显示,AP3-CNP相较于AP3有较明显的缓释作用。AP3-CNP对所选的人源肿瘤细胞的抑制作用均较好,IC_(50)在1 ng/ml左右;除SiHa细胞外,AP3-CNP与AP3对其余5种人源肿瘤细胞的抑制率无显著差异(P>0.05),表明AP3-CNP中的AP3能解离下来并抑制肿瘤细胞生长。
The change of particle size, adsorption rate and in vitro release of the carbon nanoparticles （CNP） suspension injection after adsorption of ansamitocin P3 （AP3） were investigated. Moreover, the tests of lymphatic tracing and antitumor activity of the final product AP3-CNP were carried out. An ultrafiltration centrifugal analysis was applied to separate free AP3 from AP3-CNR The dialysis assay was used for the quantification of drug release. An HPLC method was adopted to detect the drug concentration. The inhibition effects of AP3-CNP on human tumor cell lines HepG-2, Bel- 7402, HeLa, SiHa, A549 and SKOV3 were measured by CCK8 assay. The results showed that there were no significant changes in particle size and lymphatic tracing of the CNP before and after adsorption. The adsorption rate was decreased with the increasing of the concentration ofAP3. Compared with the AP3, AP3-CNP showed a significant sustained-release characteristics. The IC50 values of AP3-CNP against above six tumor cell lines were about 1 ng/ml, showing a good inhibition effect. There were no significant differences between AP3 and AP3-CNP in inhibition rates except SiHa cells. These results indicated that AP3 could desorb from the AP3-CNP and inhibit the growth of the tumor cell lines.
作者
辛倩
唐小海
冉茂盛
张雪梅
廖春美
XIN Qian;TANG Xiaohai;RAN Maosheng;ZHANG Xuemei;LIAO Chunmei(China Chongqing Lummy Pharmaceutical Co.. Ltd., Chongqing 401336;College of Life Science, Sichuan Normal University, Chengdu 610000)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2018年第4期491-497,共7页
Chinese Journal of Pharmaceuticals
基金
国家科技重大专项"重大新药创制"(2012ZX091021041和2012ZX09102101-015)
关键词
纳米炭混悬注射液
安丝菌素P3
吸附
解吸附
淋巴示踪
抗肿瘤活性
carbon nanoparticles suspension injection
ansamitocin P3
adsorption
desorption
lymphatic tracing
antitumor activity
