羧甲基壳聚糖-油酸聚合物的载药性能及抗肿瘤活性研究

Drug-Loading Performance and Antitumor Activity of Carboxymethyl Chitosan-Oleic Acid Polymer

以自制的羧甲基壳聚糖-油酸聚合物(CMCS-OA)为载体,采用透析法对盐酸阿霉素(DOX)进行包载,载药聚合物(DOX-CMCS-OA)的载药量和包封率分别达到30.28%和65.83%。体外释药实验表明,DOX-CMCS-OA在pH值为5.0和7.4下1660 min时累积释药率分别为262.29%和232.64%,偏酸性环境下释药效果更好,具有一定的pH值敏感性。细胞毒性实验表明,DOX-CMCS-OA对SGC-7901胃癌细胞和SK-MES-1肺癌细胞均具有较好的抑制作用且比DOX的毒性更低。细胞摄取实验表明,DOX-CMCS-OA具有较好的药物控释性能。CMCS-OA对DOX的包载能力较好,具有一定的缓释、长效的抗肿瘤作用。

By using self-made carboxymethyl chitosan-oleic acid(CMCS-OA)polymer as a carrier,Doxorubicin hydrochloride(DOX)was loaded by a dialysis method.The drug loading and encapsulation rate of drug-loading polymer DOX-CMCS-OA can reach 30.28%and 65.83%,respectively.The in vitro drug release experiments show that the cumulative drug release rate of the DOX-CMCS-OA are 262.29%and 232.64%at the pH values of 5.0 and 7.4 for 1660 min,respectively,indicating that the drug release effect is better under an acidic environment,and the DOX-CMCS-OA has a certain pH value sensitivity.The cytotoxicity experiments show that the DOX-CMCS-OA has a better inhibitory effect on SGC-7901 gastric cancer cells and SK-MES-1 lung cancer cells,and has less toxicity than DOX.The cellular uptake experiments show that the DOX-CMCS-OA has a better controlled release property.In conclusion,the CMCS-OA has a good encapsulation ability for DOX and has a certain sustained-release and long-term antitumor effect.