冬凌草甲素卟啉壳聚糖微球的制备及体外光动力抗肿瘤活性研究

Preparation and Photocytotoxicity in vitro of Oridonin-porphyrinchitosan Microspheres

基于光-化联合抗肿瘤的目的,通过共价偶联将5-对(6-溴已氨基苯基)-10,15,20-三苯基卟啉(BHP)引入壳聚糖侧基制备复合物,卟啉枝接率平均达30.80%;采用乳化交联法制备了冬凌草甲素卟啉壳聚糖微球,经高效液相色谱(HPLC)测得微球载药量为12.41%,包封率为8.72%,48 h体外释放量达81.74%;采用噻唑蓝(MTT)法考察合成的系列化合物对人乳腺癌细胞MCF-7的光毒性.实验结果表明:浓度为25,50和100μmol/m L的冬凌草甲素光敏微球光照30min后对MCF-7细胞的光动力杀伤率的平均值分别达(31.55±1.70)%,(71.03±0.76)%和(82.74±0.38)%,光动力杀伤效果显著.

A emulsion crosslinking method to prepare oridonin-porphyrin-chitosan microspheres with oridonin and 5-p-（6- bromohexylaminophenyl）-10,15,20-triphenylporphyrin-chitosan （BHP-CS） is reported, which in turn was synthesized from 5-p-（6-bromo- hexylaminophenyl）-10,15,20-triphenylporphyrin （BHP） and chitosan. The porphyrin grafting rate of BHP-CS reached 30.80% on average, the drug loading rate and entrapment rate of the prepared microspheres reached 12.41% and 8.72% measured by HPLC, and the accumulated release rate was 81.74% in 48 h in vitro. The thiazolyl blue tetrazolium bro- mide （MTT） method was used to evaluate the photocytotoxicities of these derivatives against MCF-7 cells. The results re- vealed that oridonin-porphyrin-chitosan microspheres showed high photocytotoxicity in concentrations of 25, 50 and 100 μmol/mL against MCF-7 cells, and the inhibit ratio of MCF-7 cells under light irradiation for 30 rain were （31.55±1.70）%, （71.03 ± 0.76）% and （82.74 ± 0.38）%, respectively.