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目的:研究羧基化多壁碳纳米管负载羟基喜树碱(HCPT)的制备工艺及负载物(HCPT-MWCNTs-COOH)的肠吸收特性。方法:比较球磨法、超声法与振荡法的吸附量差异,选择最优负载法;负载物采用FIR,紫外光谱进行表征,通过HPLC测定其含量;采用离体外翻肠囊模型研究负载物在不同肠段的吸收特性,HPLC测定样品质量浓度,计算吸收速率常数(Ka)。结果:冷冻球磨法负载量最高(12.5 mg.g-1);紫外、红外图谱变化表明碳纳米管负载了HCPT;肠吸收试验表明随HCPT质量浓度上升,肠吸收速率常数呈线性增加;高质量浓度在十二指肠、空肠、回肠、结肠的Ka分别为150.9,92.7,148.9,183.0 ng.cm-2.h-1,在各个肠段的Ka均无显著性差异。结论:负载物中HCPT溶解性增加并保护了内酯环,提高了肠透过速率;在小肠中为被动扩散吸收。
Objective: To study the preparation process of carboxylated multi-walled carbon nanotubes loaded with hydroxycamptothecin (HCPT) and the intestinal absorption characteristics of HCPT-MWCNTs-COOH. Methods: The difference of adsorption between ball mill method, ultrasonic method and oscillatory method was compared, and the optimal loading method was selected. The loaded material was characterized by FIR and UV spectrophotometry, and its content was determined by HPLC. Absorption characteristics of intestinal segments, HPLC determination of sample mass concentration, calculated absorption rate constant (Ka). Results: The highest loading capacity of frozen ball milling (12.5 mg.g-1) was obtained. The change of UV and IR spectra showed that HCPT was loaded on the carbon nanotubes. Intestinal absorption test showed that the intestinal absorption rate constant increased linearly with increasing HCPT concentration. The concentrations of Ka in the duodenum, jejunum, ileum and colon were 150.9, 92.7, 148.9 and 183.0 ng.cm-2.h-1, respectively. There was no significant difference in Ka between the intestinal segments. CONCLUSIONS: HCPT solubility increases and protects the lactone ring in the cargo, increasing intestinal transit rate and passive diffusion in the small intestine.