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OBJECTIVE To prepare triptolide lignoceric acid ester liposome and characterize it,investigate its therapeutic effect on pancreatic cancer. METHODS Firstly, triptolide lignoceric acid ester liposome was prepared by thin film dispersion method,the single factor test and Box-Behnken response surface method were used to optimize the formulation process. Secondly, liposome form was observed using transmission electron microscope, the particle size, the polydispersity index and Zeta potential of the liposome was observed using Malvin particle size instrument and the initial stability of the TPL-LA-lip was investigated. Finally, the anti-pancreatic activity of TPL-LA-lip in vivo was evaluated by Panc 02 tumor bearing mouse model. RESULTS Triptolide lignoceric acid ester liposome was prepared successfully, and the optimal process and prescription were determined. The liposome was prepared by thin film water method, phospholipid was selected PC-98T, the ratio of drug to phospholipid was 1∶10, cholesterol to phospholipid ratio was 1∶10, DSPE-mPEG2000 was 0.05%, and the preparation temperature was 55 ℃. The liposome was spherical in appearance, the encapsulation rate (EE%) was (98.30±0.32)%, the loading efficiency rate(LE%) was (8.33±0.24)%, the particle size was (105.60±0.01) nm, the Zeta potential was (-34.54±0.17) mV, and had good stability. In PBS medium containing 30% ethanol, the cumulative release of prodrug liposome was 40.35% at 24 h, and it showed good sustained-release effect. At the end of the pharmacokinetics experiment on day 15, the tumor bodies of mice in control, blank lip, TP solution, minnelide and TPL-LA-lip were (849.45±53.72)(880.45±121.45)(602.09±56.80) (265.67±23.12) (237.67±38.30) mm3, respectively. The change rates of body weight were 18.12%, 21.29%, -3.62%, 13.06% and 19.97%, respectively. Compared with the control and TP groups, the TPL-LA-lip group tumor volume was significantly different (P<0.05). In addition, there was no significant difference in body weight between the TPL-LA lip group and the negative control group, while the body weight and organs indexs of the mice treated with TP solution were significantly reduced, indicating the good biological safety of TPL-LA-lip. CONCLUSION The high lipophilic triptolide lignoceric acid ester prodrug greatly improved the formulation druggability of TP, and the liposome produced had high encapsulation rate and good stability. Prodrug technology combined with liposome carrier delivery of TP can significantly enhance the anti-pancreatic cancer effect of the drug, while reducing toxicity, providing a new idea and experimental basis for the development of triptolide prodrug nano drug delivery system.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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