Research progress on tumor-targeting paclitaxel prodrugs / 药学实践杂志

Paclitaxel is a natural compound with efficient broad-spectrum antitumor activity .However ,the clinical ap-plication has been limited owing to the undesirable drawbacks ,such as the poor water-solubility ,cardiovascular toxicity and neurotoxicity .The design of paclitaxel prodrugs is an effective measure which can improve the drug's druggability ,alleviate its toxicity adverse effect and enhance its antitumor effect .With the in-depth research of prodrugs ,tumor-targeting paclitaxel pro-drugs which using the excessive receptors ,specific enzymes ,transporters ,reactive oxide species ,glutathione in tumor tissues as well as acidosis and hypoxia in tumors as specific targets ,have made great progress .The relevant literature about paclitaxel prodrugs were reviewed in this paper ,which targeted to the specific pathological and physiological features of tumor microenvi-ronment in recent years.

Synthesis and druggability study of triptolide stearate / 药学实践杂志

Objective To synthesize a lipophilic prodrug of triptolide (TP) and improve its druggability .Methods Trip-tolidestearate (TP-SA)was synthesized via the DMAP-catalyzed DCC method and identified by MS ,1H-NMR and 13C-NMR. The shake-flask method was used to study the oil/water partition coefficient .The preparations of TP and TP-SA liposomes and emulsions were compared .Their encapsulation efficiency and stability were investigated .Results TP-SA was synthesized suc-cessfully .Its log P in octanol/water system was 2 .33 .It was difficult to prepare TP liposome or emulsion .By contrast ,TP-SA liposome and emulsion can be prepared successfully with the same formulation process .The particle size of TP-SA lipo-somes were about 90 nm and TP-SA emulsions were about 110 nm .The encapsulation efficiency was above 95% .Their stabili-ty were studied at 4℃ and 25℃ .The preparation parameters ,such as particle size and encapsulation efficiency ,had no signif-icant change in a week .Conclusion Triptolide stearate enhanced drug lipophilicity .Its druggability was improved significant-ly .These data can be used for the TP related drug design and development .