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

ABSTRACT

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 .