Abstract:
:The aim of this study is to develop an aqueous parenteral solution of docetaxel using prodrugs. Docetaxel (DTX) is a highly lipophilic drug and practically insoluble in water. To overcome insolubility of docetaxel, three kinds of docetaxel prodrugs were synthesized using succinyl linker such as DTX-G, DTX-L or DTX-S and physicochemically characterized. The solubility of docetaxel prodrugs was determined by changing the concentration and type of surfactants, cosolvents or cyclodextrins. It was observed that the novel mixture of 15% PEG 400, 2.5% Tween 80 and 20% hydroxypropyl-β-cyclodextrin significantly increased the solubility of DTX-G up to 5.7 mg/mL. After subjected to the study of the hemolytic and cytotoxic activities, it was shown that the novel mixture did not show the hemolysis compared to Taxotere. It was suggested this novel mixture might have the potential to develop an aqueous parenteral formulation.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Park MH,Keum CG,Song JY,Kim D,Cho CWdoi
10.1016/j.ijpharm.2013.12.027subject
Has Abstractpub_date
2014-02-28 00:00:00pages
1-7issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(13)01095-8journal_volume
462pub_type
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