A novel aqueous parenteral formulation of docetaxel using prodrugs.

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 Pharm

authors

Park MH,Keum CG,Song JY,Kim D,Cho CW

doi

10.1016/j.ijpharm.2013.12.027

subject

Has Abstract

pub_date

2014-02-28 00:00:00

pages

1-7

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(13)01095-8

journal_volume

462

pub_type

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