Formulation and pharmacokinetics of the parenteral fat nano-emulsion of ubenimex

doi:10.5246/jcps.2011.05.061

Abstract

Abstract:

The fat nano-emulsion, which has been used as a drug carrier, especially for the poorly water soluble drug, has drawn favorable attention recently. Ubenimex is a poorly soluble drug with no parenteral treatment available for patients. This study was aimed at the manufacture of a ubenimex loaded fat nano-emulsion for intravenous delivery by SolEmuls^® technology. The formulation and the process parameters were optimized by single-factor design and the obtained ubenimex loaded fat nano-emulsion was stable even after autoclaving. The average particle size was near 200 nm with narrow size distribution and a negative zeta potential of -44 mV. The in vitro release behavior of ubenimex from the fat nano-emulsion could be described by the double phase kinetics model and expressed by the following equation: 100 - Q = 75.27e^-0.369t + 15.94e^-0.0324t, Rα = 0.9863, Rβ = 0.9878. The pharmacokinetic study showed that the pharmacokinetic curves of both the ubenimex fat nano-emulsion and the i.v. ubenimex suspension, were similar and the main parameters showed no significant difference except t1/2. In conclusion, the fat nano-emulsion with ubenimex has potential as a safe and effective parenteral delivery system for poorly water soluble anti-cancer drugs.

Key words: Fat nano-emulsion, Ubenimex, High pressure homogenization, Pharmacokinetics

CLC Number:

R969.1

Supporting:

Xiao-Li Sun, Dong-Hua Liu, Peng Li, Wen-Fang Xu, Na Zhang^* . Formulation and pharmacokinetics of the parenteral fat nano-emulsion of ubenimex[J]. , DOI: 10.5246/jcps.2011.05.061.

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