Formulation, Characterization and Hypersensitivity Evaluation of an Intravenous Emulsion Loaded with a Paclitaxel-Cholesterol Complex

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  • Xia Xue-Jun
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College
  • Guo Rui-Fang
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College
  • Liu Yu-Ling
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College
  • Zhang Peng-Xiao
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College
  • Zhou Cui-Ping
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College
  • Jin Du-Jia
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College
  • Wang Ren-Yun
    Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College

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The objective of this paper was to develop a novel Cremophor-free, autoclave stable, intravenous emulsion for paclitaxel (PACE). A paclitaxel–cholesterol complex was used as the drug carrier to improve the solubility of paclitaxel in the oil phase of emulsions. The complex and PACE were prepared by rotary evaporation and high-pressure homogenization, respectively. Effects of oil phases, emulsifiers and pH values on the characteristics of PACE were investigated. PACE was characterized with regard to its appearance, morphology, osmolality, pH value, particle size, zeta potential, encapsulation efficiency and stability. Hypersensitivity was evaluated by guinea pig hypersensitivity reaction. The final formulation was composed of the complex, soybean oil, medium-chain triglyceridel, soybean lecithin, poloxamer 188 and glycerol. The resulting PACE had an encapsulation efficiency of 97.3% with a particle size of 135 nm and a zeta potential of −38.3 mV. Osmolality and pH of the formulation were 383 mOsmol/kg and 4.5, respectively. The formulation survived autoclaving at 115 °C for 30 min and remained stable for at least 12 months at 6 °C. PACE also exhibited a better tolerance than an equal dose of Cremophor-based paclitaxel injection in guinea pigs, as no obvious hypersensitivity reaction was observed. These results suggested that PACE has a great potential for industrial-scale production and clinical applications.

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