Preparation of and Drug Release from W/O/W Type Double Emulsions Containing Anticancer Agents

概要

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Water-in-oil-in-water (W/O/W) type double emulsions were prepared by two-step emulsification procedures. The structures of W/O/W type double emulsions and the release characteristics of cytarabine and 5-fluorouracil (5-FU) from W/O/W type double emulsions were studied. W/O/W type double emulsions were ruptured within 24h when sorbitan monooleate (SO-10) or sorbitan sesquioleate (SO-15) was used as a lipophilic emulsifier. On the other hand, W/O/W type double emulsions prepared in a hydrogenated castor oil (HCO-10) in peanut oil were still intact after 24h. Therefore, the release characteristics of drugs were studied in HCO-10 in peanut oil. The release of cytarabine from W/O/W type double emulsions was very prolonged. The release of cytarabine was enhanced with increase in the volume of inner aqueous phase or increase in the concentration of HCO-10. The concentration of cytarabine and the concentration of a hydrophilic emulsifier (HCO-60), however, had little effect on the release of cytarabine. Whereas the release of 5-FU from W/O/W type double emulsions was as fast as from a simple solution, the release was very prolonged when the pH value of the inner aqueous phase was adjusted to 10.0. These results show the utility of W/O/W type double emulsions for sustained release preparations and raise the possibility of control of drug release from W/O/W type double emulsions.
社団法人日本薬学会の論文
1983-11-25