5'-Deoxy-5-fluorouridine プロドラッグ含有リピッドマイクロスフィアによる抗癌剤のリンパ系送達
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Lipid microspheres (LM) containing lipophilic prodrug of 5'-deoxy-5-fluorouridine(5'-DFUR), 2', 3'-didecanoyl-5'-deoxy-5-fluorouridine(C 10-5'-DFUR), were prepared. The median diameter of LM containing C 10-5'-DFUR(C 10-5'-DFUR-LM) was about 200 nm, which was unchanged during storage for 1 week at 5°C. We analyzed plasma concentration and cumulative lymphatic transport of drug following oral administration of C 10-5'-DFUR-L to rats, as compared with 5'-DFUR aqueous salutions(5'-DFUR-W) or 5'-DFUR added to LM (5'-DFUR+LM). Effect of simultaneous use of C 10-5'-DFUR and soybean oil or lecithin which is components of LM on lymphatic delivery of drug was also investigated. The plasma concentration of 5'-DFUR rapidly declined following administration of 5'-DFUR-W or 5'-DFUR+LM. In contrast, the plasma concentration of 5'-DFUR was sustained for 24 hr in all cases of formulations containing C 10-5'-DFUR. On the other hand, the cumulative lymphatic transport of the drug following the co-administration of C 10-5'-DFUR and soybean oil or lecithin was higher than 5'-DFUR-W and 5'-DFUR+LM. Especially, in the case of C 10-5'-DFUR-LM, the cumulative lymphatic transport was higher than any other formulation. Those results indicate that administration of lipophilic drug incorporated in LM is effective for directed delivery of the drug to lymph duct, due partly to direct transmucosal passage of the intact LM containing the drug. / 5'-Deoxy-5-fluorouridine(5'-DFUR)の脂溶性プロドラッグ(2',3'-didecanoyl-5'-deoxy-5-fluerouridine(C10-5'-DFUR))含有リピッドマイクロスフィア(LM)を調製し(メジアン径≒200nm),ラットに経口投与した結果,血漿中5'-DFUR濃度は5'-DFUR製剤投与にくらべ持続し,薬物の累積リンパ移行量はC10-5'-DFURとLM成分(ダイズ油、レシチン)との併用時よりも高かった. これは,脂溶性薬物とカイロミクロン成分との併用と,一部,薬物を含有したLM自身の粘膜通過が,薬物のリンパ系送達に効果があるためと考える.
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