Evaluation of oral cyanocobalamin-loaded nanoparticles for intestinal absorption

  • Sugiyama Ikumi
    Division of Advanced Pharmaceutics, Department of Clinical Pharmaceutical Sciences, School of Pharmacy, Iwate Medical University, Yahaba, Japan Pharmaceutical and Health Sciences, Graduate School of Pharmaceutical Science, Iwate Medical University, Yahaba, Japan
  • Soma Yukako
    Pharmaceutical and Health Sciences, Graduate School of Pharmaceutical Science, Iwate Medical University, Yahaba, Japan
  • Sadzuka Yasuyuki
    Division of Advanced Pharmaceutics, Department of Clinical Pharmaceutical Sciences, School of Pharmacy, Iwate Medical University, Yahaba, Japan Pharmaceutical and Health Sciences, Graduate School of Pharmaceutical Science, Iwate Medical University, Yahaba, Japan

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  • 消化管での吸収を目的とした経口投与型シアノコバラミン内封ナノ粒子の開発

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Abstract

We developed a vitamin B12 (VB12)-containing formulation for oral administration that resulted in the absorption of VB12 without gastric intrinsic factor (IF). Patients who cannot secrete IF after the removal of their stomachs are at an increased risk of megaloblastic anemia (MA) and thus require continuous, invasive treatment with VB12 administration to improve absorption. A simple and noninvasive method for MA treatment or prevention is desired. We believe that pharmaceutical effort through a drug delivery system can resolve the absorption efficiency of VB12, which is administered orally when there is no IF in the stomach. Liposomes prepared with the thin film method contain charged lipids and were modified with polyethylene glycol on their membrane. The liposomes contained sufficient cyanocobalamin (Cyc) for VB12 therapy. Administering Cyc-loaded liposome (Cyc-L) resulted in a higher Cyc concentration of serum than that of the Cyc solution. Cyc loaded into liposomes is taken up more easily than in solution state without remaining in the ileum even if IF is present. These results indicate that Cyc-L is a useful formulation because it can elevate the concentration of serum Cyc via oral administration. Thus, Cyc-L may improve the quality of life of many patients who have had their stomachs removed.

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