College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.
Pharmaceutics. 2011 Aug 10;3(3):474-84. doi: 10.3390/pharmaceutics3030474.
Vitamin B12 deficiency, which may result in anemia and nerve damage if left untreated, is currently treated by administration of cyanocobalamin via oral or intramuscular routes. However, these routes are associated with absorption and compliance issues which have prompted us to investigate skin as an alternative site of administration. Delivery through skin, however, is restricted to small and moderately lipophilic molecules due to the outermost barrier, the stratum corneum (SC). In this study, we have investigated the effect of different enhancement techniques, chemical enhancers (ethanol, oleic acid, propylene glycol), iontophoresis (anodal iontophoresis) and microneedles (soluble maltose microneedles), which may overcome this barrier and improve cyanocobalamin delivery. Studies with different chemical enhancer formulations indicated that ethanol and oleic acid decreased the lag time while propylene glycol based formulations increased the lag time. The formulation with ethanol (50%), oleic acid (10%) and propylene glycol (40%) showed the maximum improvement in delivery. Iontophoresis and microneedle treatments resulted in enhanced permeation levels compared to passive controls. These enhancement approaches can be explored further to develop alternative treatment regimens.
维生素 B12 缺乏症,如果不治疗,可能导致贫血和神经损伤,目前通过口服或肌肉途径给予氰钴胺素进行治疗。然而,这些途径与吸收和依从性问题有关,这促使我们研究皮肤作为替代给药部位。然而,由于最外层屏障角质层(SC)的存在,皮肤给药仅限于小分子量和亲脂性适度的分子。在这项研究中,我们研究了不同增强技术的效果,化学增强剂(乙醇、油酸、丙二醇)、离子电渗(阳极离子电渗)和微针(可溶麦芽糖微针),这些技术可能会克服这一障碍并改善氰钴胺素的递送。不同化学增强剂配方的研究表明,乙醇和油酸降低了滞后时间,而丙二醇配方则增加了滞后时间。含有乙醇(50%)、油酸(10%)和丙二醇(40%)的配方显示出最大的递送改善效果。与被动对照相比,离子电渗和微针处理导致渗透水平增强。可以进一步探索这些增强方法,以开发替代治疗方案。