Cevc G, Gebauer D, Stieber J, Schätzlein A, Blume G
Medical Biophysics, Clinics r.d.I., The Technical University of Munich, Germany.
Biochim Biophys Acta. 1998 Jan 19;1368(2):201-15. doi: 10.1016/s0005-2736(97)00177-6.
New vehicles for the non-invasive delivery of agents are introduced. These carriers can transport pharmacological agents, including large polypeptides, through the permeability barriers, such as the intact skin. This capability depends on the self-regulating carrier deformability which exceeds that of the related but not optimized lipid aggregates by several orders of magnitude. Conventional lipid suspensions, such as standard liposomes or mixed lipid micelles, do not mediate a systemic biological effect upon epicutaneous applications. In contrast to this, the properly devised adaptable carriers, when administered on the intact skin, transport therapeutic amounts of biogenic molecules into the body. This process can be nearly as efficient as an injection needle, as seen from the results of experiments in mice and humans with the insulin-carrying vesicles. The carrier-mediated transcutaneous insulin delivery is unlikely to involve shunts, lesions or other types of skin damage. Rather than this, insulin is inferred to be transported into the body between the intact skin cells with a bio-efficiency of at least 50% of the s.c. dose action.
介绍了用于无创递送药物的新型载体。这些载体可以携带包括大分子多肽在内的药理剂穿过诸如完整皮肤等渗透屏障。这种能力取决于载体的自我调节变形能力,该能力比相关但未优化的脂质聚集体的变形能力高出几个数量级。传统的脂质悬浮液,如标准脂质体或混合脂质微球,经皮应用时不会介导全身生物学效应。与此相反,设计合理的适应性载体在完整皮肤上给药时,能将治疗剂量的生物分子输送到体内。从小鼠和人类使用携带胰岛素的囊泡的实验结果来看,这个过程几乎可以和注射针一样有效。载体介导的经皮胰岛素递送不太可能涉及分流、损伤或其他类型的皮肤损伤。相反,胰岛素被推断是通过完整的皮肤细胞之间输送到体内的,生物效率至少为皮下注射剂量作用的50%。