Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, Korea.
J Drug Target. 2012 Jul;20(6):481-501. doi: 10.3109/1061186X.2012.693499. Epub 2012 May 28.
Macromolecular therapeutics, in particular, many biologics, is the most advancing category of drugs over conventional chemical drugs. The potency and specificity of the biologics for curing certain disease made them to be a leading compound in the pharmaceutical industry. However, due to their intrinsic nature, including high molecular weight, hydrophilicity and instability, they are difficult to be administered via non-invasive route. This is a major quest especially in biologics, as they are frequently used clinically for chronic disorders, which requires long-term administration. Therefore, many efforts have been made to develop formulation for non-invasive administration, in attempt to improve patient compliance and convenience. In this review, strategies for non-invasive delivery, in particular, oral, pulmonary and nasal delivery, that are recently adopted for delivery of biologics are discussed. Insulin, calcitonin and heparin were mainly focused for the discussion as they could represent protein, polypeptide and polysaccharide drugs, respectively. Many recent attempts for non-invasive delivery of biologics are compared to provide an insight of developing successful delivery system.
大分子治疗药物，特别是许多生物制剂，是药物领域中比传统化学药物进展最快的一类。生物制剂在治疗某些疾病方面的高效性和特异性使其成为制药行业的主导化合物。然而，由于其内在性质，包括高分子量、亲水性和不稳定性，它们很难通过非侵入性途径给药。这是一个主要的难题，特别是对于生物制剂而言，因为它们经常被用于慢性疾病的临床治疗，需要长期给药。因此，人们已经做出了许多努力来开发非侵入性给药的制剂，试图提高患者的顺应性和便利性。在这篇综述中，讨论了最近用于生物制剂给药的非侵入性传递策略，特别是口服、肺部和鼻腔给药。胰岛素、降钙素和肝素主要被用作讨论对象，因为它们分别可以代表蛋白质、多肽和多糖药物。许多最近用于生物制剂非侵入性传递的尝试被进行了比较，以提供开发成功传递系统的深入了解。
