Smart John D
School of Pharmacy and Biomolecular Sciences, University of Brighton, Lewes Road, Brighton BN2 4GJ, UK.
Expert Opin Drug Deliv. 2005 May;2(3):507-17. doi: 10.1517/17425247.2.3.507.
Buccal formulations have been developed to allow prolonged localised therapy and enhanced systemic delivery. The buccal mucosa, however, while avoiding first-pass effects, is a formidable barrier to drug absorption, especially for biopharmaceutical products (proteins and oligonucleotides) arising from the recent advances in genomics and proteomics. The buccal route is typically used for extended drug delivery, so formulations that can be attached to the buccal mucosa are favoured. The bioadhesive polymers used in buccal drug delivery to retain a formulation are typically hydrophilic macro-molecules containing numerous hydrogen bonding groups. Newer second-generation bioadhesives have been developed and these include modified or new polymers that allow enhanced adhesion and/or drug delivery, in addition to site-specific ligands such as lectins. Over the last 20 years a wide range of formulations has been developed for buccal drug delivery (tablet, patch, liquids and semisolids) but comparatively few have found their way onto the market. Currently, this route is restricted to the delivery of a limited number of small lipophilic molecules that readily cross the buccal mucosa. However, this route could become a significant means for the delivery of a range of active agents in the coming years, if the barriers to buccal drug delivery are overcome. In particular, patient acceptability and the successful systemic delivery of large molecules (proteins, oligonucleotides and polysaccharides) via this route remains both a significant opportunity and challenge, and new/improved technologies may be required to address these.
口腔制剂已被开发用于实现延长局部治疗和增强全身给药。然而，口腔黏膜虽然能避免首过效应，但对药物吸收来说是一个巨大的障碍，特别是对于基因组学和蛋白质组学最新进展所产生的生物制药产品（蛋白质和寡核苷酸）。口腔给药途径通常用于延长药物递送，因此可附着于口腔黏膜的制剂更受青睐。用于口腔药物递送以保留制剂的生物粘附聚合物通常是含有大量氢键基团的亲水性大分子。已开发出更新的第二代生物粘附剂，其中包括改性或新型聚合物，除了诸如凝集素等位点特异性配体之外，这些聚合物还能实现增强的粘附和/或药物递送。在过去20年中，已开发出多种用于口腔药物递送的制剂（片剂、贴片、液体和半固体），但相对较少的制剂进入市场。目前，该途径仅限于递送少量易于穿过口腔黏膜的亲脂性小分子。然而，如果克服了口腔药物递送的障碍，在未来几年内该途径可能会成为递送一系列活性剂的重要手段。特别是，患者的可接受性以及通过该途径成功全身递送大分子（蛋白质、寡核苷酸和多糖）仍然既是一个重大机遇也是一个挑战，可能需要新的/改进的技术来解决这些问题。
