Sinha V, Singh Asmita, Kumar Ruchita V, Singh Sanjay, Kumria Rachana, Bhinge J
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
Crit Rev Ther Drug Carrier Syst. 2007;24(1):63-92. doi: 10.1615/critrevtherdrugcarriersyst.v24.i1.30.
With the advent of new technologies and radical growth in the field of biotechnology, dozens of protein and peptide drugs have been marketed. However, there are several challenges for successful delivery of such molecules. A number of routes have been used for the delivery of these fragile molecules by exploring various novel delivery technologies, including microspheres, liposomes, gel spheres, nano-spheres, niosomes, microemulsions, use of permeation enhancers, use of protease inhibitors, etc. But the route that has attracted the attention of worldwide drug delivery scientists is the oral route due to its various advantages. Even though the proteolytic activity is higher in a few segments of the gastrointestinal tract (GIT), this route has certain segments that have lower proteolytic activity, for example, the colon. The colon has captured attention as a site for the delivery of these molecules because of its greater responsiveness to absorption enhancers, protease inhibitors, and novel bioadhesive and biodegradable polymers. Although the success rate of these approaches, when used alone is pretty low, when used in combinations, these agents have demonstrated wonders in increasing the drug bioavailability. This review focuses on the challenges, pharmaceutical concepts, and approaches involved in the delivery of these fragile molecules, specifically to the colon. This review also includes studies conducted on colonic targeting of such drugs. Further studies may lead to improvements in therapy using protein/peptide drugs and refinements in the technology of colon-specific drug delivery.
随着新技术的出现以及生物技术领域的迅猛发展，数十种蛋白质和肽类药物已投放市场。然而，成功递送此类分子面临若干挑战。通过探索各种新型递送技术，包括微球、脂质体、凝胶球、纳米球、非离子表面活性剂泡囊、微乳剂、使用渗透促进剂、使用蛋白酶抑制剂等，已采用多种途径来递送这些脆弱分子。但由于其诸多优势，口服途径吸引了全球药物递送科学家的关注。尽管胃肠道（GIT）的某些部位蛋白水解活性较高，但该途径有一些蛋白水解活性较低的部位，例如结肠。结肠因其对吸收促进剂、蛋白酶抑制剂以及新型生物黏附和可生物降解聚合物具有更高的反应性，已成为递送这些分子的一个受关注部位。尽管这些方法单独使用时成功率相当低，但联合使用时，这些药剂在提高药物生物利用度方面已展现出神奇效果。本综述聚焦于递送这些脆弱分子，特别是递送至结肠所涉及的挑战、药学概念和方法。本综述还包括对此类药物结肠靶向性的研究。进一步的研究可能会改进蛋白质/肽类药物的治疗方法，并完善结肠特异性药物递送技术。
