Amidon Seth, Brown Jack E, Dave Vivek S
Wegmans School of Pharmacy, St. John Fisher College, 3690 East Avenue, Rochester, New York, 14618, USA.
AAPS PharmSciTech. 2015 Aug;16(4):731-41. doi: 10.1208/s12249-015-0350-9. Epub 2015 Jun 13.
Colon-specific drug delivery systems (CDDS) are desirable for the treatment of a range of local diseases such as ulcerative colitis, Crohn's disease, irritable bowel syndrome, chronic pancreatitis, and colonic cancer. In addition, the colon can be a potential site for the systemic absorption of several drugs to treat non-colonic conditions. Drugs such as proteins and peptides that are known to degrade in the extreme gastric pH, if delivered to the colon intact, can be systemically absorbed by colonic mucosa. In order to achieve effective therapeutic outcomes, it is imperative that the designed delivery system specifically targets the drugs into the colon. Several formulation approaches have been explored in the development colon-targeted drug delivery systems. These approaches involve the use of formulation components that interact with one or more aspects of gastrointestinal (GI) physiology, such as the difference in the pH along the GI tract, the presence of colonic microflora, and enzymes, to achieve colon targeting. This article highlights the factors influencing colon-specific drug delivery and colonic bioavailability, and the limitations associated with CDDS. Further, the review provides a systematic discussion of various conventional, as well as relatively newer formulation approaches/technologies currently being utilized for the development of CDDS.
结肠特异性给药系统(CDDS)对于治疗一系列局部疾病,如溃疡性结肠炎、克罗恩病、肠易激综合征、慢性胰腺炎和结肠癌而言是理想的。此外,结肠可能是几种药物进行全身吸收以治疗非结肠疾病的潜在部位。诸如蛋白质和肽等已知会在极端胃酸pH值下降解的药物,如果完整地递送至结肠,可被结肠黏膜全身吸收。为了实现有效的治疗效果,设计的给药系统必须将药物特异性靶向至结肠。在开发结肠靶向给药系统的过程中,已经探索了几种制剂方法。这些方法涉及使用与胃肠道(GI)生理学的一个或多个方面相互作用的制剂成分,例如沿胃肠道的pH差异、结肠微生物群的存在以及酶,以实现结肠靶向。本文重点介绍了影响结肠特异性药物递送和结肠生物利用度的因素,以及与CDDS相关的局限性。此外,本综述对目前用于开发CDDS的各种传统以及相对较新的制剂方法/技术进行了系统讨论。