结肠特异性药物递送的多颗粒制剂方法:当前观点
Multiparticulate formulation approach to colon specific drug delivery: current perspectives.
作者信息
Asghar Laila Fatima Ali, Chandran Sajeev
机构信息
Formulation Development and Pharmacokinetic Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani, Rajasthan, India.
出版信息
J Pharm Pharm Sci. 2006;9(3):327-38.
Colon specific drug delivery has gained increased importance not just for the delivery of drugs for the treatment of local diseases associated with the colon but also as potential site for the systemic delivery of therapeutic peptide and proteins. To achieve successful colon targeted drug delivery, a drug needs to be protected from degradation, release and/or absorption in the upper portion of the GI tract and then ensure abrupt or controlled release in the proximal colon. Drug modifications through covalent linkages with carrier or prodrug approach and formulation based approaches can be used for colonic delivery. Report suggests that drug carrier systems larger than 200 mm possess very low gastric transit time due to physiological condition of the bowel in colitis. And for this reason and considering the selective uptake of micron or sub-micron particles by cancerous and inflamed cells/ tissues a multiparticulate approach based on pellets, granules, microsphere or nanoparticle type formulation is expected to have better pharmacological effect in the colon. The review is aimed at understanding recent advancements made in multiparticulate formulation approach for colon specific delivery of medicaments.
结肠特异性药物递送不仅对于递送用于治疗与结肠相关的局部疾病的药物变得越来越重要,而且作为治疗性肽和蛋白质全身递送的潜在部位也日益重要。为了实现成功的结肠靶向药物递送,药物需要在胃肠道上部免受降解、释放和/或吸收,然后确保在近端结肠中突然或可控释放。通过与载体的共价连接或前药方法进行的药物修饰以及基于制剂的方法可用于结肠递送。报告表明,由于结肠炎中肠道的生理状况,大于200微米的药物载体系统具有非常短的胃转运时间。出于这个原因,并考虑到癌细胞和发炎细胞/组织对微米或亚微米颗粒的选择性摄取,基于丸剂、颗粒剂、微球或纳米颗粒型制剂的多颗粒方法有望在结肠中产生更好的药理作用。这篇综述旨在了解在用于结肠特异性药物递送的多颗粒制剂方法方面取得的最新进展。