Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard, Hamdard Nagar, New Delhi , India.
Drug Deliv. 2015 Jan;22(1):1-9. doi: 10.3109/10717544.2013.870259. Epub 2014 Jan 10.
Bisphosphonates (BPs) are widely used for prevention and treatment of osteoporosis. BPs are known as gold standard for osteoporosis (OP) treatment due to their positive results in clinical studies. But some serious side effects are associated with BPs like gastrointestinal adverse effect i.e. esophagitis and ulcer of esophagus. Oral bioavailability (BA) of BPs ranges from 0.6 to 1% due to poor absorption through gastrointestinal tract (GIT).
The main objective of this review is to explore the role of novel drug delivery systems (DDSs) for the delivering of BPs and minimizing the drawbacks associated with them.
The current review is focusing on classification, mechanism of action, and limitations of BPs, and is also dwelling on the use of novel DDSs like nanoparticles, liposomes, topical, transdermal systems, implants, bisphosphonate osteotropic DDS (BP-ODDS), microspheres, and calcium phosphate cements (CPCs) for BPs. This review also gives a critically reviewed compilation of the various in vitro and in vivo studies conducted till date.
On the basis of the exhaustive literature, it has been found that the novel DDS minimizes the side effects associated with BPs and enhances the BA. The advance drug delivery has a greater impact on reducing the undesirable effects and increasing the BA of BPs.
双膦酸盐(BPs)被广泛用于预防和治疗骨质疏松症。由于在临床研究中取得了积极的效果,BPs 被认为是骨质疏松症(OP)治疗的金标准。但是,BPs 也存在一些严重的副作用,例如胃肠道不良反应,即食管炎和食管溃疡。由于胃肠道(GIT)吸收不良,BPs 的口服生物利用度(BA)范围为 0.6%至 1%。
本综述的主要目的是探讨新型药物递送系统(DDS)在递送 BPs 中的作用,以最小化与之相关的缺点。
本综述重点介绍了 BPs 的分类、作用机制和局限性,同时还探讨了新型 DDS 的应用,如纳米粒、脂质体、局部、透皮系统、植入物、双膦酸盐靶向药物递送系统(BP-ODDS)、微球和磷酸钙水泥(CPCs)等。本综述还对迄今为止进行的各种体外和体内研究进行了批判性的汇编。
根据详尽的文献,发现新型 DDS 可最小化 BPs 相关的副作用并提高 BA。先进的药物递送对减少 BPs 的不良影响和提高 BA 具有更大的影响。