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Bisphosphonates: therapeutics potential and recent advances in drug delivery

机译:双膦酸盐:治疗潜力和药物输送的最新进展

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Context: 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).Objective: 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.Methods: 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.Conclusion: 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.
机译:背景:双膦酸盐(BPs)被广泛用于预防和治疗骨质疏松症。由于BP在临床研究中取得了积极的成果,因此被称为骨质疏松症(OP)治疗的金标准。但是,一些严重的副作用与BP有关,例如胃肠道不良反应,例如食道炎和食道溃疡。 BP的口服生物利用度(BA)由于通过胃肠道(GIT)吸收不良而介于0.6%至1%之间。目的:本综述的主要目的是探讨新型药物递送系统(DDS)在BP递送中的作用方法:本篇综述的重点是BP的分类,作用机理和局限性,还着眼于新型DDS的使用,例如纳米颗粒,脂质体,局部,透皮系统,植入物,双膦酸盐亲骨性DDS(BP-ODDS),微球和BP的磷酸钙水泥(CPC)。该综述还对迄今为止进行的各种体外和体内研究进行了严格的综述。结论:在详尽的文献基础上,已发现新型DDS可将与BP相关的副作用降到最低,并增强BA 。提前给药对减少不良反应和增加BPs的影响更大。

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