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靶向纳米系统用于递送抗肥胖药物。

Targeted Nano-Based Systems for the Anti-Obesity Agent's Delivery.

机构信息

Faculty of Pharmacy, Department of Toxicology, Gazi University, Hipodrom, Ankara, Turkey.

Biotechnology Institute, Ankara University, Gumusdere, Ankara, Turkey.

出版信息

Adv Exp Med Biol. 2024;1460:657-676. doi: 10.1007/978-3-031-63657-8_22.

Abstract

Obesity is a global health concern and a chronic disease that is accompanied by excessive fat storage in adipose and nonadipose tissues. An increase in the body-mass index (BMI) is directly proportional to the 2- to 3.9-fold increase in all-cause mortality in obesity. If left untreated for a longer period, obesity-related metabolic, cardiovascular, inflammatory, and malignant diseases reduce life expectancy. Currently, most of the anti-obesity drugs have failed and fallen into disrepute, either due to their ineffectiveness or adverse effects. In this review, depending on their enhanced pharmacokinetic and biodistribution profiles, whether nanocarriers alter the basic properties and bioactivity of anti-obesity drugs used in clinical practice are debated. First, nanocarriers can improve the safety of still-used anti-obesity drugs by lowering their systemic toxicity through increasing targeting efficacy and preventing drug carrier toxicity. Second, when the micro-ribonucleic acids (miRNAs), which are aberrantly expressed in obesity and obesity-related diseases, are encapsulated into nanoparticles, they are effective in multiple obesity-related metabolic pathways and gene networks. Finally, a synergistic anti-obesity effect with low dose and low toxicity can be obtained with the combinatory therapy applied by encapsulating the anti-obesity drug and gene in the same nanocarrier delivery vehicle.

摘要

肥胖是一个全球性的健康问题,也是一种慢性疾病,伴随着脂肪组织和非脂肪组织中脂肪的过度储存。身体质量指数(BMI)的增加与肥胖症导致的全因死亡率增加 2-3.9 倍直接相关。如果长时间得不到治疗,与肥胖相关的代谢、心血管、炎症和恶性疾病会降低预期寿命。目前,大多数减肥药要么因为无效,要么因为副作用而声名狼藉。在这篇综述中,根据其增强的药代动力学和生物分布特性,讨论了纳米载体是否改变了临床实践中使用的抗肥胖药物的基本性质和生物活性。首先,纳米载体可以通过提高靶向效果和防止药物载体毒性,降低仍在使用的抗肥胖药物的全身毒性,从而提高其安全性。其次,当微小核糖核酸(miRNAs)被包裹在纳米粒子中时,这些在肥胖和肥胖相关疾病中异常表达的微小核糖核酸在多种肥胖相关代谢途径和基因网络中都具有疗效。最后,通过将抗肥胖药物和基因封装在同一纳米载体递药系统中,联合治疗可以获得低剂量、低毒性的协同抗肥胖效果。

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