The Biotechnology and Drug Development Research Laboratory, Curtin Medical School & Curtin Health Innovation Research Institute, Curtin University, Bentley, Perth, WA, 6102, Australia; Hearing Therapeutics Department, Ear Science Institute Australia, Queen Elizabeth II Medical Centre, Nedlands, Perth, WA, 6009, Australia.
Curtin Medical School & Curtin Health Innovation Research Institute, Curtin University, Bentley, Perth, WA, 6102, Australia.
Biomaterials. 2022 Apr;283:121459. doi: 10.1016/j.biomaterials.2022.121459. Epub 2022 Mar 12.
The role of endogenous bile acids as lipid stabilizers aiding uptake of lipophilic nutrients via micelle formation and saponification effects is well documented and precedes their growing applications in pharmaceutical sciences. Their utility stems from their unique physico-chemical profile and ability to modulate immune cell signalling pathways. It has been shown that bile acids alter specific receptor-mediated pathways of cellular respiration and metabolism, providing potential clinical therapies for cardio-metabolic disorders such as diabetes mellitus, hypercholesterolemia, and heart disease. Additionally, some bile acids exert profound anti-oxidant, anti-inflammatory and immunosuppressant properties, and are effective at reducing blood pressure and alleviating hypertension. Their unique amphoteric properties and proven ability as permeability enhancers make them a desirable pharmaceutical excipient. When incorporated with various carbohydrates, polymers, hydrogels and/or polyelectrolytes to form micro- or nano-capsules, they provide enhanced thermodynamic, osmotic and structural stability, and cater for controlled delivery via specific tissue targeting, pH dependant release and temperature guided sol-gel complexation. Additionally, due to their immunosuppressant properties, they enhance the immunogenicity of encapsulated cells, increasing the feasibility of bioartificial organs as transplantable therapeutics. This review explores existing and future applications of bile acids and provides a synopsis of their role in advanced, novel therapeutic delivery systems.
内源性胆汁酸作为脂质稳定剂的作用,通过胶束形成和皂化作用帮助吸收亲脂性营养素,这一作用已得到充分证实,并且它们在药物科学中的应用也在不断增加。其用途源于其独特的物理化学特性和调节免疫细胞信号通路的能力。已经表明,胆汁酸改变了细胞呼吸和代谢的特定受体介导途径,为糖尿病、高胆固醇血症和心脏病等心血管代谢疾病提供了潜在的临床治疗方法。此外,一些胆汁酸具有显著的抗氧化、抗炎和免疫抑制特性,可有效降低血压和缓解高血压。其独特的两性特性和作为渗透增强剂的已证明能力使它们成为理想的药物赋形剂。当与各种碳水化合物、聚合物、水凝胶和/或聚电解质结合形成微胶囊或纳米胶囊时,它们提供了增强的热力学、渗透压和结构稳定性,并通过特定的组织靶向、pH 依赖性释放和温度引导的溶胶-凝胶络合来实现控制释放。此外,由于其免疫抑制特性,它们增强了囊封细胞的免疫原性,增加了生物人工器官作为可移植治疗方法的可行性。本综述探讨了胆汁酸的现有和未来应用,并概述了它们在先进的新型治疗性递药系统中的作用。