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Emerging Research and Clinical Development Trends of Liposome and Lipid Nanoparticle Drug Delivery Systems

机译：脂质体和脂质纳米粒给药系统的新兴研究和临床发展趋势

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Liposomes are spherical-enclosed membrane vesicles mainly constructed with lipids. Lipid nanoparticles are loaded with therapeutics and may not contain an enclosed bilayer. The majority of those clinically approved have diameters of 50–300 nm. The growing interest in nanomedicine has fueled lipid–drug and lipid–protein studies, which provide a foundation for developing lipid particles that improve drug potency and reduce off-target effects. Integrating advances in lipid membrane research has enabled therapeutic development. At present, about 600 clinical trials involve lipid particle drug delivery systems. Greater understanding of pharmacokinetics, biodistribution, and disposition of lipid–drug particles facilitated particle surface hydration technology (with polyethylene glycol) to reduce rapid clearance and provide sufficient blood circulation time for drug to reach target tissues and cells. Surface hydration enabled the liposome-encapsulated cancer drug doxorubicin (Doxil) to gain clinical approval in 1995. Fifteen lipidic therapeutics are now clinically approved. Although much research involves attaching lipid particles to ligands selective for occult cells and tissues, preparation procedures are often complex and pose scale-up challenges. With emerging knowledge in drug target and lipid–drug distribution in the body, a systems approach that integrates knowledge to design and scale lipid–drug particles may further advance translation of these systems to improve therapeutic safety and efficacy.
机译：脂质体是主要由脂质构成的球形封闭膜囊泡。脂质纳米颗粒装有治疗剂，可能不包含封闭的双层。经临床批准的大多数直径为50-300 nm。对纳米药物的兴趣日益增长，推动了脂质药物和脂质蛋白质的研究，这为开发脂质颗粒提供了基础，这些颗粒可提高药物效力并减少脱靶效应。整合脂质膜研究的进展已使治疗学发展成为可能。目前，约有600项临床试验涉及脂质颗粒药物递送系统。对药代动力学，生物分布和脂类药物颗粒处置的更多了解促进了颗粒表面水化技术（与聚乙二醇一起使用）减少了快速清除并为药物到达靶组织和细胞提供了充足的血液循环时间。表面水合使脂质体包裹的抗癌药阿霉素（Doxil）于1995年获得临床批准。目前有15种脂质疗法已获得临床批准。尽管许多研究涉及将脂质颗粒附着在对隐匿性细胞和组织有选择性的配体上，但制备过程通常很复杂，并且对扩大规模提出了挑战。随着有关药物靶点和体内脂质药物分布的知识不断涌现，一种将知识整合到设计和定标脂质药物颗粒的系统方法可以进一步推进这些系统的翻译，以提高治疗安全性和有效性。

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