State Key Laboratory of Advanced Drug Delivery and Release Systems, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
Liangzhu Laboratory, Zhejiang University, Hangzhou, China.
Nat Commun. 2024 Jul 5;15(1):5659. doi: 10.1038/s41467-024-50093-7.
Fully targeted mRNA therapeutics necessitate simultaneous organ-specific accumulation and effective translation. Despite some progress, delivery systems are still unable to fully achieve this. Here, we reformulate lipid nanoparticles (LNPs) through adjustments in lipid material structures and compositions to systematically achieve the pulmonary and hepatic (respectively) targeted mRNA distribution and expression. A combinatorial library of degradable-core based ionizable cationic lipids is designed, following by optimisation of LNP compositions. Contrary to current LNP paradigms, our findings demonstrate that cholesterol and phospholipid are dispensable for LNP functionality. Specifically, cholesterol-removal addresses the persistent challenge of preventing nanoparticle accumulation in hepatic tissues. By modulating and simplifying intrinsic LNP components, concurrent mRNA accumulation and translation is achieved in the lung and liver, respectively. This targeting strategy is applicable to existing LNP systems with potential to expand the progress of precise mRNA therapy for diverse diseases.
完全靶向的 mRNA 疗法需要同时进行器官特异性积累和有效的翻译。尽管取得了一些进展,但输送系统仍无法完全实现这一目标。在这里,我们通过调整脂质材料的结构和组成来重新构建脂质纳米颗粒 (LNP),从而系统地实现肺和肝(分别)靶向 mRNA 的分布和表达。设计了基于可降解核的离子型阳离子脂质的组合文库,并对 LNP 组成进行了优化。与当前的 LNP 范式相反,我们的研究结果表明胆固醇和磷脂对于 LNP 的功能是可有可无的。具体来说,去除胆固醇可以解决防止纳米颗粒在肝组织中积累的长期挑战。通过调节和简化内在的 LNP 成分,分别在肺部和肝脏中实现了 mRNA 的积累和翻译。这种靶向策略适用于现有的 LNP 系统,有可能为多种疾病的精确 mRNA 治疗进展带来突破。