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一种新型 FTY720（芬戈莫德）脂质体制剂，具有有前景的增强靶向递药作用。

A novel liposomal formulation of FTY720 (fingolimod) for promising enhanced targeted delivery.

机构信息

Center for Affordable Nanoengineering of Polymeric Biomedical Devices (CANPBD), The Ohio State University, Columbus, OH, USA; Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH, USA.

Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH, USA.

出版信息

Nanomedicine. 2014 Feb;10(2):393-400. doi: 10.1016/j.nano.2013.08.001. Epub 2013 Aug 20.

DOI:10.1016/j.nano.2013.08.001
PMID:23969101
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4134520/
Abstract

UNLABELLED

We describe here the development and characterization of the physicochemical and pharmacokinetic properties of a novel liposomal formulation for FTY720 delivery, LP-FTY720. The mean diameter of LP-FTY720 was 157 nm, and the FTY720 entrapment efficiency was ~85%. The liposomal formulation protected FTY720 from degradation in aqueous buffer and showed toxicity in CLL patient B cells comparable to that of free FTY720. Following intravenous injection in ICR mice, LP-FTY720 had an increased elimination phase half-life (28 vs. ~19 hr) and decreased clearance (235 vs. 778 mL/h/kg) compared to the free drug. Antibodies against CD19, CD20 and CD37 were incorporated into LP-FTY720, which provided targeted delivery to CLL patient B cells and thus achieved higher killing efficacy. The novel liposomal carrier of FTY720 demonstrated improved pharmacokinetic properties, comparable activity, and a potential platform for targeted delivery to CLL by overcoming the limited application of free FTY720 to B malignancy treatment.

FROM THE CLINICAL EDITOR

This team reports on a novel liposomal formulation for FTY720 delivery, demonstrating improved pharmacokinetic properties, comparable activity, and a potential platform for targeted delivery to CLL using antibodies incorporated in the liposomes. The method expected to overcome the limited application of free FTY720 to B malignancy treatment.

摘要

未加标签

我们在此描述了一种新型 FTY720 递药脂质体制剂（LP-FTY720）的理化性质和药代动力学特征的开发和表征。LP-FTY720 的平均粒径约为 157nm，FTY720 的包封效率约为 85%。该脂质体制剂可保护 FTY720 在水性缓冲液中免受降解，并显示出与游离 FTY720 相当的对 CLL 患者 B 细胞的毒性。在 ICR 小鼠中静脉注射后，LP-FTY720 的消除相半衰期（28 小时对19 小时）增加，清除率（235 对 778mL/h/kg）降低，与游离药物相比。将针对 CD19、CD20 和 CD37 的抗体纳入 LP-FTY720 中，这为 CLL 患者 B 细胞提供了靶向递送，从而实现了更高的杀伤功效。FTY720 的新型脂质体载体表现出改善的药代动力学特性、相当的活性，以及通过克服游离 FTY720 在 B 恶性肿瘤治疗中的应用受限来实现对 CLL 靶向递送的潜在平台。

临床编辑按语

该团队报告了一种新型 FTY720 递药脂质体制剂，该制剂表现出改善的药代动力学特性、相当的活性，以及通过在脂质体中加入抗体来实现对 CLL 的靶向递送的潜在平台。该方法有望克服游离 FTY720 在 B 恶性肿瘤治疗中的应用受限。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4eb9/4134520/a5280fbe4525/nihms609693f6.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4eb9/4134520/a5280fbe4525/nihms609693f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4eb9/4134520/7a76b72f4f29/nihms609693f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4eb9/4134520/bb3f1026f1af/nihms609693f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4eb9/4134520/f76c68a4e4c7/nihms609693f3.jpg
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