基于 QbD 方法的热敏脂质体的药物开发和设计。

Pharmaceutical Development and Design of Thermosensitive Liposomes Based on the QbD Approach.

机构信息

Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u 6, H-6720 Szeged, Hungary.

Department of Applied and Environmental Chemistry, Faculty of Science and Informatics, Institute of Chemistry, University of Szeged, 1, Rerrich Béla tér, H-6720 Szeged, Hungary.

出版信息

Molecules. 2022 Feb 24;27(5):1536. doi: 10.3390/molecules27051536.

This study aimed to produce thermosensitive liposomes (TSL) by applying the quality by design (QbD) concept. In this paper, our research group collected and studied the parameters that significantly impact the quality of the liposomal product. Thermosensitive liposomes are vesicles used as drug delivery systems that release the active pharmaceutical ingredient in a targeted way at ~40-42 °C, i.e., in local hyperthermia. This study aimed to manufacture thermosensitive liposomes with a diameter of approximately 100 nm. The first TSLs were made from DPPC (1,2-dipalmitoyl-sn-glycerol-3-phosphocholine) and DSPC (1,2-dioctadecanoyl-sn-glycero-3-phosphocholine) phospholipids. Studies showed that the application of different types and ratios of lipids influences the thermal properties of liposomes. In this research, we made thermosensitive liposomes using a PEGylated lipid besides the previously mentioned phospholipids with the thin-film hydration method.

本研究旨在通过应用质量源于设计（QbD）的概念来制备温敏脂质体（TSL）。在本文中，我们的研究小组收集并研究了对脂质体产品质量有显著影响的参数。温敏脂质体是用作药物递送系统的囊泡，可在约 40-42°C（即局部热疗）时以靶向方式释放活性药物成分。本研究旨在制备直径约为 100nm 的温敏脂质体。第一批 TSL 由 DPPC（1,2-二棕榈酰基-sn-甘油-3-磷酸胆碱）和 DSPC（1,2-二油酰基-sn-甘油-3-磷酸胆碱）磷脂制成。研究表明，不同类型和比例的脂质的应用会影响脂质体的热性能。在这项研究中，我们使用了一种聚乙二醇化的脂质，除了之前提到的磷脂，还使用了薄膜水化法来制备温敏脂质体。