Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, 'Iuliu Hatieganu' University of Medicine and Pharmacy, Cluj-Napoca, Romania.
Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Szeged, Hungary.
J Liposome Res. 2024 Sep;34(3):421-434. doi: 10.1080/08982104.2023.2287588. Epub 2023 Dec 3.
The development of an inhalation powder (IP) for cancer therapy is desired to improve the therapeutic response and patient compliance. The latest studies highlighted that statins, a class of drugs used in hypercholesterolemia, can have anticancer and antiinflammatory properties. Therefore, the aim of the study was to develop an IP containing liposomes loaded with simvastatin using spray drying technology, as well as to investigate the influence of formulation factors on the quality attributes of the IP by means of experimental design. Results highlighted that the composition of liposomes, namely type of phospholipid and cholesterol concentration, highly influences the quality attributes of IP, and the use of optimal concentrations of excipients, i.e. D-mannitol and L-leucine, is essential to preserve the characteristics of liposomes throughout the spray drying process. The characterization of the optimal IP formulation revealed that the total percentage of released drug is higher from the IP formulation compared to the powder of active substance (53.38 vs. 42.76%) over a period of six hours, and 39.67% of dry particles have a size less than 5 µm, making them suitable for inhalation. As a conclusion, spray drying technology can be effectively used in the development and preparation of IP containing liposomes.
人们希望开发用于癌症治疗的吸入性粉末（IP），以提高治疗效果和患者顺应性。最近的研究强调，他汀类药物是一类用于治疗高胆固醇血症的药物，具有抗癌和抗炎特性。因此，本研究的目的是使用喷雾干燥技术开发一种含有载有辛伐他汀的脂质体的 IP，并通过实验设计研究制剂因素对 IP 质量特性的影响。结果表明，脂质体的组成，即磷脂的类型和胆固醇的浓度，极大地影响了 IP 的质量特性，而使用最佳浓度的赋形剂，即 D-甘露醇和 L-亮氨酸，对于在喷雾干燥过程中保持脂质体的特性至关重要。对最佳 IP 制剂的表征表明，与活性物质的粉末相比（53.38%比 42.76%），在六小时的时间内，从 IP 制剂中释放的药物总量更高，并且 39.67%的干燥颗粒的粒径小于 5μm，使其适合吸入。总之，喷雾干燥技术可有效地用于开发和制备含有脂质体的 IP。
