Lutta Anitta, Liu Qian, Pedersen Gabriel Kristian, Dong Mingdong, Grohganz Holger, Nielsen Line Hagner, Schmidt Signe Tandrup
Department of Infectious Disease Immunology, Statens Serum Institut, Artillerivej 5, 2300, Copenhagen, Denmark.
Department of Health Technology, Technical University of Denmark, Ørsteds Plads 345C, 2800, Kgs. Lyngby, Denmark.
Drug Deliv Transl Res. 2025 Feb 22. doi: 10.1007/s13346-025-01812-0.
Polymer coating of nanoparticulate drug delivery systems may enhance the efficacy of oral delivery. Cationic liposomes were coated with pectin biopolymers using microfluidics, with systematic variation of process parameters to optimize pectin-coated liposome fabrication. A pectin/liposome weight ratio of 0.7 and a microfluidic flow rate ratio of 2:1 pectin:liposome were found to be optimal. The resulting formulations displayed particle sizes at least threefold the size of uncoated liposomes, while the surface charge shifted to a highly negative value, indicating full pectin coating of the particles. Further microscopic characterization of the pectin-coated liposomes revealed that the pectins formed a polymeric network within which the liposomes were dispersed or attached. Stability studies revealed that pectin-coated liposomes remained stable during storage, with no displacement of the coating. We determined that microfluidics is a robust method for preparing pectin-coated liposomes, despite the structural differences between the pectins, geometry of the microchip used, and pectin/liposome concentration. Ultimately, the use of microfluidics in formulation development could be highly beneficial, as the process parameters can be easily modified and the process is easily scalable and inexpensive. Additionally, pectins can offer protective properties to the liposomes particularly during oral drug delivery.
纳米颗粒药物递送系统的聚合物涂层可提高口服给药的疗效。使用微流控技术用果胶生物聚合物包覆阳离子脂质体,并系统地改变工艺参数以优化果胶包覆脂质体的制备。发现果胶/脂质体重量比为0.7以及微流控流速比为果胶:脂质体2:1时为最佳。所得制剂的粒径至少是未包覆脂质体粒径的三倍,而表面电荷转变为高度负值,表明颗粒被果胶完全包覆。对果胶包覆脂质体的进一步显微镜表征显示,果胶形成了一个聚合物网络,脂质体分散或附着在其中。稳定性研究表明,果胶包覆脂质体在储存期间保持稳定,涂层没有移位。我们确定,尽管果胶之间存在结构差异、所用微芯片的几何形状以及果胶/脂质体浓度不同,但微流控技术是制备果胶包覆脂质体的可靠方法。最终,在制剂开发中使用微流控技术可能非常有益,因为工艺参数易于修改,且该工艺易于扩展且成本低廉。此外,果胶尤其在口服药物递送过程中可为脂质体提供保护性能。