Industrial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Pilani Campus, India.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Guwahati, Assam 781101, India.
J Control Release. 2022 Sep;349:460-474. doi: 10.1016/j.jconrel.2022.07.014. Epub 2022 Jul 18.
The unique interfacial properties, huge diversity, and biocompatible nature of phospholipids make them an attractive pharmaceutical excipient. The amphiphilic nature of these molecules offers them the property to self-assemble into distinct structures. The solubility, chemical and structural properties, surface charge, and critical packing parameters of phospholipids play an essential role during formulation design. This review focuses on the relationship between the structural features of a phospholipid molecule and the formation of different lipid-based nanocarrier drug delivery systems. This provides a rationale and guideline for the selection of appropriate phospholipids while designing a drug delivery system. Finally, we refer to relevant recent case studies covering different types of phospholipid-based systems including simple to complex assemblies. Different carriers in the size range of 50 nm to a few microns can be prepared using phospholipids. The carriers can be delivered through oral, intravenous, nasal, dermal, transmucosal, and subcutaneous routes. A wide range of applicability can be achieved by incorporating various hydrophilic and lipophilic additives in the phospholipid bilayer. Advanced research has led to the discovery of phospholipid complexes and cell membrane mimicking lipids. Overall, phospholipids remain a versatile pharmaceutical excipient for drug delivery. They play multiple roles as solubilizer, emulsifier, surfactant, permeation enhancer, coating agent, release modifier, and liposome former.
磷脂具有独特的界面性质、巨大的多样性和生物相容性，使其成为一种有吸引力的药物辅料。这些分子的两亲性使它们具有自组装成不同结构的特性。磷脂的溶解度、化学和结构性质、表面电荷和临界堆积参数在配方设计中起着重要作用。本综述重点介绍了磷脂分子的结构特征与不同脂质纳米载体药物传递系统形成之间的关系。这为选择合适的磷脂提供了依据和指导，为设计药物传递系统提供了依据和指导。最后，我们参考了涵盖不同类型磷脂基系统的相关最新案例研究，包括简单到复杂的组合。可以使用磷脂制备不同尺寸范围在 50nm 到几微米之间的不同载体。载体可以通过口服、静脉内、鼻内、皮内、经粘膜和皮下途径给药。通过在磷脂双层中加入各种亲水性和疏水性添加剂，可以实现广泛的适用性。先进的研究导致了磷脂复合物和细胞膜模拟脂质的发现。总的来说，磷脂仍然是一种用于药物传递的多功能药物辅料。它们作为增溶剂、乳化剂、表面活性剂、渗透增强剂、包衣剂、释放调节剂和脂质体形成剂发挥着多种作用。
