Department of Pharmaceutics, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, India.
J Liposome Res. 2023 Mar;33(1):1-33. doi: 10.1080/08982104.2022.2069809. Epub 2022 May 11.
Phospholipids have a high degree of biocompatibility and are deemed ideal pharmaceutical excipients in the development of lipid-based drug delivery systems, because of their unique features (permeation, solubility enhancer, emulsion stabilizer, micelle forming agent, and the key excipients in solid dispersions) they can be used in a variety of pharmaceutical drug delivery systems, such as liposomes, phytosomes, solid lipid nanoparticles, etc. The primary usage of phospholipids in a colloidal pharmaceutical formulation is to enhance the drug's bioavailability with low aqueous solubility [i.e. Biopharmaceutical Classification System (BCS) Class II drugs], Membrane penetration (i.e. BCS Class III drugs), drug uptake and release enhancement or modification, protection of sensitive active pharmaceutical ingredients (APIs) from gastrointestinal degradation, a decrease of gastrointestinal adverse effects, and even masking of the bitter taste of orally delivered drugs are other uses. Phospholipid-based colloidal drug products can be tailored to address a wide variety of product requirements, including administration methods, cost, product stability, toxicity, and efficacy. Such formulations that are also a cost-effective method for developing medications for topical, oral, pulmonary, or parenteral administration. The originality of this review work is that we comprehensively evaluated the unique properties and special aspects of phospholipids and summarized how the individual phospholipids can be utilized in various types of lipid-based drug delivery systems, as well as listing newly marketed lipid-based products, patents, and continuing clinical trials of phospholipid-based therapeutic products. This review would be helpful for researchers responsible for formulation development and research into novel colloidal phospholipid-based drug delivery systems.
磷脂具有高度的生物相容性，被认为是脂质药物传递系统开发中的理想药用辅料，因为其独特的特性（渗透、增溶、乳化稳定剂、胶束形成剂和固体分散体的关键辅料），它们可以用于多种药物传递系统，如脂质体、植物磷脂体、固体脂质纳米粒等。磷脂在胶体药物制剂中的主要用途是提高低水溶性药物的生物利用度[即生物药剂学分类系统（BCS）Ⅱ类药物]、膜穿透性（即 BCS Ⅲ类药物）、增强药物摄取和释放、保护敏感的活性药物成分（APIs）免受胃肠道降解、减少胃肠道不良反应，甚至掩盖口服药物的苦味。基于磷脂的胶体药物产品可以根据各种产品需求进行定制，包括给药方式、成本、产品稳定性、毒性和疗效。对于局部、口服、肺部或肠胃外给药的药物开发来说，这些制剂也是一种具有成本效益的方法。本综述工作的创新性在于，我们全面评估了磷脂的独特性质和特殊方面，并总结了如何将各种类型的磷脂用于不同类型的脂质药物传递系统，以及列出了新上市的脂质产品、专利和正在进行的基于磷脂的治疗产品的临床试验。这篇综述将有助于负责制剂开发和研究新型胶体磷脂药物传递系统的研究人员。
