Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Int J Mol Sci. 2022 Oct 18;23(20):12487. doi: 10.3390/ijms232012487.
To improve liposomes' usage as drug delivery vehicles, cryoprotectants can be utilized to prevent constituent leakage and liposome instability. Cryoprotective agents (CPAs) or cryoprotectants can protect liposomes from the mechanical stress of ice by vitrifying at a specific temperature, which forms a glassy matrix. The majority of studies on cryoprotectants demonstrate that as the concentration of the cryoprotectant is increased, the liposomal stability improves, resulting in decreased aggregation. The effectiveness of CPAs in maintaining liposome stability in the aqueous state essentially depends on a complex interaction between protectants and bilayer composition. Furthermore, different types of CPAs have distinct effective mechanisms of action; therefore, the combination of several cryoprotectants may be beneficial and novel attributed to the synergistic actions of the CPAs. In this review, we discuss the use of liposomes as drug delivery vehicles, phospholipid-CPA interactions, their thermotropic behavior during freezing, types of CPA and their mechanism for preventing leakage of drugs from liposomes.
为了提高脂质体作为药物传递载体的应用，可使用冷冻保护剂来防止成分泄漏和脂质体不稳定。冷冻保护剂（CPA）或冷冻保护剂可以通过在特定温度下玻璃化来保护脂质体免受冰的机械应力，形成玻璃基质。大多数关于冷冻保护剂的研究表明，随着冷冻保护剂浓度的增加，脂质体的稳定性提高，聚集减少。CPA 在维持水相中脂质体稳定性方面的有效性主要取决于保护剂与双层组成之间的复杂相互作用。此外，不同类型的 CPAs 具有不同的有效作用机制；因此，几种冷冻保护剂的组合可能是有益的和新颖的，因为 CPAs 具有协同作用。在这篇综述中，我们讨论了脂质体作为药物传递载体的用途、磷脂-CPA 相互作用、它们在冷冻过程中的热致行为、CPA 的类型及其防止药物从脂质体中泄漏的机制。
