International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2021-08-13 , DOI: 10.1016/j.ijpharm.2021.121007 Jiajie Hu 1 , Zhuoyao Ni 1 , Hui Zhu 2 , Hanglin Li 1 , Yinghong Chen 3 , Yazhuo Shang 1 , Daijie Chen 2 , Honglai Liu 1
Liquid crystals (LCs) are widely used for drug delivery due to their controlled and sustained drug release properties. In this paper, drug crystallization encapsulated liquid crystal emulsion, a novel drug delivery system, was proposed. The lamellar liquid crystals formed by hydrogenated lecithin, which are similar to the skin stratum corneum lipid structure, are adopted as the drug carrier to encapsulate non-steroidal anti-inflammatory drugs (NSAIDs). As the model drug, ketoprofen exists in the hydrophobic core of emulsion as a drug crystal when squalane is used as the oil phase. The microstructure, sustained drug release behaviors, physicochemical property and biocompatibility of the system were examined by polarized light microscopy, rheological measurements, differential scanning calorimetry, X-ray diffraction, small-angle X-ray scattering, in vitro release study, and in vitro cellular cytotoxicity assay. The results have shown that the novel system lowers the drug crystal melting point and improves the thermal stability of liquid crystal structure. Besides, the excellent biocompatibility and sustained release property through the additional dissolution step of drug crystal show its application potentials in the topical cosmeceuticals. The results will also be helpful for in-depth understanding of the physical state of encapsulated drug in the liquid crystal carrier systems.
中文翻译:
一种新型给药系统——药物结晶包封液晶乳液
液晶 (LC) 因其可控和持续的药物释放特性而被广泛用于药物递送。在本文中,提出了一种新型药物递送系统——药物结晶包封液晶乳液。采用氢化卵磷脂形成的层状液晶,类似于皮肤角质层脂质结构,作为药物载体包裹非甾体抗炎药(NSAIDs)。作为模型药物,当使用角鲨烷作为油相时,酮洛芬以药物晶体的形式存在于乳剂的疏水核中。通过偏光显微镜、流变测量、差示扫描量热法、X射线衍射、小角X射线散射、体外释放研究和体外细胞毒性试验。结果表明,新体系降低了药物晶体的熔点,提高了液晶结构的热稳定性。此外,通过药物晶体的额外溶解步骤,优异的生物相容性和缓释性能显示出其在外用药妆品中的应用潜力。该结果也将有助于深入了解液晶载体系统中包封药物的物理状态。通过药物晶体的额外溶解步骤,优异的生物相容性和缓释性能显示了其在外用药妆品中的应用潜力。该结果也将有助于深入了解液晶载体系统中包封药物的物理状态。通过药物晶体的额外溶解步骤,优异的生物相容性和缓释性能显示了其在外用药妆品中的应用潜力。该结果也将有助于深入了解液晶载体系统中包封药物的物理状态。