The Institute of Nanotechnology and Advanced Materials, Department of Chemistry, Bar-Ilan University, Ramat-Gan 5290002, Israel.
Pre-Clinical Research Center: Faculty of Life Sciences, Bar-Ilan University, Ramat-Gan 5290002, Israel.
Molecules. 2020 Sep 2;25(17):4013. doi: 10.3390/molecules25174013.
Risperidone (RSP) is an atypical antipsychotic drug widely used to treat schizophrenia and bipolar disorder. Nanoparticles (NPs) are being developed as in vivo targeted drug delivery systems, which cross the blood-brain barrier and improve pharmacokinetics and drug effectiveness. Here, biodegradable proteinoids were synthesized by thermal step-growth polymerization from the amino acids l-glutamic acid, l-phenylalanine and l-histidine and poly (l-lactic acid). Proteinoid NPs containing RSP were then formed by self-assembly, overcoming the insolubility of the drug in water, followed by PEGylation (poly ethylene glycol (PEG) conjugation to increase the stability of the NPs in the aqueous continuous phase. These NPs are biodegradable owing to their peptide and ester moieties. They were characterized in terms of diameter, size distribution, drug loading, and long-term storage. Behavioral studies on mice found enhanced antipsychotic activity compared to free RSP.
利培酮（RSP）是一种广泛用于治疗精神分裂症和双相情感障碍的非典型抗精神病药物。纳米颗粒（NPs）正在被开发为体内靶向药物递送系统，以穿越血脑屏障并改善药代动力学和药物功效。在这里，通过氨基酸 l-谷氨酸、l-苯丙氨酸和 l-组氨酸与聚（l-乳酸）的热逐步聚合合成了可生物降解的蛋白原。然后通过自组装形成含有 RSP 的蛋白原 NPs，克服了药物在水中的不溶性，随后进行 PEG 化（聚乙二醇（PEG）缀合以增加 NPs 在水连续相中的稳定性。这些 NPs 由于其肽和酯部分而具有生物降解性。对其粒径、粒径分布、载药量和长期储存进行了表征。对小鼠的行为研究发现，与游离 RSP 相比，其具有增强的抗精神病活性。
