Oh Seoeun, Park Soo-Yong, Seo Hyung Il, Chung Ildoo
Department of Polymer Science and Engineering, Pusan National University, Busan 46241, Republic of Korea.
Department of Surgery, Biomedical Research Institute, Pusan National University Hospital, Pusan National University School of Medicine, Busan 49241, Republic of Korea.
Pharmaceutics. 2024 Dec 27;17(1):28. doi: 10.3390/pharmaceutics17010028.
The use of polymeric nanoparticles (NPs) in drug delivery systems offers the advantages of enhancing drug efficacy and minimizing side effects; In this study, L-threonine polyurethane (LTPU) NPs have been fabricated by water-in-oil-in-water emulsion and solvent evaporation using biodegradable and biocompatible LTPU. This polymer was pre-synthesized through the use of an amino acid-based chain extender, desaminotyrosyl L-threonine hexyl ester (DLTHE), where urethane bonds are formed by poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) triblock copolymer and 1,6-hexamethylene diisocyanate (HDI). LTPU is designed to be degraded by hydrolysis and enzymatic activity due to the presence of ester bonds and peptide bonds within the polymer backbone. LTPU NPs were fabricated by water-in-oil-in-water double emulsion solvent evaporation methods; The polymerization of LTPU was confirmed by H-NMR, C-NMR, and FT-IR spectroscopies. The molecular weights and polydispersity, determined with GPC, were 28,800 g/mol and 1.46, respectively. The morphology and size of NPs, characterized by DLS, FE-SEM, TEM, and confocal microscopy, showed smooth and spherical particles with diameters less than 200 nm; In addition, the drug loading, encapsulation efficiency, and drug release profiles, using UV-Vis spectroscopy, showed the highest encapsulation efficiency with 2.5% carboplatin and sustained release profile.
在药物递送系统中使用聚合物纳米颗粒（NPs）具有提高药物疗效和最小化副作用的优点；在本研究中，通过水包油包水乳液和溶剂蒸发法，使用可生物降解且生物相容的L - 苏氨酸聚氨酯（LTPU）制备了LTPU NPs。该聚合物是通过使用基于氨基酸的扩链剂脱氨酪氨酸L - 苏氨酸己酯（DLTHE）预合成的，其中氨基甲酸酯键由聚（乳酸）-聚（乙二醇）-聚（乳酸）（PLA - PEG - PLA）三嵌段共聚物和1,6 - 六亚甲基二异氰酸酯（HDI）形成。由于聚合物主链中存在酯键和肽键，LTPU被设计为可通过水解和酶活性降解。LTPU NPs通过水包油包水双乳液溶剂蒸发法制备；通过H - NMR、C - NMR和FT - IR光谱确认了LTPU的聚合。用凝胶渗透色谱法测定的分子量和多分散性分别为28,800 g/mol和1.46。通过动态光散射（DLS）、场发射扫描电子显微镜（FE - SEM）、透射电子显微镜（TEM）和共聚焦显微镜表征的NPs的形态和尺寸显示，颗粒光滑且呈球形，直径小于200 nm；此外，使用紫外 - 可见光谱法测定的载药量、包封率和药物释放曲线显示，对于2.5%的卡铂，包封率最高且具有缓释曲线。
