Nita Loredana E, Chiriac Aurica P, Mititelu-Tartau Liliana, Stoleru Elena, Doroftei Florica, Diaconu Alina
"Petru Poni" Institute of Macromolecular Chemistry, 41A Grigore Ghica Voda Alley, 700487 Iasi, Romania.
"Petru Poni" Institute of Macromolecular Chemistry, 41A Grigore Ghica Voda Alley, 700487 Iasi, Romania.
Int J Pharm. 2015 Sep 30;493(1-2):328-40. doi: 10.1016/j.ijpharm.2015.07.061. Epub 2015 Jul 26.
Owing to the special characteristics and abilities polymeric networks have received special interest for a range of biomedical applications especially for drug delivery systems. This study was devoted to preparation of new polymeric compounds based on maleic anhydride and 3,9-divinyl-2,4,8,10-tetraoxaspiro (5.5) undecane copolymer (poly maleic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro (5.5) undecane) (PMAU) patterned as a network for bioconjugation and tested as drug carrier systems. The PMAU copolymer was improved in its functionality by opening the maleic anhydride ring with different amounts of erythritol, which is free of side effects in regular use and a multifunctional compound, and also confers antioxidant character for the new compounds. The new polymeric matrices were loaded with acetaminophen, codeine and their fixed dose combinations. The investigation demonstrated the capability of the new structures to be used as polymer networks for linking bioactive compounds and to perform controlled delivery. The physico-chemical investigations--Fourier transform infrared spectroscopy (FTIR) spectra, contact angle, zeta potential (ZP - z, PMAU and its derivatives samples loaded with medicines present decreased values of zeta potential attesting the bioconjugate formation and as well their stability), and hydrodynamic radius, near infrared chemical imaging evaluation (new specific bands being registered for bio-conjugate with acetaminophen around of 1150-1200 nm and 1700 nm, and also between 1150 and 1200 nm in case of the codeine bio-conjugate), scanning electron microscopy (SEM) studies, X-ray diffraction analysis--evidenced the formation of the bioconjugates in relation to the chemical composition of the polymer matrices, while in vitro release study and in vivo tests confirm the capacity for drug delivery of the prepared bioactive systems.
由于聚合物网络具有特殊的特性和能力，它们在一系列生物医学应用中，特别是药物递送系统方面受到了特别关注。本研究致力于基于马来酸酐和3,9 - 二乙烯基 - 2,4,8,10 - 四氧杂螺[5.5]十一烷共聚物（聚马来酸酐 - 共 - 3,9 - 二乙烯基 - 2,4,8,10 - 四氧杂螺[5.5]十一烷）（PMAU）制备新型聚合物化合物，该聚合物呈网络状用于生物共轭，并作为药物载体系统进行测试。通过用不同量的赤藓糖醇打开马来酸酐环来改善PMAU共聚物的功能，赤藓糖醇在常规使用中无副作用且是一种多功能化合物，还赋予新化合物抗氧化特性。新的聚合物基质负载了对乙酰氨基酚、可待因及其固定剂量组合。研究表明，这些新结构有能力用作连接生物活性化合物的聚合物网络并实现控释。物理化学研究——傅里叶变换红外光谱（FTIR）光谱、接触角、zeta电位（ZP - z，负载药物的PMAU及其衍生物样品的zeta电位值降低，证明了生物共轭物的形成及其稳定性）、流体动力学半径、近红外化学成像评估（对乙酰氨基酚生物共轭物在1150 - 1200 nm和1700 nm附近记录到新的特定谱带，可待因生物共轭物在1150和1200 nm之间也有）、扫描电子显微镜（SEM）研究、X射线衍射分析——证明了与聚合物基质化学成分相关的生物共轭物的形成，而体外释放研究和体内试验证实了所制备的生物活性系统的药物递送能力。
