PLA membranes loaded with dba analogs. Controlled release study during hydrolitic degradation

GA. Alcántara Blanco, N. Urdaneta, M. Sabino
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Abstract

In this research two dibenzylideneacetone (DBA) analogs compounds: (1E,4E)-1-(4-(dimethylamino)phenyl)-5-(4-methoxyphenyl)penta-1,4-dien-3-one (DBA-1) and (1E,4E)-1-(4-methoxyphenyl)-5-(4-nitrophenyl)penta-1,4-dien-3-one (DBA-2) were encapsulated in poly(lactic acid) (PLA) membranes. These DBA analogs can have several applications such as in the development of controlled drug release systems and tissue engineering.  The membranes were elaborated by solvent casting. It was found that these fluorescent compounds have a small percentage of hemolysis in human blood red cells at concentrations between 200-500 µg/mL. Therefore, they can be considered not-toxic at these concentrations. The hydrolytic degradation of PLA membranes loaded with the DBA analogs was studied at a temperature of 37 °C under solutions at acid, neutral, and basic pH conditions for a maximum time of six weeks. The hydrolysis was monitored by measuring the loss of mass of the membranes, changes in pH environments, variations in the molecular weight of PLA matrix, and changes in surface morphology observed through Scanning the Electron Microscopy (SEM) technique. Applying UV-visible spectrophotometry, the amount released from the DBA analogs in the PLA membranes was determined during the degradation time, and finally, the release profile was obtained. It was observed employing SEM that the membranes presented a major degradation under basic pH conditions, with a higher percentage of release in an acid medium for both analogues of DBA studied
PLA膜装载dba类似物。水解降解过程的控释研究
本研究将两种二苄基丙酮(DBA)类似物(1E,4E)-1-(4-(二甲氨基)苯基)-5-(4-甲氧基苯基)- 1,4-二烯-3-one (DBA-1)和(1E,4E)-1-(4-甲氧基苯基)-5-(4-硝基苯基)- 1,4-二烯-3-one (DBA-2)包封在聚乳酸(PLA)膜中。这些DBA类似物可以有几个应用,如在控制药物释放系统和组织工程的发展。采用溶剂铸造法制备膜。发现这些荧光化合物在200-500µg/mL之间的浓度下对人红细胞有小比例的溶血作用。因此,在这些浓度下,它们可以被认为是无毒的。研究了负载DBA类似物的PLA膜在37°C的温度下,在酸性、中性和碱性pH条件下的水解降解时间最长为6周。通过测量膜的质量损失、pH环境的变化、PLA基质分子量的变化以及通过扫描电子显微镜(SEM)技术观察到的表面形貌变化来监测水解过程。采用紫外可见分光光度法测定了DBA类似物在PLA膜中降解时间内的释放量,并得到了释放曲线。通过扫描电镜观察到,在基本的pH条件下,膜呈现出主要的降解,在酸性介质中,DBA的两种类似物的释放率更高
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