Microparticles prepared from sulfenamide-based polymers.
Microparticles prepared from sulfenamide-based polymers.
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DOI：
10.3109/02652048.2013.814728
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发表时间：
2014
影响因子：
3.9
通讯作者：
Salem AK
中科院分区：
文献类型：
--
作者：
D'Mello SR;Yoo J;Bowden NB;Salem AK
聚亚磺酰胺（PSN）是一类新型的生物可降解和生物相容性高分子，其主链上沿着有一个SN键（RSNR 2）。这些聚合物在2012年之前是未知的，当时报道了它们的合成和医学相关性质。本研究的目的是开发微粒作为药物控释系统使用聚亚磺酰胺作为基质材料。通过水包油包水双乳液溶剂蒸发法制备微粒。为了生产载药颗粒，使用FITC-葡聚糖作为模型亲水性化合物。在最佳配方条件下，通过扫描电子显微镜检查PSN微粒的外部形态，以显示具有低多分散性的光滑表面的球形颗粒的形成。通过Zetasizer分析，微粒具有净负表面电荷（-23 mV）。发现颗粒的药物包封效率和药物负载取决于药物分子量、用于制造FITC-葡聚糖负载的微粒的FITC-葡聚糖的量、PSN和表面活性剂的浓度以及内部和外部水相的体积。发现FITC-葡聚糖分布在整个PSN微粒中，并且以初始爆发释放，随后随着时间的推移更连续地释放。共聚焦激光扫描显微镜用于定性观察PSN微粒的细胞摄取，并指示颗粒在细胞质和细胞核中的定位。
Polysulfenamides (PSN), with a SN linkage (RSNR2) along the polymer backbone, are a new class of biodegradable and biocompatible polymers. These polymers were unknown prior to 2012 when their synthesis and medicinally relevant properties were reported. The aim of this study was to develop microparticles as a controlled drug delivery system using polysulfenamide as the matrix material. The microparticles were prepared by a water-in-oil-in-water double emulsion solvent evaporation method. For producing drug-loaded particles, FITC-dextran was used as a model hydrophilic compound. At the optimal formulation conditions, the external morphology of the PSN microparticles was examined by scanning electron microscopy to show the formation of smooth-surfaced spherical particles with low polydispersity. The microparticles had a net negative surface charge (−23 mV) as analyzed by the zetasizer. The drug encapsulation efficiency of the particles and the drug loading were found to be dependent on the drug molecular weight, amount of FITC-dextran used in fabricating FITC-dextran loaded microparticles, concentration of PSN and surfactant, and volume of the internal and external water phases. FITC-dextran was found to be distributed throughout the PSN microparticles and was released in an initial burst followed by more continuous release over time. Confocal laser scanning microscopy was used to qualitatively observe the cellular uptake of PSN microparticles and indicated localization of the particles in both the cytoplasm and the nucleus.