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两种皮质类固醇药物存在下硅橡胶的固化行为。

Curing behavior of silicone elastomer in the presence of two corticosteroid drugs.

机构信息

Novel Drug Delivery Systems Department, Iran Polymer and Petrochemical Institute, Tehran, Iran.

出版信息

J Biomed Mater Res B Appl Biomater. 2012 Aug;100(6):1636-44. doi: 10.1002/jbm.b.32732. Epub 2012 Jun 16.

Abstract

Silicone rubbers are widely used as carriers for delivery of drugs intended for parenteral administration as implantable devices. Drugs having different functional groups can significantly affect curing profile of silicone rubber, which in turn may negatively affect their biological applicability due to the loss in mechanical and drug retaining properties. To this end, the effects of two corticosteroid analogs (up to 2 %w/w of drug loading) that is, dexamethasone (DEX) and its sodium phosphate ester (DSP) on curing behavior of a non-restricted, two part RTV silicone rubber was studied using different characterization techniques including spectroscopic (FTIR), calorimetric (DSC), oscillating disk rheometry, and swelling studies. The results showed that curing time extends longer for DSP-loaded samples compared to the non-loaded silicone rubber. The presence of DSP in the formulation interferes in the curing of silicone elastomers, probably due to the thermal decomposition of DSP according to the spectral changes observed in FTIR spectra as confirmed by DSC analysis. Rheometric studies showed depreciated properties for silicone elastomers upon compounding with DSP. Swelling measurements indicated to lowered crosslink density for networks and increasing M(c) upon adding DSP to the formulations which can be attributed to disruption in crosslinking reaction by sodium phosphate moieties of DSP.

摘要

硅橡胶作为药物传递载体,广泛应用于可植入的药物给药系统。具有不同官能团的药物会显著影响硅橡胶的固化特性,从而可能由于机械性能和药物保持性能的丧失而对其生物适用性产生负面影响。为此,研究了两种皮质类固醇类似物(高达 2%w/w 的药物负载),即地塞米松(DEX)及其磷酸酯钠盐(DSP),对非限制、双组分 RTV 硅橡胶固化行为的影响,采用了不同的表征技术,包括光谱学(FTIR)、量热法(DSC)、振荡圆盘流变学和溶胀研究。结果表明,与未负载硅橡胶相比,DSP 负载样品的固化时间更长。DSP 的存在会干扰硅橡胶弹性体的固化,这可能是由于 DSP 按照 FTIR 光谱中观察到的光谱变化进行热分解,这一点通过 DSC 分析得到了证实。流变学研究表明,DSP 与硅橡胶共混后,硅橡胶的性能有所下降。溶胀测量表明,DSP 的加入降低了网络的交联密度和 M(c),这可能归因于 DSP 的磷酸酯部分对交联反应的破坏。

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