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首页> 外文期刊>Journal of biomedical materials research. Part B, Applied biomaterials. >In Vitro Tobramycin Elution Analysis from a Novel beta-Tricalcium Phosphate-Silicate-Xerogel Biodegradable Drug-Delivery System
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In Vitro Tobramycin Elution Analysis from a Novel beta-Tricalcium Phosphate-Silicate-Xerogel Biodegradable Drug-Delivery System

机译：新型β-磷酸三钙-硅酸盐-干凝胶生物可降解药物递送系统的妥布霉素体外洗脱分析

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摘要

This in vitro research analyzed local tobramycin elution characteristics from a novel, biodegradable drug delivery system, consisting of a beta-TCP bone substitute, VITOSS~(TM), encapsulated with silicate xerogel prepared by the sol-gel process. Tobramycin elution from silicate-xerogel-encapsulated VITOSS was compared directly with non-silicate-xerogel-encap-sulated VITOSS to assess whether xerogels are effective in delivering greater tobramycin quantities in a controllable, sustained manner crucial for microbial inhibition. Tobramycin elution characteristics indicate an initial release maximum during the first 24 h that diminishes gradually several days after impregnation. The copious tobramycin quantity eluted from the VITOSS/silicate-xerogel systems is attributed to various factors: the intrinsic ultraporosity and hydrophilicity of VITOSS, the ability of tobramycin to completely dissolve in aqueous media, tobramycin complexation with highly polar SO_4~(-2) salts that further assist dissolution, and ionic exchanges between VITOSS and the environment. Silicate-xerogel-encapsulated VITOSS eluted 60.65 and 61.31 percent of impregnated tobramycin, whereas non-silicate-xerogel-encapsulated VITOSS eluted approximately one-third less impregnated tobramycin, at 21.53 and 23.60 percent. These results suggest that silicate xerogel optimizes tobramycin elution because of its apparent biodegradability. This mechanism occurs through xerogel superficial acidic sites undergoing exchanges with various ions present in the leaching buffer. Tobramycin elution kinetics were evaluated, and demonstrate that first-order elution rate constants are considerably less when silicate xerogels are employed, following a more uniform exponential decay-type mechanism, thus bolstering controlled release. Overall, tobramycin elution rates adhere to linear-type Higuchi release profiles. Elution rate constants are initially first order, and taper into zero-order elution kinetics in the latter stages of release. Because VITOSS and silicate xerogel are completely biodegradable, essentially all impregnated tobramycin will be delivered to the surgical site after implantation.
机译：这项体外研究分析了一种新型的可生物降解的药物递送系统的局部妥布霉素洗脱特性，该系统由β-TCP骨替代物VITOSS〜（TM）组成，并通过溶胶-凝胶法制备了硅酸盐干凝胶。将硅酸盐-干凝胶包封的VITOSS中的妥布霉素洗脱液与非硅酸盐-干凝胶包封的VITOSS直接进行比较，以评估干凝胶是否以可控制的，持续的方式有效递送更大的妥布霉素量，这对于抑制微生物至关重要。妥布霉素的洗脱特性表明，最初的最大释放量在最初的24小时内最大，在浸渍后数天逐渐减少。从VITOSS /硅酸盐-干凝胶系统中洗脱的妥布霉素的量归因于多种因素：VITOSS固有的超孔隙度和亲水性，妥布霉素在水性介质中的完全溶解能力，妥布霉素与高极性SO_4〜（-2）盐的络合进一步帮助溶解，以及VITOSS与环境之间的离子交换。硅酸盐干凝胶包封的VITOSS洗脱了60.65％和61.31％的浸渍妥布霉素，而非硅酸盐干凝胶包封的VITOSS洗脱了大约三分之一的浸渍妥布霉素，分别为21.53和23.60％。这些结果表明，硅酸盐干凝胶具有明显的生物降解性，因此可以优化妥布霉素的洗脱。这种机制是通过干凝胶表面的酸性位点与浸出缓冲液中存在的各种离子交换而发生的。对妥布霉素的洗脱动力学进行了评估，结果表明，采用硅酸盐干凝胶时，一阶洗脱速率常数要小得多，遵循更均匀的指数衰减型机理，从而增强了控释作用。总体而言，妥布霉素的洗脱速率符合线性型Higuchi释放曲线。洗脱速率常数最初是一阶的，在释放的后期逐渐变为零级洗脱动力学。由于VITOSS和硅酸盐干凝胶是完全可生物降解的，因此植入后基本上所有浸渍的妥布霉素都将被递送至手术部位。

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