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Combined effects of drugs and plasticizers on the properties of drug delivery films
Journal of Bioactive and Compatible Polymers ( IF 1.7 ) Pub Date : 2016-02-16 , DOI: 10.1177/0883911515627178
Cheryl L Jennings 1 , Thomas D Dziubla 2 , David A Puleo 1
Affiliation  

Formation of scar tissue may be reduced or prevented if wounds are locally treated with a combination of molecules tuned to the different healing phases, guiding tissue regeneration along a scar free path. To this end, drug delivery devices made of cellulose acetate phthalate and Pluronic F-127 were loaded with either quercetin or pirfenidone and plasticized with either triethyl citrate or tributyl citrate. Quercetin inhibits oxidative stress, and pirfenidone has been shown to reduce production of pro-inflammatory and fibrogenic molecules. The combined effects of drug and plasticizer on erosion, release, and mechanical properties of the drug delivery films were investigated. Triethyl citrate-plasticized films containing quercetin released drug at a slower rate than did tributyl citrate films. Pirfenidone-loaded films released drug at a faster rate than erosion occurred for both types of plasticizers. Higher plasticizer contents of both triethyl citrate and tributyl citrate increased the elongation and decreased the elastic modulus. In contrast, increased pirfenidone loading in both triethyl citrate and tributyl citrate films resulted in a significantly higher modulus, an antiplasticizer effect. Adding pirfenidone significantly decreased elongation for all film types, but quercetin-loaded samples had significantly greater elongation with increasing drug content. Films containing quercetin elongated more than did pirfenidone-loaded films. Quercetin is over 1.5 times larger than pirfenidone, has water solubility over 12 times lower, and has 6 times more bonding sites than pirfenidone. These differences affected how the two drugs interacted with cellulose acetate phthalate and Pluronic F-127 and thereby determined polymer properties. Drug release, erosion, and mechanical properties of association polymer films can be tailored by the characteristics of the drugs and plasticizers included in the system.

中文翻译:

药物和增塑剂对给药薄膜性能的综合影响

如果用针对不同愈合阶段的分子组合局部治疗伤口,引导组织沿无疤痕路径再生,则可以减少或防止疤痕组织的形成。为此,由邻苯二甲酸醋酸纤维素和 Pluronic F-127 制成的给药装置装载有槲皮素或吡非尼酮,并用柠檬酸三乙酯或柠檬酸三丁酯增塑。槲皮素抑制氧化应激,吡非尼酮已被证明可以减少促炎和纤维化分子的产生。研究了药物和增塑剂对药物递送膜的侵蚀、释放和机械性能的综合影响。含有槲皮素的柠檬酸三乙酯增塑薄膜比柠檬酸三丁酯薄膜释放药物的速度更慢。装载吡非尼酮的薄膜以比两种增塑剂发生的侵蚀更快的速度释放药物。柠檬酸三乙酯和柠檬酸三丁酯的较高增塑剂含量增加了伸长率并降低了弹性模量。相比之下,柠檬酸三乙酯和柠檬酸三丁酯薄膜中吡非尼酮负载量的增加导致显着更高的模量,一种抗增塑剂效果。添加吡非尼酮可显着降低所有薄膜类型的伸长率,但载有槲皮素的样品随着药物含量的增加,伸长率显着提高。含有槲皮素的薄膜比载有吡非尼酮的薄膜伸长得更多。槲皮素比吡非尼酮大 1.5 倍以上,水溶性比吡非尼酮低 12 倍以上,结合位点是吡非尼酮的 6 倍。这些差异影响了这两种药物如何与邻苯二甲酸醋酸纤维素和 Pluronic F-127 相互作用,从而决定了聚合物的特性。缔合聚合物薄膜的药物释放、侵蚀和机械性能可以根据系统中包含的药物和增塑剂的特性进行调整。
更新日期:2016-02-16
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