Novel microstructured sildenafil dosage forms as wound healing promoters
Novel microstructured sildenafil dosage forms as wound healing promoters
复制标题
作为伤口愈合促进剂的新型微结构西地那非剂型
DOI：
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发表时间：
2014
影响因子：
6.6
通讯作者：
N. Elgindy
中科院分区：
文献类型：
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作者：
W. Samy;A. Ghoneim;N. Elgindy
目的：研究可生物降解聚合物与枸橼酸西地那非（SC）联合应用对伤口愈合的可能益处。方法：以壳聚糖（P1）和壳聚糖/阿拉伯胶（P2）为原料，采用喷雾干燥法制备可生物降解的SC微粉制剂。采用差示扫描量热法、扫描电镜、粒度分析、流动性和溶胀性等对粉体进行了表征。还将粉末掺入微结构凝胶中，并测试粉末和凝胶的体外SC释放。通过测量切除伤口的面积收缩和组织学来测试体内伤口愈合加速。测试接受粉末制剂的大鼠中切口伤口的愈合后拉伸强度（TS）。结果：粉末在微米级范围内，显示没有SC-聚合物相互作用。粉末流动性差，休止角（θ）为41 - 48°，安慰剂粉末Po 1的吸湿性高，达到107%。观察到P1和G1制剂的切除伤口愈合良好，分别显示伤口面积减少98.4%和98.5%，而对照组为83%。切口伤口得到改善，P1显示TS值为6.9，而对照组为3.7 kg/cm 2。支持组织学检查。结论：喷雾干燥壳聚糖/SC粉末（P1）及其凝胶形式（G1）可能是有前途的伤口愈合促进剂，组织学检查支持。
Purpose: Study the possible benefit of combining biodegradable polymers with sildenafil citrate (SC) in wound healing. Method: Biodegradable micronized powdered formulations of SC were prepared by spray drying using chitosan (P1) or chitosan/gum Arabic (P2). Powders were characterized by differential scanning calorimetry, Scanning electron microscope, particle size analysis, flow and swelling behavior. The powders were also incorporated into microstructured gels and in vitro SC release from powders and gels was tested. In vivo wound healing acceleration was tested by measuring area contraction of excision wounds and histologically. Post-healing tensile strength (TS) for incision wounds in rats receiving powder formulations was tested. Results: The powders were in the micron-size range showing no SC–polymers interaction. Powders had poor flow with angle of repose (θ) of 41 – 48°, and high moisture uptake reaching 107% for placebo powder Po1. Good excision wound healing was seen with P1 and G1 formulations showing 98.4 and 98.5% reduction in wound area, respectively, compared with 83% for the control. Incision wounds were improved with P1 showing TS value of 6.9 compared with 3.7 kg/cm2 for control. Histological examinations supported. Conclusion: Spray-dried chitosan/SC powder (P1) and its gel form (G1) could be promising wound healing promoters as supported by the histological examinations.