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新型微结构西地那非剂型作为伤口愈合促进剂。

Novel microstructured sildenafil dosage forms as wound healing promoters.

作者信息

Samy Wael M, Ghoneim Asser I, Elgindy Nazik A

机构信息

Alexandria University, Department of Industrial Pharmacy, Faculty of Pharmacy , Alexandria , Egypt +2 03 3630 815 ; +2 03 4873 273 ;

出版信息

Expert Opin Drug Deliv. 2014 Oct;11(10):1525-36. doi: 10.1517/17425247.2014.929662. Epub 2014 Jun 18.

DOI:10.1517/17425247.2014.929662
PMID:24940608
Abstract

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 P₁. 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.

摘要

目的

研究将可生物降解聚合物与枸橼酸西地那非(SC)联合用于伤口愈合的潜在益处。

方法

采用壳聚糖(P₁)或壳聚糖/阿拉伯胶(P₂)通过喷雾干燥制备SC的可生物降解微粉化制剂。通过差示扫描量热法、扫描电子显微镜、粒度分析、流动性和溶胀行为对粉末进行表征。将粉末掺入微结构凝胶中,并测试粉末和凝胶中SC的体外释放。通过测量切除伤口的面积收缩并进行组织学检查来测试体内伤口愈合加速情况。对接受粉末制剂的大鼠切口伤口愈合后的抗张强度(TS)进行测试。

结果

粉末处于微米尺寸范围,未显示出SC与聚合物的相互作用。粉末流动性差,休止角(θ)为41 - 48°,安慰剂粉末P₁的吸湿率高达107%。P1和G1制剂显示出良好的切除伤口愈合效果,伤口面积分别减少了98.4%和98.5%,而对照组为83%。P1改善了切口伤口,其TS值为6.9,而对照组为3.7 kg/cm²。组织学检查提供了支持。

结论

组织学检查表明,喷雾干燥的壳聚糖/SC粉末(P₁)及其凝胶形式(G₁)有望成为伤口愈合促进剂。

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