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Development of controlled release silicone adhesive–based mupirocin patch demonstrates antibacterial activity on live rat skin against Staphylococcus aureus

机译:基于控释有机硅粘合剂的莫匹罗星贴剂的开发证明了对活大鼠皮肤的抗金黄色葡萄球菌的活性

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Background: Peritonitis is the most serious complication of peritoneal dialysis. Staphylococcus aureus infections could lead to peritonitis which causes reversal of peritoneal dialysis treatment back to hemodialysis. The aim of this study was to develop a controlled release silicone adhesive-based mupirocin patch for prophylactic effect and analyze its antibacterial effectiveness against S. aureus . Methods: The matrix patches were prepared by using different polymers, with and without silicone adhesive, dibutyl sebacate and mupirocin. The patches were characterized for mechanical properties, drug content, moisture content, water absorption capacity and Fourier transform infrared spectrum. In vitro release studies were performed by using Franz diffusion cell. In?vitro disk diffusion assay was performed on the Mueller–Hinton Agar plate to measure the zone of inhibition of the patches. The in vivo study was performed on four groups of rats with bacterial counts at three different time intervals, along with skin irritancy and histopathologic studies. Results: The patches showed appropriate average thickness (0.63–1.12 mm), tensile strength (5.08–10.08 MPa) and modulus of elasticity (21.53–42.19 MPa). The drug content ranged from 94.5% to 97.4%, while the moisture content and water absorption capacities at two relative humidities (75% and 93%) were in the range of 1.082–3.139 and 1.287–4.148 wt%, respectively. Fourier transform infrared spectra showed that there were no significant interactions between the polymer and the drug. The highest percentage of drug release at 8 hours was 47.94%. The highest zone of inhibition obtained was 28.3 mm against S. aureus . The in vivo studies showed that the bacterial colonies were fewer at 1 cm (7×101 CFU/mL) than at 2 cm (1.3×102 CFU/mL) over a 24-hour period. The patches were nonirritant to the skin, and histopathologic results also showed no toxic or damaging effects to the skin. Conclusion: The in vitro and in vivo studies indicated that controlled release patches reduced the migration of S. aureus on the live rat skin effectively, however, a longer duration of study is required to determine the effectiveness of the patch on a suitable peritonitis-induced animal model.
机译:背景:腹膜炎是腹膜透析最严重的并发症。金黄色葡萄球菌感染可能导致腹膜炎,导致腹膜透析治疗逆转回到血液透析。这项研究的目的是开发一种基于控释的有机硅粘合剂的莫匹罗星贴剂,具有预防作用,并分析其对金黄色葡萄球菌的抗菌效果。方法:使用不同的聚合物(有无硅酮粘合剂,癸二酸二丁酯和莫匹罗星)制备基质贴剂。对贴剂的机械性能,药物含量,水分含量,吸水率和傅立叶变换红外光谱进行了表征。通过使用Franz扩散池进行体外释放研究。在Mueller-Hinton琼脂平板上进行体外圆盘扩散测定,以测量斑块的抑制区域。体内研究是在四组大鼠中进行的,细菌的计数在三个不同的时间间隔进行,同时还有皮肤刺激性和组织病理学研究。结果:贴片显示适当的平均厚度(0.63–1.12 mm),抗张强度(5.08–10.08 MPa)和弹性模量(21.53–42.19 MPa)。药物含量在94.5%至97.4%之间,而在两个相对湿度(75%和93%)下的水分含量和吸水量分别在1.082–3.139和1.287–4.148 wt%的范围内。傅里叶变换红外光谱表明,聚合物与药物之间没有明显的相互作用。 8小时的最高药物释放百分比为47.94%。获得的对金黄色葡萄球菌的最高抑制区为28.3 mm。体内研究表明,细菌菌落在1 cm(7×10 1 CFU / mL)少于2 cm(1.3×10 2 CFU / mL)在24小时内。贴剂对皮肤无刺激性,组织病理学结果也显示对皮肤没有毒性或破坏性作用。结论:体外和体内研究表明,控释贴剂有效地减少了金黄色葡萄球菌在活大鼠皮肤上的迁移,但是,需要更长的研究时间才能确定该贴剂在合适的腹膜炎诱导下的有效性。动物模型。

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