左氧氟沙星原体皮肤给药凝胶的研制与表征。

Lina Abdel Salam, Mona Abdelmottaleb, A. Geneidi
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引用次数: 2

摘要

左氧氟沙星是一种用于治疗复杂细菌感染的抗菌药物。利用非离子表面活性剂(跨和间)采用凝聚相分离法制备左氧氟沙星负载前质体凝胶。对前质体凝胶的不同参数进行了评价,包括粒径(PS)、zeta电位(ZP)、药物包裹效率(EE%)、体外药物释放和体外渗透研究。实验结果表明,所制配方的EE%范围为32.22±0.86 ~ 54.83±1.17%。左氧氟沙星的包封效果最好。原体的粒径范围为447±204 nm ~ 1089±17 nm。span 20制备的前体凝胶的囊泡大小最小。制备的原体zeta电位范围为20.95±0 mV ~ 60.92±0.09 mV。所得配方的多分散性指数为0.198±3.23 ~ 0.967±0.36。几乎所有的配方在4小时内都显示出从33.028%到97.56%的线性释放曲线。6 h后,80 span的药物沉积水平高于80 span,分别为18.296%和9.44%。稳定性研究表明,左氧氟沙星前体凝胶在贮存3个月后,其EE%、PS、ZP均无明显变化。总之,所研究的前体凝胶制剂作为左氧氟沙星纳米载体的皮肤应用显示出有希望的结果。
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Formulation and Characterization of Proniosomal Gels loaded with Levofloxacin for dermal drug Delivery.
Formulation of proniosomal gels and evaluation of their potential in dermal drug delivery of levofloxacin, an antibacterial drug used to treat complicated bacterial infections. Levofloxacin-loaded proniosomal gels were prepared using coacervation phase separation using nonionic surfactants (spans and tweens). Different parameters of the proniosomal gels were evaluated, including particle size (PS), zeta potential (ZP), drug entrapment efficiency percentage (EE%), in vitro drug release, and ex vivo permeation studies. Based on the experimental results, the EE% for the prepared formulas ranged from 32.22±0.86 to 54.83±1.17%. Comparatively to others, levofloxacin could be best encapsulated using span 20. The particle size of the proniosomes ranged from 447±204 nm to 1089±17 nm. Proniosomal gel prepared with span 20 had the smallest vesicle size. The zeta potential range of prepared proniosomes was from 20.95±0 mV to 60.92±0.09 mV. The prepared formulations were found to have a polydispersity index ranging from 0.198±3.23 to 0.967±0.36. Almost all of the formulas displayed a linear release profile ranging from 33.028 to 97.56 percent over 4 hours. A higher level of drug deposition was observed with span 80 compared to tween 80 after 6 h: 18.296% versus 9.44%. The stability study showed that there was no significant change in EE%, PS, or ZP of levofloxacin proniosomal gels after 3 months of storage. In conclusion, the dermal application of the investigated proniosomal gel formulations demonstrated promising results as nanocarriers for levofloxacin.
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