Purpose

In this study, the preparation of self-assembled polymer-free in situ forming nanovesicles (ISNs) based on non-ionic surfactants (NISs) is presented.

Methods

A 2²·4¹ full factorial experimental design was adopted for the development of novel polymer-free ISNs loaded with tenoxicam utilizing the emulsion method. The type of NIS (Brij® 52 or Span® 60), the cholesterol percentage (30, 50, or 60 w/w%), and the internal phase percentage (20 or 30 v/v%) were chosen as the independent variables. Percentage drug released after 1 h (Q₁), vesicle particle size (PS), and mean dissolution time (MDT) were the dependent variables. Selected formulation was investigated morphologically using transmission electron microscopy.

Results

Results revealed that the formation had spherical dense shape. All independent factors significantly affected the percentage drug release after the first hour (Q₁), and the MDT, while only the type of NIS had a significant effect on PS. The highest control of drug release was observed in formulation containing Span® 60 with lower internal phase percentage (MDT = 20.06 ± 0.40 h) as well as the smallest PS (123.75 ± 16.68 nm).

Conclusion

The obtained results indicated the potentiality of the invented ISNs in controlling the release of tenoxicam in a desirable economical biphasic pattern compared to other in situ formulations.

中文翻译：

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无聚合物可注射原位形成的纳米囊泡作为可控肠胃外药物输送系统的新平台

目的

在这项研究中，提出了基于非离子表面活性剂（NISs）的自组装的无聚合物原位形成纳米囊泡（ISNs）的制备。

方法

采用2 ² ·4 ¹全析因实验设计，通过乳液法开发了载有替诺昔康的新型无聚合物ISN。选择NIS的类型（Brij®52或Span®60），胆固醇百分比（30、50或60 w / w％）和内相百分比（20或30 v / v％）作为自变量。1小时后释放的药物百分比（Q ₁），囊泡粒径（PS）和平均溶出时间（MDT）是因变量。使用透射电子显微镜对选择的制剂进行形态学研究。

结果

结果显示该地层具有球形致密形状。所有独立因素均显着影响第一小时（Q ₁）和MDT后的药物释放百分比，而只有NIS类型对PS有显着影响。在含有Span®60且内相百分比较低（MDT = 20.06±0.40 h）且PS最小（123.75±16.68 nm）的制剂中，观察到了最高的药物释放控制。

结论

所获得的结果表明，与其他原位制剂相比，本发明的ISN具有以理想的经济双相模式控制替诺昔康释放的潜力。