Background and Aim: Meloxicam (MX) is a potent hydrophobic non-steroidal anti-inflammatory drug used to reduce inflammation and pain. However, its oral dosage form can cause many adverse gastrointestinal effects. In the present study, a poloxamer P407 based hydrogel system containing transfersomes or flavosomes has been prepared as a potential therapeutic vehicle for the topical delivery of MX.
Methods: In this study, MX was encapsulated in conventional liposomes, transfersomes, and flavosomes. The obtained liposomal vesicles were characterized in terms of size, drug entrapment efficiency, zeta potential, and stability. These MX-loaded liposomal formulations were further incorporated into a poloxamer P407 gel and evaluated using rheological properties, a stability study and an ex vivo permeation study through human cadaver skin by both HPLC analysis and confocal laser scanning microscopy (CLSM).
Results: The developed deformable liposomes exhibited homogeneous vesicle sizes less than 120 nm with a higher entrapment efficiency as compared to conventional liposomes. The deformable liposomal gel formulations showed improved permeability compared to a conventional liposomal gel and a liposome-free gel. The enhancement effect was also clearly visible by CLSM.
Conclusion: These deformable liposomal hydrogel formulations can be a promising alternative to conventional oral delivery of MX by topical administration. Notably, flavosome-loaded gel formulations displayed the highest permeability through the deeper layers of the skin and shortened lag time, indicating a potential faster on-site pain relief and anti-inflammatory effect.

Keywords: flavosome, transfersome, flavonoid, ex vivo skin permeation, poloxamer P407


中文翻译：

---

用于美洛昔康皮肤和透皮递送的可变形脂质体水凝胶

背景和目的：美洛昔康 (MX) 是一种有效的疏水性非甾体抗炎药，用于减轻炎症和疼痛。然而，其口服剂型会引起许多不良的胃肠道反应。在本研究中，基于泊洛沙姆 P407 的含有转移体或黄酮体的水凝胶系统已被制备为用于局部递送 MX 的潜在治疗载体。
方法：在这项研究中，MX 被封装在传统的脂质体、转移体和黄体中。获得的脂质体囊泡在大小、药物包埋效率、zeta 电位和稳定性方面进行了表征。将这些载有 MX 的脂质体制剂进一步掺入泊洛沙姆 P407 凝胶中，并通过 HPLC 分析和共聚焦激光扫描显微镜 (CLSM) 使用流变特性、稳定性研究和通过人体尸体皮肤的离体渗透研究进行评估。
结果：与传统脂质体相比，开发的可变形脂质体表现出小于 120 nm 的均匀囊泡尺寸，具有更高的包封效率。与常规脂质体凝胶和无脂质体凝胶相比，可变形脂质体凝胶制剂显示出改善的渗透性。CLSM 也清楚地看到了增强效果。
结论：这些可变形的脂质体水凝胶制剂可以替代传统的局部给药口服 MX。值得注意的是，负载黄酮体的凝胶制剂通过皮肤深层表现出最高的渗透性，并缩短了滞后时间，表明可能更快地缓解现场疼痛和抗炎作用。

关键词：黄酮体，转移体，类黄酮，体外皮肤渗透，泊洛沙姆 P407