Purpose

Few studies have so far described the improved activity of NSAIDs when formulated into nanoemulsions to be applied topically. However, no report is yet available about the topical application of micelles containing NSAIDs. Additionally, the serum concentration of drugs following topical application of nanoemulsions/micelles has not been reported to this point.

Methods

In the present study, an oil-in-water nanoemulsion containing ibuprofen (NE-Ibu) was prepared and investigated for topical delivery of the drug. Carbopol 934 was used to produce a topical gel from NE-Ibu (NE-Ibu gel). Then, its anti-inflammation activity was evaluated in vivo and compared with commercial Ibu gel and topical gel of the corresponding micelle containing Ibu (i.e., MI-Ibu gel). Furthermore, skin permeation and serum concentration of the drug in the formulations were evaluated using HPLC.

Key Findings

The results showed that the anti-inflammatory activity of NE-Ibu gel and MI-Ibu gel increased in comparison to the commercial one. Also, serum concentration following application of NE-Ibu gel and MI-Ibu gel was not significantly different from the commercial preparation.

Conclusion

Arguably, the nanoemulsion and the micelle-based gels could enhance Ibu penetration through the skin and the preparations may be introduced as appropriate candidates for topical delivery of hydrophobic drugs.

中文翻译：

---

由胶束或纳米乳液配制的布洛芬局部凝胶改善抗炎活性和最小系统吸收

目的

迄今为止，很少有研究描述了将 NSAIDs 配制成用于局部应用的纳米乳剂时改善的活性。然而，目前还没有关于含有非甾体抗炎药的胶束的局部应用的报告。此外，目前尚未报道局部应用纳米乳剂/胶束后药物的血清浓度。

方法

在本研究中，制备并研究了一种含有布洛芬 (NE-Ibu) 的水包油纳米乳，用于药物的局部给药。Carbopol 934 用于从 NE-Ibu (NE-Ibu gel) 生产局部凝胶。然后，在体内评估其抗炎活性，并与市售的伊布凝胶和含有伊布的相应胶束（即MI-伊布凝胶）的局部凝胶进行比较。此外，使用HPLC评估制剂中药物的皮肤渗透性和血清浓度。

主要发现

结果表明，NE-Ibu凝胶和MI-Ibu凝胶的抗炎活性与商业凝胶相比有所增加。此外，使用 NE-Ibu 凝胶和 MI-Ibu 凝胶后的血清浓度与商业制剂没有显着差异。

结论

可以说，纳米乳液和基于胶束的凝胶可以增强布洛芬通过皮肤的渗透，并且这些制剂可以作为局部递送疏水药物的合适候选者而引入。