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用于口腔黏膜、皮肤和眼部局部给药的脂质纳米颗粒制剂的当前挑战与未来发展

Current Challenges and Future of Lipid nanoparticles formulations for topical drug application to oral mucosa, skin, and eye.

作者信息

Guilherme Viviane A, Ribeiro Ligia N M, Tofoli Giovana Radomille, Franz-Montan Michelle, de Paula Eneida, de Jesus Marcelo Bispo

机构信息

Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, Sao Paulo. Brazil.

Laboratory of Inflammation, Sao Leopoldo Mandic Institute and Research Center, Rua Jose Rocha Junqueira 13, 13045-75, Campinas, Sao . Brazil.

出版信息

Curr Pharm Des. 2017 Nov 21. doi: 10.2174/1381612823666171122103849.

Abstract

BACKGROUND

Topical drug administration offers an attractive route with minimal invasiveness. It also avoids limitations of intravenous administration such as the first pass metabolism and presystemic elimination within the gastrointestinal tract. Furthermore, topical drug administration is safe, have few side effects, is easy to apply, and offers a fast onset of action. However, the development of effective topical formulations still represents a challenge for the desired effect to be reached, locally or systemically. Solid lipid nanoparticles and nanostructured lipid carriers are particular candidates to overcome the problem of topical drug administration. The nanometric particle size of lipid nanoparticles favors the physical adhesion to the skin or mucosal, what can also be attained with the formation of hybrid (nanoparticles/polymer) systems.

METHODS

In this review, we discuss the major challenges for lipid nanoparticles formulations for topical application to oral mucosa, skin, and eye, highlighting the strategies to improve the performance of lipid nanoparticles for topical applications. Next, we critically analyzed the in vitro and in vivo approaches used to evaluate lipid nanoparticles performance and toxicity.

CONCLUSION

We addressed some major drawbacks related to lipid nanoparticle topical formulations and concluded the key points that have to be overcome to help them to reach the market in topical formulations to oral mucosa, skin and eye.

摘要

背景

局部给药提供了一种侵入性最小的理想给药途径。它还避免了静脉给药的局限性,如首过代谢和胃肠道内的系统前消除。此外,局部给药安全、副作用少、易于应用且起效快。然而,开发有效的局部制剂仍然是一个挑战,难以实现局部或全身的预期效果。固体脂质纳米粒和纳米结构脂质载体是克服局部给药问题的特别候选者。脂质纳米粒的纳米级粒径有利于其与皮肤或黏膜的物理粘附,这也可以通过形成杂化(纳米粒/聚合物)系统来实现。

方法

在本综述中,我们讨论了脂质纳米粒制剂用于口腔黏膜、皮肤和眼部局部应用的主要挑战,强调了提高脂质纳米粒局部应用性能的策略。接下来,我们批判性地分析了用于评估脂质纳米粒性能和毒性的体外和体内方法。

结论

我们阐述了脂质纳米粒局部制剂的一些主要缺点,并总结了为帮助它们以局部制剂形式进入口腔黏膜、皮肤和眼部市场而必须克服的关键点。

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