4.4 Article

A rutin nanocrystal gel as an effective dermal delivery system for enhanced anti-photoaging application

Journal

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 47, Issue 3, Pages 429-439

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2021.1890113

Keywords

Rutin; nanocrystal; dermal delivery; anti-photoaging; gel

Funding

  1. National Natural Science Foundation of China [81803477, 81872817]
  2. National Key Research and Development Program of China [2017YFA0205402]
  3. Natural Science Foundation of Jiangsu Province [BK20180557]
  4. Postdoctoral Research Funding Program of Jiangsu Province [2020Z282]

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In this study, a novel freeze-dried rutin nanocrystal was developed to enhance the saturation solubility of rutin, and further formulated into a targeted rutin nanocrystal gel for improved transdermal delivery efficiency. The results demonstrated that the rutin nanocrystal gel significantly enhanced the permeated amounts of rutin on mice and effectively prevented skin photoaging and tissue damage induced by UV irradiation. This study validated that the nanocrystal gel was an ideal carrier for the epidermal application of rutin, providing a valuable platform for enhancing the transdermal bioavailability of insoluble drugs.
As a natural flavonoid compound, rutin could scavenge free radicals effectively to achieve remarkable antioxidant and anti-photoaging activity. Unfortunately, the extremely low water solubility of rutin often leads to the poor percutaneous permeability and unsatisfactory bioavailability, which has greatly restricted its clinical application. In this study, a novel freeze-dried rutin nanocrystal was developed to improve its saturation solubility, which was further redispersed in carbopol gel to formulate the targeted rutin nanocrystal gel (NC-gel) for enhanced transdermal delivery efficiency. Benefit from the advantages of NC-gel, the permeated amounts of rutin on mice in the NC-gel group was more than three times enhancement over that of the coarse drug gel group. Furthermore, the results of pharmacodynamic studies in vivo demonstrated that NC-gel could effectively prevent the skin photoaging and tissue damage induced by UV irradiation. Taken together, these results validated that NC-gel was an ideal carrier for the epidermal application of rutin to obtain excellent anti-photoaging effect, which further might provide a valuable platform for improving the transdermal bioavailability of insoluble drugs.

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