5-Fluorouracil, innovative drug delivery systems to enhance bioavailability for topical use

Background: 5-Fluorouracil (5-FU) is a well-known chemotherapy drug, used for over 70 years in the treatment of several types of cancer. Topically, 5-FU has shown potential effect to treat premalignant and malignant lesions. However, the efficiency of topical 5-FU administration is limited to treat superficial pre-carcinogenic lesions. Objective: In this review we present the main characteristics of 5-FU, including its mechanism of action, dissolution, and bioavailability. Moreover, we highlight the delivery systems under development that include 5-FU carriers in topical treatments. Results: Microemulsions and nanocarriers have demonstrated significant impact on the bioavailability of 5-FU in vitro and in vivo, increasing the drug effects on deeper layers of the skin, which has shown promising results in the treatment of precancemus and cancerous lesions. According to authors of clinical pilot studies, 5-FU occlusive dressing, 5-FU chemowrap, 5-FU transdermal, and their combination, resulting in a triple therapy, are more effective compared with cream formulation to treat precancer widespread in a skin area. Conclusion: Thus, by this review, we demonstrate that the delivery system under consideration greatly impacts 5-FU effects on the skin.

Automated summary

5-Fluorouracil (5-FU) is a chemotherapy drug used for over 70 years, with potential in treating precancerous and cancerous lesions when used topically. Microemulsions and nanocarriers significantly impact the bioavailability of 5-FU, increasing drug effects on deeper skin layers and showing promising results in lesion treatment. Delivery systems like occlusive dressing, chemowrap, and transdermal 5-FU, along with their combination, are more effective than cream formulations in treating widespread precancerous lesions in the skin.