<p>Skin cancer is caused by the uncontrolled proliferation of aberrant skin cells due to excessive exposure to ultraviolet (UV) radiation, affecting over a million individuals annually. This study aims to develop a 5-fluorouracil (5-FU) and lepidine (LPD) dual drug-loaded nanoemulsion (NE) gel to ameliorate DMBA-UVB induced skin cancer. The prepared NE was transformed into an NE gel using an optimized concentration of 1.0% w/w Carbopol 934 P, while the conventional gel, consisting of Carbopol 934 P with the same concentration, was also prepared for comparison. Both gels were analyzed based on several parameters. An in vivo efficacy study was conducted on experimentally induced skin cancers, assessing tumor number, area, volume, histopathology, biochemical estimations, and anti-inflammatory responses. The 5-FU and LPD dual drug-loaded NE (FL-NE) gel produced a significant (<i>p</i> &lt; 0.001) reduction in tumor volume, area, and number. Histopathological analysis demonstrated a marked reduction in keratin pearls, a defining feature of squamous cell carcinoma, along with improvements in epidermal dysplasia. Additionally, antioxidant and anti-inflammatory activity tests showed that FL-NE gel was significantly more effective (<i>p</i> &lt; 0.001) than the conventional gel. These findings conclude that the 5-FU and LPD co-loaded NE gel developed in this study shows strong potential in ameliorating skin cancer.</p> Graphical Abstract <p></p>

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Nanoemulsion Gel for Co-delivery of 5-Fluorouracil and Lepidine to Mitigate Skin Cancer: Physicochemical Characterization and Pre-clinical Assessment

  • Zeba Usmani,
  • Zakiya Usmani,
  • Mohd Akhtar,
  • Abdul Ahad,
  • Mohd Aqil,
  • Mohd Mujeeb

摘要

Skin cancer is caused by the uncontrolled proliferation of aberrant skin cells due to excessive exposure to ultraviolet (UV) radiation, affecting over a million individuals annually. This study aims to develop a 5-fluorouracil (5-FU) and lepidine (LPD) dual drug-loaded nanoemulsion (NE) gel to ameliorate DMBA-UVB induced skin cancer. The prepared NE was transformed into an NE gel using an optimized concentration of 1.0% w/w Carbopol 934 P, while the conventional gel, consisting of Carbopol 934 P with the same concentration, was also prepared for comparison. Both gels were analyzed based on several parameters. An in vivo efficacy study was conducted on experimentally induced skin cancers, assessing tumor number, area, volume, histopathology, biochemical estimations, and anti-inflammatory responses. The 5-FU and LPD dual drug-loaded NE (FL-NE) gel produced a significant (p < 0.001) reduction in tumor volume, area, and number. Histopathological analysis demonstrated a marked reduction in keratin pearls, a defining feature of squamous cell carcinoma, along with improvements in epidermal dysplasia. Additionally, antioxidant and anti-inflammatory activity tests showed that FL-NE gel was significantly more effective (p < 0.001) than the conventional gel. These findings conclude that the 5-FU and LPD co-loaded NE gel developed in this study shows strong potential in ameliorating skin cancer.

Graphical Abstract