The Impact of Improving Dermal Permeation on the Efficacy and Targeting of Liposome Nanoparticles as a Potential Treatment for Breast Cancer

• Main Authors: Heba F. Salem (Author), Amr Gamal (Author), Haitham Saeed (Author), Alaa S. Tulbah (Author)
• Format: Book
• Published: MDPI AG, 2021-10-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

Breast cancer is the most frequent malignancy in women. This work focuses on developing deformable liposomes as a potential carrier for breast cancer treatment and studying the impact of improving dermal permeation on the efficacy and targeting of liposomes. Raloxifene (RXF), an oestrogen antagonist, was used as a model drug. Using Box-Behnken design, different formulations of RXF-loaded deformable liposome (RLDL) were prepared using different propylene glycol, phospholipid and cholesterol concentrations. The percentage of entrapment efficiency (Y₁), particle size (Y₂), zeta potential (Y₃) and steady-state flux (Y₄) of the prepared formulations were all evaluated. Y₁ and Y₄ were significantly increased and Y₂ and Y₃ were significantly decreased when the propylene glycol concentration was increased. The optimization was obtained and the optimum formulation was that including phospholipid (1.40% <i>w</i>/<i>w</i>), cholesterol (0.15% <i>w</i>/<i>w</i>) and propylene glycol (10% <i>v</i>/<i>v</i>). The selected optimum formulation displayed a % EE of 78.34 ± 1.04% with a steady-state flux of 4.21 ± 0.02 µg/cm²/h. In order to investigate bioavailability, antitumor effectiveness and permeation, the optimum formulation was selected and included in a carbopol gel. The optimum gel formulation had 2.77 times higher bioavailability and, as a result, considerable antitumor action as compared to oral RXF. In conclusion, optimum RLDL gel may be an effective breast cancer treatment.

Item Description

10.3390/pharmaceutics13101633
1999-4923