The Impact of Improving Dermal Permeation on the Efficacy and Targeting of Liposome Nanoparticles as a Potential Treatment for Breast Cancer
Authors: Heba F Salem
Amr Gamal
Alaa S Tulbah
Haitham Saeed
Journal: Pharmaceutics (2021)
Discipline: PHARMACOLOGY & TOXICOLOGY
Keywords: bioavailability; breast cancer; deformable liposomes; propylene glycol; raloxifene.
Affiliations: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 625617, Egypt., Clinical Pharmacy Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 625617, Egypt., Department of Pharmaceutics, College of Pharmacy, Umm Al Qura University, Makkah 21421, Saudi Arabia.

Abstract:  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% w/w), cholesterol (0.15% w/w) and propylene glycol (10% v/v). 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. 

Retracted: No

PubPeer comments:
 Figure 2. * Panels here look similar to panels in a 2014 paper by a shared researcher, i.e. Bassel Haj et al., Pediatr Surg Int (2014) 30:181u2013188, DOI 10.1007 s00383-013-3448-8 - https: pubpeer.com publications 5BF7F508C3966AF8B0B20E82A4E804 * Blue boxes: The 2005 Sham panel looks similar to the 2014 IR panel * Red boxes: The 2005 SBS panel looks similar to the 2014 IR-O3 panel. ![file] , 
 Could the authors please comment on a potential conflict of interest between this paper and a provisional patent application? U.S. Provisional Patent Application No. 60 575,803 was filed on June 2, 2004, and later replaced by PCT Patent Application No. PCT IL2005 000587, filed on June 2 2005, as per https: patents.google.com patent US8026211B2 en From the invention:  A method for increasing intestinal function is provided. The method comprising orally and or enterally administering to a subject in need thereof a therapeutically effective amount of insulin, thereby increasing intestinal function (...) The present invention relates to methods and formulations for increasing intestinal function, which may be used for treating short bowel syndrome. ,