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

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.

Exploring the Synergistic Effect of Bergamot Essential Oil with Spironolactone Loaded Nano-Phytosomes for Treatment of Acne Vulgaris: In Vitro Optimization, In Silico Studies, and Clinical Evaluation

“…Moreover, it was observed that X 2 had a positive effect on ZP which may be owed to that the cholesterol molecule contains a hydroxyl group in its structure. Besides, it is a rigid molecule that aids in improving the stability and rigidity of the lipid bilayer [ 23 ]. Similar findings were reported by Salem et al (2021) who found that the negative charges in vesicles were increased when cholesterol was increased [ 23 ].…”

Enhancing the Bioavailability and Efficacy of Vismodegib for the Control of Skin Cancer: In Vitro and In Vivo Studies

“…A sample of the VLI and VLL formulations was deposited onto a carbon-coated copper grid and visualized by Transmission Electron Microscopy (TEM, Carl Zeiss, Oberkochen, Germany) at suitable magnifications [13].…”

“…They can enhance the pharmacokinetics, selectivity, and efficacy of drugs while lowering their toxicity [4,11,12]. Liposomes were first described as nanoparticles Pharmaceuticals 2022, 15, 126 2 of 14 for transdermal use [11,13]. Phospholipids and cholesterol are the main components of liposomes.…”

“…Phospholipids and cholesterol are the main components of liposomes. Liposomes can enhance the pharmacokinetics and the efficacy of drugs, but they lack the ability to effectively penetrate the skin [11,13]. A new generation of liposomes was designed to enhance the liposome's physic-chemical properties.…”

Nano Methotrexate versus Methotrexate in Targeting Rheumatoid Arthritis

“…In light of this, a prospective MTX-GNPs formula has been prepared to encapsulate MTX, in order to achieve better drug permeation and bioavailability. In addition, new topically applied methodologies are being investigated [ 18 ]. In general, linking MTX to GNPs aids in more effective and selective uptake, a property distinct to nanocarriers, which improves therapeutic potential and lowers effective doses [ 19 ].…”