Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

Abstract

In the present study, luteolin (LT)-loaded nanosized vesicles (LT-NVs) were prepared by a solvent evaporation–hydration method using phospholipid and edge activator. The formulation was optimized using three factors at a three-level Box–Behnken design. The formulated LT-NVs were prepared using the three independent variables phospholipid (A), edge activator (B) and sonication time (C). The effect of used variables was assessed on the vesicle size (Y1) and encapsulation efficiency (Y2). The selection of optimum composition (LT-NVopt) was based on the point prediction method of the software. The prepared LT-NVopt showed the particle size of 189.92 ± 3.25 nm with an encapsulation efficiency of 92.43 ± 4.12% with PDI and zeta potential value of 0.32 and −21 mV, respectively. The formulation LT-NVopt was further converted into Carbopol 934 gel (1% w/v) to enhance skin retention. LT-NVoptG was further characterized for viscosity, spreadability, drug content, drug release, drug permeation and antioxidant, antimicrobial and cytotoxicity assessment. The evaluation result revealed optimum pH, viscosity, spreadability and good drug content. There was enhanced LT release (60.81 ± 2.87%), as well as LT permeation (128.21 ± 3.56 µg/cm2/h), which was found in comparison to the pure LT. The antioxidant and antimicrobial study results revealed significantly (p ˂ 0.05) better antioxidant potential and antimicrobial activity against the tested organisms. Finally, the samples were evaluated for cytotoxicity assessment using skin cancer cell line and results revealed a significant difference in the viability % at the tested concentration. LT-NVoptG showed a significantly lower IC50 value than the pure LT. From the study, it can be concluded that the prepared LT-NVoptG was found to be an alternative to the synthetic drug as well as conventional delivery systems.

Nano-scale drug delivery systems for luteolin: advancements and applications

“…In a study, Lu-loaded nanovesicles were further transformed into Carbopol 934 gel (LT-NV-optG). 120 Compared with pure Lu, LT-NV-optG displayed suitable viscosity, pH, coatability, and sustained release characteristics, leading to a 2fold enhancement in permeability. Additionally, LT-NV-optG demonstrated no skin irritation and exhibited an enhanced inhibitory effect on skin cancer cell lines.…”

Development of Solid Lipid Nanoparticle-Loaded Polymeric Hydrogels Containing Antioxidant and Photoprotective Bioactive Compounds of Safflower (Carthamus tinctorius L.) for Improved Skin Delivery

“…Through several studies, it has been reported to have antioxidant activity in preventing/treating age-related diseases and oxidative stress such as neuronal and cardiovascular disorders , as well as cancer. , This is presumably because it contains chemical compounds such as quercetin (QU) , and luteolin (LU). , Due to their potential to contribute a hydrogen atom to the DPPH radical, these bioactive components demonstrated the synergistic impact of a high radical scavenging activity. However, there are a few limitations caused by the original nature, such as low solubility in water resulting in reduced skin permeation abilities. − In addition, the stratum corneum, which is the outermost layer of the skin, acts as a penetration barrier by blocking the delivery of active ingredients into the skin. This is important because the potential efficacy of QU and LU in preventing cell damage until necrosis mainly occurs in the epidermis. , Various approaches in terms of drug targeting and carrier systems with different routes of administration were studied to overcome these limitations and achieve more effective therapeutic efficacy. − …”

In Vitro Evaluation of Kaempferol-Loaded Hydrogel as pH-Sensitive Drug Delivery Systems

“…With the different pH of the medium, the drug will be intelligently released. Imran Kazmi et al [ 23 ] studied the treatment of skin cancer with luteolin-loaded CBP hydrogel. Maimoona Qindeel et al [ 24 ] studied CBP hydrogel loaded with methotrexate for the treatment of rheumatoid arthritis.…”