Development of a novel polymer-based carrier for deformable liposomes for the controlled dermal delivery of naringenin

In recent years, the incidence of skin cancer has increased worldwide, presenting a significant burden on healthcare services. Chemotherapy intervention is often not appropriate for all patients due to localized adverse effects on skin physiology. The aim of this study was, therefore, to consider the development of a novel phytochemical-based deformable liposomal formulation suspended in an aqueous gel for the controlled-release of naringenin. Naringenin is an antioxidant, free radical scavenger, anti-inflammatory agent, and immune system modulator thus may be potentially useful as a pharmacological anti-cancer agent. Formulated liposomes incorporating an increasing loading of Tween 20 (from 0% w/w to 10% w/w) demonstrated a significant decrease in deformability index (DI) (80.71 +/- 2.02-59.17 +/- 4.42 %), indicating an increase in elasticity. The release of naringenin over 24 h was directly affected by Tween-20 concentration, decreasing from 100.72%+/- 4.98% to 79.53%+/- 3.68% for 0% and 2% w/w Tween 20, respectively. Further, the incorporation of deformable liposomes into hydroxyethylcellulose (HEC) and hydroxypropyl methylcellulose (HPMC) gels resulting in a further retardation of naringenin release, 23.21%+/- 1.17% and 19.83%+/- 1.50%, respectively, over 24 h. Incubation of 1,1 '-dioctadecyl-3,3,3 ',3 '-tetramethylindocarbocyanine perchlorate-loaded liposomes with human dermal fibroblast (HDF) and keratinocyte cells demonstrated intracellular accumulation within 2 h, confirming deformable liposomes may be beneficial in improving drug penetration across dermal cells and would be valuable in emerging controlled-release formulations.

Automated summary

The study aimed to develop a novel phytochemical-based deformable liposomal formulation for controlled-release of naringenin, a compound with potential anti-cancer properties. Testing showed that increasing Tween 20 loading in the liposomes decreased deformability and affected naringenin release, with further retardation observed when incorporated into HEC and HPMC gels. The deformable liposomes demonstrated improved drug penetration across dermal cells, indicating their potential value in controlled-release formulations.