Study summary · research use only
Bioactive Glycyrrhizic Acid Ionic Liquid Self-Assembled Nanomicelles for Enhanced Transdermal Delivery of Anti-Photoaging Signal Peptides
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
This study developed ionic-liquid-based self-assembled nanomicelles (GAO/PAL-4-SM) from glycyrrhizic acid (GA) and oxymatrine (OMT) to improve transdermal delivery of the signal peptide palmitoyl pentapeptide-4 (PAL-4). Molecular dynamics simulations and density functional theory calculations were used to optimize the GAO components, and 10wt.% GAO-SM was reported to promote permeation and subcutaneous retention of PAL-4, aided by increased miscibility and interaction with the stratum corneum. In cellular and animal photoaging experiments (species not specified for the animal model), GAO/PAL-4-SM was associated with increased collagen and hyaluronic acid regeneration, reduced inflammation and apoptosis, and accelerated macrophage M2 polarization, along with reduced skin wrinkles and increased elasticity.
Abstract
Sigal peptides have garnered remarkable efficacy in rejuvenating photoaged skin and delaying senescence. Nevertheless, their low solubility and poor permeability bring about a formidable challenge in their transdermal delivery. To address this challenge, bioactive ionic liquids (ILs) synthesized from natural glycyrrhizic acid (GA) and oxymatrine (OMT) with eminent biocompatibility is first prepared. The components ratios and inherent forming mechanisms of GA-OMT (GAO) are optimized by molecular dynamics simulations and density functional theory calculations. Remarkably, GAO can significantly improve the sparingly soluble properties of palmitoyl pentapeptide-4 (PAL-4), a model peptide drug. Subsequently, GAO self-assembled micelles loading PAL-4 (GAO/PAL-4-SM) are fabricated without additional auxiliary materials. The permeation and subcutaneous retention of PAL-4 are significantly promoted with 10wt.% GAO-SM. Moreover, GAO ILs facilitated PAL-4 permeation by enhancing its miscibility and interaction with stratum corneum (SC), offering a pulling effect and micellar structures for PAL-4, as elucidated by computational simulations. In cellular and animal photoaging experiments, GAO/PAL-4-SM possessed remarkable capabilities in boosting collagen and hyaluronic acid regeneration, mitigating inflammation and apoptosis, accelerating macrophage M2 polarization, thereby lessening skin wrinkles and leveraging elasticity. Collectively, the research innovatively designed an ILs self-assembled nano-micellar transdermal delivery system to enhance the permeability and anti-photoaging effect of signal peptides.
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