Leuphasyl

Pentapeptide-18 as an anti-aging candidate: Spectroscopic characterization and molecular interaction analysis.

Dilan Akhan, Bilge Bicak, Elif Akalin +1 more

Skin aging is predominantly associated with the progressive breakdown of the dermal extracellular matrix (ECM), leading to visible manifestations such as wrinkle development caused by repetitive facial muscle movements and a gradual reduction in collagen and elastin synthesis. This degeneration is intensified by external factors including ultraviolet exposure, tobacco use, and nutritional imbalance, which interfere with major intracellular signaling pathways-namely TGF-β, TNF-α, MAPK, PI3K/AKT, and NF-κB-that collectively regulate inflammatory responses, oxidative stress, and ECM remodeling. Pentapeptide-18 (Leuphasyl®), a bioactive peptide known for its neuromodulatory properties, has demonstrated the ability to mitigate wrinkle formation by inhibiting neurotransmitter release, while simultaneously improving skin hydration, elasticity, and texture. In this study, the anti-aging activity of Pentapeptide-18 was comprehensively examined through a combination of experimental analyses and computational modeling. Structural optimization and electronic property evaluation were performed using density functional theory (DFT) calculations with the 6-31 + +G(d,p) basis set, complemented by frontier molecular orbital (HOMO-LUMO) and molecular electrostatic potential (MEP) analyses. Theoretical vibrational frequencies were assigned via potential energy distribution (PED) analysis and validated experimentally using FTIR, ATR-FTIR, and Raman spectroscopy. Additionally, molecular docking and molecular dynamics simulations were employed to investigate the binding behavior of Pentapeptide-18 with key molecular targets implicated in skin aging, including TGF-β, TNF-α, MAPK, PI3K/AKT, and NF-κB. Pharmacokinetic and drug-likeness properties were further assessed through ADMET (absorption, distribution, metabolism, excretion, and toxicity). The collective findings provide mechanistic insight into the molecular interactions and stability of Pentapeptide-18, reinforcing its potential as a safe, effective, and non-invasive candidate for advanced anti-aging skin care applications.

Retinol and Oligopeptide-Loaded Lipid Nanocarriers as Effective Raw Material in Anti-Acne and Anti-Aging Therapies.

Małgorzata Pawłowska, Marta Marzec, Waldemar Jankowiak +1 more

The use of lipid nanocarriers as components of cosmetic formulations may provide an opportunity to fully exploit the beneficial properties of pentapeptide-18 and retinol while reducing the undesirable effects that occur during retinoid therapy. This study aimed to evaluate the effectiveness of semi-solid formulations enriched with retinol and oligopeptide-loaded lipid nanocarriers. Solid lipid nanoparticles were produced using a high-shear homogenization method. The work included physicochemical characterization of the cosmetic products, and evaluation of their stability as well as their efficacy. The resulting semi-solid preparations were determined to be stable regardless of their storage temperature. No effect of the presence of lipid nanoparticles on the shelf-life stability of the cosmetic products was observed. A temperature of 25 °C was considered the recommended storage temperature for the tested semi-solid formulations. Beneficial effects of the cosmetic products were proven (in vivo study on volunteers), i.e., a significant reduction in the level of sebum secretion (anti-acne therapy) and a decrease in the number of facial wrinkles (anti-aging therapy). In addition, the protective properties of the lipid nanoparticles themselves against the skin were confirmed, reducing the irritating effect of retinol that is usually the case with classic retinoid therapies.