Abstract
In this study semisolid formulations containing AcYPFF (N-acetyl-Tyr-Pro-Phe-Phe-NH2) tetrapeptide were obtained and characterized in terms of rheology, stability by multiple light scattering and particle size distribution by laser diffraction. Additionally, the release studies of tetrapeptide from formulations obtained were performed. The influence of different factors such as semisolid and membrane type on tetrapeptide release rate was examined. The release experiments of tetrapeptide modified with palmitoyl group (PalmYPFF) were also carried out. The results proved that formulation type and its rheological properties strongly determined the permeation process of the tetrapeptide. The fastest release of tetrapeptide was observed from hydrogel that had the lowest viscosity. The kinetic data of tetrapeptide released from oil-in-water (o/w) and water-in-oil (w/o) emulsions prepared at elevated temperature showed good fit to the Higuchi equation, whereas when AcYPFF was released from oil-in-water (o/w) emulsion prepared with the addition of auto-emulsifier high linearity with Korsmeyer–Peppas model was observed. While when tetrapeptide was released from Hydrogel the most suitable model was the first-order kinetics. It was suggested that mechanism that led to the release of tetrapeptide from all formulations was non-Fickian diffusion transport. The presence of palmitoyl group changed the solubility of tetrapeptide both in formulation and receptor fluid and thus the release rate of active compound was modified.
Highlights
In recent years, the low molecular weight peptides have revolutionized the skincare and pharmaceutical industries and have become significant ingredients applied in topical formulations (Lupo and Cole 2007)
Acetyl-Tyr-Pro-Phe-Phe-NH2 (AcYPFF) is a synthetic derivative of endomorphin-2 (H-Tyr-Pro-Phe-PheNH2) that is known as opioid peptide (Van Dorpe et al 2010), which is applied as a pharmaceutical agent
The results proved that different factors had an impact on the release rate of active compound
Summary
The low molecular weight peptides have revolutionized the skincare and pharmaceutical industries and have become significant ingredients applied in topical formulations (Lupo and Cole 2007). Low molecular weight peptides applied in topical applications can be divided into three main groups depending on their activity—signal peptides, carrier peptides and neurotransmitter peptides (Olejnik et al 2013; Lupo 2005). Acetyl-Tyr-Pro-Phe-Phe-NH2 (AcYPFF) is a synthetic derivative of endomorphin-2 (H-Tyr-Pro-Phe-PheNH2) that is known as opioid peptide (Van Dorpe et al 2010), which is applied as a pharmaceutical agent. The cosmetic application of the oligopeptides such as R1-Tyr-Pro-Phe-PheNH2 and their derivatives were reported for the first time in the patent no. The most preferred structure of this invention was the oligopeptide N-acetyl-Tyr-Pro-Phe-Phe-NH2. AcYPFF was applied as the hair treatment agent which is added to the composition in the form
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