Physico-chemical characterization of formulations containing endomorphin-2 derivatives

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.

Design of 3‐aminophenol‐grafted polymer‐modified zinc sulphide nanoparticles as drug delivery system

“…The results of the Korsmeyer–Peppas models demonstrated a high fitting coefficient value (R 2 ) for the famotidine‐releasing process. The Korsmeyer–Peppas model values for the release exponent (n < 0.5) of famotidine suggest a controlled diffusion mechanism for famotidine release with a quasi‐Fickian process [ 35 , 36 ].…”

Neurocosmetics in Skincare—The Fascinating World of Skin–Brain Connection: A Review to Explore Ingredients, Commercial Products for Skin Aging, and Cosmetic Regulation

“…Skinasensyl ® LS 9749 (liquid synthetic tetrapeptide) and Skinasensyl ® LS 9852 (powdered synthetic tetrapeptide) from BASF are other two functional ingredients designed to soothe sensitive skin [204][205][206]. These ingredients improve skin comfort by reducing overreactions that lead to burning and stinging [207]. Furthermore, both Skinasensyl ® LS 9749 and Skinasensyl ® LS 9852 inhibit the release of the neuromediator CGRP from sensory neurons, and increase the skin's tolerance threshold [207][208][209].…”

“…These ingredients improve skin comfort by reducing overreactions that lead to burning and stinging [207]. Furthermore, both Skinasensyl ® LS 9749 and Skinasensyl ® LS 9852 inhibit the release of the neuromediator CGRP from sensory neurons, and increase the skin's tolerance threshold [207][208][209].…”

Functionalized polystyrene beads as carriers in release studies of two herbicides: 2,4-dichlorophenoxyacetic acid and 2-methyl-4-chlorophenoxyacetic acid

“…(1) where F-fraction of herbicide released at time "t," M t -amount of herbicide released at time "t," M-total amount of herbicide release at time "t," K-kinetic constant, n-release exponent, t-time (Dash et al 2010;Goscianska et al 2016;Lewandowski et al 2014;Olejnik et al 2017;Sahoo et al 2012).…”