Development of Lecithin Nanoemulsion Based Organogels for Permeation Enhancement of Metoprolol through Rat Skin

Abstract

Background. Drugs with low oral bioavailability due to the first pass metabolism are good candidates for transdermal delivery.Objectives. The aim of this work was preparation of transdermal nanoemulsion of metoprolol which has high first pass metabolism. Methods. Three commercially available types of lecithin (200, 100p, and 170), three short chain alcohol (n-butanol, isopropyl alcohol, and n-propanol), and isopropyl myristate (IPM) were used as surfactant, cosurfactant, and oil phase, respectively. The aqueous phase was composed of metoprolol tartrate. Nanoemulsions with different surfactant/cosurfactant weight ratio, various amounts of drug, and different types of alcohol were prepared, and their phase diagrams were studied. Drug release, permeability, and diffusion coefficient of the drug were studied using hairless rat skin. Results. A significant increase in drug solution rate was observed with increasing the metoprolol content in the nanoemulsions, while it decreased when lecithin concentration increased from 40% to 60%. Increasing the water content resulted in a significant increase in metoprolol release. N-butanol enhanced the drug flux from nanoemulsions more than n-propanol and isopropyl alcohol. The o/w nanoemulsions of metoprolol showed high flux and permeability through the skin. Conclusion. Both w/o and o/w nanoemulsions of metoprolol could enhance permeation and diffusion of metoprolol through rat skin.

Nanoemulsion: A Review on Mechanisms for the Transdermal Delivery of Hydrophobic and Hydrophilic Drugs

“…When the water-soluble metoprolol was formulated in o/w NE, it exhibited higher in vitro release compared to w/o NE. However, there was no significant difference between the 2 types of NE regarding rat skin permeation and no mechanism was suggested [126].…”

Development of pharmaceutical clear gel based on Peceol®, lecithin, ethanol and water: Physicochemical characterization and stability study

“…This resulting gel was found to be clear, thermodynamically stable, viscoelastic and thermoreversible . These properties have generated much interest over the years for the potential use of the lecithin gel for mucosal and topical drug delivery of hydrophilic, lipophilic and amphiphilic active substances [30][31][32][33][34][35].…”

Biocompatible Nutmeg Oil-Loaded Nanoemulsion as Phyto-Repellent

“…NT 6 exhibited non-Newtonian plastic behavior, whereas NT 11 showed Newtonian flow behavior ( Figure 5) due to the difference in the water ratio. Varshosaz et al (2013) stated that the coalescence of inner water droplets in the emulsion system gave effect on the behavior of the emulsion system. A nanoemulsion with low viscosity would not be adequate for an insect repellent product meant for topical skin application because it would tend to flow easily (Khurana et al, 2013).…”