Preparation and Characterization of a Lecithin Nanoemulsion as a Topical Delivery System

Abstract

Purpose of this study was to establish a lecithin nanoemulsion (LNE) without any synthetic surfactant as a topical delivery vehicle and to evaluate its topical delivery potential by the following factors: particle size, morphology, viscosity, stability, skin hydration and skin penetration. Experimental results demonstrated that an increasing concentration of soybean lecithin and glycerol resulted in a smaller size LNE droplet and increasing viscosity, respectively. The droplet size of optimized LNE, with the glycerol concentration above 75% (w/w), changed from 92 (F10) to 58 nm (F14). Additionally, LNE, incorporated into o/w cream, improved the skin hydration capacity of the cream significantly with about 2.5-fold increase when the concentration of LNE reached 10%. LNE was also demonstrated to improve the penetrability of Nile red (NR) dye into the dermis layer, when an o/w cream, incorporated with NR-loaded LNE, applied on the abdominal skin of rat in vivo. Specifically, the arbitrary unit (ABU) of fluorescence in the dermis layer that had received the cream with a NR-loaded LNE was about 9.9-fold higher than the cream with a NR-loaded general emulsion (GE). These observations suggest that LNE could be used as a promising topical delivery vehicle for lipophilic compounds.

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

“…Full factorial experimental design During the nanoemulsion development, a two-level 2 3 full factorial experimental design was used to identify and estimate the main and interaction effects of three different formulation factors (oil type -A, oil content -B, and presence of model drug -C) on critical quality attributes of the developed nanoemulsions. Each factor was varied at two coded (-1, +1) levels, in which the -1 level corresponds to the lower value and +1 to the upper value of each independent variable (Table 2).…”

“…Considering the formulation and physicochemical characteristics, nanoemulsions have been associated with a number of advantages such as a low surfactant concentration, a uniform and very small droplet size, low viscosity, and high solubilization capacity for lipophilic drugs. Additionally, the improved penetration through biological barriers, possible enhanced bioavailability and organ targeting could be expected with these systems [1][2][3][4][5][6]. Although lipid nanoemulsions have been traditionally employed for parenteral nutrition and intravenous delivery of lipophilic drugs -with several approved products on the market -the additional efforts are required to optimize nanoemulsion formulation, stability, and overall drug delivery [1,7].…”

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“…Xerosis is said to be one of the very significant parameter in AD pathophysiology, which has both cause and effect dimensions to it. Formulations which increase skin hydration are expected to useful in management of AD 10,25 . Ex-vivo studies across rodent skin in a Franz diffusion cell demonstrated that less than 10% drug permeates transdermally into the receptor compartment from optimized formulation as well as marketed cream preparation.…”

Formulation, development, and optimization of a novel octyldodecanol-based nanoemulsion for transdermal delivery of ceramide IIIB

“…This leads to increased skin hydration, which may promote the absorption of topically applied drugs or cosmetics. 12 The very small droplet size greatly reduces the gravitational force, 13 and Brownian motion largely prevents gravitationally driven sedimentation or creaming. 6,10,14 The transparent nature of O/W nanoemulsions, their good fluidity, and the absence of any thickeners give them a pleasant aesthetic character and skin feel.…”