Abstract

This article introduces the formulation of alcohol-free, lecithin microemulsion-based gels (MBGs) prepared with gelatin as gelling agent. The influence of oil, water, lecithin and hydrophilic and lipophilic additives (linkers) on the rheological properties and appearance of these gels was systematically explored using ternary phase diagrams. Clear MBGs were obtained in regions of single phase microemulsions (μEs) at room temperature. Increasing the water content in the formulation increased the elastic modulus of the gels, while increasing the oil content had the opposite effect. The hydrophilic additive (PEG-6-caprylic/capric glycerides) was shown to reduce the elastic modulus of gelatin gels, particularly at high temperatures. In contrast to anionic (AOT) μEs, the results suggest that in lecithin (nonionic) μEs, the introduction of gelatin “dehydrates” the μE. Finally, when the transdermal transport of lidocaine formulated in the parent μE and the resulting MBG were compared, only a minor retardation in the loading and release of lidocaine was observed.

Highlights

  • Transdermal drug delivery provides convenient and controlled delivery of drugs to patients with minimum discomfort [1]

  • This work introduced the formulation of alcohol-free, lecithin-based, gelatine microemulsionbased gels (MBGs)

  • When gelatin was added to bicontinuous lecithin μEs, the results suggest that some of the water initially solubilised in the μE was used to produce a dispersed network of gelatin fibers embedded in an oil-rich bicontinuous μE

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Summary

Introduction

Transdermal drug delivery provides convenient and controlled delivery of drugs to patients with minimum discomfort [1]. Microemulsions (μEs) have been proposed to overcome this barrier function and improve transdermal drug permeation [3,4,5,6,7,8,9,10,11]. Periocular ophthalmic delivery is the least invasive method of delivery of drugs to the anterior and posterior section of the eye [12,13,14,15].The resistance to drug transport in periocular delivery is associated with the structure of corneal epithelium and stroma that act as protective barriers that regulate transport to and from the eye through the cornea and sclera [16]. Eye drops formulated using μEs have been shown to improve the solubility of hydrophobic drugs and improve the efficacy of eye drop formulations [17,18,19]

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