Fabrication of Alginate-Based O/W Nanoemulsions for Transdermal Drug Delivery of Lidocaine: Influence of the Oil Phase and Surfactant

Transdermal drug delivery of lidocaine is a good choice for local anesthetic delivery. Microemulsions have shown great effectiveness for the transdermal transport of lidocaine. Oil-in-water nanoemulsions are particularly suitable for encapsulation of lipophilic molecules because of their ability to...

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Bibliographic Details
Published in:	Molecules (Basel, Switzerland) Switzerland), 2021-04, Vol.26 (9), p.2556
Main Authors:	Sarheed, Omar, Dibi, Manar, Ramesh, Kanteti V R N S, Drechsler, Markus
Format:	Article
Language:	eng
Subjects:	Administration, Cutaneous Alginates Alginates - chemistry Alginates - pharmacology Alginic acid Beeswax Dilution Drug delivery Drug Delivery Systems Emulsions - chemistry Emulsions - pharmacology Fabrication Fatty acids Humans in vitro skin permeation Lidocaine Lidocaine - chemistry Lidocaine - pharmacology Light scattering Lipids Lipophilic Microemulsions Nanoemulsions Nanostructures - chemistry Oil oil type Particle size phase inversion temperature (PIT) method Photon correlation spectroscopy pig skin Pigskins Skin Structural analysis Surface-Active Agents - chemistry surfactant concentration Surfactants Transdermal medication Ultrasound
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Summary:	Transdermal drug delivery of lidocaine is a good choice for local anesthetic delivery. Microemulsions have shown great effectiveness for the transdermal transport of lidocaine. Oil-in-water nanoemulsions are particularly suitable for encapsulation of lipophilic molecules because of their ability to form stable and transparent delivery systems with good skin permeation. However, fabrication of nanoemulsions containing lidocaine to provide an extended local anesthetic effect is challenging. Hence, the aim of this study was to address this issue by employing alginate-based o/w nanocarriers using nanoemulsion template that is prepared by combined approaches of ultrasound and phase inversion temperature (PIT). In this study, the influence of system composition such as oil type, oil and surfactant concentration on the particle size, in vitro release and skin permeation of lidocaine nanoemulsions was investigated. Structural characterization of lidocaine nanoemulsions as a function of water dilution was done using DSC. Nanoemulsions with small droplet diameters (d < 150 nm) were obtained as demonstrated by dynamic light scattering (DLS) and cryo-TEM. These nanoemulsions were also able to release 90% of their content within 24-h through PDMS and pig skin and able to the drug release over a 48-h. This extended-release profile is highly favorable in transdermal drug delivery and shows the great potential of this nanoemulsion as delivery system.
ISSN:	1420-3049 1420-3049