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

Abstract

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.

Biomedical application of microemulsion delivery systems: A review

“…The addition of dispersed phase in excess or in response to an abrupt change in temperature leads to phase inversion of a microemulsion. This phase inversion results in drastic changes in the physical behavior of microemulsion such as a change in particle size and hence influences the in vivo and in vitro drug release [14]. The transitional phase inversion can be attained by altering the curvature of the surfactant and hence compelling a conversion from o/w microemulsion at lower temperatures to w/o microemulsion at a higher temperature for non-ionic surfactant.…”

“…Mobility of the hydrocarbon tail can be enhanced by using medium chain length alcohols and hence allow enhanced oil penetration into this region [13]. The development of microemulsion by phase titration method is an impetuous emulsification process and can be demonstrated using a phase diagram [14] (Figure 1). The complex interactions between the various components of the microemulsion system can be studied by using a phase diagram.…”

Biomaterials and Extracellular Vesicle Delivery: Current Status, Applications and Challenges

“…More specifically, SA is a derivative of alginic acid and is composed of α-1-guluornic (G) and 1,4-linked-β-D-mannuronic (M) monomers [ 55 ]. Alginate has been used to deliver various classes of drugs including NSAIDs [ 56 ], chemotherapeutics [ 57 , 58 ], and anesthetics [ 59 ]. Hormones such as insulin [ 60 ] and salmon calcitonin [ 61 ] have also been delivered via alginate.…”

Physicochemical Characteristics of Chitosan-Based Hydrogels Containing Albumin Particles and Aloe vera Juice as Transdermal Systems Functionalized in the Viewpoint of Potential Biomedical Applications

“…The oil-in-water nanoemulsions were proposed as drug carriers because such systems are considered particularly suitable for encapsulation of lipophilic molecules. The prepared drug delivery systems showed stability and allowed the release of the drug through the skin within 24 and 48 h [ 9 ]. Transdermal plasters also based on the emulsions have been developed, e.g., by Patel et al [ 10 ] and Fardous et al [ 11 ].…”