Abstract
It is necessary for local anesthetics to pass through the stratum corneum to provide rapid pain relief. Many techniques have been reported to enhance intradermal penetration of local anesthetics such as vesicular lipid carriers. Ethosomes are lipid vesicles containing phospholipids, ethanol at relatively high concentration. We hypothesized that synergistic effects of phospholipids and high concentration of ethanol in formulation could accelerate penetration of nanoethosomes in deep layers of skin. Lidocaine-loaded nanoethosomes were prepared and characterized by size and zeta analyzer, scanning electron microscopy (SEM) and X-ray diffractometer (XRD). Furthermore, encapsulation efficiency (EE), loading capacity (LC), and skin penetration capability were evaluated by in vitro and in vivo experiments. results showed that the particle size, zeta potential, EE and LC of optimum formulation were 105.4 ± 7.9 nm, -33.6 ± 2.4 mV, 40.14 ± 2.5 %, and 8.02 ± 0.71 respectively. SEM results confirmed the non-aggregated nano-scale size of prepared nanoethosomes. Particle size of ethosomes and EE of Lidocaine were depended on the phospholipid and ethanol concentrations. XRD results demonstrated the drug encapsulation in amorphous status interpreting the achieved high drug EE and LC values. In vitro and in vivo assays confirmed the appropriate skin penetration of Lidocaine with the aid of nanoethosomes and existence of deposition of nanoethosomes in deep skin layers, respectively. The developed nanoethosomes are proposed as a suitable carrier for topical delivery of anesthetics such as Lidocaine.
Highlights
Local anesthetics cause a reversible loss of sensation in a portion of the body, and they reversibly block impulse conduction along nerve axons and other excitable membranes
Several studies have focused on the use of liposomes to improve percutaneous delivery; because of the absence of deep skin penetration and because liposomes remain limited to the upper layer of the stratum corneum, it is commonly agreed that conventional liposomes are not suitable as carriers for transdermal drug delivery.[10,11,12,13,14]
Increasing the ethanol concentration from 10% to 40% resulted in the production of nanoethosomes with a higher particle size
Summary
Local anesthetics cause a reversible loss of sensation in a portion of the body, and they reversibly block impulse conduction along nerve axons and other excitable membranes. Topical formulations may offer significant benefits for preventing procedural pain.[3,4] Several problems can arise with conventional topical preparations, e.g., negligible uptake because of the barrier function of the stratum corneum and late onset of action To overcome these limitations, nanoparticulate drug carriers, lipid-based systems, have been introduced to disrupt and weaken the highly organized intercellular lipids, thereby enhancing intradermal drug penetration, increasing the duration of local action, and preventing systemic absorption of drugs, and reducing the side effects associated with the systemic absorption of anesthetics.[5,6,7,8,9] Different vesicular systems, especially liposomes, have been studied by numerous investigators. The incorporation of Lidocaine into vesicular systems, which provides efficient drug delivery through skin, may open up a new market for pharmaceutical and cosmetic industries
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