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Nanoethosomes for Dermal Delivery of Lidocaine.

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.

SUBMITTER: Babaie S

PROVIDER: S-EPMC4729340 | biostudies-other | 2015 Nov

REPOSITORIES: biostudies-other

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Nanoethosomes for Dermal Delivery of Lidocaine.

Babaie Soraya S Ghanbarzadeh Saeed S Davaran Soodabeh S Kouhsoltani Maryam M Hamishehkar Hamed H

Advanced pharmaceutical bulletin 20151130 4

<h4>Purpose</h4>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 de ...[more]

PMID: 26819928

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Project description:The composition of topical and transdermal formulations is known to determine the rate and the extent of drug delivery to and through the skin. However, to date, the role of excipients in these formulations on skin delivery of actives has received little attention from scientists in the field. Monitoring skin absorption of both drug and vehicle may provide insights into the mechanism by which excipients promote permeation and may facilitate the design of effective and safer products. Previously, we have investigated the use of quantitative Confocal Raman Spectroscopy (CRS) to investigate the delivery of an active to the skin, and we also reported the first fully quantitative study that compared this method with the well-established in vitro permeation test (IVPT) model. To further explore the potential of quantitative CRS in assessing topical delivery, the present work investigated the effects of commonly used excipients on the percutaneous absorption of a model drug, ibuprofen (IBU). Permeation of IBU and selected solvents following finite dose applications to human skin was determined in vitro and in vivo by Franz diffusion studies and quantitative CRS, respectively. The solvents used were propylene glycol (PG), dipropylene glycol (DPG), tripropylene glycol (TPG), and polyethylene glycol 300 (PEG 300). Overall, the cumulative amounts of IBU that permeated at 24 h in vitro were similar for PG, DPG, and TPG (p > 0.05). These three vehicles outperformed PEG 300 (p < 0.05) in terms of drug delivery. Concerning the vehicles, the rank order for in vitro skin permeation was DPG ≥ PG > TPG, while PEG 300 did not permeate the skin. A linear relationship between maximum vehicle and IBU flux in vitro was found, with a correlation coefficient (R2) of 0.95. When comparing in vitro with in vivo data, a positive in vitro-in vivo (IVIV) correlation between the cumulative permeation of IBU in vitro and the total amount of IBU that penetrated the stratum corneum (SC) in vivo was observed, with a Pearson correlation coefficient (R2) of 0.90. A strong IVIV correlation, R2 = 0.82, was found following the linear regression of the cumulative number of solvents permeated in vitro and the corresponding skin uptake in vivo measured with CRS. This is the first study to correlate in vivo permeation of solvents measured by CRS with data obtained by in vitro diffusion studies. The IVIV correlations suggest that CRS is a powerful tool for profiling drug and vehicle delivery from dermal formulations. Future studies will examine additional excipients with varying physicochemical properties. Ultimately, these findings are expected to lead to new approaches for the design, evaluation, and optimization of formulations that target actives to and through the skin.

Project description:BackgroundPost-herpetic neuralgia (PHN) is a common type of neuropathic pain that can severely affect quality of life. NGX-4010, a capsaicin 8% dermal patch, is a localized treatment that can provide patients with significant pain relief for up to 3 months following a single 60-minute application. The NGX-4010 application can be associated with application-site pain and in previous clinical trials pretreatment with a topical 4% lidocaine anesthetic was used to enhance tolerability. The aim of the current investigation was to evaluate tolerability of NGX-4010 after pretreatment with lidocaine 2.5%/prilocaine 2.5% anesthetic cream.MethodsTwenty-four patients with PHN were pretreated with lidocaine 2.5%/prilocaine 2.5% cream for 60 minutes before receiving a single 60-minute application of NGX-4010. Tolerability was assessed by measuring patch application duration, the proportion of patients completing over 90% of the intended treatment duration, application site-related pain using the Numeric Pain Rating Scale (NPRS), and analgesic medication use to relieve such pain. Safety was assessed by monitoring adverse events (AEs) and dermal irritation using dermal assessment scores.ResultsThe mean treatment duration of NGX-4010 was 60.2 minutes and all patients completed over 90% of the intended patch application duration. Pain during application was transient. A maximum mean change in NPRS score of +3.0 was observed at 55 minutes post-patch application; pain scores gradually declined to near pre-anesthetic levels (+0.71) within 85 minutes of patch removal. Half of the patients received analgesic medication on the day of treatment; by Day 7, no patients required medication. The most common AEs were application site-related pain, erythema, edema, and pruritus. All patients experienced mild dermal irritation 5 minutes after patch removal, which subsequently decreased; at Day 7, no irritation was evident. The maximum recorded dermal assessment score was 2.ConclusionNGX-4010 was well tolerated following pretreatment with lidocaine 2.5%/prilocaine 2.5% cream in patients with PHN. The tolerability of the patch application appeared comparable with that seen in other studies that used 4% lidocaine cream as the pretreatment anesthetic. This study is registered at http://www.clinicaltrials.gov as number NCT00916942.

Dataset Information

Nanoethosomes for Dermal Delivery of Lidocaine.

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Nanoethosomes for Dermal Delivery of Lidocaine.

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