Effective permeation of 2.5 and 5% lidocaine hydrochloride in human skin using iontophoresis technique

Manjunatha, Roopa G.; Sharma, Sunil; Narayan, Ravi Prakash; Koul, Veena

doi:10.1111/ijd.14107

Cited by 7 publications

(6 citation statements)

References 24 publications

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“…Topical anesthetics like LID block reversibly the free nerve-ending conductions in the dermis and mucosa. This process can be limited by drug diffusion through the epidermis, since in healthy skin the drug has to pass through the stratum corneum to reach dermal tissue at therapeutic concentrations [ 56 ]. The versatility of 3D-bioprinting was exploited in this work to produce different types of skin substitutes (full-thickness healthy skin and dermal layer tissue) to study the effect of epidermis barrier on LID diffusion and to mimic the open wound skin tissue.…”

Section: Resultsmentioning

confidence: 99%

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

et al. 2020

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The delivery of bioactive agents using active wound dressings for the management of pain and infections offers improved performances in the treatment of wound complications. In this work, solid lipid microparticles (SLMPs) loaded with lidocaine hydrochloride (LID) were processed and the formulation was evaluated regarding its ability to deliver the drug at the wound site and through the skin barrier. The SLMPs of glyceryl monostearate (GMS) were prepared with different LID contents (0, 1, 2, 4, and 10 wt.%) using the solvent-free and one-step PGSS (Particles from Gas-Saturated Solutions) technique. PGSS exploits the use of supercritical CO2 (scCO2) as a plasticizer for lipids and as pressurizing agent for the atomization of particles. The SLMPs were characterized in terms of shape, size, and morphology (SEM), physicochemical properties (ATR-IR, XRD), and drug content and release behavior. An in vitro test for the evaluation of the influence of the wound environment on the LID release rate from SLMPs was studied using different bioengineered human skin substitutes obtained by 3D-bioprinting. Finally, the antimicrobial activity of the SLMPs was evaluated against three relevant bacteria in wound infections (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa). SLMPs processed with 10 wt.% of LID showed a remarkable performance to provide effective doses for pain relief and preventive infection effects.

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Section: Resultsmentioning

confidence: 99%

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

et al. 2020

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“…Moreover, the results showed that H90 1 P 2 -L had the highest amount of released lidocaine HCl, which was a significant difference from H5 1 P 2 -L and H50 1 P 2 -L. At 60 min, the results had related to dissolving ability, since H90 1 P 2 -L showed the fastest dissolving ability. Thus, H90 1 P 2 -L should release the highest amount of lidocaine HCl, while the needles of H5 1 P 2 -L and H50 1 P 2 -L did not completely dissolve, so the released amount of lidocaine HCl was lower than for H90 1 P 2 -L. Interestingly, all three formulations provided an adequate released amount of lidocaine HCl to reach an anesthetic effect (approximately 135 μg/cm 2 or 239 μg/1.77 cm 2 ) [ 20 ]. Moreover, the released amount of lidocaine HCl will not cause the side effects since the toxic dose of lidocaine HCl is when the dose exceeds 4.5 mg/kg [ 37 ].…”

Section: Resultsmentioning

confidence: 99%

“…Lidocaine HCl is generally administered via an intravenous or intramuscular injection to provide a high bioavailability, but it causes pain during insertion [ 18 ]. Due to its poor permeability, the slow penetration of lidocaine HCl is a major drawback of its topical use, since it typically takes at least ~1–2 h to reach a therapeutic effect [ 20 ]. However, lidocaine HCl shows a rapid onset of action (~20–60 s) [ 21 ], which is promising for its use with dissolving MNs, which can rapidly provide the therapeutic anesthetic effect of lidocaine HCl through the skin without pain during skin insertion.…”

Section: Introductionmentioning

confidence: 99%

HPMC/PVP K90 Dissolving Microneedles Fabricated from 3D-Printed Master Molds: Impact on Microneedle Morphology, Mechanical Strength, and Topical Dissolving Property

Chanabodeechalermrung,

Chaiwarit,

Chaichit

et al. 2024

Polymers

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Three-dimensional (3D) printing can be used to fabricate custom microneedle (MN) patches instead of the conventional method. In this work, 3D-printed MN patches were utilized to fabricate a MN mold, and the mold was used to prepare dissolving MNs for topical lidocaine HCl (L) delivery through the skin. Topical creams usually take 1–2 h to induce an anesthetic effect, so the delivery of lidocaine HCl from dissolving MNs can allow for a therapeutic effect to be reached faster than with a topical cream. The dissolving-MN-patch-incorporated lidocaine HCl was constructed from hydroxypropyl methylcellulose (HPMC; H) and polyvinyl pyrrolidone (PVP K90; P) using centrifugation. Additionally, the morphology, mechanical property, skin insertion, dissolving behavior, drug-loading content, drug release of MNs and the chemical interactions among the compositions were also examined. H51P2-L, H501P2-L, and H901P2-L showed an acceptable needle appearance without bent tips or a broken structure, and they had a low % height change (<10%), including a high blue-dot percentage on the skin (>80%). These three formulations exhibited a drug-loading content approaching 100%. Importantly, the composition-dependent dissolving abilities of MNs were revealed. Containing the lowest amount of HPMC in its formulation, H901P2-L showed the fastest dissolving ability, which was related to the high amount of lidocaine HCl released through the skin. Moreover, the results of an FTIR analysis showed no chemical interactions among the two polymers and lidocaine HCl. As a result, HPMC/PVP K90 dissolving microneedles can be used to deliver lidocaine HCl through the skin, resulting in a faster onset of anesthetic action.

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“…Ibuprofen is a very popular non-steroidal analgesic and anti-inflammatory drug [ 20 ]. The lidocaine is used as topical anesthetic in dermatology and cosmetology to alleviate the pain from non-surgical cosmetic procedures [ 60 ]. Caffeine is very popular anti-aging agent applied in cosmetic preparations.…”

Section: Discussionmentioning

confidence: 99%

“…In the in vitro penetration experiments, an abdomen porcine skin was used due to their similar permeability to human skin. Numerous histopathological studies confirmed its similarity to human skin [60,61]. The porcine skin obtained from the local slaughterhouse was used.…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

Epilobium angustifolium L. Essential Oil—Biological Activity and Enhancement of the Skin Penetration of Drugs—In Vitro Study

et al. 2021

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Epilobium angustifolium L. is a popular medicinal plant found in many regions of the world. This plant contains small amounts of essential oil whose composition and properties have not been extensively investigated. There are few reports in the literature on the antioxidant and antifungal properties of this essential oil and the possibility of applying it as a potential promoter of the skin penetration of drugs. The essential oil was obtained by distillation using a Clavenger type apparatus. The chemical composition was analyzed by the GC-MS method. The major active compounds of E. angustifolium L. essential oil (EOEa) were terpenes, including α-caryophyllene oxide, eucalyptol, β-linalool, camphor, (S)-carvone, and β-caryophyllene. The analyzed essential oil was also characterized by antioxidant activity amounting to 78% RSA (Radical Scavenging Activity). Antifungal activity against the strains Aspergillus niger, A. ochraceus, A. parasiticum, and Penicillium cyclopium was also determined. The largest inhibition zone was observed for strains from the Aspergillus group. The EOEa enhanced the percutaneous penetration of ibuprofen and lidocaine. After a 24 h test, the content of terpene in the skin and the acceptor fluid was examined. It has been shown that the main compounds contained in the essential oil do not penetrate through the skin, but accumulate in it. Additionally, FTIR-ATR analysis showed a disturbance of the stratum corneum (SC) lipids caused by the essential oil application. Due to its rich composition and high biological activity, EOEa may be a potential candidate to be applied, for example, in the pharmaceutical or cosmetic industries. Moreover, due to the reaction of the essential oil components with SC lipids, the EOEa could be an effective permeation enhancer of topically applied hydrophilic and lipophilic drugs.

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Effective permeation of 2.5 and 5% lidocaine hydrochloride in human skin using iontophoresis technique

Abstract: Study shows that modulated IOP can be a promising alternative method in clinical settings aside from continuous IOP. Based on the clinical requirements, IOP can be used at 2.5 and 5% lidocaine concentration depending on need of relatively short or very short onset action.

Cited by 7 publications

References 24 publications

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

HPMC/PVP K90 Dissolving Microneedles Fabricated from 3D-Printed Master Molds: Impact on Microneedle Morphology, Mechanical Strength, and Topical Dissolving Property

Epilobium angustifolium L. Essential Oil—Biological Activity and Enhancement of the Skin Penetration of Drugs—In Vitro Study

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