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Local anesthesia is essential in dental practices, particularly for managing pain in tooth socket wounds, yet improving drug delivery systems remains a significant challenge. This study explored the physicochemical characteristics of lidocaine hydrochloride (LH) incorporated into a polyelectrolyte complex and poloxamer thermosensitivity hydrogel, assessing its local anesthetic efficacy in mouse models and its onset and duration of action as topical anesthetics in clinical trials. The thermoresponsive hydrogel exhibited a rapid phase transition within 1–3 minutes and demonstrated pseudo-plastic flow behavior. Its release kinetics followed Korsmeyer-Peppas, with 50% of biodegradation occurring over 48 h. In mouse models, certain thermogels showed superior anesthetic effects, with rapid onset and prolonged action, as evidenced by heat tolerance in tail-flick and hot plate models. In clinical trials, the LH-loaded thermoresponsive hydrogel provided rapid numbness onset, with anesthesia (Ton) beginning at an average of 46.5 ± 22.5 seconds and lasting effectively (Teff) for 202.5 ± 41.0 seconds, ranging from 120 to 240 seconds, indicating sustained release. These results highlight the promising properties of these formulations: rapid onset, prolonged duration, mucoadhesion, biodegradability, and high anesthesia effectiveness. This study demonstrates the potential for advancing local anesthesia across various medical fields, emphasizing the synergy between material science and clinical applications to improve patient care and safety. [ABSTRACT FROM AUTHOR]

Background and Aims: The aim of this study was to prolong the anesthetic effect of lidocaine (LC) in the oral cavity for use in the treatment of oral mucositis and to compare the in vitro characteristics of the film formulations prepared by using either chitosan extracted from Metapenaeus stebbingi (M. stebbingi) or commercial chitosan. Methods: In this study, the in vitro properties of the film formulations extracted and prepared with commercial chitosan were successfully compared with the addition of different types and amounts of plasticizer and cross-linking agent. In the evaluation of the formulations, different parameters such as structure, thickness, degree of swelling, moisture content, drug content, texture profile analysis, release kinetics according to the in vitro drug release, and cytotoxicity evaluation were taken into consideration. Results: Films prepared using chitosan extracted with 5% glycerol addition showed the highest strength and lowest elongation properties compared to other films (p<0.05). The thickness of the films varied between 500-1400 µm in all formulations. While it was observed that formulations prepared with medium molecular weight commercial chitosan had high surface roughness, the lowest swelling degree was observed for these formulations (77.41 ± 3.65-84.76 ± 6.34). The highest degree of swelling was calculated for the formulations prepared with extracted chitosan (137.23 ± 7.86). The in vitro dissolution rate results demonstrated that the increase in the molecular weight of chitosan caused a decrease in the release rate of lidocaine, while at the same time, formulations with added crosslinking agents exhibited a slower release profile. Cytotoxicity studies revealed cell viability at different polymer concentrations. Conclusion: All the in vitro characterization results showed that extracted chitosan from M. stebbingi shells can be a good alternative for pharmaceutical use. [ABSTRACT FROM AUTHOR]

There is an urgent need for research into effective interventions for pain management to improve patients' life quality. Traditional needle and syringe injection were used to administer the local anesthesia. However, it causes various discomforts, ranging from brief stings to trypanophobia and denial of medical operations. In this study, a dissolving microneedles (MNs) system made of composite matrix materials of polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), and sodium hyaluronate (HA) was successfully developed for the loading of lidocaine hydrochloride (LidH). The morphology, size and mechanical properties of the MNs were also investigated. After the insertion of MNs into the skin, the matrix at the tip of the MNs was swelled and dissolved by absorption of interstitial fluid, leading to a rapid release of loaded LidH from MNs' tips. And the LidH in the back patching was diffused into deeper skin tissue through microchannels created by MNs insertion, forming a prolonged anesthesia effect. In addition, the back patching of MNs could be acted as a drug reservoir to form a prolonged local anesthesia effect. The results showed that LidH MNs provided a superior analgesia up to 8 h, exhibiting a rapid and long-lasting analgesic effects. Additionally, tissue sectioning and in vitro cytotoxicity tests indicated that the MNs patch we developed had a favorable biosafety profile. [ABSTRACT FROM AUTHOR]

Background: The use of Procaine hydrochloride in cardioplegia has been discontinued due to challenges importing the product from outside the country despite its crucial role in preserving myocardium during heart surgery. However, Lidocaine hydrochloride, an anti-arrhythmic medication, functions similarly to Procaine hydrochloride. Both medications are compared regarding their effectiveness in preventing ventricular fibrillation, the most common type of heart arrhythmia, after releasing the aortic cross-clamp in cardiac surgery. Materials and Methods: This is a retrospective study in which data was collected from medical records of patients who were operated on with coronary artery bypass grafts between May 2017 and August 2023. Patient demographics and early outcomes between the two groups were analyzed. Results: A total of 328 patients who underwent CABG were divided into 2 groups, respectively. Group "P" received cardioplegia solutions with Procaine hydrochloride, whilst group "L" received cardioplegia solutions with Lidocaine hydrochloride. The average age of the participants was 64.19 years old in group P and 64.24 years old in group L. The duration of the aortic cross-clamp was significantly different between the two groups, with durations of 76.06 minutes and 87.79 minutes, respectively, showing a p-value of less than 0.01 in statistical analysis. Following the release of aortic cross-clamping, the occurrence of ventricular fibrillation was observed in 37 patients (43%) in the first group and 49 patients (56.9%) in the second group, with no significant difference noted. After defibrillation at 10 joules, there were 21 patients (24.4%) in the first group and 13 patients (15.1%) in the second group, indicating a significant difference. Additionally, no significant difference was observed in the duration of the CCU stay between both groups. Conclusion: Cardioplegic solution containing Lidocaine hydrochloride provides the same clinical result as Procaine hydrochloride in coronary artery bypass grafting surgery. [ABSTRACT FROM AUTHOR]

The aim of the work is the development of chromatographic conditions, the study of the validation characteristics of the method of quantitative determination of phenylephrine hydrochloride, nitrofural, lidocaine hydrochloride and diphenhydramine hydrochloride, panthenol, povidone in the joint presence in the nasal spray by a complex method of liquid chromatography with UV detection. Evaluation of the quantitative content of active components after manufacturing and during the shelf life. Materials and methods. Agilent 1260 liquid chromatographs, equipped with a diode-matrix detector from the company "Agilent technologies", USA. Chromatographic columns 250×4.6 mm in size, filled with octadecylsilyl silica gel for chromatography (Zorbax StableBond SB-Aq, Agilent company), mobile phase A - phosphate buffer solution pH 7.0 - acetonitrile P (1650:350), mobile phase B - acetonitrile P; elution mode - gradient; mobile phase flow rate - 1.0 ml/min; detection wavelengths - 220 nm (for panthenol, phenylephrine, povidone, diphenhydramine) and 235 nm (for nitrofural and lidocaine). Results. Chromatographic separation conditions were developed for the co-presence determination of six target substances: panthenol, phenylephrine hydrochloride, nitrofural, povidone, lidocaine hydrochloride and diphenhydramine hydrochloride. The suitability of the technique for this task was confirmed by determining the validation characteristics. The methodology at the appropriate level is characterized by specificity, linearity, correctness and convergence in the range of application for panthenol (range 20.33–38.26 mg/ml, ΔZ=0.93≤max ΔZ=3.20, a=0.63≤max a=5.12, r=0.9978≥min r=0.9924), phenylephrine hydrochloride (range 1.70–3.21 mg/ml, ΔZ=0.51≤max ΔZ=3.20, a=0.15≤max a=5.12, r=0.9984≥min r=0.9924), nitrofural (range 0.137–0.257 mg/ml, ΔZ=0.91≤max ΔZ=3.20, a=0.032≤max a=5.12, r=0.9987≥min r=0.9924) povidone (range 20,44–38,50 mg/ml, ΔZ=0.23≤max ΔZ=3.20, a=2.33 ≤ max a=5.12, r=0.9942≥min=0.9924), lidocaine hydrochloride (range 6.80– 12.81 mg/ml, ΔZ=0.34≤max ΔZ=3.20, a=0.66 ≤ max a=5.12, r=0.9988≥min r=0.9924), diphenhydramine hydrochloride (range 1.36–2.56 mg/ml, ΔZ=0.20≤max ΔZ=3.20, a=0.15≤max a=5.12, r=0.9980≥min r=0.9924). There are no significant changes when stored at 25 °C for 6 months. [ABSTRACT FROM AUTHOR]

In the present article chitosan-based aerogel particles with the impregnated lidocaine hydrochloride via supercritical adsorption method were studied. During the research particles of 1% chitosan aerogel were obtained by the dripping method. Drying of the obtained gels was carried out in a supercritical fluid. The impregnation of lidocaine hydrochloride into the pores of the chitosan-based aerogel was carried out by supercritical adsorption with varying process temperature. The article presents the schemes of apparatuses for the drying process and supercritical adsorption. Using the method of high-performance liquid chromatography, the amount of impregnated drug in the obtained aerogel samples was determined. The sorption capacity of the obtained particles was determined using a solution simulating blood, Earle's Balanced Salt Solution. It was found that the samples have a sorption capacity comparable to the sorption capacity of aerogel particles without impregnated lidocaine hydrochloride. Using X-ray phase analysis, the state of the drug in the pores of the chitosan-based aerogel was investigated. In the course of the research work a release kinetics of lidocaine hydrochloride from aerogel particles was also obtained using a dissolution tester Sotax AT 7 Smart, the "rotating paddle" method. The results of the conducted analytical studies demonstrate that when an active pharmaceutical ingredients is impregnated into aerogel particles by supercritical adsorption, it is possible to obtain a local hemostatic agent with a therapeutic anesthetic effect and a controlled dosage of the active pharmaceutical substance to relieve pain when used. [ABSTRACT FROM AUTHOR]

Cubosomes, which are modified cubic phase systems, are looking very promising as a method of delivering both hydrophilic and lipophilic drugs. Transdermal delivery of cubosomes is currently gaining more importance over conventional topical delivery of drugs. The proposed study aimed to produce Lidocaine hydrochloride loaded cubosomes. This study was designed to prepare various formulations of Lidocaine nano cubsomal dispersions at different concentrations of lipid and stabilizer using optimization technique. For the purpose of prolonging the duration of the local anaesthetic action, Lidocaine-loaded cubosomes were developed by bottom up method utilizing Glyceryl mono oleate and Poloxamer 407 in various ratios using the "Quality by Design" approach, 32 factorial design employing statistical software. Within the confidence intervals, the 32 statistical design was effective at forecasting the optimized formulation's composition. Surface morphology, particle size, drug content, poly dispersibility index, zeta potential, entrapment efficiency, and in vitro drug release studies were conducted on the prepared formulations. Several mathematical models were used to conduct and assess an in vitro drug release investigation. The maximal entrapment efficiency for the LH8 formulation, which was validated to have optimum cubosomes dispersion, was reported to be 78 % with vesicle size as 150 nm, Zeta potential 21.5 mV and Poly Dispersibility Index as 0.08 along with an in vitro drug release 80.03 % by the end of 24 hours. A stable dispersion with appreciable results of evaluation parameters of cubosomal dispersion was conferred with formulation LH8. Hence from amongst the nine formulations developed, it is concluded that LH8 is selected as the optimized dispersion to be incorporated into a gel formulation. [ABSTRACT FROM AUTHOR]

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Abstract In this study, it was aimed to introduce a transdermal drug delivery system with dissolving microneedles (DMNs) based on gelatin (GEL) and sodium carboxymethyl cellulose (NaCMC) for lidocaine hydrochloride (LidoHCl) delivery. Different ratios of GEL and NaCMC were mixed, loaded with an active agent of LidoHCl, and treated with glutaraldehyde (GTA) as a crosslinker agent. Prepared hydrogels were cast into a silicon mold. Hereby, microneedles (MNs) with 500 µm height, 35° needle angle, 40-µm tip radius, and 960-µm tip-to-tip distance were fabricated. Samples containing LidoHCl 40%, GEL/NaCMC 5:1 (wt/wt), and polymer/GTA ratio 3.1 (wt/wt) showed the highest drug release ability (t

Modern medicines for the treatment of wounds are developed on the basis of knowledge about their phase healing. The main principle of wound treatment is the creation and maintenance of a moist environment, stable temperature, absorption of excess exudate, minimization of the risk of sensitization, increased intervals between dressings, easy removal of coatings from the surface of the wound. The implementation of this principle is the basis of our research on the creation of a cryogel – a supermacroporous hydrogel that is formed at subzero temperatures by polymerization of monomers or cryogel formation of oligomers without the use of toxic organic solvents and with controlled textural and structural characteristics. A comprehensive study of cryogels has like theoretical as practical interest, because they can serve as a perspectiving new material in pharmacy for obtaining new medicines. The purpose of our research was to substantiate the composition of the cryogel with lidocaine hydrochloride and decamethoxine based on the conducted pharmacotechnological, physicochemical and biopharmaceutical research methods. Model samples (№№ 1–10) with different contents of lidocaine hydrochloride, decamethoxine, and auxiliary substances were selected as research objects. Pharmacotechnological, physicochemical and biopharmaceutical research methods were used. The technological and biopharmaceutical factors of development pharmaceutical composition in the form of a cryogel with lidocaine hydrochloride and decamethoxine were studied. Based on the results of the research, we found that samples (№№ 1–10) are homogeneous without signs of delamination, no changes are observed (aggregation of particles, sediment, odor). Samples №№ 3, 9 and 10 differ in the presence/absence of API. It was shown that APIs do not affect the absorption capacity of the studied samples. Comparative studies confirm our assumption that the presence of PG in the cryogel increases the absorption of liquid by the samples. The prolongation of the action in the composition depends on the presence of PG in the sample of composition. The prolonged effect of pharmaceutical composition was established. For further research, sample № 10 (lidocaine hydrochloride – 0.4; decamethoxine – 0.03; PVA 15% – 20.0; PG – 10.0) was chosen.

In the treatment of pain, especially chronic pain, the rule of multimodal therapy applies, based on various painkillers mechanisms of action. The aim of the conducted study was to evaluate the in vitro penetration of ketoprofen (KET) and lidocaine hydrochloride (LH) through the human skin from a vehicle with transdermal properties. The results obtained with the use of the Franz chamber showed statistically significantly higher penetration of KET from the transdermal vehicle as compared to commercial preparations. It was also shown that the addition of LH to the transdermal vehicle did not change the amount of KET permeated. The study also compared the penetration of KET and LH by adding various excipients to the transdermal vehicle. Comparing the cumulative mass of KET that penetrated after the 24-h study, it was observed that the significantly highest permeation was found for the vehicle containing additionally Tinctura capsici, then for that containing camphor and ethanol, and the vehicle containing menthol and ethanol as compared to that containing Pentravan® alone. A similar tendency was observed in the case of LH, where the addition of Tinctura capsici, menthol and camphor led to a statistically significant higher penetration. Adding certain drugs such as KET and LH to Pentravan®, and substances such as menthol, camphor or capsaicin, can be an interesting alternative to administered enteral drugs especially in the group of patients with multiple diseases and polypragmasy. [ABSTRACT FROM AUTHOR]

In this study, it was aimed to introduce a transdermal drug delivery system with dissolving microneedles (DMNs) based on gelatin (GEL) and sodium carboxymethyl cellulose (NaCMC) for lidocaine hydrochloride (LidoHCl) delivery. Different ratios of GEL and NaCMC were mixed, loaded with an active agent of LidoHCl, and treated with glutaraldehyde (GTA) as a crosslinker agent. Prepared hydrogels were cast into a silicon mold. Hereby, microneedles (MNs) with 500 µm height, 35° needle angle, 40-µm tip radius, and 960-µm tip-to-tip distance were fabricated. Samples containing LidoHCl 40%, GEL/NaCMC 5:1 (wt/wt), and polymer/GTA ratio 3.1 (wt/wt) showed the highest drug release ability (t < 10 min) with proper mechanical properties in comparison with other samples. Due to the drug release in a short time (fewer than 10 min), this drug delivery system can be used for rapid local anesthesia for pain relief as well as before minor skin surgeries. [ABSTRACT FROM AUTHOR]

The properties of sodium hyaluronate (HA), such as hygroscopicity, flexibility, the ability to form hydrogels, as well as biocompatibility and biodegradability, are beneficial for the applications in pharmaceutical technology, cosmetics industry, and aesthetic medicine. The aim of this study was to prepare HA-based hydrogels doped with active pharmaceutical ingredient (API): a cationic drug—lidocaine hydrochloride or anionic drug—sodium. The interaction between the carrier and the implemented active pharmaceutical substances was evaluated in prepared systems by applying viscometric measurements, performing release tests of the drug from the obtained formulations, and carrying out FTIR and DSC. The data from release studies were analyzed using the zero-, first-, and second-order kinetics and Higuchi, Korsmeyer-Peppas, and Hixon-Crowell models. The respective kinetic parameters: the release rate constants, the half-release time and, in the case of the Korsmeyer-Peppas equation, the n parameter were calculated. The variability between the obtained release profiles was studied by calculating the difference (f1) and the similarity factor (f2) as well as employing statistical methods. It was revealed that the incorporation of the drugs resulted in an increase in the viscosity of the hydrogels in comparison to the respective drug-free preparations. The dissolution study showed that not entire amount of the added drug was released from the formulation, suggesting an interaction between the carrier and the drug. The FTIR and DSC studies confirmed the bond formation between HA and both medicinal substances. [ABSTRACT FROM AUTHOR]

The problem of drug delivery often concentrates on the prolongation of drug activity. Application of natural polymers which are biodegradable and inexpensive is in the interest of many researchers. The aim of this study was the application of newly synthesized starch derivatives as potential functional excipients proposed for hydrophilic gel with lidocaine hydrochloride (LH) to prolong drug release from the hydrogel matrix. In our study, we investigated the effect of starch modified with citric acid on the release kinetics of LH using UV-VIS and Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), as well as viscosity and pH measurements. We demonstrated the effectiveness of citric-acid-modified starch in prolonging the release of LH from methylcellulose gel. [ABSTRACT FROM AUTHOR]

Most of the time, castration is an elective procedure performed to make the camel docile and manage its behavior. There are also instances, where it is performed as a treatment of testicular abnormalities such as orchitis, irreparable traumatic injuries, and tumors. In the current study, a 7‐year‐old bull dromedary camel was brought to Addis Ababa University College of Veterinary Medicine and Agriculture, Feseha Gebre Ab VTH, with a history of recurrent swelling of the left testicle for a month. Based on history and clinical examination, the case was diagnosed as unilateral orchitis and admitted for open castration of both testes. Two percent lidocaine hydrochloride was injected into each testicle to provide a spermatic nerve block, and then, two parallel incisions were made through the scrotal skin on either side of the median raphe. The testicles were pulled out through these incisions, ligated, and transected. The scrotal incisions were left open to heal by themselves. Postoperatively, antibiotic and anti‐inflammatory drugs were administered for 3 successive days. Finally, the camel was regularly followed for 1 week and recovers uneventfully. [ABSTRACT FROM AUTHOR]

In the treatment of pain, especially chronic pain, the rule of multimodal therapy applies, based on various painkillers mechanisms of action. The aim of the conducted study was to evaluate the in vitro penetration of ketoprofen (KET) and lidocaine hydrochloride (LH) through the human skin from a vehicle with transdermal properties. The results obtained with the use of the Franz chamber showed statistically significantly higher penetration of KET from the transdermal vehicle as compared to commercial preparations. It was also shown that the addition of LH to the transdermal vehicle did not change the amount of KET permeated. The study also compared the penetration of KET and LH by adding various excipients to the transdermal vehicle. Comparing the cumulative mass of KET that penetrated after the 24-h study, it was observed that the significantly highest permeation was found for the vehicle containing additionally Tinctura capsici, then for that containing camphor and ethanol, and the vehicle containing menthol and ethanol as compared to that containing Pentravan® alone. A similar tendency was observed in the case of LH, where the addition of Tinctura capsici, menthol and camphor led to a statistically significant higher penetration. Adding certain drugs such as KET and LH to Pentravan®, and substances such as menthol, camphor or capsaicin, can be an interesting alternative to administered enteral drugs especially in the group of patients with multiple diseases and polypragmasy.

Abstract Most of the time, castration is an elective procedure performed to make the camel docile and manage its behavior. There are also instances, where it is performed as a treatment of testicular abnormalities such as orchitis, irreparable traumatic injuries, and tumors. In the current study, a 7‐year‐old bull dromedary camel was brought to Addis Ababa University College of Veterinary Medicine and Agriculture, Feseha Gebre Ab VTH, with a history of recurrent swelling of the left testicle for a month. Based on history and clinical examination, the case was diagnosed as unilateral orchitis and admitted for open castration of both testes. Two percent lidocaine hydrochloride was injected into each testicle to provide a spermatic nerve block, and then, two parallel incisions were made through the scrotal skin on either side of the median raphe. The testicles were pulled out through these incisions, ligated, and transected. The scrotal incisions were left open to heal by themselves. Postoperatively, antibiotic and anti‐inflammatory drugs were administered for 3 successive days. Finally, the camel was regularly followed for 1 week and recovers uneventfully.

Buccal film formulations, including antifungal nystatin, anti-inflammatory agent hydrocortisone acetate, and local anesthetic lidocaine hydrochloride for pain relief, were developed. Bioadhesive films were fabricated with hydrophilic polymers, hydroxyethyl cellulose (HEC), and xanthan gum (XG) and dried in the incubator. Textural, swelling, and bioadhesive properties, physicochemical and in vitro release characteristics, and antifungal activities of bioadhesive films were evaluated. Bioadhesive films significantly extended nystatin release by prolonging retention time of the target area formulation while rapidly releasing hydrocortisone acetate and lidocaine HCl, reducing drug administration. The polymer type affected bioadhesion strength and erosion ratio, and XG formulations had more polymer suitability. Consequently, XT-O2 formulation that was prepared with xanthan gum and tween 80, was best for its highest antifungal film activity (20.00 ± 0.07 mm), released nystatin (44.296% ± 1.695), and lowest erosion matrix (36.719% ± 0.249). The selected formulation can be used for compatibility, stability and in vivo studies targeted oral candidiasis infections. [ABSTRACT FROM AUTHOR]

Backgrounds: A new generic formulation of 3.5% lidocaine hydrochloride ophthalmic gel has been developed in China. This study aimed to evaluate the pharmacokinetics and effectiveness of this lidocaine hydrochloride gel for ocular surface anesthesia. Methods: In the pharmacokinetics study, the new form of 3.5% lidocaine hydrochloride gel or Akten™ 3.5% lidocaine hydrochloride gel was applied in eyes of 70 rabbits. The ocular tissues and plasma samples were collected after the application of 3.5% lidocaine hydrochloride gel or Akten lidocaine gel and analyzed using the liquid chromatography with tandem mass spectrometry (LC-MS/MS) method to determine the concentration of lidocaine. A multicenter, randomized, double-blind prospective clinical trial was conducted in Chinese adults. Two hundred twenty participants were 1:1 randomized into the sham gel group or the lidocaine hydrochloride group. The primary efficacy endpoint was defined as the percentage of subjects achieving anesthesia by 5 min. Results: The animal pharmacokinetics study showed the lidocaine level was significantly higher in the choroid at 15 min and the vitreous body at 15 and 30 min; it was lower in tears at 8 h for 3.5% lidocaine hydrochloride gel than Akten (P ≤ 0.05). Our clinical trial showed that the percentage of subjects achieving anesthesia within 5 min in the lidocaine hydrochloride gel group was significantly higher than the sham gel group (86.92%-18.18%, P < 0.0001). The incidence of adverse events was relatively low and favorable for both groups. Conclusion: This new formulation of lidocaine hydrochloride gel, with pharmacokinetics similar to Akten, may exert a sustained, effective, and safe anesthetic effect. The clinical trial for this new generic formulation of lidocaine hydrochloride has been registered with the Drug Clinical Trial Registration and Information Publicity Platform established by State Food and Drug Administration of China (Registration No. CTR20160593). [ABSTRACT FROM AUTHOR]

Li-Zhou Wang,1,&ast; Xiao-Xia Hu,2,&ast; Xiang-Chun Shen,2,3 Tian-Cheng Wang,4 Shi Zhou1 1Department of Interventional Radiology, The Affiliated Hospital of Guizhou Medical University, Guiyang, Guizhou, People’s Republic of China; 2The State Laboratory of Functions and Application of Medicinal Plants, Guizhou Medical University, Guiyang, Guizhou, People’s Republic of China; 3School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, Guizhou, People’s Republic of China; 4Department of Radiology, The Second Xiangya Hospital of Central South University, Changsha, Hunan, People’s Republic of China&ast;These authors contributed equally to this workCorrespondence: Tian-Cheng WangDepartment of Radiology, The Second Xiangya Hospital of Central South University, Changsha, Hunan, 410011, People’s Republic of ChinaTel +86 15073190153Email 421176806@qq.comShi ZhouDepartment of Interventional Radiology, The Affiliated Hospital of Guizhou Medical University, Guiyang, Guizhou, 550004, People’s Republic of ChinaTel +86 13809477708Email zhoushi@gmc.edu.cnObjective: To investigate the sustained release of lidocaine from a lidocaine–epirubicin–lipiodol emulsion created by water-in-oil (W/O) technique in vivo and evaluate the efficacy and safety of intraarterial lidocaine administration for intra- and postoperative pain control in transarterial chemoembolization (TACE) for hepatocellular carcinoma (HCC).Methods: The in vivo concentrations of lidocaine were determined in tumor tissues after VX2 rabbit models for hepatic tumor were administered with intra-arterial lidocaine–epirubicin–lipiodol emulsion. A prospective randomized controlled clinical trial was performed, enrolling 70 consecutive patients who underwent TACE. Patients were randomized into two groups: Group A received an immediate bolus intraarterial lidocaine injection before TACE, and Group B received a lidocaine–epirubicin–lipiodol emulsion during TACE. Pain intensity was compared between the two groups using a visual analog scale (VAS) score before (Tbefore) and at 0 h (T0), 4 h (T4), 8 h (T8), 24 h (T24), 48 h (T48), and 72 h (T72) after the procedure. Adverse events and intake of analgesics were evaluated and compared between the two groups.Results: The concentrations of lidocaine in tumor tissues were higher in experimental group than in control group at T0.5 (P=0.004), T1 (P=0.038), T4 (P=0.036), and T8 (P=0.029). In the clinical trial, VAS scores in Group B were significantly lower than in Group A at T0 (P=0.006), T4 (P=0.001), T8 (P=0.002), and T24 (P=0.005). The tramadol intake in Group B was significantly lower than in Group A (P=0.021). No significant difference was observed regarding the incidence of adverse events between the two groups.Conclusion: This study demonstrated the effectiveness and safety of intraarterial lidocaine administration using the W/O technique in controlling intra- and post-TACE pain.Keywords: carcinoma, hepatocellular, chemoembolization, therapeutic, lidocaine hydrochloride, pain management

The main purpose of this study was to assess a lidocaine hydrochloride-loaded chitosan-pectin-hyaluronic polyelectrolyte complex for rapid onset and sustained release in dry socket wound treatment. Nine formulations (LCs) of lidocaine hydrochloride (LH) loaded into a chitosan–pectin–hyaluronic polyelectrolyte complex (PEC) were assessed using full factorial design (two factors × three levels). The formulations ranged between 4 and 10% w/w LH and 0.5–1.5% w/w HA. The following physicochemical properties of LCs were characterized: size, zeta potential, % entrapment efficiency, viscosity, mucoadhesiveness, % drug release, morphology, storage stability, and cytotoxicity. The particle size, zeta potential, % EE, viscosity, and % mucoadhesion increased with increasing LH and HA concentrations. Rapid release of LH followed a zero-order model, and a steady-state percentage of the drug was released over 4 h. LCs were found to be non-cytotoxic compared to LH solution. LH loaded into PEC demonstrated appropriate characteristics—including suitable rate of release—and fit a zero-order model. Furthermore, it was not cytotoxic and showed good stability in a high-HA formula, making it a promising candidate for future topical oral formulations.

Medicinal aerosols for external use are a less popular form of the drug than aerosols for internal use, i.e., inhalation aerosols. Most common are dermal and nasal aerosols. If the aerosol is used on damaged skin, it must be sterile. Aerosols intended for use on damaged epidermis form a bandage after spraying, protecting the wound from external contamination. The use of natural polymers such as alginates is also widespread in the treatment of wounds and burns. Alginates gel creates hydrogels with a high degree of hydration. This process happens by adding electrolytes. A moist environment promotes proper wound healing processes. What is more, bandages reduce the risk of wound infection. The aim of this work was to develop the composition and technology of manufacture for an aerosol gel based on the natural polymer such as sodium alginate. The active ingredient used as a topical anesthetic in the formulations was lidocaine hydrochloride in 1% concentration. It is characterized by a local anesthetic effect and is used in creams, ointments, and gels commercially available in pharmacies. After the aerosol is sprayed on the surface, the gel covers it evenly and does not need to be spread. The form of a gel gives a feeling of cooling to the burned area, and lidocaine hydrochloride is designed to anesthetize it additionally. Rheological evaluation of the obtained gels was a performer. Effects of the addition of the active substance and excipients on the viscosity of the formulations were investigated. The efficacy of antimicrobial preservation was assessed to select the preservative. In addition, the amount of propellant and a suitable valve and spray atomizer were also chosen for each aerosol to reduce the foaming effect. Quantitative determination of the active substance present in the aerosol composition was performed using high-performance liquid chromatography (HPLC) with isocratic elution. The method used was validated for specificity, accuracy, precision, and linearity. Based on the calibration curve, limits of detection and quantification (LOD and LOQ) for lidocaine hydrochloride were also calculated. The optimal concentration of sodium alginate in the developed gel is 0.6%, which was confirmed by the viscosity test results. The preservative was bronopol in concentration 0,01%. Isopropanol and colloidal silica were included in the formulation to reduce the foam created after the aerosol was sprayed on the substrate. The amount of propellant in relation to the amount of the gel was around 10:90 (m/m).

Background. Purulent wound healing is a pressing surgical challenge relevant in 30−35% of patient cases. To the more, wound infectious agents elaborate resistance to available drugs warranting the development of new drug combinations exserting a multidirectional effect on the wound process.Objective. Using a purulent wound model to experimentally evaluate the efficiency of a new multicomponent wound coating comprised of polyethylene oxide and carboxymethylcellulose sodium-immobilised dioxidine, methyluracil, metronidazole and lidocaine hydrochloride in comparison with a legal approved wound coating drug preparation of beeswax and propolis-based dioxidine ointment.Methods. The antimicrobial activity range (disk-diffusion method) and local anaesthetic effect (Rainier’s method) of the developed wound coating have been assessed. The healing process was studied in a purulent wound model with 72 Wistar rats divided between two equal groups. The following methods were applied: visual wound inspection (wound cleansing time, absence of wound-surrounding tissue oedema, granulation and epithelisation), planimetric parameter estimation (wound area, healing rate, wound area reduction ratio), wound contamination and pH measurement, wound section cell morphometry (granulocyte, macrophage, lymphocyte and fibroblast counts, cell index estimation). Daily dressings were applied for 15 days.Results. The developed wound coating exhibited high efficiency against Gram-positive and Gram-negative bacteria in the zone of inhibition tests. Its local anaesthetic effect was significantly superior to the approved drug by the duration of action. The wound area reduction was 94.2 (93.7; 94.8)% in the experimental group and 86 (84.2; 88.8)% in the control (differences statistically significant) already on day 10. A maximal healing rate in both groups was registered in phase 1 of the wound process being 1.4 times higher in experiment compared to the control. The wound contamination was significantly lower in experiment vs. control on day 8 (p = 0.0075). Wound pH negatively correlated with the fibroblast count and positively — with the contamination level.Conclusion. The study demonstrates high efficiency of the developed wound coating against infectious agents and its positive healing impact via reducing phase 1 and stimulating proliferation in phase 2 of the wound process.

The properties of sodium hyaluronate (HA), such as hygroscopicity, flexibility, the ability to form hydrogels, as well as biocompatibility and biodegradability, are beneficial for the applications in pharmaceutical technology, cosmetics industry, and aesthetic medicine. The aim of this study was to prepare HA-based hydrogels doped with active pharmaceutical ingredient (API): a cationic drug—lidocaine hydrochloride or anionic drug—sodium. The interaction between the carrier and the implemented active pharmaceutical substances was evaluated in prepared systems by applying viscometric measurements, performing release tests of the drug from the obtained formulations, and carrying out FTIR and DSC. The data from release studies were analyzed using the zero-, first-, and second-order kinetics and Higuchi, Korsmeyer-Peppas, and Hixon-Crowell models. The respective kinetic parameters: the release rate constants, the half-release time and, in the case of the Korsmeyer-Peppas equation, the n parameter were calculated. The variability between the obtained release profiles was studied by calculating the difference (f1) and the similarity factor (f2) as well as employing statistical methods. It was revealed that the incorporation of the drugs resulted in an increase in the viscosity of the hydrogels in comparison to the respective drug-free preparations. The dissolution study showed that not entire amount of the added drug was released from the formulation, suggesting an interaction between the carrier and the drug. The FTIR and DSC studies confirmed the bond formation between HA and both medicinal substances.

This study aimed to develop photo-triggered implantable polymeric microneedles (MNs) for successful drug delivery in a transdermal analgesia system. The prepared iron oxide nanoparticles (Fe3O4NPs) were coated with polydopamine (PDA) followed by polyvinylpyrrolidone (PVP) and polycaprolactone (PCL). While the PCL/PVP-Fe3O4NPs synthesis, the absorption band of PVP at 1656 cm−1 shifted to 1665 cm−1 which indicate the presence of interaction between Fe+ and C = O groups. The size and morphology of PCL/PVP-Fe3O4NPs were examined by scanning electron microscope and transmission electron microscope (SEM and TEM) analysis. The results confirmed that the prepared PCL/PVP-Fe3O4NPs were spherical with sizes ranging from 9 to 11 nm. The lidocaine hydrochloride content in the microneedles was 3.72 ± 0.31 mg and A + 2.2S ≤ L representing that the drug was uniformly distributed. The insertion ability of lidocaine hydrochloride@PCL/PVP-Fe3O4NPs-DMNs was tested by porcine skin. The results demonstrated outstanding insertion ability and potential for drug delivery. In addition, near-infrared (NIR) irradiation has the potential to penetrate the skin and enhance lidocaine hydrochloride-releasing activity. The in vivo experimental data confirmed that lidocaine hydrochloride@PCL/PVP-Fe3O4NPs-DMNs allowed for painless drug delivery by breaking the barrier of the stratum corneum. To conclude, lidocaine hydrochloride can be safely delivered through the transdermal analgesic system, with a quick onset time. [ABSTRACT FROM AUTHOR]

Abstract Background Since January 2019, surgical castration of male piglets must be performed using local anaesthesia, if farmers deliver pigs to the primary exporting slaughterhouses according to the “Danish quality scheme”; a voluntary initiative taken by the Danish pig industry. The approved procedure for local anaesthesia in Denmark is a three-step injection method with procaine. A comparison of lidocaine and procaine with the same concentration and injection methods of local anaesthetics has not previously been studied. The purpose of this study was to investigate the effect of two injection methods and two local anaesthetics on piglets’ avoidance behaviour (vocalisation and resistance movements) as well as the time spent on the procedures. The study included 203 male piglets that were randomly assigned to one of five treatments: 1. Control: Sham-handling without injection of local anaesthesia, 2. Pro3: Procaine injection using a three-step method, 3. Pro2: Procaine injection using a two-step method, 4. Lid3: Lidocaine injection using a three-step method, 5. Lid2: Lidocaine injection using a two-step method. During injection of local anaesthesia and castration, vocalisation was measured using a decibel meter and resistance movements were registrated by video recordings. Results During castration, piglets treated with local anaesthesia showed significantly reduced vocalisation and resistance movements and time spent on castration was also significantly reduced compared to the control group. During injection of the local anaesthesia, the piglets had significantly increased vocalisation and resistance movements compared to the control group. Piglets injected with lidocaine had a significantly reduced resistance movement score and a tendency to reduced vocalisation compared to piglets injected with procaine. No differences in avoidance behaviour were found between the injection methods. Conclusions The use of local anaesthesia, irrespective of the method and local anaesthetic, was effective in reducing vocalisation and resistance movements during surgery as well as the time spent on castration.

Abstract Background Uterine fibroid is a common benign pelvic tumor and abdominal myomectomy may cause excessive intraoperative bleeding, which may lead to adverse outcomes. Objective This study was planned to evaluate the effectiveness of the injection of lidocaine plus epinephrine to reduce intraoperative bleeding in abdominal myomectomy. Methods During October 2019 and May 2020, 60 eligible women with uterine fibroids were enrolled in a randomized controlled trial. Our patients were divided into two groups of lidocaine plus epinephrine defined as Group L and placebo defined as Group P. In group L, lidocaine 3 mg/kg plus 0.5 ml of adrenaline which reached to 50 cc with saline solution and in group P, 50 ml of normal saline was used. Both the combined solution and normal saline were infiltrated to the serous and myometrium above and around the fibroid before incision. Patients' demographic data, total operative time, hemoglobin changes, and the degree of surgical difficulty were evaluated and compared between the two groups. Results There was no significant difference between the two groups in terms of demographic data. Hemoglobin changes (p

Background: Iontophoresis is one of the widely used noninvasive and painless transdermal drug delivery technique. Objective: Transdermal delivery of Lidocaine Hydrochloride using continuous and modulated iontophoresis were evaluated across human skin ex-vivo and further assessed for skin tolerance in-vivo in the Swiss albino mice. Methods: Continuous DC was modified into modulated DC by introducing ON-OFF time in continuous DC. Iontophoresis studies were conducted on human skin samples for 60 min. Results: Drug permeation of 2% lidocaine HCl was enhanced in current density-, duty cycle- and time-dependent manner across human skin. The lidocaine HCl concentration obtained with modulated DC and continuous DC iontophoresis were about three-fold and four-fold higher than passive group respectively for all current densities across human skin. Continuous DC iontophoresis was found to be more effective than modulated DC. However, no significant difference was observed in transport of lidocaine HCl between 75% and 100% (continuous) duty cycle at all current density. Further, in-vivo reversibility studies with mice confirmed that modulated iontophoresis was well tolerated by the tissue and the injury caused is transient and reversible. Conclusion: For clinical application, modulated DC iontophoresis with 75% duty cycle at 0.5 mA/cm2 current density would be recommended.

The problem of drug delivery often concentrates on the prolongation of drug activity. Application of natural polymers which are biodegradable and inexpensive is in the interest of many researchers. The aim of this study was the application of newly synthesized starch derivatives as potential functional excipients proposed for hydrophilic gel with lidocaine hydrochloride (LH) to prolong drug release from the hydrogel matrix. In our study, we investigated the effect of starch modified with citric acid on the release kinetics of LH using UV-VIS and Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), as well as viscosity and pH measurements. We demonstrated the effectiveness of citric-acid-modified starch in prolonging the release of LH from methylcellulose gel.

Doris Grablowitz,1 Monika Sulovsky,2 Sonja Höller,3 Zrinka Ivezic-Schoenfeld,3 Souyet Chang-Rodriguez,3 Martin Prinz3 1Medizinisch Ästhetisches Zentrum Wien, Wien 1010, Austria; 2YUVELL® Fine Aesthetics, Wien 1010, Austria; 3Croma-Pharma GmbH, Leobendorf 2100, AustriaCorrespondence: Martin PrinzCroma-Pharma GmbH, Industriezeile 6, Leobendorf 2100, AustriaTel +43 2262 684 68-0Fax +43 2262 684 68-165Email martin.prinz@croma.atPurpose: Nasolabial folds (NLFs) are one of the most noticeable signs of facial aging. NLFs negatively affect self-confidence and social acceptance often leading to a person’s desire to improve their appearance using dermal fillers. The hyaluronic acid injectable gel implant Princess® FILLER Lidocaine (PFL) is a minimally invasive easy to administer the product. In this investigation, we assessed the safety and efficacy of PFL to correct moderate to severe NLFs over a 36-week period.Methods: Adult women and men with moderate to severe NLFs received one injection of PFL to both NLFs. After 2 weeks, a touch-up treatment could be performed, if deemed necessary by the investigator. The change in NLF severity was assessed using the Nasolabial Fold Severity Rating Scale (NFL-SRS) developed by Croma-Pharma and the Global Aesthetic Improvement Scale (GAIS).Results: Out of 60 analyzed subjects, 59 (98.3%) had improved their NLF severity by at least 1 grade on the NFL-SRS at week 4, 58 subjects (96.7%) at weeks 24 and 36. All subjects showed aesthetic improvement (GAIS), at weeks 4 and 24. The investigator judged the aesthetics as very much improved (score of 1) in 45 (75.0%) at week 4, 48 (80.0%) at week 24, and in 39 of 60 subjects, respectively (65.0%) at week 36. Thirty-six weeks post-initial treatment, 56 of 60 subjects (93.3%) were very satisfied or satisfied with the treatment. Adverse device effects (ADEs) were mild or moderate and resolved at latest 25 days post-onset. The most commonly reported ADEs were injection site hematoma and injection site pain.Conclusion: PFL was safe and effective in reducing the severity of NLFs. Most subjects were (very) satisfied with the treatment outcome throughout a 36 weeks investigation period.Keywords: hyaluronic acid, dermal filler, lidocaine hydrochloride, mid to deep dermis, facial wrinkles, injection

The main purpose of this study was to assess a lidocaine hydrochloride-loaded chitosan-pectin-hyaluronic polyelectrolyte complex for rapid onset and sustained release in dry socket wound treatment. Nine formulations (LCs) of lidocaine hydrochloride (LH) loaded into a chitosan–pectin–hyaluronic polyelectrolyte complex (PEC) were assessed using full factorial design (two factors × three levels). The formulations ranged between 4 and 10% w/w LH and 0.5–1.5% w/w HA. The following physicochemical properties of LCs were characterized: size, zeta potential, % entrapment efficiency, viscosity, mucoadhesiveness, % drug release, morphology, storage stability, and cytotoxicity. The particle size, zeta potential, % EE, viscosity, and % mucoadhesion increased with increasing LH and HA concentrations. Rapid release of LH followed a zero-order model, and a steady-state percentage of the drug was released over 4 h. LCs were found to be non-cytotoxic compared to LH solution. LH loaded into PEC demonstrated appropriate characteristics—including suitable rate of release—and fit a zero-order model. Furthermore, it was not cytotoxic and showed good stability in a high-HA formula, making it a promising candidate for future topical oral formulations. [ABSTRACT FROM AUTHOR]

Lidocaine is a primary local anesthesia that blocks the ionic fluxes required for the beginning and operation of impulses in the neuronal membrane. The benefits of local anesthetics, such as enhancing patient acceptance, prohibiting systemic toxicity and delivering continuous drug delivery, make them the attracting field for pharmaceutical researchers. The nanoparticles were prepared by solvent evaporation W1/O/W2 emulsion method and in the ratios of 1 to 1, 1 to 2 and 1 to 3 drug to polymer. The production yield, loading efficiency, particle size, poly dispersity index and zeta potential of selected formulation were 84.30%, 80.60%, 192 nm, 0.18 mV and + 4 2. 8 mV, respectively. DSC and FTIR studies showed that no chemical interactions between drug and polymer Formulations showed an initial burst release, which is a reason for the good capacity of the polymer to maintain the drug in it and lead to a primary slow release. [ABSTRACT FROM AUTHOR]

Chitosan/collagen composite scaffolds encapsulating allantoin and lidocaine hydrochloride were formulated in various ratios and characterized in vitro for their applications in wound healing. After fabrication, scaffolds were characterized in terms of topographical properties, surface roughness, and swelling behavior, and then their stabilities were monitored by hydrolytic and enzymatic degradation studies. Following compatibility studies among the active ingredients, drugs were encapsulated within scaffolds, and encapsulation efficiency and drug release studies were carried. Finally, in vitro cell viability and scratch wound healing assays were carried to assess scaffolds as wound dressings. Results suggest that blending of polymers with drugs changed topographical properties and surface roughness prominently. It is found that the formulation with chitosan/collagen ratio of 70/30 is more resistant to both hydrolytic and enzymatic degradation routes due to having favored properties of both collagen and chitosan. In vitro drug release studies indicated rapid release of drugs, hence the scaffolds could be advantageous for patients that need an immediate anesthetic effect in wound healing therapy. The cell culture studies demonstrated that the chitosan/collagen composite scaffolds showed no toxicity, and cell migrations were increased depending on the collagen ratio in scaffolds. These results suggest that chitosan/collagen scaffolds combined with allantoin and lidocaine hydrochloride could be a promising candidate for wound healing applications. [ABSTRACT FROM AUTHOR]

Dental diseases are often accompanied by painful sensations, so usually symptomatic treatment of these pathologies includes local anesthetics, as which we have selected anesthetic of local action – lidocaine hydrochloride. The aim of the research is to substantiate the rational concentration of lidocaine hydrochloride in the composition of the dental gel being developed by pharmacological screening of its model samples. The object of the study is dental gel with tincture "Phytodent" (PJSC “CPP “Red Star”, Ukraine), choline salicylate 80% (Basf Pharma, Switzerland) and lidocaine hydrochloride (Societa Italiana Medicinali Scandicci, Italy). The anesthetic was injected into the gel at various concentrations – 1.0%, 1.5% and 2.0%. The study of local anesthetic/analgesic activity of gel test samples was performed by the Randall-Selitto method using an electronic Pressure Analgesiometer (IITC Life Science, USA). The study was conducted on male rats weighing 190–210 g. The animals were divided into three groups: animals of the 1st group were applied with 2.0% lidocaine hydrochloride gel (sample number 1), the second group – with 1.5% concentration (sample number 2), the third group – with 1.0% lidocaine content (sample number 3). The animal was held in the hands of a researcher, its limb was placed in analgesiometer. Determined the force of pressure in grams, which causes the reaction of the paw pull back / squeal in response to a painful stimulus. Analgesic activity was studied on the model of kaolin edema, which was simulated by sub-planar introduction of kaolin solution (10 mg/ml) in the amount of 0.1 ml/100 grams of body weight (administration under the aponeurosis of the posterior paw). In animals, the initial pain sensitivity was evaluated 1 hour after the introduction of the phlogogenic agent, after which the gel was applied to the foot, and in 1 hour 15 minutes, 1 hour 30 minutes and 2 hours after the exudative edema modelling. Calculated the percentage of change to the initial threshold of tactile sensitivity, as well as the percentage of change to the level of algesia (pain response) 1 hour after the introduction of the phlogogenic agent. Statistical processing of the data was performed using Student's t-criterion. According to the results, pronounced pain syndrome was detected in animals of all three groups 1 hour after the introduction of the phlogogenic agent. The use of gel with 1.0% concentration of lidocaine hydrochloride did not show a significant antinociceptive effect and could be considered as a tendency for analgesia. The pronounced local anesthetic effect was observed with the use of gel test specimens with the anesthetic concentrations of 1.5% and 2.0% after 15 and 30 minutes and lasted for at least 2 hours. The drug developed was compared with the dental gel “Kamistad®” (Stada Arzneimittel AG, Germany), which also contains lidocaine hydrochloride in an amount of 2.0%. Taking into account the fact that reliable statistical differences in the severity of analgesic activity between the test samples of gel number 1 and number 2 were not detected, it can be argued that lower lidocaine concentration 1.5% in the composition of the developed dental gel can be used. In addition, the claimed dental gel exceeded the referent drug "Kamistad®" (Stada Arzneimittel AG, Germany) by the expressiveness of antinociceptive effect.

A new high-performance liquid chromatography (HPLC) method for the simultaneous quantitative determination of active pharmaceutical substances and preservatives in a new dental medication has been developed. The optimization of HPLC method parameters was done through studies of a mobile phase composition and a detection wavelength. Our developing method uses an ACE C18 column (250 × 4.6 mm, 5 µm) and a gradient mode for separation with the acetonitrile and phosphate buffer solution (adjusted to pH 3.0) as mobile phases. The flow rate is 1 ml/min, and the detection was set at 260 nm (DAD). The method was evaluated according to the ICH guidelines and the State Pharmacopoeia of Ukraine in terms of specificity, accuracy, linearity and precision (repeatability and intermediate precision). The limit of detection and the limit of quantification were also calculated. The developed method was put in place for the analysis of a combined dental gel to a quantitative determination of the APIs (choline salicylate, lidocaine hydrochloride) and preservatives (methylparaben, propylparaben). [ABSTRACT FROM AUTHOR]

Background: Since January 2019, surgical castration of male piglets must be performed using local anaesthesia, if farmers deliver pigs to the primary exporting slaughterhouses according to the "Danish quality scheme"; a voluntary initiative taken by the Danish pig industry. The approved procedure for local anaesthesia in Denmark is a three-step injection method with procaine. A comparison of lidocaine and procaine with the same concentration and injection methods of local anaesthetics has not previously been studied. The purpose of this study was to investigate the effect of two injection methods and two local anaesthetics on piglets' avoidance behaviour (vocalisation and resistance movements) as well as the time spent on the procedures. The study included 203 male piglets that were randomly assigned to one of five treatments: 1. Control: Sham-handling without injection of local anaesthesia, 2. Pro3: Procaine injection using a three-step method, 3. Pro2: Procaine injection using a two-step method, 4. Lid3: Lidocaine injection using a three-step method, 5. Lid2: Lidocaine injection using a two-step method. During injection of local anaesthesia and castration, vocalisation was measured using a decibel meter and resistance movements were registrated by video recordings. Results: During castration, piglets treated with local anaesthesia showed significantly reduced vocalisation and resistance movements and time spent on castration was also significantly reduced compared to the control group. During injection of the local anaesthesia, the piglets had significantly increased vocalisation and resistance movements compared to the control group. Piglets injected with lidocaine had a significantly reduced resistance movement score and a tendency to reduced vocalisation compared to piglets injected with procaine. No differences in avoidance behaviour were found between the injection methods. Conclusions: The use of local anaesthesia, irrespective of the method and local anaesthetic, was effective in reducing vocalisation and resistance movements during surgery as well as the time spent on castration. [ABSTRACT FROM AUTHOR]

The technique of the qualitative and quantitative determination of active substances – decamethoxine and lidocaine hydrochloride in a new combination drug for preventing and treating inflammatory diseases of the oral cavity was developed.The aim of the work was to develop a methodology to identify and determine the active pharmaceutical ingredient in the composition of the dental gel.The objects were specimens of the developed dental gel containing lidocaine hydrochloride and decamethoxine. The study was conducted using high performance liquid chromatography (HPLC).The conditions for HPLC chromatographic investigations, providing sufficient selectivity and separation efficiency of the gel components were proposed.It was determined that the content of the dental gel component is within acceptable limits, and metrological characteristics of the method allow to recommend it to control the gel quality. 1 gram of the gel contains: decamethoxine – 0.591 mg/g (at a rate of 0.45–0.55 mg/g), lidocaine hydrochloride – 0.396 mg/g (at a rate of 0.36–0.44 mg/g).Approximate retention time of decamethoxine peak is 18.4 min, lidocaine hydrochloride – 13.5 min. Retention time of the peak of decamethoxine and lidocaine hydrochloride investigational solution and reference solution did not exceed 2%.

Background: Two percent lidocaine hydrochloride is the gold standard for dental anesthesia against which newer local anesthetic agents may be compared. 0.75% ropivacaine is a newer, long-acting amide local anesthetic agent with inherent vasoconstriction property. Aim: This study aims to compare the efficacy of 0.75% ropivacaine and 2% lidocaine hydrochloride with 1:200,000 adrenaline in pain control in extraction of mandibular posterior teeth. Settings and Design: This is a prospective, double-blind, and split-mouth study. Subjects and Methods: Twenty patients were divided into two groups according to the right and left sides of patient – side A and side B. The side, where 0.75% ropivacaine was to be administered, was randomly selected by flip coin method. Then, the pterygomandibular and long buccal nerve blocks were administered with 0.75% ropivacaine and necessary dental extraction was performed. After 1 week, the same procedure was repeated using 2% lidocaine hydrochloride with 1:200,000 adrenaline. The parameters assessed were pain on injection, onset of anesthesia, pain during the extraction, and duration of anesthesia. Statistical Analysis Used: The nonparametric data were assessed by Mann Whitney “U” test. Results: The mean onset of action for solution A was 7.15 ± 4.934 min and for solution B was 9.75±5.128 min. This was statistically significant. The mean duration of action, pain on injection, and pain during extraction were not significant. Conclusion: This study clearly states that there is no clear advantage of using 0.75% ropivacaine in pterygomandibular nerve block over the gold standard. However, more clinical studies with larger sample size are necessary.

To treat anal fissure, internal anal sphincterotomy may be associated with surgical risks and incidence of incontinence. Botulinum toxin injection into the anal sphincter is invasive and expensive. Headache and hypotension hindered topical treatment with glyceryl trinitrate. Greater patient compliance, potentiated efficacy, reduced side effects, and lower cost are the major advantages offered by the combination therapy. Therefore, combination topical gels of nifedipine (NIF), lidocaine hydrochloride (LDH) and betamethasone valerate (BMV) were prepared and evaluated regarding viscosity, pH, drug content, and in vitro release. Compatibility study of drug–drug and drug-excipient mixtures preceded the formulation. Stability study was performed. A prospective randomized clinical trial was conducted for six weeks to assess the efficacy of the optimized formula in the treatment of anal fissure either acute (AAF, 37 patients) or chronic (CAF, 34 patients) in comparison with three single drug market products. The compatibility was indicated except in case of LDH with each of poloxamer 407 (P407), methylparaben, and propylparaben as well as BMV with P407. The gels showed acceptable viscosity ranges, tolerated pH values, and drugs content limits complying with the pharmacopeial limit. The gel containing 10% Transcutol® (F2) was selected as optimized formula due to the significant (p

Objective: To study the intervention effect of Yuquan Decoction on OSF carcinogenesis and the expression of c-Myc protein, cyclin D1 and 茁-catenin. Methods: In this study, 92 patients with OSF canceration who were treated in our hospital from April 2018 to April 2019 were divided into western medicine group and traditional Chinese medicine group according to the complete random method, 46 cases in each group. Western medicine group was given triamcinolone acetonide injection plus lidocaine hydrochloride injection. The traditional Chinese medicine group was given Yuquan Decoction on the basis of Western medicine group. The changes of 茁-catenin, FIB, c-Myc, IL-6, TGF-茁1 and Cyclin D1 were detected and compared before and after treatment. And the therapeutic effect and adverse reactions of the two groups were compared. Results: After treatment, the total effective rate (91.30%) of Chinese medicine group was significantly higher than that of Western medicine group (67.39%, P<0.05). After treatment, the expressions of 茁-catenin, FIB, c-Myc, IL-6, TGF-茁1 and Cyclin D1 in the two groups were lower than those before treatment (P<0.05); after treatment, the expressions of 茁-catenin, FIB, c-Myc, IL-6, TGF-茁1 and Cyclin D1 in the traditional Chinese medicine group were significantly lower than those in the western medicine group (P<0.05). After treatment, the opening degree of the Chinese medicine group was smaller, the burning pain was lighter and the fibrous strips was less than those of the western medicine group (P<0.05). The adverse reaction rate (2.17%) in the Chinese medicine group was significantly lower than that in the western medicine group (13.04%, P<0.05). Conclusions: The efficacy and safety of Yuquan Decoction in treating OSF canceration were significantly better than that of triamcinolone acetonide injection combined with lidocaine hydrochloride injection, which may be related to its significant down-regulation of c-Myc, Cyclin D1 and beta-catenin expression and improvement of clinical symptoms. [ABSTRACT FROM AUTHOR]

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Alveolar osteitis is a complication that can occur after tooth extraction, whereby exposed bone results in severe throbbing pain for the patient and can be prone to infection. The current treatment options are widely regarded as sub-optimal. The aim of this project was to investigate in vitro the plausibility of a dual-action monolithic drug-loaded thermosensitive hydrogel that undergoes thermal gelation within the tooth socket and releases both anaesthetic and antimicrobial agents. Hydrogels containing different levels of lidocaine HCl and metronidazole were prepared based upon Carbopol 934P NF and Pluronic F-127 blends. Membrane-less drug release was determined from the set hydrogels into phosphate buffered saline (PBS) at 37 °C as a function of time, following analysis by HPLC. Gelation characteristics and hydrogel dissolution characteristics were also determined. At 23.38% Pluronic F-127, sol–gel transition commenced at 23 °C and gelation was completely at 37 °C (physiological temperature). Setting times varied with Pluronic content and there was an inverse relationship between drug release and Pluronic content. Sustained and dose dependent release of both drugs was observed at therapeutically relevant levels over 24 h, via a combination of diffusion, dissolution and surface erosion processes. Based on the amounts of drugs released, it was determined that hydrogels containing up to 0.5% lidocaine and 0.1% metronidazole exhibited low risk of cytotoxicity to primary human gingival fibroblasts. In an in vivo scenario, the sol-phase formulation would make contact with all inner surfaces of a tooth socket prior to transitioning to monolithic gel-phase and provide sustained release of lidocaine and metronidazole at sub-toxic levels, thereby providing simultaneous pain relief, protection from ingress of debris and pathological bacteria. [ABSTRACT FROM AUTHOR]

An HPLC-UV method for quantitative determination of lidocaine and miramistin in a combination wound-healing gel is reported. The method was validated for specificity, linearity, accuracy, and precision. The linear range for lidocaine hydrochloride was 0.08 – 0.12 mg/mL; for miramistin, 0.04 – 0.06 mg/mL. The linear correlation coefficients were 0.9992 and 0.9996 for lidocaine hydrochloride and miramistin, respectively. The method could be used for quantitative evaluation of lidocaine and miramistin in combination medicines. [ABSTRACT FROM AUTHOR]

Background: Iontophoresis is one of the widely used noninvasive and painless transdermal drug delivery technique. Objective: Transdermal delivery of Lidocaine Hydrochloride using continuous and modulated iontophoresis were evaluated across human skin ex-vivo and further assessed for skin tolerance in-vivo in the Swiss albino mice. Methods: Continuous DC was modified into modulated DC by introducing ON-OFF time in continuous DC. Iontophoresis studies were conducted on human skin samples for 60 min. Results: Drug permeation of 2% lidocaine HCl was enhanced in current density-, duty cycle- and time-dependent manner across human skin. The lidocaine HCl concentration obtained with modulated DC and continuous DC iontophoresis were about three-fold and four-fold higher than passive group respectively for all current densities across human skin. Continuous DC iontophoresis was found to be more effective than modulated DC. However, no significant difference was observed in transport of lidocaine HCl between 75% and 100% (continuous) duty cycle at all current density. Further, in-vivo reversibility studies with mice confirmed that modulated iontophoresis was well tolerated by the tissue and the injury caused is transient and reversible. Conclusion: For clinical application, modulated DC iontophoresis with 75% duty cycle at 0.5 mA/cm2 current density would be recommended. [ABSTRACT FROM AUTHOR]

Purpose: Nasolabial folds (NLFs) are one of the most noticeable signs of facial aging. NLFs negatively affect self-confidence and social acceptance often leading to a person's desire to improve their appearance using dermal fillers. The hyaluronic acid injectable gel implant Princess® FILLER Lidocaine (PFL) is a minimally invasive easy to administer the product. In this investigation, we assessed the safety and efficacy of PFL to correct moderate to severe NLFs over a 36-week period. Methods: Adult women and men with moderate to severe NLFs received one injection of PFL to both NLFs. After 2 weeks, a touch-up treatment could be performed, if deemed necessary by the investigator. The change in NLF severity was assessed using the Nasolabial Fold Severity Rating Scale (NFL-SRS) developed by Croma-Pharma and the Global Aesthetic Improvement Scale (GAIS). Results: Out of 60 analyzed subjects, 59 (98.3%) had improved their NLF severity by at least 1 grade on the NFL-SRS at week 4, 58 subjects (96.7%) at weeks 24 and 36. All subjects showed aesthetic improvement (GAIS), at weeks 4 and 24. The investigator judged the aesthetics as very much improved (score of 1) in 45 (75.0%) at week 4, 48 (80.0%) at week 24, and in 39 of 60 subjects, respectively (65.0%) at week 36. Thirty-six weeks post-initial treatment, 56 of 60 subjects (93.3%) were very satisfied or satisfied with the treatment. Adverse device effects (ADEs) were mild or moderate and resolved at latest 25 days post-onset. The most commonly reported ADEs were injection site hematoma and injection site pain. Conclusion: PFL was safe and effective in reducing the severity of NLFs. Most subjects were (very) satisfied with the treatment outcome throughout a 36 weeks investigation period. [ABSTRACT FROM AUTHOR]

The mouth can be affected by important inflammatory processes resulting from localized or systemic diseases such as diabetes, AIDS and leukemia, among others, and are manifested in various types of buccal sores typically presenting pain. This work focuses on the design, formulation, and characterization of four semisolid formulations for oral mucosa in order to symptomatically treat these painful processes. The formulations have two active pharmaceutical ingredients, triamcinolone acetonide (TA) and lidocaine hydrochloride (LIDO). The formula also contains, as an excipient, Orabase®, which is a protective, hydrophobic, and anhydrous adhesive vehicle, used to retain or facilitate the application of active pharmaceutical ingredients to the oral mucosa. After designing the formulations, an analytical method for TA was validated using HPLC so as to achieve reliable analytical results. Franz-type diffusion cells were used to perform drug release studies using synthetic membrane, and permeation studies using buccal mucosa, estimating the amount and rate of TA permeated across the tissue. Additionally, sublingual permeation studies were carried out to evaluate a scenario of a continuous contact of the tongue with the applied formulation. Permeation fluxes and the amount of TA retained within sublingual mucosa were similar to those in buccal mucosa, also implying anti-inflammatory activity in the part of the tongue that is in direct contact with the formulation. In addition, the dynamic conditions of the mouth were recreated in terms of the presence of phosphate buffered saline, constant movement of the tongue, pH, and temperature, using dissolution equipment. The amount of TA released into the phosphate buffered saline in dynamic conditions (subject to being ingested) is well below the normal oral doses of TA, for which the formulation can be considered safe. The formulations applied to buccal or sublingual mucosas under dynamic conditions permit the successful retention of TA within either tissue, where it exerts anti-inflammatory activity. The four formulations studied show a pseudoplastic and thixotropic behavior, ideal for topical application. These results evidence the potential of these topical formulations in the treatment of inflammatory processes in the buccal mucosa.