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Lidocaine is the most commonly used local anesthetic worldwide, known for its rapid onset and moderate duration of anesthesia. However, it is short-lived and does not effectively promote effective topical anesthesia in the oral cavity when used alone. Our aim was to investigate whether an approximate 50% encapsulation of lidocaine in poly(ε-caprolactone) nanocapsules (LDC-Nano) would be able to increase its permeation and analgesic efficacy and reduce cytotoxicity. In this study, we characterized LDC-Nano and conducted MTT tests with HaCaT cells to assess their in vitro cytotoxicity. Additionally, in vitro permeation assays across the pig esophageal epithelium and the anesthetic efficacy of the hind paw incision model in rats were performed. Plain lidocaine (LDC) was compared with LDC-Nano and lidocaine hydrochloride plus epinephrine (LDC-Epi). The physicochemical characteristics of LDC-Nano were satisfactory (pH: 8.1 ± 0.21; polydispersity index: 0.08 ± 0.01; mean diameter (nm): 557.8 ± 22.7; and encapsulation efficiency (%): 51.8 ± 1.87) and remained stable for up to 4 months. LDC-Nano presented similar in vitro cytotoxicity to LDC but was higher than LDC-Epi (LD50: LDC = 0.48%; LDC-Nano = 0.47%; and LDC-Epi = 0.58%; p < 0.0001). Encapsulation increased the permeability coefficient about 6.6 times and about 7.5 the steady-state flux of lidocaine across the mucosal epithelium. Both encapsulation and epinephrine improved anesthesia duration, with epinephrine demonstrating superior efficacy (100% of animals were anesthetized up to 100, 30, and 20 min when LDC-Epi, LDC-nano, and LDC were used, respectively). Although LDC-Epi demonstrated superior in vivo anesthetic efficacy, the in vitro permeation and cytotoxicity of LDC-Nano indicate promising avenues for future research, particularly in exploring its potential application as a topical anesthetic in the oral cavity.
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Abstract Background Postoperative cough may occur after tracheal intubation, but it is indistinct which drug is best at diminishing these events. Additionally, airway reflexes are commonly accompanied by severe hemodynamics responses during emergence. Objectives To evaluate the role of topical airway anesthesia on immediate post-extubation cough/bucking and extubation time. Methods Randomized clinical trials from MEDLINE, EMBASE, CENTRAL, and LILACS published until December 23, 2020 were included. Our primary outcome was postoperative cough/bucking incidence which was compared between local anesthetics and controls. Extubation times were likewise considered. Predisposition appraisal and subgroup, affectability investigations were likewise performed. Results The pooled analysis found a 45% reduction in cough incidence after treatment with topical airway local anesthetic (RR = 0.55; 95% CI: 0.42 to 0.72; p< 0.001). The number needed to treat (NNT) was 4.61. The intervention showed no differences in reduction of the extubation time (mean difference = -0.07; 95% CI: -0.14 to 0.28; p= 0.49). Conclusion Topical airway anesthesia demonstrated better than placebo or no medication in reducing immediate post-extubation cough/bucking. Further studies could have this objective to combine the different ways to perform better outcomes for patients.
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Humanos , Tosse/prevenção & controle , Intubação Intratraqueal , Período Pós-Operatório , Extubação , Anestesia Geral , Anestesia Local , Anestésicos LocaisRESUMO
BACKGROUND: Postoperative cough may occur after tracheal intubation, but it is indistinct which drug is best at diminishing these events. Additionally, airway reflexes are commonly accompanied by severe hemodynamics responses during emergence. OBJECTIVES: To evaluate the role of topical airway anesthesia on immediate post-extubation cough/bucking and extubation time. METHODS: Randomized clinical trials from MEDLINE, EMBASE, CENTRAL, and LILACS published until December 23, 2020 were included. Our primary outcome was postoperative cough/bucking incidence which was compared between local anesthetics and controls. Extubation times were likewise considered. Predisposition appraisal and subgroup, affectability investigations were likewise performed. RESULTS: The pooled analysis found a 45% reduction in cough incidence after treatment with topical airway local anesthetic (RR.á=.á0.55; 95% CI: 0.42 to 0.72; p.á<.á0.001). The number needed to treat (NNT) was 4.61. The intervention showed no differences in reduction of the extubation time (mean difference = -0.07; 95% CI: -0.14 to 0.28; p.á=.á0.49). CONCLUSION: Topical airway anesthesia demonstrated better than placebo or no medication in reducing immediate post-extubation cough/bucking. Further studies could have this objective to combine the different ways to perform better outcomes for patients.
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Tosse , Intubação Intratraqueal , Humanos , Tosse/prevenção & controle , Anestésicos Locais , Anestesia Local , Período Pós-Operatório , Extubação , Anestesia GeralRESUMO
Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTCNLC-HG4%) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity. Compared to control formulations, the use of TTCNLC-HG4% slowed in vitro permeation of the anesthetic across the nasal mucosa, maintained cytotoxicity against neuroblastoma cells, and provided a three-fold increase in analgesia duration, as observed using the tail-flick test in mice. The results obtained here open up perspectives for future clinical evaluation of the thermoreversible hybrid hydrogel, which contains TTC-loaded NLC, with the aim of creating an effective, topical, intranasal, needle-free anesthesia for use in dentistry.
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ARTICLE TITLE AND BIBLIOGRAPHIC INFORMATION: Intrapocket topical anesthetic versus injected anesthetic for pain control during scaling and root planing in adult patients: systematic review and meta-analysis. Wambier LM, de Geus JL, Boing TF, Chibinski ACR, Wambier DS, Rego RO, Loguercio AD, Reis A. J Am Dent Assoc 2017;148(11):814-24.e812. SOURCE OF FUNDING: Institutional, State University of Ponta Grossa, Ponta Grossa, Paraná, Brazil. TYPE OF STUDY/DESIGN: Systematic review with meta-analysis of data.
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Anestesia Dentária , Raspagem Dentária , Adulto , Brasil , Humanos , Bolsa Periodontal , Aplainamento RadicularRESUMO
The aim of this study was to evaluate the in vitro cytotoxicity and the in vivo analgesic effect and local toxicity of the local anesthetic butamben (BTB) encapsulated in conventional or elastic liposomes incorporated in gel formulations. The results showed that both gel formulations of liposomal BTB reduced the cytotoxicity (p < 0.001; one-way ANOVA/Tukey's test) and increased the topical analgesic effect (p < 0.05; one-way ANOVA/Tukey's test) of butamben, compared to plain BTB gel. The gel formulations presented good rheological properties, and stability assays detected no differences in physicochemical stability up to 30 d after preparation. Moreover, histological assessment revealed no morphological changes in rat skin after application of any of the gel formulations tested.
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Anestesia Local/efeitos adversos , Benzocaína/análogos & derivados , Modelos Animais de Doenças , Géis/toxicidade , Lipossomos/toxicidade , Células 3T3 , Administração Tópica , Animais , Benzocaína/administração & dosagem , Benzocaína/química , Benzocaína/toxicidade , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Géis/administração & dosagem , Géis/química , Injeções Intraperitoneais , Lipossomos/administração & dosagem , Lipossomos/química , Camundongos , Camundongos Endogâmicos BALB C , Ratos , Ratos WistarRESUMO
INTRODUCTION: Topical anesthesia is widely used in dentistry to reduce pain caused by needle insertion and injection of the anesthetic. However, successful anesthesia is not always achieved using the formulations that are currently commercially available. As a result, local anesthesia is still one of the procedures that is most feared by dental patients. Drug delivery systems (DDSs) provide ways of improving the efficacy of topical agents. Areas covered: An overview of the structure and permeability of oral mucosa is given, followed by a review of DDSs designed for dental topical anesthesia and their related clinical trials. Chemical approaches to enhance permeation and anesthesia efficacy, or to promote superficial anesthesia, include nanostructured carriers (liposomes, cyclodextrins, polymeric nanoparticle systems, solid lipid nanoparticles, and nanostructured lipid carriers) and different pharmaceutical dosage forms (patches, bio- and mucoadhesive systems, and hydrogels). Physical methods include pre-cooling, vibration, iontophoresis, and microneedle arrays. Expert opinion: The combination of different chemical and physical methods is an attractive option for effective topical anesthesia in oral mucosa. This comprehensive review should provide the readers with the most relevant options currently available to assist pain-free dental anesthesia. The findings should be considered for future clinical trials.
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Anestesia Local/métodos , Sistemas de Liberação de Medicamentos , Mucosa Bucal/metabolismo , Administração Tópica , Química Farmacêutica , Ciclodextrinas/química , Humanos , Hidrogéis , Iontoforese , Lipídeos/química , Lipossomos , Nanopartículas , Nanoestruturas , Polímeros/químicaRESUMO
Purpose: To evaluate and describe the precautions involved in the technique of intravitreal injection of antiangiogenic drugs adopted by the ophthalmologists who are members of the Brazilian Society of Retina and Vitreous (SBRV). Methods: A questionnaire containing 22 questions related to precautions taken before, during, and after intravitreal injection was sent electronically to 920 members of SBRV between November 15, 2013 and April 31, 2014. Results: 352 responses (38%) were obtained. There was a predominance of men (76%) from the southwest region of Brazil (51%). The professional experience varied between 6 and 15 years after medical specialization (50%). Most professionals (76%) performed an average of 1 to 10 intravitreal injections a week, and 88% of the procedures were performed in the operating room using povidone iodine (99%), sterile gloves, and blepharostat (94%). For inducing topical anesthesia, usage of anesthetic eye drops was the most used technique (65%). Ranibizumab (Lucentis®) was the most common drug (55%), and age-related macular degeneration (AMD) was the most treated disease (57%). Regarding the complications treated, 6% of the ophthalmologists had treated at least one case of retinal detachment, 20% had treated cases of endophthalmitis, 9% had treated cases of vitreous hemorrhage, and 12% had encountered cases of crystalline lens touch. Conclusion: Intravitreal injection is a procedure routinely performed by retina specialists and has a low incidence of complications. Performing the procedure in the operating room using an aseptic technique was preferred by most of the respondents. Ranibizumab was the most used drug, and AMD was the most treated disease. .
Objetivo: Avaliar e descrever os cuidados envolvidos durante o procedimento de injeção intravítrea de drogas antiangiogênicas realizado pelos oftalmologistas membros da Sociedade Brasileira de Retina e Vítreo (SBRV). Métodos: Foi enviado um questionário aos 920 membros da SBRV, por meio de correio eletrônico, entre o período de 15/11/2013 a 31/04/2014, contendo 22 questões, relacionado aos cuidados pré, intra e pós-operatório da injeção intravítrea. Resultados: Foram obtidas 352 respostas (38% dos sócios). Houve um predomínio do sexo masculino (76%), procedentes da região Sudeste (51%). O tempo de experiência profissional se concentrou entre 6 a 15 anos após o término da especialização (50%). A maioria dos participantes tem média semanal de 1 a 10 (76%), sendo 88% das vezes realizado dentro do centro cirúrgico, utilizando iodopovidona (99%), luvas e blefarostato estéreis (94%). A anestesia tópica com colírio anestésico foi a técnica mais utilizada (65%). Entre os participantes, ranibizumabe (Lucentis®) é a droga mais utilizada (55%) e a degeneração macular relacionada a idade (DMRI) é a doença mais tratada (57%). Das complicações citadas pelos oftalmologistas, 6% já vivenciaram pelo menos um caso de descolamento de retina, 20% endoftalmite, 9% hemorragia vítrea e 12% toque cristaliniano. Conclusão: A injeção intravítrea é um procedimento realizado rotineiramente por retinólogos, com baixo índice de complicações. A realização do procedimento no centro cirúrgico com técnica asséptica é preferida pelos pesquisados. A droga mais utilizada foi o ranibizumabe e a doença mais tratada foi a DMRI. .
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Feminino , Humanos , Masculino , Injeções Intravítreas/métodos , Oftalmologia , Sociedades Médicas , Anestesia Local/métodos , Inibidores da Angiogênese/administração & dosagem , Anticorpos Monoclonais Humanizados/administração & dosagem , Brasil , Endoftalmite/induzido quimicamente , Pesquisas sobre Atenção à Saúde , Injeções Intravítreas/efeitos adversos , Degeneração Macular/tratamento farmacológico , Soluções Oftálmicas/administração & dosagem , Povidona-Iodo , Doenças Retinianas/tratamento farmacológico , Centros Cirúrgicos , Inquéritos e QuestionáriosRESUMO
OBJECTIVE: To characterize liposomal-lidocaine formulations for topical use on oral mucosa and to compare their in vitro permeation and in vivo anesthetic efficacy with commercially available lidocaine formulations. MATERIALS AND METHODS: Large unilamellar liposomes (400 nm) containing lidocaine were prepared using phosphatidylcholine, cholesterol, and α-tocoferol (4:3:0.07, w:w:w) and were characterized in terms of membrane/water partition coefficient, encapsulation efficiency, size, polydispersity, zeta potential, and in vitro release. In vitro permeation across pig palatal mucosa and in vivo topical anesthetic efficacy on the palatal mucosa in healthy volunteers (double-blinded cross-over, placebo controlled study) were performed. The following formulations were tested: liposome-encapsulated 5% lidocaine (Liposome-Lido5); liposome-encapsulated 2.5% lidocaine (Liposome-Lido2.5); 5% lidocaine ointment (Xylocaina®), and eutectic mixture of lidocaine and prilocaine 2.5% (EMLA®). RESULTS: The Liposome-Lido5 and EMLA showed the best in vitro permeation parameters (flux and permeability coefficient) in comparison with Xylocaina and placebo groups, as well as the best in vivo topical anesthetic efficacy. CONCLUSION: We successfully developed and characterized a liposome encapsulated 5% lidocaine gel. It could be considered an option to other topical anesthetic agents for oral mucosa.
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Anestésicos Locais/química , Lidocaína/química , Mucosa Bucal/metabolismo , Administração Tópica , Adolescente , Adulto , Anestésicos Locais/metabolismo , Animais , Avaliação Pré-Clínica de Medicamentos , Feminino , Géis , Humanos , Cinética , Lidocaína/metabolismo , Lipossomos , Masculino , Permeabilidade , Sus scrofa , Adulto JovemRESUMO
INTRODUCTION: Intravitreal injection (IVT) is one of the most common vitreoretinal procedures, a large majority are performed with local anesthesia. The purpose of this study was to investigate the safety to the cornea and anesthetic efficacy of five concentrations of lidocaine gel. METHODS: A prospective clinical trial was conducted testing lidocaine gel in five preparations: 2, 3.5, 5, 8 and 12%. Patients with macular degeneration, diabetic edema or retina vein occlusion were scheduled for intravitreal treatment received topical anesthesia with lidocaine gel 5 and 10 min before the procedure. Patients answered the visual analog scale for pain during the procedure. Corneal and conjunctival was evaluated using the Oxford scale. RESULTS: In total, 260 patients were randomized into five groups. The mean pain scores (± standard deviation) were 2.63 (± 1.68) in the 2% group, 2.08 (± 1.35) in the 3.5%; 2.00 (± 1.65) in the 5%, 1.93 (± 1.40) in the 8% and 1.83 (± 1.35) in the 12% group. Mean pain score among all groups was similar (p = 0.077). There was no significant difference between groups in regard to keratitis mean score (p = 0.897). CONCLUSIONS: Lidocaine gel at concentrations from 2 to 12% induced similar anesthetic effect for IVTs, without adverse effects on cornea and conjunctiva.