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1.
Adv Drug Deliv Rev ; 171: 164-186, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33539853

RESUMO

The COVID-19 pandemic is a serious threat to global health and the global economy. The ongoing race to develop a safe and efficacious vaccine to prevent infection by SARS-CoV-2, the causative agent for COVID-19, highlights the importance of vaccination to combat infectious pathogens. The highly accessible cutaneous microenvironment is an ideal target for vaccination since the skin harbors a high density of antigen-presenting cells and immune accessory cells with broad innate immune functions. Microarray patches (MAPs) are an attractive intracutaneous biocargo delivery system that enables safe, reproducible, and controlled administration of vaccine components (antigens, with or without adjuvants) to defined skin microenvironments. This review describes the structure of the SARS-CoV-2 virus and relevant antigenic targets for vaccination, summarizes key concepts of skin immunobiology in the context of prophylactic immunization, and presents an overview of MAP-mediated cutaneous vaccine delivery. Concluding remarks on MAP-based skin immunization are provided to contribute to the rational development of safe and effective MAP-delivered vaccines against emerging infectious diseases, including COVID-19.


Assuntos
Vacinas contra COVID-19/imunologia , COVID-19/imunologia , Desenvolvimento de Medicamentos/tendências , SARS-CoV-2/imunologia , Pele/imunologia , Adesivo Transdérmico/tendências , Administração Cutânea , COVID-19/metabolismo , COVID-19/prevenção & controle , Vacinas contra COVID-19/administração & dosagem , Vacinas contra COVID-19/metabolismo , Desenvolvimento de Medicamentos/métodos , Humanos , Imunidade Inata/efeitos dos fármacos , Imunidade Inata/fisiologia , SARS-CoV-2/efeitos dos fármacos , SARS-CoV-2/metabolismo , Pele/efeitos dos fármacos , Pele/metabolismo
2.
Epilepsy Behav ; 111: 107162, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32575009

RESUMO

OBJECTIVE: The objective of the study was to describe the effect of the vaginal ring and transdermal patch on lamotrigine serum levels in women with epilepsy. BACKGROUND: Previous studies demonstrate that oral hormonal contraceptives containing synthetic estrogen increase lamotrigine clearance through induction of glucuronidation. This leads to variable lamotrigine serum concentrations throughout monthly cycles in women who are on combined oral contraceptives (COCs). The effects of estrogen-containing nonoral hormonal contraceptive methods, including the vaginal ring and transdermal patch, on lamotrigine pharmacokinetics are not well described. METHODS: Retrospective chart review was performed to identify serum lamotrigine levels drawn from women with epilepsy while on the active phase of vaginal ring or transdermal patch and while off contraception. Wilcoxon signed-rank tests for paired data were used to compare the difference in dose-corrected lamotrigine concentration in plasma between values while on hormonal contraception to those while off contraception in patients using a vaginal ring. RESULTS: Six patients were using the vaginal ring, and one patient was using the transdermal patch. Lamotrigine dose-corrected concentrations were decreased during the active phase of the vaginal ring compared with concentrations during the period off contraception (p = .04). There was one patient without a decrease in concentration, but the other five patients on the vaginal ring had a decrease in dose-corrected lamotrigine concentration ranging from 36 to 70% while on the vaginal ring. Similarly, one patient using the transdermal patch had a decrease of 37% in dose-corrected lamotrigine concentration while on the patch. CONCLUSIONS: The findings support that the vaginal ring contraceptive method decreases lamotrigine concentrations during the active phase of treatment. This has important implications for contraceptive counseling and maintaining therapeutic levels in women of childbearing age with epilepsy.


Assuntos
Anticonvulsivantes/sangue , Anticoncepcionais Femininos/sangue , Dispositivos Anticoncepcionais Femininos/tendências , Epilepsia/sangue , Lamotrigina/sangue , Adesivo Transdérmico/tendências , Adulto , Anticonvulsivantes/uso terapêutico , Anticoncepcionais Femininos/uso terapêutico , Interações Medicamentosas/fisiologia , Epilepsia/tratamento farmacológico , Feminino , Humanos , Lamotrigina/uso terapêutico , Pessoa de Meia-Idade , Estudos Retrospectivos , Adulto Jovem
3.
J Patient Saf ; 14(4): e97-e101, 2018 12.
Artigo em Inglês | MEDLINE | ID: mdl-30451718

RESUMO

BACKGROUND: Although problems during transdermal patch administration are primarily caused by insufficient knowledge, patient education programs are lacking. We compared patient education by a clinical pharmacist on knowledge on correct patch administration with routine counseling during patient-physician consultation in a pilot study. METHODS: After baseline assessment of knowledge and difficulties with patch administration, patients in the outpatient pain clinic of Heidelberg University Hospital were allocated to intervention (n = 12) or control group (n = 11). In both groups, identical information leaflets on transdermal patch use were dispensed. Intervention patients additionally received verbal counseling on correct patch administration by a clinical pharmacist. After 4 weeks, patients were called for a follow-up assessment on knowledge and perspective on administration difficulties. RESULTS: Patients reported several difficulties with transdermal patch administration, such as local skin reaction, difficulties with opening the packaging, and poor adhesion. Although patient education increased the ratio of correct answers in the intervention group twice as much than in the control group, overall knowledge was comparable between groups after education (P = 0.602). CONCLUSIONS: Patients encountered numerous problems with transdermal patch administration although on long-term use. Patient education can improve knowledge on correct patch administration. However, the pilot study demonstrated the need for further efforts to improve ease of use of transdermal patch, such as patch adhesion.


Assuntos
Analgésicos Opioides/uso terapêutico , Educação de Pacientes como Assunto/métodos , Adesivo Transdérmico/tendências , Administração Cutânea , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Projetos Piloto
7.
Int J Pharm ; 496(2): 240-9, 2015 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-26611668

RESUMO

Thromboembolic complications are the most common preventable cause of mortality and morbidity in trauma patients. Thrombosis is also the common cause of ischemic heart disease (acute coronary syndrome), stroke, and venous thromboembolism. Heparin, as a potent anticoagulant, has been used in clinical practice for more than five decades and remains the major medicine for the prevention and treatment of venous thromboembolism. However it binds to the endothelium and has a high affinity for plasma proteins resulting in a short half-life and unpredictable bioavailability. Transdermal drug delivery can address the problems of short half-life and unpredictable bioavailability. Other advantages of transdermal drug delivery include convenience, improved patient compliance, prompt termination of dosing and avoidance of the first-pass effect. This review focuses on different approaches used for transdermal delivery of heparin.


Assuntos
Anticoagulantes/metabolismo , Sistemas de Liberação de Medicamentos/tendências , Heparina/metabolismo , Pele/metabolismo , Adesivo Transdérmico/tendências , Administração Cutânea , Animais , Anticoagulantes/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Heparina/administração & dosagem , Humanos , Pele/efeitos dos fármacos , Trombose/tratamento farmacológico , Trombose/metabolismo
8.
J Pharm Sci ; 104(2): 740-9, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25448542

RESUMO

The goal of this study is to develop thermostable microneedle patch formulations for influenza vaccine that can be partially or completely removed from the cold chain. During vaccine drying associated with microneedle patch manufacturing, ammonium acetate and 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) buffer salts stabilized influenza vaccine, surfactants had little effect during drying, drying temperature had weak effects on vaccine stability, and drying on polydimethylsiloxane (PDMS) led to increased stability compared with drying on stainless steel. A number of excipients, mostly polysaccharides and some amino acids, further stabilized the influenza vaccine during drying. Over longer time scales of storage, combinations of stabilizers preserved the most vaccine activity. Finally, dissolving microneedle patches formulated with arginine and calcium heptagluconate had no significant activity loss for all three strains of seasonal influenza vaccine during storage at room temperature for 6 months. We conclude that appropriately formulated microneedle patches can exhibit remarkable thermostability that could enable storage and distribution of influenza vaccine outside the cold chain.


Assuntos
Vacinas contra Influenza/química , Agulhas , Adesivo Transdérmico , Vacinação , Química Farmacêutica , Estabilidade de Medicamentos , Humanos , Adesivo Transdérmico/tendências , Vacinação/tendências
9.
Recent Pat Drug Deliv Formul ; 9(1): 88-94, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-24981287

RESUMO

The present critical review is related to the self-modified patch based drug delivery system for controlled (trans) dermal drug delivery. The composition itself is modified into the patch and adheres when comes in contact with the skin and acts as a rate-controlling matrix layer (patch). The self adhesiveness property of the formulation itself is enough to hold the patch in place on the skin for the - duration of treatment while allowing the patch to be promptly backed by without any skin irritation and formulation residue. This patent review is useful for the knowledge of self modified patch associated drug delivery for controlled topical or transdermal delivery of pharmaceutical and cosmetic agents.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Patentes como Assunto , Absorção Cutânea , Adesivo Transdérmico , Administração Cutânea , Animais , Química Farmacêutica/métodos , Química Farmacêutica/tendências , Sistemas de Liberação de Medicamentos/tendências , Humanos , Absorção Cutânea/efeitos dos fármacos , Absorção Cutânea/fisiologia , Adesivo Transdérmico/tendências
10.
Rev. Soc. Esp. Dolor ; 20(6): 308-323, nov.-dic. 2013.
Artigo em Espanhol | IBECS | ID: ibc-118531

RESUMO

Objetivo: Proponer a partir del consenso de un panel de expertos de ambito estatal que integre la experiencia clinica y la evidencia disponible mas actual, recomendaciones sobre el uso clinico de los tratamientos por via topica para el manejo del dolor neuropatico periferico (DNP). Métodos: Se proponen, a partir de una revision bibliografica sobre las distintas opciones terapeuticas topicas en DNP, una serie de criterios profesionales y recomendaciones clinicas para la mejora del uso de dichos agentes topicos. Se empleo el metodo Delphi modificado en dos rondas para contrastar las opiniones de un panel nacional de 52 reconocidos expertos, seleccionados mediante una estrategia en “bola de nieve” de entre el colectivo de anestesiologos de unidades del dolor (94 %) y otros especialistas (neurologos y traumatologos). Se evaluaron 61 recomendaciones clinicas agrupadas en 6 areas tematicas: a) DNP: tratamiento topico versus sistemico (11 items); b) dolor neuropatico postquirurgico, postraumatico y munones dolorosos (12 items); c) neuralgia posherpetica, intercostal y del trigemino (9 items); d) DNP por atrapamiento (8 items); e) sindrome de dolor regional complejo (11 items); y f) neuropatia diabetica (ND) y otras polineuropatias (por VIH, alcohol, toxicidad, etc.) (10 items). Se empleo una escala ordinal de tipo Likert de 9 puntos (desacuerdo/ acuerdo) para evaluar cada recomendacion. Tras la primera ronda de encuesta, se facilito al panel informacion del resultado (resultados estadisticos y opiniones libres de los panelistas) y se solicito la reconsideracion del voto sobre los items no consensuados. Resultados: Tras la primera ronda del panel se logró consenso en 37 de las 61 cuestiones planteadas. Al final de la segunda ronda el acuerdo ascendió hasta 46 ítems (75 %). En general, se aprecia consenso entre los expertos sobre la conveniencia de introducir los tratamientos tópicos en primera línea de tratamiento del DNP y sobre su mejor aceptación por los pacientes frente a los sistémicos. Asimismo, fue criterio compartido que la combinación de estos fármacos tópicos con los tratamientos sistémicos es una opción a considerar en el manejo de varios tipos de DNP. También se alcanzó un alto grado de acuerdo en aceptar, desde un punto de vista fisiopatológico, la indicación del tratamiento con parche de capsaicina al 8 % para varios tipos de DNP. Conclusión: Los expertos en el manejo clínico del DNP muestran un elevado nivel de acuerdo profesional con diversas recomendaciones terapéuticas analizadas en el estudio. La difusión de tales recomendaciones puede ayudar a la mejora del manejo rutinario de fármacos tópicos para el dolor neuropático en nuestro sistema sanitario (AU)


Objective: To propose consensus from a panel of state level that integrates clinical experience and the most current evidence, recommendations on the clinical use of topical treatments for the management of peripheral neuropathic pain (PNP). Methods: We propose, based on a literature review on topical therapeutic options in PNP, a series of professional standards and clinical recommendations for improving the use of these topical agents. We used the modified Delphi method in two rounds to contrast the views of a national panel of 52 renowned experts, selected by a “snowball” strategy among the group of anesthesiologists pain units (94 %) and other specialists (neurologist and trauma). We evaluated 61 clinical recommendations grouped into 6 areas: a) PNP systemic versus topical treatment (11 items); b) postsurgical neuropathic pain, post-traumatic and painful stumps (12 items); c) post-herpetic neuralgia, intercostal and trigeminal (9 items); d) PNP entrapment (8 items); e) CRPS (11 items); and f) diabetic neuropathy (DN) and other polyneuropathy (HIV, alcohol, toxicity, etc.) (10 items). We used a Likert- type ordinal scale of 9 points (disagree/agree) to evaluate each recommendation. After the first round of the survey, information was provided requested to reconsider the vote on itemsnot agree. Results: After the first round the panel consensus was achieved in 37 of the 61 issues raised. At the end of the second round of the agreement amounted to 46 (75 %). In general, there was consensus among experts on whether to introduce topical treatment in first line treatment of PNP and its greater acceptance by patients compared with systemic. He was also a shared view consider in the management of various types of PNP. Also reached a high level of agreement to accept, from a physiological point of view, the indication for treatment with capsaicin patch 8 % for various types of PNP. Conclusions: Experts in the clinical management of PNP show a high level of professional agreement with various therapeutic recommendations for study. The dissemination of such recommendations can help improving the routine management of topical drugs for neuropathic pain in our health system (AU)


Assuntos
Humanos , Masculino , Feminino , Doenças do Sistema Nervoso Periférico/tratamento farmacológico , Administração Tópica , Polineuropatias/complicações , Polineuropatias/tratamento farmacológico , Capsaicina/uso terapêutico , Adesivo Transdérmico , Doenças do Sistema Nervoso Periférico/complicações , Doenças do Sistema Nervoso Periférico/fisiopatologia , Clínicas de Dor/organização & administração , Clínicas de Dor/normas , Clínicas de Dor , Capsaicina/metabolismo , Capsaicina/farmacocinética , Adesivo Transdérmico/tendências
11.
Neurol Clin ; 31(3 Suppl): S37-50, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-23931953

RESUMO

The rotigotine transdermal system is a dopamine receptor agonist delivered over a 24-hour period. It is approved for the treatment of idiopathic Parkinson's disease (PD). This article reviews the development of the rotigotine transdermal system, including rotigotine's receptor profile, steady-state pharmacokinetics, and metabolism. Preclinical studies of rotigotine in animal models of PD and proof-of-concept studies in patients with PD are reviewed. These preclinical and clinical studies established this system as an effective method for providing continuous rotigotine delivery across the skin providing the basis for continued clinical development of rotigotine for the treatment of early and advanced PD.


Assuntos
Agonistas de Dopamina/administração & dosagem , Doença de Parkinson/tratamento farmacológico , Tetra-Hidronaftalenos/administração & dosagem , Tiofenos/administração & dosagem , Adesivo Transdérmico/tendências , Animais , Agonistas de Dopamina/metabolismo , Avaliação Pré-Clínica de Medicamentos/métodos , Humanos , Doença de Parkinson/sangue , Tetra-Hidronaftalenos/metabolismo , Tiofenos/metabolismo
13.
Life Sci ; 89(13-14): 430-8, 2011 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-21777594

RESUMO

AIM: The purpose of this study was to develop transdermal films (TFs) with the addition of different polymer ratios that incorporated 0.5% tenoxicam in order to ensure maximum controlled and sustained drug release capacity. Tenoxicam is a non-steroidal anti-inflammatory drug (NSAID) widely used in the treatment of rheumatic diseases and characterized by its efficacy and reduced side effects in comparison to other NSAIDs. MAIN METHODS: Transdermal films of tenoxicam were designed with the Eudragit L30D-55copolymer with permeation enhancers like polyethylene glycol (PEG) and propylene glycol (PG) incorporated at different concentrations using the casting evaporation technique. Evaluations of these formulae were performed through mechanical characterizations and Fourier Transform Infrared Spectroscopy [FTIR]. In-vitro release studies were performed during 24h using diffusion cells. The film formulations with optimum in vitro-release rate have been taken up for testing of the anti-inflammatory effects and the sustaining action of tenoxicam. The in-vivo studies performed included carrageenan-induced hind paw edema and skin biopsies in Wistar rats. KEY FINDINGS: Formulation (F7) had the best effective combination [glycerol (0.25g), PEG200 (0.5g), PEG400 (1g) and PG (10%) and 0.5% dispersed drug] among all of the tenoxicam TF formulations studied. Also, this formula had the highest release value than formula 1 (F1) that contains [glycerol (2.5g), PEG200 (0.5g), PEG400 (0.5g) and 0.5% dissolved drug] or a commercially available gel after 24h. FTIR revealed that there was an interaction between the polymer and the drug. The drug-polymer interaction occurring between tenoxicam and Eudragit L30D-55 seems to cause a drag effect, leading to a delay of the tenoxicam release from the Eudragit L film. SIGNIFICANCE: When the films were applied half an hour before the subplantar injection of carrageenan in the hind paw of Wistar rats, it was observed that formula F7 provided maximum inhibition of paw edema in rats over 24h in contrast to both formula F1 and the marketed piroxicam gel as a reference. This was also confirmed histopathologically from skin biopsies. Thus, we show that tenoxicam can be formulated into transdermal films to sustain its release characteristics, and the polymeric composition of PEG200/PEG400 at a ratio of 1:2 and 10% PG was found to be the best choice to manufacture tenoxicam TF.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Edema/tratamento farmacológico , Piroxicam/análogos & derivados , Pele/efeitos dos fármacos , Adesivo Transdérmico , Animais , Anti-Inflamatórios não Esteroides/uso terapêutico , Edema/induzido quimicamente , Edema/patologia , Extremidade Inferior/patologia , Masculino , Metacrilatos/química , Piroxicam/administração & dosagem , Piroxicam/uso terapêutico , Polietilenoglicóis/química , Polímeros/química , Propilenoglicol/química , Ratos , Ratos Wistar , Pele/patologia , Adesivo Transdérmico/tendências
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