Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-ß-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity.

The subclass naphthoquinone represents a substance group containing several compounds with important activities against various pathogenic microorganisms. Accordingly, we evaluated O-allyl-lawsone (OAL) antiparasitic and antifungal activity free and encapsulated in 2-hydroxypropyl-ß-cyclodextrin (OAL MKN) against Trypanosoma cruzi and Sporothrix spp. OAL and OAL MKN were synthesized and characterized by physicochemical methods. The IC50 values of OAL against T. cruzi were 2.4 µM and 96.8 µM, considering epimastigotes and trypomastigotes, respectively. At the same time, OAL MKN exhibited a lower IC50 value (0.5 µM) for both trypanosome forms and low toxicity for mammalian cells. Additionally, the encapsulation showed a selectivity index approximately 240 times higher than that of benznidazole. Regarding antifungal activity, OAL and OAL MKN inhibited Sporothrix brasiliensis growth at 16 µM, while Sporothrix schenckii was inhibited at 32 µM. OAL MKN also exhibited higher selectivity toward fungus than mammalian cells. In conclusion, we described the encapsulation of O-allyl-lawsone in 2-hydroxypropyl-ß-cyclodextrin, increasing the antiparasitic activity compared with the free form and reducing the cytotoxicity and increasing the selectivity towardSporothrix yeasts and the T. cruzi trypomastigote form. This study highlights the potential development of this inclusion complex as an antiparasitic and antifungal agent to treat neglected diseases.

A novel naphthoquinone derivative shows selective antifungal activity against Sporothrix yeasts and biofilms.

Sporotrichosis is a subcutaneous mycosis that affects humans and animals, with few therapeutic options available in the pharmaceutical market. We screened the in vitro antifungal activity of fourteen 1,4-naphthoquinones derivative compounds against Sporothrix brasiliensis and Sporothrix schenckii, the main etiological agents of sporotrichosis in Latin America. The most active compound was selected for further studies exploring its antibiofilm activity, effects on yeast morphophysiology, interaction with itraconazole, and selectivity to fungal cells. Among the fourteen 1,4-naphthoquinones tested, naphthoquinone 5, a silver salt of lawsone, was the most active compound. Naphthoquinone 5 was able to inhibit Sporothrix biofilms and induced ROS accumulation, mitochondrial disturbances, and severe plasmatic membrane damage in fungal cells. Furthermore, naphthoquinone 5 was ten times more selective towards fungal cells than fibroblast, and the combination of itraconazole with naphthoquinone 5 improved the inhibitory activity of the azole. Combined, the data presented here indicate that the silver salt naphthoquinone 5 exerts promising in vitro activity against the two main agents of sporotrichosis with important antibiofilm activity and a good toxicity profile, suggesting it is a promising molecule for the development of a new family of antifungals.

An Update on the Synthesis and Applications of Bis(Naphthoquinones): An Important Class of Molecules against Infectious Diseases and other Conditions.

Naphthoquinones are important molecules belonging to the general class of quinones, and many of these compounds have become drugs that are in the pharmaceutical market for the treatment of several diseases. A special subclass of compounds is that of the bis(naphthoquinones), which have two linked naphthoquinone units. In the last few years, several synthetic approaches toward such valuable compounds have been described, as well as their evaluation against numerous important biological targets. In this review, we provide a thorough discussion on the various synthetic methods reported for the synthesis of bis(naphthoquinone) analogues, also highlighting the biological activities of these substances.

In Vitro and In Vivo Antifungal Activity of Buparvaquone against Sporothrix brasiliensis.

Sporotrichosis has become an important zoonosis in Brazil, and Sporothrix brasiliensis is the primary species transmitted by cats. Improvement of animal treatment will help control and limit the spread and geographic expansion of sporotrichosis. Accordingly, buparvaquone, an antiprotozoal hydroxynaphthoquinone agent marketed as Butalex, was evaluated in vitro and in vivo against feline-borne isolates of S. brasiliensis. Buparvaquone inhibited in vitro fungal growth at concentrations 4-fold lower than itraconazole (the first-choice antifungal used for sporotrichosis) and was 408 times more selective for S. brasiliensis than mammalian cells. Yeasts treated with a subinhibitory concentration of buparvaquone exhibited mitochondrial dysfunction, reactive oxygen species and neutral lipid accumulation, and impaired plasma membranes. Scanning electron microscopy images also revealed buparvaquone altered cell wall integrity and induced cell disruption. In vivo experiments in a Galleria mellonella model revealed that buparvaquone (single dose of 5 mg/kg of body weight) is more effective than itraconazole against infections with S. brasiliensis yeasts. Combined, our results indicate that buparvaquone has a great in vitro and in vivo antifungal activity against S. brasiliensis, revealing the potential application of this drug as an alternative treatment for feline sporotrichosis.

Characterization and trypanocidal activity of a ß-lapachone-containing drug carrier.

The treatment of Chagas disease (CD), a neglected parasitic condition caused by Trypanosoma cruzi, is still based on only two drugs, nifurtimox (Nif) and benznidazole (Bz), both of which have limited efficacy in the late chronic phase and induce severe side effects. This scenario justifies the continuous search for alternative drugs, and in this context, the natural naphthoquinone ß-lapachone (ß-Lap) and its derivatives have demonstrated important trypanocidal activities. Unfortunately, the decrease in trypanocidal activity in the blood, high toxicity to mammalian cells and low water solubility of ß-Lap limit its systemic administration and, consequently, clinical applications. For this reason, carriers as drug delivery systems can strategically maximize the therapeutic effects of this drug, overcoming the above mentioned restrictions. Accordingly, the aim of this study is to investigate the in vitro anti-T. cruzi effects of ß-Lap encapsulated in2-hydroxypropyl-ß-cyclodextrin (2HP-ß-CD) and its potential toxicity to mammalian cells.

Formulation and Evaluation of a Novel Itraconazole-Clotrimazole Topical Emulgel for the Treatment of Sporotrichosis.

In recent years, the development of new pharmaceutical formulations for the treatment of sporotrichosis has become a relevant research field. In this work, we aimed to develop an emulgel containing itraconazole and clotrimazole to ensure therapeutic effectiveness against Sporothrix brasiliensis. The topical use of a formulation that combines both drugs represents an interesting option for the complementary treatment of sporotrichosis. The emulgel formulation was prepared and evaluated for its zeta potential, viscosity, in vitro antifungal activity and stability at different storage conditions. The results showed that the newly developed emulgel displayed promising physicochemical characteristics, as well as a good in vitro inhibitory activity against S. brasiliensis yeasts. The results obtained in this work suggest that the emulgel containing itraconazole and clotrimazole might highly be efficient and a complementary therapy to oral administration in the treatment of sporotrichosis.

Synthesis and biological evaluation of ß-lapachone and nor-ß-lapachone complexes with 2-hydroxypropyl-ß-cyclodextrin as trypanocidal agents.

We study ßLAP and its derivative nor-ß-Lapachone (NßL) complexes with 2-hydroxypropyl-ß-cyclodextrin to increase the solubility and bioavailability. The formation of true inclusion complexes between ßLAP or NßL in 2-HP-ß-CD in solid solution was characterization by FT-IR, DSC, powder X-ray was and was confirmed by one- and two-dimensional 1H NMR experiments. Additionally, the biological activities of ßLAP, NßL, ICßLAP, and ICNßL were investigated through trypanocidal assays with T. cruzi and cytotoxicity studies with mouse peritoneal macrophages. Originally, we tested these complexes against T. cruzi viability and observed higher biological activities and lower cytotoxicity when compared to ßLAP and NßL. Thus, the complexation of ßLAP and NßL with 2-HP-ß-CD increases the drug solubility, in addition vectorization was observed, increasing the biological activity against epimastigotes and trypomastigotes T. cruzi forms. Reduced the toxicity of the compounds against mammalian cells. In addition, the selectivity indices higher of the inclusion complexes comparing to substance free and those of benznidazole.

Investigation of a Microemulsion Containing Clotrimazole and Itraconazole for Transdermal Delivery for the Treatment of Sporotrichosis.

The aim of this study was to develop a microemulsion (ME) formulation containing an association of itraconazole (ITC) and clotrimazole (CLT) as a transdermal delivery system for the treatment of sporotrichosis. Pseudoternary phase diagrams were constructed to optimize the ME formulation. The ME formulation selected contained 1% (w/w) ITC and 1% (w/w) CLT and was composed of 23.07% Tween® 60 (surfactant), 23.07% propylene glycol (cosurfactant/cosolvent), 30.77% benzyl alcohol (oil), and 21.09% water. The ITC/CLT-loaded ME (ITC/CLT-ME) had a droplet size value of 217 ± 0.9 nm, with a polydispersity index of 0.5 ± 0.1. Permeation experiments on pig ear skin were conducted for ITC/CLT-ME, and the results indicated that the drug permeation performance was influenced by CLT, indicating that CLT acts as a promoter enhancer. In the in vitro antifungal activity assay using Sporothrix brasiliensis yeast, the inhibition halo produced by ITC/CLT-ME exhibited a mean diameter of 43.67 ± 2.31 mm. The ITC/CLT-ME formulation did not cause skin irritation in mice. The results suggest that ITC/CLT-ME is a promising tool for the transdermal treatment of sporotrichosis.

Development of a Method for the Quantification of Clotrimazole and Itraconazole and Study of Their Stability in a New Microemulsion for the Treatment of Sporotrichosis.

Sporotrichosis occurs worldwide and is caused by the fungus Sporothrix brasiliensis. This agent has a high zoonotic potential and is transmitted mainly by bites and scratches from infected felines. A new association between the drugs clotrimazole and itraconazole is shown to be effective against S. brasiliensis yeasts. This association was formulated as a microemulsion containing benzyl alcohol as oil, Tween® 60 and propylene glycol as surfactant and cosurfactant, respectively, and water. Initially, the compatibility between clotrimazole and itraconazole was studied using differential scanning calorimetry (DSC), thermogravimetric analysis (TG), Fourier transform infrared spectroscopy (FTIR), and X-ray powder diffraction (PXRD). Additionally, a simple and efficient analytical HPLC method was developed to simultaneously determine the concentration of clotrimazole and itraconazole in the novel microemulsion. The developed method proved to be efficient, robust, and reproducible for both components of the microemulsion. We also performed an accelerated stability study of this formulation, and the developed analytical method was applied to monitor the content of active ingredients. Interestingly, these investigations led to the detection of a known clotrimazole degradation product whose structure was confirmed using NMR and HRMS, as well as a possible interaction between itraconazole and benzyl alcohol.

Synthesis, Stability Studies, and Antifungal Evaluation of Substituted α- and ß-2,3-Dihydrofuranaphthoquinones against Sporothrix brasiliensis and Sporothrix schenckii.

Sporotrichosis is a neglected fungal infection caused by Sporothrix spp., which have a worldwide distribution. The standard antifungal itraconazole has been recommended as a first-line therapy. However, failure cases in human and feline treatment have been reported in recent years. This study aimed to synthesize several α- and ß-2,3-dihydrofuranaphthoquinones and evaluate them against Sporothrix schenckii and Sporothrix brasiliensis-the main etiological agents of sporotrichosis in Brazil. The stability of these compounds was also investigated under different storage conditions for 3 months. The samples were removed at 0, 60, and 90 days and assessed by ¹H-NMR, and their in vitro antifungal susceptibility was tested. Furthermore, we evaluated the superficial changes caused by the most effective and stable compounds using scanning electron microscopy and determined their effects when combined with itraconazole. Nine dihydrofuranaphthoquinones showed good antifungal activity and stability, with MIC values of 2⁻32 µM. Compounds 6 and 10 were the most active dihydrofuranaphthoquinones in vitro for both species; in fungi, these compounds induced yeast⁻hyphae conversion and alteration in the hyphae and conidia structures. Compound 10 also exhibited a synergistic activity with itraconazole against S. schenckii, with a ΣFIC index value of 0.3. Our results indicate that Compounds 6 and 10 are potential candidates for the development of new antifungal agents for the treatment of sporotrichosis.

α- and ß-Lapachone Isomerization in Acidic Media: Insights from Experimental and Implicit/Explicit Solvation Approaches.

Combined experimental and mixed implicit/explicit solvation approaches were employed to gain insights into the origin of switchable regioselectivity of acid-catalyzed lapachol cyclization and α-/ß-lapachone isomerization. It was found that solvating species under distinct experimental conditions stabilized α- and ß-lapachone differently, thus altering the identity of the thermodynamic product. The energy profile for lapachol cyclization revealed that this process can occur with low free-energy barriers (lower than 8.0 kcal mol-1 ). For α/ß isomerization in a dilute medium, the computed enthalpic barriers are 15.1 kcal mol-1 (α→ß) and 14.2 kcal mol-1 (ß→α). These barriers are lowered in concentrated medium to 11.5 and 12.6 kcal mol-1 , respectively. Experimental determination of isomers ratio was quantified by HPLC and NMR measurements. These findings provide insights into the chemical behavior of lapachol and lapachone derivatives in more complex environments.

The Antifungal Activity of Naphthoquinones: An Integrative Review.

Naphthoquinones are the most commonly occurring type of quinones in nature. They are a diverse family of secondary metabolites that occur naturally in plants, lichens and various microorganisms. This subgroup is constantly being expanded through the discovery of new natural products and by the synthesis of new compounds via innovative techniques. Interest in quinones and the search for new biological activities within the members of this class have intensified in recent years, as evidenced by the evaluation of the potential antimicrobial activities of quinones. Among fungi of medical interest, yeasts of the genus Candida are of extreme importance due to their high frequency of colonization and infection in humans. The objective of this review is to describe the development of naphthoquinones as antifungals for the treatment of Candida species and to note the most promising compounds. By using certain criteria for selection of publications, 68 reports involving both synthetic and natural naphthoquinones are discussed. The activities of a large number of substances were evaluated against Candida albicans as well as against 7 other species of the genus Candida. The results discussed in this review allowed the identification of 30 naphthoquinones with higher antifungal activities than those of the currently used drugs.

Acreditação no âmbito da assistência farmacêutica hospitalar: uma abordagem qualitativa de seus impactos / Accreditation in the field of hospital pharmacy services: a qualitative approach of its effects

Resumo Este estudo analisa o impacto do processo de acreditação na assistência farmacêutica hospitalar, visando identificar evidências de mudanças e melhorias do serviço prestado pela farmácia hospitalar. Grupos focais foram conduzidos com farmacêuticos e clientes internos do serviço de farmácia de cinco hospitais privados do Estado do Rio de Janeiro intencionalmente selecionados. Foram realizadas gravações, posteriormente transcritas, para análise do conteúdo dos diálogos e categorização temática. Segundo as narrativas revelaram, a acreditação resultou em investimentos de infraestrutura e recursos humanos, implantação de novos processos e discreta mudança de atuação do farmacêutico, alavancada pela farmácia clínica. Observou-se que tais modificações contribuíram para uma transformação contínua da assistência farmacêutica hospitalar, com modesta melhora da eficiência, qualidade e segurança do serviço prestado. Quando considerados os resultados finalísticos, a satisfação foi parcial, já que o ciclo da assistência farmacêutica ainda não se completa, fragilizando os processos recém-implantados em prol da qualidade do atendimento oferecido ao paciente. Apesar disso, o impacto no desempenho global da farmácia hospitalar foi considerado positivo, permitindo concluir que as diretrizes da acreditação apontaram o caminho para o desenvolvimento dos serviços avaliados, na medida em que exigiram o cumprimento de padrões necessários a uma assistência farmacêutica de qualidade.

Abstract This study analyzes the impact of the accreditation process on hospital pharmacy services, aiming to identify evidence of changes and improvements in the service provided by the hospital pharmacy. Focus groups were conducted with pharmacists and internal clients of the pharmacy service of five private hospitals in the state of Rio de Janeiro intentionally selected. Recordings were made, later transcribed, to analyze the content of the dialogues and thematic categorization. According to the narratives, the accreditation resulted in investments both in infrastructure and human resources, implementation of new processes and discreet change in the performance of the pharmacist, leveraged by the clinical pharmacy. It was observed that such modifications contributed to a continuous transformation of hospital pharmacy services, with a modest improvement in the efficiency, quality and safety of the service provided. When considering the final results, the satisfaction was partial, since the pharmaceutical assistance cycle is not yet complete, weakening the processes recently implemented in favor of the quality of care offered to the patient. Despite of this aspect, the impact on the overall performance of the hospital pharmacy was considered positive, allowing to conclude that the accreditation guidelines pointed the way for the development of the evaluated services, as they required the fulfillment of the standards necessary for qualifiedpharmacy services.

Magistral drugs in hospitalized newborns and children / Medicamentos magistrais em recém-nascidos e crianças hospitalizados

Abstract Objective: Study the use of magistral oral solutions and suspensions in infants and children at a university hospital. Methods: This is a descriptive study based on the analysis of the assessed hospital's magistral drug request forms regarding the patients in the neonatal ICU, Obstetrics, Pediatrics and Pediatric Emergency from January 2012 to December 2013. The frequency of drug requests and dispensation was evaluated and the consumption of each active ingredient of the preparations was expressed as number of “infant defined daily dose” (iDDD) and of iDDD/100 bed-days. Results: A total of 657 forms were analyzed - a monthly average of 27 pediatric preparations. The neonatal ICU accounted for 69.6% of these requests. Twenty-one drug items were used, of which the most common were folinic acid (88 requests), sulfadiazine (85) and captopril (73). The consumption of the active principle in these preparations varied in number of iDDD, from 7.5 (hydralazine) to 16,520.0 (folic acid), and in number of iDDD/100 bed-days in the neonatal ICU, from 0.1 (zinc sulfate) to 146.1 (folic acid). Conclusions: The constant consumption of magistral oral solutions and suspensions by newborns and children of the assessed hospital indicates the need for such preparations as a pediatric therapeutic alternative in this hospital.

Resumo Objetivo: Estudar o uso de soluções e suspensões orais magistrais em recém-nascidos e crianças de um hospital universitário. Métodos: Foi feito um estudo descritivo a partir da análise dos formulários de solicitação de manipulação do hospital estudado referentes aos pacientes da UTI-neonatal, obstetrícia, pediatria e emergência pediátrica de janeiro de 2012 a dezembro de 2013. As frequências das solicitações e dispensações desses medicamentos foram avaliadas e o consumo de cada princípio ativo das preparações foram expressos sob a forma de número de infant defined daily dose (iDDD) e de iDDD/100 leitos-dia. Resultados: Foram analisados 657 formulários - média mensal de 27 preparações pediátricas. A UTI-neonatal foi responsável por 69,6% dessas solicitações. Foram usados 21 itens de medicamentos, destacou-se o uso de ácido folínico (88 solicitações), sulfadiazina (85) e captopril (73). O consumo de princípio-ativo nessas preparações variou, em número de iDDD, de 7,5 (hidralazina) a 16.520 (ácido fólico) e em número de iDDD/100 leitos-dia da UTI-neonatal, de 0,1 (sulfato de zinco) a 146,1 (ácido fólico). Conclusões: O consumo constante das soluções e suspensões orais magistrais pelos recém-nascidos e crianças do hospital estudado indica a necessidade dessas preparações como opção terapêutica pediátrica nesse hospital.

Magistral drugs in hospitalized newborns and children. / Medicamentos magistrais em recém­nascidos e crianças hospitalizados.

OBJECTIVE: Study the use of magistral oral solutions and suspensions in infants and children at a university hospital. METHODS: This is a descriptive study based on the analysis of the assessed hospital's magistral drug request forms regarding the patients in the neonatal ICU, Obstetrics, Pediatrics and Pediatric Emergency from January 2012 to December 2013. The frequency of drug requests and dispensation was evaluated and the consumption of each active ingredient of the preparations was expressed as number of "infant defined daily dose" (iDDD) and of iDDD/100 bed-days. RESULTS: A total of 657 forms were analyzed - a monthly average of 27 pediatric preparations. The neonatal ICU accounted for 69.6% of these requests. Twenty-one drug items were used, of which the most common were folinic acid (88 requests), sulfadiazine (85) and captopril (73). The consumption of the active principle in these preparations varied in number of iDDD, from 7.5 (hydralazine) to 16,520.0 (folic acid), and in number of iDDD/100 bed-days in the neonatal ICU, from 0.1 (zinc sulfate) to 146.1 (folic acid). CONCLUSIONS: The constant consumption of magistral oral solutions and suspensions by newborns and children of the assessed hospital indicates the need for such preparations as a pediatric therapeutic alternative in this hospital.

Avaliação tecnológica em saúde: uso da carboximetilcelulose a 2% no tratamento das úlceras de perna / Health technology assessment: use of carboxymethylcellulose 2% in treating leg ulcers / Evaluación de tecnologías en salud: uso de la carboximetilcelulosa al 2% en tratamiento de las úlceras de pierna

Estudo de intervenção terapêutica do tipo ensaio clínico não controlado. Objetivou avaliar o custo e a efetividade da carboximetilcelulose 2% no tratamento das úlceras de perna. Foi aplicado instrumento de avaliação clínica em 20 pacientes de hospital universitário (Niterói-Rio de Janeiro), entre janeiro e outubro de 2010. Após 90 dias de tratamento, os resultados evidenciaram que no grupo A, feridas maiores que 100cm², houve redução de 15% da área lesional. No grupo B, feridas menores que 100cm², houve cicatrização total em 33,3% dos casos. Os custos foram proporcionais à área lesional; quanto maior a área, maior o custo do tratamento. Ao comparar o produto com outros géis do mercado nacional, identificou-se significativa redução do preço da carboximetilcelulose 2% (p<0,01) produzida na universidade. Conclui-se que a carboximetilcelulose 2% foi efetiva na redução do tamanho das úlceras, no aumento do tecido de granulação e na diminuição dos custos do tratamento.

This therapeutic intervention study took the form of an uncontrolled clinical trial. It aimed to evaluate the cost and effectiveness of carboxymethylcellulose 2% in treating leg ulcers. A clinical evaluation instrument was applied to twenty volunteers at a university hospital in Niteroi, Rio de Janeiro State, between January and October 2010. After ninety days of treatment, the results of group A (lesions larger than 15.5 sq.in.) showed 15% reduction in lesion area. In group B (wounds smaller than 15.5 sq.in.), healing was total in 33.3% of cases. The costs were proportional to ulcer area: larger areas entailed higher costs. When this product was compared with other gels on the Brazilian market, the carboxymethylcellulose 2% produced at the university was observed to yield significant cost reductions (p<0.01). In conclusion, carboxymethylcellulose 2% was effective in reducing leg ulcers, increasing tissue granulation area and lowering treatment costs.

Estudio de intervención terapéutica del tipo ensayo clínico no controlado. Objetivo: evaluar el costo y la eficacia de la carboximetilcelulosa 2% en el tratamiento de úlceras de piernas. Se utilizó un instrumento de evaluación clínica junto a 20 pacientes de un hospital universitario (Niterói, Río de Janeiro), entre enero y octubre de 2010. Después de 90 días de tratamiento, los resultados mostraron que, en el grupo A, de los que tenían heridas más grandes que 100 cm², hubo una reducción de un 15% de la zona lesionada. En el grupo B, de personas cuyas heridas eran menores que 100 cm², la cicatrización completa se observó en el 33,3% de los casos. Los costos fueron proporcionales a la zona lesionada, cuanto más extensa el área lesionada, más alto el costo del tratamiento. Cuando se comparan el producto con otros geles del mercado nacional, se reveló una reducción significativa del precio de la carboximetilcelulosa 2% (p<0,01) producida en la universidad. En conclusión, la carboximetilcelulosa 2% fue eficaz en la reducción del tamaño de las úlceras, en el aumento del tejido de granulación y en la reducción de los costos de tratamiento.

Effectiveness of papain gel in venous ulcer treatment: randomized clinical trial.

OBJECTIVE: to assess the effectiveness of 2% papain gel compared to 2% carboxymethyl cellulose in the treatment of chronic venous ulcer patients. METHOD: randomized controlled clinical trial with 12-week follow-up. The sample consisted of 18 volunteers and 28 venous ulcers. In the trial group, 2% papain gel was used and, in the control group, 2% carboxymethyl cellulose gel. RESULTS: the trial group showed a significant reduction in the lesion area, especially between the fifth and twelfth week of treatment, with two healed ulcers and a considerable increase in the amount of epithelial tissue in the wound bed. CONCLUSION: 2% papain gel demonstrated greater effectiveness in the reduction of the lesion area, but was similar to 2% carboxymethyl cellulose gel regarding the reduction in the amount of exudate and devitalized tissue. Multicenter research is suggested to evidence the effectiveness of 2% papain gel in the healing of venous ulcers. UTN number: U1111-1157-2998.

[Effectiveness Of 2% And 4% Papain Gels In The Healing Of Venous Ulcers]. / Efetividade dos géis de papaína a 2% e 4% na cicatrização de úlceras venosas.

OBJECTIVE: To analyze the effectiveness of 2% and 4% papain gels in tissue repair of venous ulcers. METHOD: Quasi-experimental study with consecutive sample of 16 patients with 30 venous ulcers treated at the outpatient clinic of a teaching hospital, from April to November in 2011, using a form for clinical assessment of the patient and its lesion. Variables were analyzed by Wilcoxon and McNemar test (p < 0.05). RESULTS: Most participants were female; aged between 51 and 59 years; obese; with hypertension. Regarding ulcers, there was an average decrease of 7.9 cm2 (50% of its original size) in 90 days; 20% of the ulcers completely healed within 56.67 days. There was an increase in epithelialization, significant reduction in the slough and edema, improved depth, in the type and amount of exudate (p < 0.0001). CONCLUSION: 2% and 4% papain gels were effective in healing venous ulcers.

Effectiveness of papain gel in venous ulcer treatment: randomized clinical trial / Efetividade do gel de papaína no tratamento de úlceras venosas: ensaio clínico randomizado / Efectividad del gel de papaína en el tratamiento de úlceras venosas: ensayo clínico aleatorio

to assess the effectiveness of 2% papain gel compared to 2% carboxymethyl cellulose in the treatment of chronic venous ulcer patients.

avaliar a efetividade do gel de papaína a 2% comparado ao gel de carboximetilcelulose a 2% no tratamento de pacientes com úlceras venosas crônicas.

evaluar la efectividad del gel de papaína a 2% comparado con el gel de carboximetilcelulosa a 2% en el tratamiento de pacientes con úlceras venosas crónicas.