Tacrolimus action pathways in an ointment base for hypertrophic scar prevention in a rabbit ear model

Abstract Background: Tacrolimus is used to prevent unaesthetic scars due to its action on fibroblast activity and collagen production modulation. Objectives: To evaluate the action pathways, from the histopathological point of view and in cytokine control, of tacrolimus ointment in the prevention of hypertrophic scars. Methods: Twenty-two rabbits were submitted to the excision of two 1-cm fragments in each ear, including the perichondrium. The right ear received 0.1% and 0.03% tacrolimus in ointment base twice a day in the upper wound and in the lower wound respectively. The left ear, used as the control, was treated with petrolatum. After 30 days, collagen fibers were evaluated using special staining, and immunohistochemistry analyses for smooth muscle actin, TGF-β and VEGF were performed. Results: The wounds treated with 0.1% tacrolimus showed weak labeling and a lower percentage of labeling for smooth muscle actin, a higher proportion of mucin absence, weak staining, fine and organized fibers for Gomori's Trichrome, strong staining and organized fibers for Verhoeff when compared to controls. The wounds treated with 0.03% tacrolimus showed weak labeling for smooth muscle actin, a higher proportion of mucin absence, strong staining for Verhoeff when compared to the controls. There was absence of TGF-β and low VEGF expression. Study limitations: The analysis was performed by a single pathologist. Second-harmonic imaging microscopy was performed in 2 sample areas of the scar. Conclusions: Both drug concentrations were effective in suppressing TGF-β and smooth muscle actin, reducing mucin, improving the quality of collagen fibers, and the density of elastic fibers, but only the higher concentration influenced elastic fiber organization.

Uso de Fluorescência de Raios X (XRF) para fins de comparação entre a composição elementar da barba de timão Stryphnodendron adstringens (Mart) Coville com outras pomadas cicatrizantes / Use of X-ray Fluorescence (XRF) for purposes of comparison between the elemental composition of barba de timão Stryphnodendron adstringens (Mart) Coville and other healing ointments

Introdução: A Barba de timão é uma planta de origem do cerrado brasileiro, que vem sendo estudada por suas propriedades medicinais, tais como: antibacteriana, cicatrizante, coagulante sanguíneo, dentre outras. A cicatrização é um processo pelo qual o organismo tende a reparar uma lesão ou perda de tecido. Objetivo: Este trabalho compara a composição química da barba de timão com algumas pomadas cicatrizantes de origem farmacêuticas já presentes e disponíveis no mercado. Assim, pode-se relacionar a propriedade cicatrizante desta planta por meio de seus componentes químicos. Materiais e Métodos: Para realizar tal comparação, foi utilizada com amostra a planta barba de timão comercializada em mercados especializados e as pomadas, sulfato de neomicina e a sulfadiazina de prata. Para a análise multielementar, foi utilizada a espectroscopia por fluorescência de raios X (XRF). Com o espectro fornecido pela XRF foi possível comparar os elementos químicos das amostras. Conclusão: O espectro mostrou que a barba de timão tem propriedades químicas semelhantes, assemelhando-se com os componentes químicos encontrados na amostra de sulfato de neomicina, adicionada de três compostos químicos, K, Ca e Br, que também são importantes no processo de cicatrização. Ao comparar com a sulfadiazina de prata, o único elemento que se difere do fitoterápico, além do três já citados, é a Ag. (AU)

Introduction: Barba de timão is a plant of the Brazilian Cerrado origin, which is already studied for its medicinal properties, such as: antibacterial, healing, blood coagulant, etc. Healing is a process by which the body tends to repair an injury or loss of tissue. Objective: This work compares the chemical composition of barba timão with some pharmaceutical healing scouring ointments already present and used in the market. Thus, we can relate the healing properties of this plant. Material and Methods: In order to make such a comparison, it was used the barba timão plant marketed in specialized markets, and the ointments neomycin sulfate and silver sulfadiazine. For multielement analysis, X-ray fluorescence spectroscopy (XRF) was used. With the spectrum provided by the XRF it was possible to compare the chemical elements of the samples. Conclusion: The spectrum shows that the barba timão has similar chemical properties, it resembles the chemical components found in the sample of neomycin sulfate, but with three more chemical compounds that is K, Ca and Br, that are also important in the healing process. When comparing with silver sulfadiazine, the only element that differs beyond the K and Ca of the phytotherapic, is the Ag of the ointment sample. (AU)

Study of Fluconazole Release from O/W Cream and Water Soluble Ointment Bases.

Aims: Study the release of fluconazole from different O/W creams and PEG ointments. Study Design: In this study, different formulations were prepared with changing one of the added excipients and study the effect of this change on the drug release and then the selected formulations were subjected to antifungal activity study. Place and Duration of Study: Faculty of Pharmacy, Department of Pharmaceutics, Assiut University, Assiut, Egypt, between December 2011 and March 2012. Methodology: O/W creams were prepared with changing either fatty alcohol type or the concentration of the added emulsifying agent. Also, the PEG ointments were prepared with changing the type of the liquid PEG (low molecular weight). Then, the viscosity and the fluconazole release from the prepared formulations were studied. Results: Changing the fatty alcohol type from stearyl to cetostearyl and cetyl alcohol in the O/W creams caused an increase in the viscosity and a decrease in the drug release. Also, changing the liquid PEG from PEG 400 to PEG 600 resulted in an increase in the formulation viscosity and subsequent decrease in the drug release. Both F1 and F6 showed a good inhibition to the fungal growth against Candida albicans and Trichophyton mentagrophyte using cup plate method, also PEG base showed a slight fungal growth inhibition. Conclusion: Results obtained showed that the PEG ointment formulations exhibited higher fluconazole release after three hours over the O/W cream formulations. Also, the nature of the PEG base may be adjunctive to the efficacy of the antifungal agent.

Estudo químico de duas plantas medicinais da amazônia: Philodendron scabrum k. Krause (araceae) e Vatairea guianensis aubl. (fabaceae) / Chemical study of two Amazonian medicinal plants: Philodendron scabrum K. Krause (Araceae) and Vatairea guianensis Aubl. (Fabaceae)

Este trabalho relata o estudo químico de duas plantas medicinais da Amazônia: Philodendron scabrum K. krause (Araceae) e Vatairea guianensis Aubl. (Fabaceae). As composições dos óleos essenciais dos cipós de P. scabrum e dos frutos de V. guianensis, respectivamente, foram analisadas em CG-DIC e CG-EM. Os constituintes majoritários dos cipós de P. scabrum foram óxido de cariofileno (19,42%), α-copaeno (16,08%) e ß-bisaboleno (10,01%); e nos frutos de V. guianensis foram o ácido (9Z)-octadecenoico (24,95%) e o ácido docosahexaenoico (24,17%). ß-sitosterol e o alquilresorcinol 1-hexadecanoil-2,6-dihidroxibenzeno foram isolados do extrato etanólico dos cipós de P. scabrum; e do extrato etanólico dos frutos de V. guianensis, foram isoladas as antraquinonas crisofanol e fisciona. As determinações estruturais foram baseadas em dados de RMN de ¹H e 13C. RMN, uni e bidimensional e comparação com dados da literatura.

This work describes the chemical study of two medicinal plants of the Amazon Philodendron scabrum K. Krause (Araceae) and Vatairea guianensis Aubl. (Fabaceae). Essential oils composition from stems of Philodendron scabrum K. Krause (Araceae) and fruits of Vatairea guianensis Aubl. (Fabaceae), respectively were analyzed in GC-FID and GC-MS. The major constituents from stems of P. scarabum were caryophyllene oxide (22.42%), α-copaene (16.08%) and ß-bisabolene (12.01%) and from fruits of V. guianensis were (9Z)-octadecenoic acid (24.95%) and docosahexenoic acid (24.17%). ß-sitosterol and alkylresorcinol 1-hexadecanoyl-2,6-dihydroxybenzene were isolated from ethanolic extracts from stems of P. scabrum and from ethanolic extracts from fruits of V. guianensis, the athraquinones chrysophanol and physcion were isolated. The structure of isolated compounds we determinate wered based on data from ¹H and 13C NMR, including two dimensional analyses and comparison with literature data.

Microencapsulación de sustancias oleosas mediante secado por aspersión / Microencapsulation of oily substances by aspersion drying

Para administrar por vía oral compuestos oleosos como los extractos lipídicos de origen natural, los aceites esenciales volátiles y las vitaminas liposolubles, se hace necesario presentarlos en forma de cápsulas blandas. Una alternativa a esta forma de presentación es la microencapsulación, que ofrece una solución para modificar el estado físico y presentarlos en una forma sólida para su administración por vía oral. Esta alternativa permite enmascarar el olor y sabor desagradable de productos que van a ser administrados por vía oral, además de proteger de la oxidación a los ácidos grasos presentes. El secado por aspersión es uno de los métodos más utilizados a escala industrial para la obtención de microcápsulas. Debido a su creciente uso en la industria farmacéutica, en el presente trabajo se recopila el estado del arte en el uso de esta tecnología para la microencapsulación de sustancias oleosas

To administer oral oily compounds such as lipid extracts of natural origin, volatile essential oils and liposoluble vitamins, it is necessary that presentation be in soft capsulae. An alternative to this form of presentation is the microencapsulation being a solution to modify the physical state and to achieve a solid form for its oral administration. This alternative allows masking the smell and the unpleasant flavor of oral products ant also to protect the oxidation of fatty acids present. The aspersion dry is one of the more used methods at industrial scale to microcapsulae achievement. Because of its increasing use in pharmaceutical industry in present paper is gathered the art of state in the use of this technology for oily substances microencapsulation

Erosive oral lichen planus and its management: a case series.

Lichen planus (LP), although a dermatosis, is more common in the oral mucous membrane than in the skin. Lesions of oral LP are classically found on the buccal mucosa and gingiva. Among the various types, the reticular lesions are asymptomatic and require no treatment, but pain and severe discomfort accompany the erosive or ulcerative lesions. Malignant transformation to squamous cell carcinoma developing in areas of erosive oral LP (EOLP) being a possibility, it is important for clinicians to maintain a high index of suspicion for all intraoral lichenoid lesions. Therefore, periodic follow-up of all patients with EOLP is recommended. In view of the above, this paper highlights the management of four cases of EOLP with topical corticosteroid and CO2 laser surgery.

Comparison of dexpanthenol and zinc oxide ointment with ointment base in the treatment of irritant diaper dermatitis from diarrhea: a multicenter study.

BACKGROUND: Severity of irritant diaper dermatitis (IDD) from diarrhea varies from patient to patient depending on the nature of feces and the number of bowel movements. The purpose of the present study was to compare the effectiveness of dexpanthenol and zinc oxide ointment with ointment base in the treatment of irritant diaper dermatitis from acute diarrhea in children by measuring transepidermal water loss (TEWL). MATERIAL AND METHOD: Forty-six children with diarrhea were prospectively, block randomized, investigator-blinded to receive dexpanthenol and zinc oxide ointment on one side and ointment base on the other side. TEWL was measured before and on days 1, 3, and 7 of treatment together with the assessment of severity score. The efficacy of treatment was defined by complete clearance of the lesion. RESULTS: TEWL in the treated and control side was not different before the application of the topical medication. In the present study, the efficacy of 5% dexpanthenol and zinc oxide ointment on D3 was 39% (18from 46 patients) compared to 32% in the ointment base side. On D7, the efficacy of the treated side was 58.7% and the ointment base side was 56%. The patients who still had skin lesions were those who had prolonged diarrhea. On the treated side, the mean of TEWL was lower than the control side on DI (p = 0.18) and had significant improvement on D3 (p = 0. 002). At the end of the present study, TEWL on the treated side was less than TEWL of the control side but it did not have statistical significance (p = 0.07). There was no rash or sign of abnormality on the treated side at the end of D7. CONCLUSION: In the treatment of lDD from acute diarrhea, 5% dexpanthenol and zinc oxide ointment significantly decreased TEWL in the treated side more than the ointment base on day 3 but the severity score was not significantly different on days 1, 3 and 7.

Factors of influence on quality evaluation of adhesive property on cataplasma / 中国中药杂志

<p><b>OBJECTIVE</b>To provide experimental proof for establishing a standard quality evaluation method of adhesive property on Cataplasma by studying the factors of effect on evaluation of adhesive quality on Cataplasma.</p><p><b>METHOD</b>With 180 degrees peel off test, tensile shear and adhesive force test, the influence caused by the square of samples, texture of fabric base and the moisture loss was tested with multifunctional material tester and first stickiness tester.</p><p><b>RESULT</b>The peel off strength of 40 mm wide sample is 26% lower than that of the 20 mm wide sample (P < 0.05), and tensile shear strength had no significant difference. The peel off strength of transverse fabric base was higher than that of lengthways fabric base (P < 0.01). The tensile shear strength of transverse fabric base was lower than that of lengthways fabric base (P < 0.05). The sample with 35% moisture lost had a maximum tensile shear strength and the sample which lost 30% moisture lost had a maximum peel off strength; The sample which lost 20% moisture lost had a maximum first adhesive force.</p><p><b>CONCLUSION</b>The square of samples, the texture of fabric base and the moisture loss of samples can all affect the evaluation of adhesive quality on Cataplasma.</p>

Enfermedad por adyuvantes en humanos asociada a la aplicación de sustancias oleosas. Análisis de 30 pacientes / Human adjuvant diseaseassociated to the application of oil substances. Analysis of 30 patients

Objetivo: informar las manifestaciones clínicas y serológicas de pacientes con enfermedad por adyuvantes (EAH). Métodos: se analizaron los datos clínicos y serológicos de pacientes con enfermedad por adyuvantes que fueron atendidos de enero de 1993 a diciembre de 1996 en el departamento de Medicina Interna del Hospital de Especialidades del Centro Médico Nacional La Raza. Se investigaron las sustancias aplicadas, las manifestaciones clínicas, las alteraciones de laboratorio detectadas, la evolución de los pacientes y el tratamiento recibido. Resultados: se estudió a 30 mujeres con edad promedio de 35 ñ 12 años. En todos los casos existió el antecedente de aplicación de diversos aceites no identificados. Fueron 15 los pacientes que presentaron manifestaciones inespecíficas de enfermedad del tejido conjuntivo. El resto cumplieron con criterios de padecimientos definidos: lupus eritematoso sistémico (5), artritis reumatoide (4), síndrome de sobreposición (2), hepatitis autoinmune (1), tiroiditis autoinmune (1) y colitis ulcerosa crónica inespecífica (1). Se trataron con analg,sicos antiinflamatorios no esteroides, esteroides y en algunos casos antifibróticos e inmunosupresores. Cuando fue posible se extrajo quirúrgicamente el tejido fibronecrótico. La mayoría de los pacientes mejoró con el tratamiento; sin embargo, ninguna se curó y sucedieron tres fallecimientos. Conclusión: la enfermedad por adyuvantes es un padecimiento de alta morbilidad, con respuesta terap,utica parcial y es capaz de provocar la muerte. La enfermedad por adyuvantes debe tenerse presente en pacientes con manifestaciones de enfermedad autoinmune y con el antecedente de aplicación de sustancias oleosas.

Estudio comparativo entre una fórmula de aceite mineral vs. un champú de pediculicida para el tratamiento de la infestación por piojos / Comparative study with one formula of mineral oil vs. one shampoo with the treatment of the louse infection

La infestación por piojos se ha hecho difícil de curar con pediculicidas de uso común por la aparición de resistencia a los insecticidas. La aplicación tópica de sustancias oleosas que actúan como sofocantes ha sido reportada anecdóticamente como un tratamiento efectivo y exento de efectos adversos. El objetivo del presente estudio fue comparar una loción de aceite mineral vs. un champú pediculicida de tetrametrina y butóxido de piperonilo en el tratamiento de la infestación por Pediculus capitis. Se realizó un estudio comparativo, abierto, no aleatorio, en una muestra de 44 niñas de un preescolar de Caracas infestadas por Pediculus capitis. El grupo experimental (n=22) recibió aceite mineral y el grupo control (n=22) recibió champú pediculicida según las indicaciones de los fabricantes. Se consideró curada a la paciente que no presentaba piojos después de revisiones sucesivas durante 2 semanas. La curación lograda con aceite mineral fue 100 por ciento [IC95 por ciento: 82 por ciento-100 por ciento] y 27 por ciento [IC95 por ciento: 11 por ciento-50 por ciento] con el champú pediculicida (p<0,001). El aceite mineral eliminó las liendres en 86 por ciento [IC95 por ciento: 64 por ciento-96 por ciento] de los sujetos y, el champú pediculicida en 36 por ciento [IC95 por ciento: 18 por ciento-59 por ciento] (p=0,0007). Se reportaron efectos desfavorables asociados al champú pediculicida en 36 por ciento [IC95 por ciento: 18 por ciento-59 por ciento] de los sujetos y asociados al aceite mineral en 0 por ciento [IC95 por ciento: 0 por ciento-19 por ciento] (p=0,003). El aceite mineral fue considerado excelente o bueno por 100 por ciento [IC95 por ciento: 82 por ciento-100 por ciento] de los sujetos y el champú pediculicida por 17 por ciento [IC95 por ciento: 5 por ciento-40 por ciento] (p<0,0001). En conclusión una loción de aceite mineral es más efectiva, más segura y mejor aceptada que un champú pediculicida de tetramentrina y butóxido de piperonilo en el tratamiento de la infestación por piojos

Utilización de quitina en formas farmacéuticas. I Ungüento / Use of chitin in pharmaceutical forms. I Ointment

Se realizó un estudio tecnológico en la forma farmacéutica ungüento, para lo cual se empleó quitina como principio activo. Se utilizaron 2 tipos de base, oleosa e hidrosoluble, la primera con mejores características. Se estudiaron la liberación in vitro del fármaco, así como la cinética de este proceso, y se llegó a la conclusión de que el mayor porcentaje de quitina liberada fue en base oleosa. Se siguió en ambos casos una cinética de orden cero

Bases dermatológicas utilizadas en preparados magistrales para ácne y rosácea / Dermatological vehicles utilized in masterly preparations for acne and rosacea

Las bases dermatológicas son preparaciones semisólidas que están destinadas a la aplicación de medicamentos en forma externa. La prescripcón de recetas magistrales permite a los dermatológos individulaizar en forma adecuada las terapias de sus pacientes. Las bases pueden ser clasificadas según su composición en: bases oleaginosas, bases de absorción, emulsiones (aceite/agua, agua/aceite), bases hidrosolubles y geles. Por su bajo o nulo contenido en materia grasa, las bases más indicadas en acné o rosácea son las emulsiones de aceite en agua, las bases hidrosolubles, elaboradas con polietilenglicoles, y los geles. Es importante tener presente la posibilidad de interacciones o incompatibilidades entre diversos principios activos y las bases

Homologous fibronectin enhances healing of excised wounds in rats

In order to evaluate the effects of a topical application of homologous fibronectin on the healing of skin wounds, we made 2 excisional wounds on the back skin of each rat, applied ointment with or without fibronectin purified from citrated homologous plasma, and evaluated the effect according to wound size and microscopic findings. Excised lesions treated with carrier alone, but the difference was significant only in the early phase of wound healing, 2 and 3 days, according to wound size and microscopic changes. A significant decrease in wound size could be found in both groups, treated with ointment containing and not containing fibronectin, between day 4 and 9 when wound contraction was a major contributor to wound closure. Therefore it can be concluded that topical application of fibronectin has a beneficial effect on wound healing during its early phase, but no significant influence on wound contraction.

Identificación y cuantificación de benzocaina y eugenol en un ungüento analgésico dental / Identification and quantification of benzocaine and eugenol in a dental analgesic unguent

Se desarrolla un método analítico donde se describen las especificaciones de calidad para el ungüento analgésico dental. Se identifica la benzocaína por espectrofotometría en la zona UV en concentración de 10 y 100 *g/mL, y se determina el valor de la extinción específica en ambos máximos característicos para la benzocaína, utilizándose para la valoración. Se identificó y valoró el grupo amino aromático. Se demostró que los excipientes no interfieren en la valoración , y se obtuvo un recuperado de 100 ñ 2 % por los 3 métodos. Se propone un método para la valoración del eugenol, mediante la reacción de los grupos fenólicos presentes en la molécula, por fotometría con p-fenilendiamina sulfato en medio de bicarbonato de sodio y posterior oxidación con ferricianuro de potasio, locual forma un compuesto azul violáceo medible espectrofotométricamente a 596 nm; se comprobó en este máximo de absorción la conformidad con la ley de Beer. Se obtuvieron resultados reproducibles para la cuantificación del eugenol en el ungüento y se observó que ni la benzocaína, ni los excipientes de la formulación interfieren en este método