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1.
J Dermatolog Treat ; 31(2): 147-151, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29770722

RESUMO

Introduction: Topical corticosteroids, available in an array of vehicles are used to control a variety of inflammatory skin diseases. Patients preferences for different vehicles may affect their willingness to use treatment. We assess corticosteroid vehicle preference and potential impact of topical characteristics on adherence and quality of life in patients with psoriasis.Methods: Subjects with psoriasis were recruited from Wake Forest University Dermatology Clinic. Subjects sampled desoximetasone 0.25% spray, betamethasone valerate 0.1% cream, triamcinolone acetonide 0.1% ointment, fluocinonide 0.05% gel, betamethasone valerate 0.1% lotion, clobetasol propionate 0.05% foam, and fluocinonide 0.05% solution in a predetermined randomized order. Subjects completed a Vehicle Preference Measure, Determinants of Adherence Measure, and a Determinants of Quality of Life Measure.Results: Patients preferences for the various products were highly variable. Regarding Determinants of Adherence, patients perception of absorption of the medication was ranked as 'quite important/extremely important' by 85% of total subjects. A majority of patients rated medication side effects as 'quite important/extremely important' when asked to consider topical characteristics effect on quality of life.Discussion: There was wide variation in patient preference for topical medication vehicles used for treating psoriasis. Several vehicle characteristics were considered important to adherence. Given the marked variation in vehicle preference, topical treatment should be individualized according to patients preferences.


Assuntos
Glucocorticoides/uso terapêutico , Veículos Farmacêuticos/química , Psoríase/tratamento farmacológico , Administração Tópica , Valerato de Betametasona/efeitos adversos , Valerato de Betametasona/química , Valerato de Betametasona/uso terapêutico , Clobetasol/efeitos adversos , Clobetasol/química , Clobetasol/uso terapêutico , Desoximetasona/efeitos adversos , Desoximetasona/química , Desoximetasona/uso terapêutico , Composição de Medicamentos , Feminino , Fluocinonida/efeitos adversos , Fluocinonida/uso terapêutico , Glucocorticoides/efeitos adversos , Glucocorticoides/química , Humanos , Masculino , Pessoa de Meia-Idade , Preferência do Paciente/psicologia , Psoríase/patologia , Qualidade de Vida
2.
J Sep Sci ; 42(22): 3413-3420, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31529758

RESUMO

Low-potency corticosteroid betamethasone valerate and vitamin-A tazarotene are used in combination for effective treatment of psoriasis. There is no robust high-performance liquid chromatography analytical technique available for simultaneous estimation of betamethasone valerate and tazarotene in conventional and nanocarriers based formulations. A simple, accurate, robust isocratic high-performance liquid chromatography method was developed for simultaneous estimation of betamethasone valerate and tazarotene in topical pharmaceutical formulations. The developed method was validated as per the regulatory guidelines. The validated method was linear over the concentration range of 150-6000 ng/mL (r2  > 0.999) at 239 nm wavelength. Limits of detection and quantification of two analytes were 50 and 150 ng/mL, respectively. The %relative standard deviation for intraday and interday precision was less than 2%. The method was also evaluated in the presence of forced degradation conditions. The developed method was successfully applied for in vitro and ex vivo drug release studies of in-house designed nanoformulations.


Assuntos
Valerato de Betametasona/análise , Nanopartículas/química , Ácidos Nicotínicos/análise , Animais , Valerato de Betametasona/metabolismo , Cromatografia Líquida de Alta Pressão , Composição de Medicamentos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Camundongos , Ácidos Nicotínicos/metabolismo , Pele/química , Pele/metabolismo
3.
Int J Pharm ; 565: 41-49, 2019 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-31022503

RESUMO

The aim of the present study was to assess the potential of biocompatible polymeric nanosheets as topical and transdermal drug-delivery devices. Nanosheets are two-dimensional nanostructures with a thickness in the nanometer order, and their extremely large aspect ratios result in unique properties, including high transparency, flexibility, and adhesiveness. Nanosheet formulations containing betamethasone valerate (BV) as a model drug and consisting of poly (L-lactic acid) or poly (lactic-co-glycolic) acid were fabricated through a spin-coating-assisted layer-by-layer method using a water-soluble sacrificial membrane. The fabricated formulations could incorporate and release higher amounts of BV compared with a commercial ointment, and the amounts could be controlled by the polymers used, the amount of BV added, and the use of controlled-release membranes. The presence of BV had a minimal effect on thickness, transparency, adhesiveness, and moisture permeability of nanosheets, permitting their application to any area of skin for a long period of time. Therefore, this biocompatible polymeric nanosheet formulation represents a novel and promising topical and transdermal drug delivery device, which has potential to deliver drugs regardless of the area of skin.


Assuntos
Sistemas de Liberação de Medicamentos , Nanoestruturas/administração & dosagem , Poliésteres/administração & dosagem , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/administração & dosagem , Administração Tópica , Adulto , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Valerato de Betametasona/administração & dosagem , Valerato de Betametasona/química , Liberação Controlada de Fármacos , Feminino , Glucocorticoides/administração & dosagem , Glucocorticoides/química , Humanos , Masculino , Nanoestruturas/química , Poliésteres/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Ratos Pelados , Pele/metabolismo , Suínos , Adulto Jovem
4.
MAGMA ; 32(1): 157-162, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30610404

RESUMO

OBJECTIVE: To investigate if it was feasible to quantify the renal excretion of topically applied corticosteroids by 19F MRS. MATERIALS AND METHODS: Five participants, one healthy and four with skin diseases, were treated with ointment containing betamethasone 17-valerate. Urine samples were collected for up to 87 h after the initial application. A sample of ointment mixed with urine served as a study control. Organic fractions were obtained after sample freeze drying, and resolved in deuterated chloroform prior to acquisition of 19F MR spectra at 470 MHz for typically 8 h. RESULTS: We detected fluorine signals in 40 of the 62 fractions of organic extracts. The corticosteroid was detected in samples from all patients, ranging from 0.1 to 2.8% of the applied steroid. No fluorine signal was obtained in samples from the healthy volunteer. DISCUSSION: 19F MRS can be utilized to detect topically applied corticosteroids in urine. However, more work is required to optimize and control for extraction procedures, complete spectral assignments and reliable quantification.


Assuntos
Corticosteroides/administração & dosagem , Corticosteroides/urina , Valerato de Betametasona/química , Imagem por Ressonância Magnética de Flúor-19 , Espectroscopia de Ressonância Magnética , Dermatopatias/tratamento farmacológico , Administração Tópica , Adulto , Idoso , Clorofórmio , Dermatite de Contato/tratamento farmacológico , Dermatite de Contato/urina , Feminino , Voluntários Saudáveis , Humanos , Masculino , Pessoa de Meia-Idade , Pomadas , Projetos Piloto , Prurido/tratamento farmacológico , Prurido/urina , Psoríase/tratamento farmacológico , Psoríase/urina , Pele/efeitos dos fármacos , Dermatopatias/urina , Urinálise/métodos
5.
Drug Dev Ind Pharm ; 45(2): 323-332, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30404554

RESUMO

Betamethsone valerate (BMV), a medium potency topical corticosteroid, is one of the most commonly employed pharmacological agents for the management of atopic dermatitis in both adults and children. Despite having remarkable pharmacological efficacy, these agents have limited clinical implication due to poor penetration across the startum cornum (SC). To mitigate issues related to targeted delivery, stability, and solubility as well as to potentiate therapeutic and clinical implication, the nanodelivery systems have gained remarkable recognition. Therefore, this study was aimed to encapsulate BMV into the chitosan nanoparticles (CS-NPs) for optimum dermal targeting and improved penetration across the SC. The prepared NPs were characterized for particle size, zeta potential, polydispersity index, entrapment efficiency, loading capacity, crystallinity, thermal behavior, morphology, in vitro release kinetics, drug permeation across the SC, and percentage of drug retained into various skin layers. Results showed that optimized BMV-CS-NPs exhibited optimum physicochemical characteristics including small particle size (< 250 ± 28 nm), higher zeta potential (+58 ± 8 mV), and high entrapment efficiency (86 ± 5.6%) and loading capacity (34 ± 7.2%). The in vitro release study revealed that BMV-CS-NPs displayed Fickian-diffusion type mechanism of release in simulated skin surface (pH 5.5). Drug permeation efficiency and the amount of BMV retained into the epidermis and the dermis were comparatively higher in case of BMV-CS-NPs compared to BMV solution. Conclusively, we anticipated that BMV-CS-NPs could be a promising nanodelivery system for efficient dermal targeting of BMV and improved anti-AD efficacy.


Assuntos
Anti-Inflamatórios/administração & dosagem , Valerato de Betametasona/administração & dosagem , Administração Tópica , Animais , Anti-Inflamatórios/química , Valerato de Betametasona/química , Quitosana , Dermatite Atópica/tratamento farmacológico , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Tamanho da Partícula , Pressão , Ratos , Ratos Wistar , Pele/efeitos dos fármacos , Solventes
6.
Drug Deliv Transl Res ; 9(2): 520-533, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-29488170

RESUMO

Atopic dermatitis (AD) is a chronically relapsing eczematous skin disease characterised by frequent episodes of rashes, severe flares, and inflammation. Till date, there is no absolute therapy for the treatment of AD; however, topical corticosteroids (TCs) are the majorly prescribed class of drugs for the management of AD in both adults and children. Though, topical route is most preferable; however, limited penetration of therapeutics across the startum cornum (SC) is one of the major challenges for scientists. Therefore, the present study was attempted to fabricate a moderate-potency TC, betamethasone valerate (BMV), in the form of chitosan nanoparticles (CS-NPs) for optimum dermal targeting and improved penetration across the SC. To further improve the targeting efficiency of BMV and to potentiate its therapeutic efficacy, the fabricated BMV-CS-NPs were coated with hyaluronic acid (HA). The prepared NPs were characterised for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, loading capacity, crystallinity, thermal behaviour, morphology, in vitro release kinetics, drug permeation across the SC, and percentage of drug retained into various skin layers. Results showed that optimised HA-BMV-CS-NPs exhibited optimum physicochemical characteristics including finest particle size (< 300 ± 28 nm), higher zeta potential (+ 58 ± 8 mV), and high entrapment efficiency (86 ± 5.6%) and loading capacity (34 ± 7.2%). The in vitro release study revealed that HA-BMV-CS-NPs displayed Fickian diffusion-type mechanism of release in simulated skin surface (pH 5.5). Drug permeation efficiency of BMV was comparatively higher in case of BMV-CS-NPs; however, the amount of drug retained into the epidermis and the dermis was comparatively higher in case of HA-BMV-CS-NPs, compared to BMV-CS-NPs. Conclusively, we anticipate that HA-BMV-CS-NPs could be a promising nanodelivery system for efficient dermal targeting of BMV and improved anti-AD efficacy.


Assuntos
Valerato de Betametasona , Quitosana , Sistemas de Liberação de Medicamentos , Glucocorticoides , Ácido Hialurônico , Nanopartículas , Animais , Valerato de Betametasona/administração & dosagem , Valerato de Betametasona/química , Quitosana/administração & dosagem , Quitosana/química , Composição de Medicamentos , Liberação Controlada de Fármacos , Glucocorticoides/administração & dosagem , Glucocorticoides/química , Ácido Hialurônico/administração & dosagem , Ácido Hialurônico/química , Cinética , Nanopartículas/administração & dosagem , Nanopartículas/química , Ratos Wistar , Pele/metabolismo , Absorção Cutânea
7.
J Dermatol Sci ; 92(2): 117-126, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30166055

RESUMO

BACKGROUND: Psoriasis is a Th1/Th17-mediated inflammatory dermatosis treated with topical corticosteroids and vitamin D3 analogs (VD3 As). OBJECTIVE: To compare the effects of a VD3 A maxacalcitol and betamethasone valerate (BV) steroid lotion on topical imiquimod (IMQ)-induced psoriasiform skin inflammation. METHODS: Female BALB/c mice were treated with vehicle, maxacalcitol or BV lotion on the skin for 3 days, and IMQ cream for 6 days. q-PCR, H&E, immunohistochemistry and immunofluorescence studies were performed on skin samples. Additionally, mice were treated with vehicle, maxacalcitol or BV lotion for 3 days and CD4+CD25+ regulatory T cells (Tregs) and CD4+CD25- cells from each group were isolated from lymph nodes. Adoptive transfer of the cells was performed on recipient mice which were treated with IMQ cream for 6 days, and skin samples were obtained for q-PCR and H&E staining. RESULTS: Maxacalcitol and BV were comparable in regards clinical improvement, although maxacalcitol reduced the MHC Class II+ inflammatory cell infiltration more than BV in IMQ skin. While both treatments downregulated IL-17 A, IL-17 F, IL-22, IL-12p40, TNF-α and IL-6 mRNA expression levels, only maxacalcitol downregulated IL-23p19 expression. Significantly increased Foxp3+ cell infiltrations and IL-10 expression were noted in maxacalcitol-treated IMQ skin. Adoptive transfer of Treg cells from maxacalcitol-treated donor mice improved IMQ-induced inflammation clinically and histopathologically more than the recipients of Treg cells from BV-treated donor groups, showing reduced levels of inflammatory cytokines and increased IL-10 expression. CONCLUSION: These results indicate that maxacalcitol reduces psoriasiform skin inflammation by inducing Treg cells as well as downregulating IL-23 and IL-17 production.


Assuntos
Calcitriol/análogos & derivados , Fármacos Dermatológicos/farmacologia , Interleucina-17/metabolismo , Interleucina-23/metabolismo , Psoríase/tratamento farmacológico , Linfócitos T Reguladores/efeitos dos fármacos , Transferência Adotiva , Animais , Valerato de Betametasona/farmacologia , Valerato de Betametasona/uso terapêutico , Calcitriol/farmacologia , Calcitriol/uso terapêutico , Fármacos Dermatológicos/uso terapêutico , Regulação para Baixo , Feminino , Humanos , Imiquimode/imunologia , Interleucina-17/imunologia , Interleucina-23/imunologia , Camundongos , Camundongos Endogâmicos BALB C , Psoríase/imunologia , Psoríase/patologia , Pele/citologia , Pele/imunologia , Pele/patologia , Linfócitos T Reguladores/imunologia , Linfócitos T Reguladores/metabolismo , Resultado do Tratamento
9.
Oncogene ; 37(42): 5633-5647, 2018 10.
Artigo em Inglês | MEDLINE | ID: mdl-29904102

RESUMO

Solar ultraviolet (sUV) irradiation is a major environmental carcinogen that can cause inflammation and skin cancer. The costs and morbidity associated with skin cancer are increasing, and therefore identifying molecules that can help prevent skin carcinogenesis is important. In this study, we identified the p53-related protein kinase (PRPK) as a novel oncogenic protein that is phosphorylated by the T-LAK cell-originated protein kinase (TOPK). Knockdown of TOPK inhibited PRPK phosphorylation and conferred resistance to solar-simulated light (SSL)-induced skin carcinogenesis in mouse models. In the clinic, acute SSL irradiation significantly increased epidermal thickness as well as total protein and phosphorylation levels of TOPK and PRPK in human skin tissues. We identified two PRPK inhibitors, FDA-approved rocuronium bromide (Zemuron®) or betamethasone 17-valerate (Betaderm®) that could attenuate TOPK-dependent PRPK signaling. Importantly, topical application of either rocuronium bromide or betamethasone decreased SSL-induced epidermal hyperplasia, neovascularization, and cutaneous squamous cell carcinoma (cSCC) development in SKH1 (Crl: SKH1-Hrhr) hairless mice by inhibiting PRPK activation, and also reduced expression of the proliferation and oncogenesis markers, COX-2, cyclin D1, and MMP-9. This study is the first to demonstrate that targeting PRPK could be useful against sUV-induced cSCC development.


Assuntos
Carcinogênese/metabolismo , Carcinoma de Células Escamosas/enzimologia , Quinases de Proteína Quinase Ativadas por Mitógeno/metabolismo , Proteínas Serina-Treonina Quinases/metabolismo , Neoplasias Cutâneas/enzimologia , Animais , Valerato de Betametasona/farmacologia , Carcinogênese/efeitos dos fármacos , Carcinoma de Células Escamosas/patologia , Inibidores Enzimáticos/farmacologia , Humanos , Camundongos , Camundongos Pelados , Rocurônio/farmacologia , Neoplasias Cutâneas/patologia , Raios Ultravioleta/efeitos adversos
10.
J Chromatogr Sci ; 56(8): 716-723, 2018 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-29800112

RESUMO

Topical pharmaceutical preparations containing betamethasone esters are widely prescribed for treatment of severe inflammatory skin conditions. Some betamethasone esters-containing preparations are formulated with either an antibacterial or an antifungal agent or a vitamin D3 derivative. A fast reversed-phase high-performance liquid chromatography method has been developed for the simultaneous determination of three betamethasone esters-containing binary mixtures along with the excipients of their dosage forms using clobetasone butyrate as internal standard. The first mixture was betamethasone valerate and fusidic acid (Mixture I) with chlorocresol as preservative. The second mixture was betamethasone dipropionate (BTD) and clotrimazole (Mixture II) with benzyl alcohol as preservative. The third mixture was BTD and calcipotriol monohydrate (Mixture III). Optimized chromatographic separation was achieved on a Discovery® C18 (4.6 × 250 mm, 5 µm) column, using water: acetonitrile (35:65, v/v) as mobile phase at flow rate of 1 mL/min with UV detection at 230 nm. The method was validated according to ICH guidelines. The regression coefficients were > 0.999 for all drugs. The method was successfully applied for the determination of the studied drugs in bulk, synthetic mixtures and dosage forms. The developed method is accurate, sensitive, selective and precise and can be used for routine analysis in quality control laboratories.


Assuntos
Anti-Inflamatórios/análise , Valerato de Betametasona/análise , Betametasona/análogos & derivados , Cromatografia Líquida de Alta Pressão/métodos , Administração Tópica , Anti-Inflamatórios/administração & dosagem , Betametasona/administração & dosagem , Betametasona/análise , Valerato de Betametasona/administração & dosagem , Cromatografia de Fase Reversa/métodos , Ésteres/administração & dosagem , Ésteres/análise , Limite de Detecção , Conservantes Farmacêuticos/administração & dosagem , Conservantes Farmacêuticos/análise
11.
J Dermatol Sci ; 90(3): 284-294, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29500077

RESUMO

BACKGROUND: Chronic eczema such as atopic dermatitis imposes significant socio-econo-psychologic burdens on the affected individuals. In addition to conventional topical treatments, phototherapy is recommended for patients with extensive lesions. Although immunosuppression is believed to explain its primary effectiveness, the underlying mechanisms of phototherapy remain unsolved. Ultraviolet irradiation generates various tryptophan photoproducts including 6-formylindolo[3,2-b]-carbazole (FICZ). FICZ is known to be a potent endogenous agonist for aryl hydrocarbon receptor (AHR); however, the biological role of FICZ in chronic eczema is unknown. OBJECTIVE: To investigate the effect of FICZ on chronic eczema such as atopic dermatitis. METHODS: We stimulated HaCaT cells and normal human epidermal keratinocytes (NHEKs) with or without FICZ and then performed quantitative reverse transcriptase polymerase chain reaction, immunofluorescence, and siRNA treatment. We used the atopic dermatitis-like NC/Nga murine model and treated the mice for 2 weeks with either Vaseline® as a control, FICZ ointment, or betamethasone 17-valerate ointment. The dermatitis score, transepidermal water loss, histology, and expression of skin barrier genes and proteins were evaluated. RESULTS: FICZ significantly upregulated the gene expression of filaggrin in both HaCaT cells and NHEKs in an AHR-dependent manner, but did not affect the gene expression of other barrier-related proteins. In addition, FICZ improved the atopic dermatitis-like skin inflammation, clinical scores, and transepidermal water loss in NC/Nga mice compared with those of control mice. On histology, FICZ significantly reduced the epidermal and dermal thickness as well as the number of mast cells. Topical FICZ also significantly reduced the gene expression of Il22. CONCLUSION: These findings highlight the beneficial role of FICZ-AHR and provide a new strategic basis for developing new drugs for chronic eczema.


Assuntos
Carbazóis/farmacologia , Dermatite Atópica/tratamento farmacológico , Dermatophagoides farinae/imunologia , Imunossupressores/farmacologia , Pele/efeitos dos fármacos , Animais , Fatores de Transcrição Hélice-Alça-Hélice Básicos/genética , Fatores de Transcrição Hélice-Alça-Hélice Básicos/metabolismo , Valerato de Betametasona/uso terapêutico , Carbazóis/uso terapêutico , Linhagem Celular , Citocromo P-450 CYP1A1 , Dermatite Atópica/imunologia , Dermatite Atópica/patologia , Feminino , Humanos , Imunossupressores/uso terapêutico , Interleucinas/metabolismo , Proteínas de Filamentos Intermediários/metabolismo , Queratinócitos/imunologia , Queratinócitos/patologia , Camundongos , RNA Mensageiro/metabolismo , RNA Interferente Pequeno/metabolismo , Receptores de Hidrocarboneto Arílico/genética , Receptores de Hidrocarboneto Arílico/metabolismo , Pele/imunologia , Pele/metabolismo , Regulação para Cima , Perda Insensível de Água/efeitos dos fármacos
12.
Eur J Dermatol ; 28(1): 71-77, 2018 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-29521638

RESUMO

BACKGROUND: The stratum corneum is an almost impermeable barrier. Recently, microneedles have been used to increase drug delivery passing the stratum corneum by incorporating the drug within the microneedle or by coating the surface of the microneedle with the drug. OBJECTIVE: This study was performed to investigate whether applying a biodegradable microneedle patch after topical steroid application increases penetration of the steroid in vitro, as well as treatment efficacy in patients with prurigo nodularis. MATERIALS & METHODS: In vitro penetration of topical steroids after biodegradable microneedle patch application was measured using a 3D skin model. To evaluate the treatment efficacy of the combination of biodegradable microneedle and topical steroids, a split-body clinical study was performed. RESULTS: Penetration of topical steroid in the in vitro skin model was significantly greater in the microneedle-applied skin. In a split-body clinical study with prurigo nodularis patients, the area and height of skin lesions decreased after four weeks of treatment on both sides, however, the microneedle patch side exhibited a significantly greater decrease in both area and height, compared to the control side. The pruritus visual analogue scale was also significantly lower on the microneedle side. CONCLUSION: We suggest that simply applying a microneedle patch after topical steroid application could be a useful strategy for treating refractory skin diseases such as prurigo nodularis.


Assuntos
Anti-Inflamatórios/administração & dosagem , Valerato de Betametasona/administração & dosagem , Ácido Hialurônico/administração & dosagem , Prurigo/tratamento farmacológico , Implantes Absorvíveis , Adulto , Anti-Inflamatórios/farmacocinética , Valerato de Betametasona/farmacocinética , Implantes de Medicamento , Feminino , Humanos , Ácido Hialurônico/farmacocinética , Masculino , Agulhas , Prurigo/metabolismo , Prurido/tratamento farmacológico , Tomografia de Coerência Óptica
13.
Lasers Med Sci ; 33(4): 909-916, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29480422

RESUMO

Macular amyloidosis (MA) represents a common variant of primary localized cutaneous amyloidosis. It has a characteristic female predominance; none of the treatment modalities described is either curative or uniformly effective in patients with macular amyloidosis. To determine the effect of fractional CO2 laser in macular amyloidosis in comparison to fractional CO2 laser-assisted drug delivery of topical steroids and topical vitamin C, the study includes 10 female patients with cutaneous macular amyloidosis aged between 20 and 62 years. Patients were treated with four sessions of fractional CO2 laser with 4 weeks interval. Laser treatments were performed using fractional CO2 laser with the following parameters (power 18 W, spacing 800 µm, dwell time 600 µs, stacking 3). The lesion is divided into three areas: area 1, treated by fractional laser only; area 2, treated by fractional laser followed by topical corticosteroid application under occlusion for 24 h; and area 3, treated by fractional laser followed by topical vitamin C serum application under occlusion for 24 h. All lesions were examined clinically and histologically before the therapy and 1 month after the end of the therapy to evaluate the degree of improvement. All treated areas show significant decrease in pigmentation score after treatment, significant drop in rippling (P value < 0.016), and improvement of lichenification; as regards the histological improvement, there was a significant decrease of the amyloid amount after treatment. As regards the amyloid amount, results show significant decrease in the amount of amyloid in all of the three treated areas. Area 2 reported the highest decrease in the amyloid amount followed by areas 1 and 3. One patient (10%) was highly satisfied by the treatment, 6 (60%) reported moderate degree of satisfaction, while only 3 (30%) reported mild satisfaction. Minimal complication occurred in the form of post-inflammatory hyperpigmentation in 1 patient. None of the patients suffered pain, ulceration, or infection. Fractional CO2 alone can be used to improve the texture of macular amyloidosis. If used to assist the delivery of topical steroids and topical vitamin C, improvement can be highly increased.


Assuntos
Amiloidose Familiar/radioterapia , Ácido Ascórbico/administração & dosagem , Valerato de Betametasona/administração & dosagem , Glucocorticoides/administração & dosagem , Lasers de Gás/uso terapêutico , Dermatopatias Genéticas/radioterapia , Administração Tópica , Adulto , Amiloidose Familiar/tratamento farmacológico , Feminino , Humanos , Pessoa de Meia-Idade , Estudos Prospectivos , Dermatopatias Genéticas/tratamento farmacológico , Pigmentação da Pele , Resultado do Tratamento , Adulto Jovem
15.
J Dermatolog Treat ; 29(1): 55-64, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28521549

RESUMO

BACKGROUND: Alopecia areata (AA) is one of the most common causes of localized hair loss. There is no universally proven therapy that induces and sustains remission of hair growth in AA. OBJECTIVE: To compare the efficacy and safety of topical latanoprost, minoxidil and betamethasone valerate on hair growth in patients with AA. PATIENTS AND METHODS: Hundred patients with AA classified into five groups of 20 treated with: Group I, latanoprost 0.1% lotion; Group II, minoxidil 5% lotion; Group III, betamethasone valerate 0.1% solution; Group IV, combination of latanoprost lotion and betamethasone valerate solution and Group V, a vehicle lotion control group. RESULTS: There was a statistically significant improvement in all therapeutic groups when compared with control group and reduction of severity of alopecia tool score of scalp and beard before and after treatment for all therapeutic groups. CONCLUSION: Latanoprost, minoxidil and betamethasone valerate are effective and safe in the treatment of patchy AA. The use of latanoprost added to the therapeutic efficacy of topical betamethasone valerate in the treatment of AA and could be an effective adjunctive topical therapy for AA.


Assuntos
Alopecia em Áreas/tratamento farmacológico , Valerato de Betametasona/uso terapêutico , Minoxidil/uso terapêutico , Prostaglandinas F Sintéticas/uso terapêutico , Administração Tópica , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Alopecia em Áreas/patologia , Criança , Pré-Escolar , Feminino , Humanos , Latanoprosta , Masculino , Pessoa de Meia-Idade , Recidiva , Método Simples-Cego , Resultado do Tratamento , Adulto Jovem
16.
AAPS PharmSciTech ; 19(1): 371-383, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28744617

RESUMO

This study aims to investigate the use of palm olein as the oil phase for betamethasone 17-valerate (BV) emulsions. The physicochemical properties of the formulations were characterized. In vitro drug release study was performed with the Hanson Vertical Diffusion Cell System; the samples were quantified with HPLC and the results were compared with commercial products. Optimized emulsion formulations were subjected to stability studies for 3 months at temperatures of 4, 25, and 40°C; the betamethasone 17-valerate content was analyzed using HPLC. The formulations produced mean particle size of 2-4 µm, viscosities of 50-250 mPa.s, and zeta potential between -45 and -68 mV. The rheological analyses showed that the emulsions exhibited pseudoplastic and viscoelastic behavior. The in vitro release of BV from palm olein emulsion through cellulose acetate was 4.5 times higher than that of commercial products and more BV molecules deposited in rat skin. Less than 4% of the drug was degraded in the formulations during the 3-month period when they were subjected to the three different temperatures. These findings indicate that palm olein-in-water emulsion can be an alternative vehicle for topical drug delivery system with superior permeability.


Assuntos
Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Valerato de Betametasona/administração & dosagem , Valerato de Betametasona/química , Emulsões/química , Óleo de Palmeira/química , Administração Tópica , Animais , Celulose/análogos & derivados , Cromatografia Líquida de Alta Pressão , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Elasticidade , Masculino , Tamanho da Partícula , Veículos Farmacêuticos , Ratos , Ratos Wistar , Reologia , Absorção Cutânea , Temperatura , Viscosidade
17.
Contact Dermatitis ; 78(1): 76-82, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28960334

RESUMO

BACKGROUND: Corticosteroids are among the most commonly used topical drugs. Contact allergy to these exists, but can be easily missed. Corticosteroid screening markers have been included in the baseline series with the aim of detecting most of the sensitized patients. OBJECTIVES: To assess the prevalence of contact allergy to topical corticosteroids in Spain and examine the usefulness of corticosteroid markers to detect contact allergy to corticosteroids. METHODS: In total, 3699 patients referred to 20 dermatology departments across Spain for patch testing with the baseline series, including budesonide and tixocortol pivalate, were also tested with six supplementary corticosteroids (methylprednisolone aceponate, mometasone furoate, prednicarbate, clobetasol propionate, betamethasone 17-valerate, and betamethasone 17,21-dipropionate). Additionally, 2547 (68.8%) patients were tested with hydrocortisone 17-butyrate. RESULTS: Fifty-four patients showed positive reactions to at least one of all tested corticosteroids (1.46%). Thirty-nine (1.05%) reacted to at least one of the additionally tested corticosteroids; among these, 24 of 39 (61.5%) did not react to any of the corticosteroid allergy screening markers tested. CONCLUSIONS: More than half of the patients who were allergic to the additionally tested corticosteroids were not detected with the corticosteroid allergy markers. An update of the corticosteroid allergy screening markers is encouraged, with consideration of group 3 corticosteroids.


Assuntos
Dermatite Alérgica de Contato/diagnóstico , Dermatite Alérgica de Contato/epidemiologia , Fármacos Dermatológicos/efeitos adversos , Testes do Emplastro , Administração Cutânea , Adulto , Betametasona/administração & dosagem , Betametasona/efeitos adversos , Betametasona/análogos & derivados , Valerato de Betametasona/administração & dosagem , Valerato de Betametasona/efeitos adversos , Clobetasol/administração & dosagem , Clobetasol/efeitos adversos , Dermatite Alérgica de Contato/etiologia , Fármacos Dermatológicos/administração & dosagem , Feminino , Humanos , Hidrocortisona/administração & dosagem , Hidrocortisona/efeitos adversos , Hidrocortisona/análogos & derivados , Masculino , Metilprednisolona/administração & dosagem , Metilprednisolona/efeitos adversos , Metilprednisolona/análogos & derivados , Furoato de Mometasona/administração & dosagem , Furoato de Mometasona/efeitos adversos , Valor Preditivo dos Testes , Prednisolona/administração & dosagem , Prednisolona/efeitos adversos , Prednisolona/análogos & derivados , Prevalência , Estudos Prospectivos , Espanha/epidemiologia
18.
Curr Drug Deliv ; 15(5): 641-651, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-28925874

RESUMO

BACKGROUND: Betamethasone Valerate (BV) is a potent topical corticosteroid. Preparation of nanostructured lipid carriers (NLC) involves process parameters optimization and formulations were developed. It is available in several conventional formulations like creams and ointments which have well-known problems of frequent dosing and consequently additional side effects. The aim is to ascertain the probability of NLC as an exclusive carrier for betamethasone valerate topical application with regard to release modulation and improved therapeutic effect. METHOD: Preparation of BVNLC formulations involves rigorous broad range optimization of process parameters viz. selection of lipids, surfactants, formulation technique, stirring time, stirring speed and homogenization cycles. Accordingly, optimized parameters were selected and formulation table was developed. Characterizations of developed NLC comprise particle shape, size, zeta potential, percent drug entrapment, in vitro drug release studies. The optimized NLC formulation was gelled and evaluated for ex vivo permeation studies and preclinical anti-inflammatory testing. RESULTS: The permeation studies revealed that enhancement ratio of BVNLC based gel was 2.59 folds higher as compared to plain BV gel. Release models indicated anomalous (non-fickian) diffusion viz. drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. Preclinical studies indicated a significant (P < 0.05) extended anti-inflammatory effect and 16.5% inhibition compared to plain gel. CONCLUSION: The outcome of entire characterization advocates that the developed formulation is efficient as once a day dosing in therapy of atopic dermatitis.


Assuntos
Anti-Inflamatórios/administração & dosagem , Valerato de Betametasona/administração & dosagem , Portadores de Fármacos/administração & dosagem , Lipídeos/administração & dosagem , Nanoestruturas/administração & dosagem , Administração Tópica , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacocinética , Valerato de Betametasona/química , Valerato de Betametasona/farmacocinética , Carragenina , Dermatite Atópica/tratamento farmacológico , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Liberação Controlada de Fármacos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Géis , Lipídeos/química , Lipídeos/farmacocinética , Masculino , Nanoestruturas/química , Permeabilidade , Ratos Wistar , Pele/metabolismo , Absorção Cutânea
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