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1.
Biophys Chem ; 294: 106958, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-36682087

RESUMO

Gentamicin is used to treat brucellosis, an infectious disease caused by the Brucella species but the drug faces several issues such as low efficacy, instability, low solubility, and toxicity. It also has a very short half-life, therefore, requiring frequent dosing. Consequently, several other antibiotics are also being used for the treatment of brucellosis as a single dose as well as in combination with other antibiotics but none of these therapies are satisfactory. Nanoparticles in particular polymer-based ones utilizing polymers that are biodegradable and biocompatible for instance PLGA are a method of choice to overcome such drug delivery issues and enable potential targeted delivery. The current study focuses on the evaluation of the structural and dynamical properties of a drug-polymer system consisting of gentamicin drug and PLGA polymer nanoparticles in the water representing a targeted drug delivery system for the treatment of brucellosis. For this purpose, all-atom molecular dynamics simulations were carried out on the drug-polymer systems in the absence and presence of the surfactant bis(2-Ethylhexyl) sulfosuccinate (AOT) to determine the structural and dynamical properties as well as the effect of the surfactant on these properties. We also investigated systems in which the polymer constituents were in the form of monomeric units toward decoupling the primary interactions of the monomer units and polymer effects. The simulation results explain the nature of the interactions between the drug and the polymer as well as transport properties in terms of drug diffusion coefficients, which characterize the molecular behavior of gentamicin-polymer nanoparticles for use in brucellosis.


Assuntos
Brucelose , Nanopartículas , Humanos , Gentamicinas/química , Gentamicinas/uso terapêutico , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/uso terapêutico , Ácido Poliglicólico/química , Ácido Poliglicólico/uso terapêutico , Simulação de Dinâmica Molecular , Teoria da Densidade Funcional , Ácido Láctico/química , Ácido Láctico/uso terapêutico , Antibacterianos/química , Sistemas de Liberação de Medicamentos , Brucelose/tratamento farmacológico , Glicolatos/uso terapêutico , Tensoativos
3.
J Cosmet Dermatol ; 21(9): 3905-3909, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34971480

RESUMO

BACKGROUND: Acanthosis nigricans (AN) is a common dermatosis that presents with hyperpigmented, velvety thick plaques over intertriginous areas. Though a number of treatment modalities including chemical peels have been used, none provide long-term and sustained improvement. AIM AND OBJECTIVES: Our study evaluated the efficacy and safety of regular sessions of salicylic acid-mandelic acid peeling over axillary AN lesions, which was followed by daily application of a topical combination of glycolic acid, urea, and cetylated fat esters for maintenance of effect for 9 months. METHODOLOGY: A retrospective pilot study was conducted in Indian patients (Fitzpatrick skin type 4 or 5), aged 18-50 with benign hereditary AN involving the underarms, with or without affection of other typical sites. Data were retrieved of seventeen patients with AN involving the axillae. Patients were started on combination salicylic-mandelic acid peel given every 2 weeks for a total of 6 sessions. Maintenance was done by night application of combination cream of glycolic acid, urea, and cetylated fat esters, which was continued for 9 months after completion of peeling sessions. Lesions were evaluated every 3 months of 9 months for improvement in pigmentation and skin thickening. RESULTS: All the patients (100%) showed significant improvement in both pigmentation and thickening of lesions. In terms of improvement in skin thickening, very good improvement was seen in 41%, while 29% patients had moderate improvement. In terms of improvement in pigmentation, 35% each had very good and moderate improvement. Post peel erythema (100%) and burning sensation (90%) were the most common encountered adverse effects which lasted for only 1-2 days. Patients were followed up for another 9 months during which no relapses were seen. CONCLUSION: Combination of keratolytic chemical peels and topical mild keratolytic application ensures better therapeutic outcome in patients of AN with long lasting effect.


Assuntos
Acantose Nigricans , Abrasão Química , Melanose , Anormalidades da Pele , Abrasão Química/efeitos adversos , Glicolatos/uso terapêutico , Humanos , Ceratolíticos/efeitos adversos , Ácidos Mandélicos , Melanose/tratamento farmacológico , Projetos Piloto , Estudos Retrospectivos , Ácido Salicílico , Resultado do Tratamento , Ureia/efeitos adversos
4.
Pigment Cell Melanoma Res ; 34(6): 1000-1014, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-33998768

RESUMO

Hyperpigmentation of the skin refers to a dermatological condition which alters the color of the skin, making it discolored or darkened. The treatments for hyperpigmentation disorders often take very long to show results and have poor patient compliance. The first-line treatment for hyperpigmentation involves topical formulations of conventional agents such as hydroquinone, kojic acid, and glycolic acid followed by oral formulations of therapeutic agents such as tranexamic acid, melatonin, and cysteamine hydrochloride. The second-line approaches include chemical peels and laser therapy given under the observation of expert professionals. However, these therapies pose certain limitations and adverse effects such as erythema, skin peeling, and drying and require long treatment duration to show visible effects. These shortcomings of the conventional treatments provided scope for further research on newer alternatives for managing hyperpigmentation. Some of these therapies include novel formulations such as solid lipid nanocarriers, liposomes, phytochemicals, platelet-rich plasma, microneedling. This review focuses on elaborating on several hyperpigmentation disorders and their mechanisms, the current, novel and emerging treatment options for management of hyperpigmentation.


Assuntos
Glicolatos/uso terapêutico , Hidroquinonas/uso terapêutico , Hiperpigmentação/tratamento farmacológico , Pironas/uso terapêutico , Pele/metabolismo , Humanos , Hiperpigmentação/metabolismo
5.
Dermatol Surg ; 47(5): e179-e183, 2021 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-33625140

RESUMO

BACKGROUND: Melasma is an acquired challenging pigmentary skin problem, which commonly affects the face. A wide range of therapeutic modalities is available, yet none is satisfactory. OBJECTIVE: To compare efficacy and safety of trichloroacetic acid (TCA) 20% peeling with either modified Jessner's solution (MJs) or with glycolic acid (GA) 70% peeling in the treatment of melasma. PATIENTS AND METHODS: Thirty adult Egyptian women with melasma were recruited in the study. After cleansing the face, MJs was applied on one side of the face and GA 70% on the other side. Then, TCA 20% was applied in one uniform coat on both sides of the face. Assessment of the clinical response was guided by calculating the melasma area, severity index (MASI), modified MASI, and hemi-MASI scores before and after the end of treatment. RESULTS: Both combinations showed significant reduction in MASI, modified MASI, and hemi-MASI scores (p value = .000, for each). Moreover, the hemi-MASI score after MJs and TCA20% showed a significant decrease compared with GA70% and TCA20% (p value = .013). CONCLUSION: Both modalities are successful, safe options for treating melasma. Moreover, combining MJs with TCA 20% is more efficacious.


Assuntos
Abrasão Química/métodos , Etanol/uso terapêutico , Glicolatos/uso terapêutico , Ácido Láctico/uso terapêutico , Melanose/tratamento farmacológico , Resorcinóis/uso terapêutico , Salicilatos/uso terapêutico , Ácido Tricloroacético/uso terapêutico , Adulto , Combinação de Medicamentos , Quimioterapia Combinada , Feminino , Humanos
6.
J Cosmet Dermatol ; 20(3): 776-780, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33458927

RESUMO

BACKGROUND: Improvement in skin luminosity and dyschromia such as postinflammatory hyperpigmentation (PIH) and actinic photodamage are leading causes for cosmetic consultation. Formulation of topical at home treatment is challenging, using a range of modalities, to help hinder or prevent inflammatory mediators without further irritating the skin. Glycolic acid is a known antioxidant; in various free acid levels, it has been introduced as a topical therapy aimed at reducing pigmentation and improving skin texture, tone, and luminosity. METHODS: In a 12-week clinical study, a novel, topical facial emulsion containing 10% glycolic acid, 2% phytic acid, and soothing complex in emulsion was evaluated for its effectiveness in treating skin quality in American female volunteers with Fitzpatrick skin types II-VI. Efficacy evaluations were performed at pretreatment baseline, weeks 2, 4, 8, and 12, and included expert clinical grading, and self-assessment questionnaires. Cutaneous tolerability was also evaluated by assessing subjective and objective irritation of the treatment area. RESULTS: Significant improvement in the appearance of skin PIH, hyperpigmentation, texture, and tone homogeneity was observed beginning at week 4 and continued through week 12. CONCLUSIONS: The findings suggest that the test product is well suited for at-home skincare. It was both well-tolerated and an effective treatment option for addressing hyperpigmentation and overall skin luminosity.


Assuntos
Hiperpigmentação , Ácido Fítico , Emulsões , Feminino , Glicolatos/uso terapêutico , Humanos , Hiperpigmentação/induzido quimicamente , Hiperpigmentação/tratamento farmacológico , Resultado do Tratamento
7.
J Cutan Med Surg ; 25(1): 77-86, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32929988

RESUMO

Post-inflammatory hyperpigmentation (PIH) is an acquired hypermelanosis that can result from inflammatory dermatologic disease, trauma, or iatrogenesis from procedures. This condition disproportionately affects individuals with skin of color, and it can place a significant psychosocial burden on affected patients. The management of PIH is, therefore, of great interest to clinicians, especially dermatologists. The treatment of established PIH has long been a principal focus within the literature, with publications on the topic outnumbering publications on prophylaxis of PIH. Prophylaxis strategies to prevent PIH vary greatly in clinical practice, likely due to the absence of an evidence-based consensus. Published approaches to PIH prophylaxis include pretreatment (topical alpha hydroxy acids, retinoids, hydroquinone, and brimonidine) and post-treatment strategies (photoprotection, corticosteroids, and tranexamic acid). This review will examine the current literature on prophylaxis of PIH from energy-based device treatments.


Assuntos
Hiperpigmentação/prevenção & controle , Terapia a Laser/efeitos adversos , Corticosteroides/uso terapêutico , Agonistas de Receptores Adrenérgicos alfa 2/uso terapêutico , Antifibrinolíticos/uso terapêutico , Antioxidantes/uso terapêutico , Tartarato de Brimonidina/uso terapêutico , Glicolatos/uso terapêutico , Humanos , Hidroquinonas/uso terapêutico , Hiperpigmentação/diagnóstico , Hiperpigmentação/etiologia , Inflamação/etiologia , Ceratolíticos/uso terapêutico , Retinoides/uso terapêutico , Protetores Solares/uso terapêutico , Ácido Tranexâmico/uso terapêutico
8.
G Ital Dermatol Venereol ; 155(6): 744-748, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33070577

RESUMO

BACKGROUND: The most common therapeutic approach to acne is a combined treatment of retinoid and benzoyl peroxide, with oral antibiotics recommended for moderate-to-severe cases. These kinds of therapies often lead to adverse reactions, leading to the request for new therapeutic options. Recently, the combined use of three salicylic acid-based products for the topical treatment of acne has been related to a significant improvement in acne lesions. METHODS: A multicenter prospective observational study was carried out on patients with a diagnosis of mild comedonal-papular facial acne to provide new evidence on the clinical effectiveness, tolerability and acceptability of three salicylic acid-based products for the topical treatment of acne in the daily clinical practice. Clinical effectiveness on lesions improvement, the evaluation of personal discomfort related to acne and the assessment of overall clinical outcome were the primary endpoints. Treatment acceptability and tolerability were also evaluated. RESULTS: The treatment with the three salicylic acid-based products has been related to a significant improvement on acne lesions over 8 weeks of treatment, along with a reduction of personal discomfort related to acne and an improvement on lesions appearance. The products have also shown good acceptability and tolerability. CONCLUSIONS: The results of this observational study support the effective and well-tolerated use of a combined treatment with three salicylic acid-based products for the topical treatment of acne.


Assuntos
Acne Vulgar/tratamento farmacológico , Fármacos Dermatológicos/uso terapêutico , Dermatoses Faciais/tratamento farmacológico , Ácido Salicílico/uso terapêutico , Dermatopatias Papuloescamosas/tratamento farmacológico , Adulto , Peróxido de Carbamida/administração & dosagem , Peróxido de Carbamida/uso terapêutico , Fármacos Dermatológicos/administração & dosagem , Combinação de Medicamentos , Feminino , Glicolatos/administração & dosagem , Glicolatos/uso terapêutico , Humanos , Masculino , Niacinamida/administração & dosagem , Niacinamida/uso terapêutico , Estudos Prospectivos , Ácido Salicílico/administração & dosagem , Taurina/administração & dosagem , Taurina/uso terapêutico , Resultado do Tratamento , Escala Visual Analógica , Vitamina E/administração & dosagem , Vitamina E/uso terapêutico , Adulto Jovem
9.
J Evid Based Med ; 13(4): 275-283, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33034949

RESUMO

OBJECTIVE: The effects of topical azelaic acid, salicylic acid, nicotinamide, sulfur, zinc, and fruit acid (alpha-hydroxy acid) for acne are unclear. We aimed to assess the effects of these topical treatments by collecting randomized controlled trials. METHODS: We searched The Cochrane Skin Group Specialised Register, CENTRAL, MEDLINE, Embase, and LILACS up to May 2019. We also searched five trials registers. Two review authors independently extracted data and assessed risk of bias. Meta analyses were performed by using Review Manager 5 software. RESULTS: We included a total of 49 trials involving 3880 participants. In terms of treatment response (measured using participants' global self-assessment of acne improvement, PGA), azelaic acid was probably less effective than benzoyl peroxide (RR = 0.82, 95% CI 0.72-0.95). However, there was probably little or no difference in PGA when comparing azelaic acid to tretinoin (RR = 0.94, 95% CI 0.78-1.14). There may be little or no difference when comparing salicylic acid to tretinoin (RR = 1.00, 95% CI 0.92-1.09). There were no studies measured PGA when evaluating nicotinamide. With respect to alpha-hydroxy acid, there may be no difference in PGA when comparing glycolic acid to salicylic-mandelic acid (RR = 1.06, 95% CI 0.88-1.26). We were uncertain about the effects of sulfur and zinc. Adverse events associated with these topical treatments were always mild and transient. CONCLUSIONS: Moderate-quality evidence was available for azelaic acid and low- to very-low-quality evidence for other topical treatments. Risk of bias and imprecision limit our confidence in the evidence.


Assuntos
Acne Vulgar/tratamento farmacológico , Fármacos Dermatológicos/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Glicolatos/uso terapêutico , Niacinamida/uso terapêutico , Ácido Salicílico/uso terapêutico , Enxofre/uso terapêutico , Zinco/uso terapêutico , Administração Cutânea , Fármacos Dermatológicos/administração & dosagem , Ácidos Dicarboxílicos/administração & dosagem , Frutas/química , Glicolatos/administração & dosagem , Humanos , Niacinamida/administração & dosagem , Ácido Salicílico/administração & dosagem , Enxofre/administração & dosagem , Resultado do Tratamento , Zinco/administração & dosagem
10.
Cochrane Database Syst Rev ; 5: CD011368, 2020 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-32356369

RESUMO

BACKGROUND: Acne is an inflammatory disorder with a high global burden. It is common in adolescents and primarily affects sebaceous gland-rich areas. The clinical benefit of the topical acne treatments azelaic acid, salicylic acid, nicotinamide, sulphur, zinc, and alpha-hydroxy acid is unclear. OBJECTIVES: To assess the effects of topical treatments (azelaic acid, salicylic acid, nicotinamide, zinc, alpha-hydroxy acid, and sulphur) for acne. SEARCH METHODS: We searched the following databases up to May 2019: the Cochrane Skin Group Specialised Register, CENTRAL, MEDLINE, Embase, and LILACS. We also searched five trials registers. SELECTION CRITERIA: Clinical randomised controlled trials of the six topical treatments compared with other topical treatments, placebo, or no treatment in people with acne. DATA COLLECTION AND ANALYSIS: We used standard methodological procedures expected by Cochrane. Key outcomes included participants' global self-assessment of acne improvement (PGA), withdrawal for any reason, minor adverse events (assessed as total number of participants who experienced at least one minor adverse event), and quality of life. MAIN RESULTS: We included 49 trials (3880 reported participants) set in clinics, hospitals, research centres, and university settings in Europe, Asia, and the USA. The vast majority of participants had mild to moderate acne, were aged between 12 to 30 years (range: 10 to 45 years), and were female. Treatment lasted over eight weeks in 59% of the studies. Study duration ranged from three months to three years. We assessed 26 studies as being at high risk of bias in at least one domain, but most domains were at low or unclear risk of bias. We grouped outcome assessment into short-term (less than or equal to 4 weeks), medium-term (from 5 to 8 weeks), and long-term treatment (more than 8 weeks). The following results were measured at the end of treatment, which was mainly long-term for the PGA outcome and mixed length (medium-term mainly) for minor adverse events. Azelaic acid In terms of treatment response (PGA), azelaic acid is probably less effective than benzoyl peroxide (risk ratio (RR) 0.82, 95% confidence interval (CI) 0.72 to 0.95; 1 study, 351 participants), but there is probably little or no difference when comparing azelaic acid to tretinoin (RR 0.94, 95% CI 0.78 to 1.14; 1 study, 289 participants) (both moderate-quality evidence). There may be little or no difference in PGA when comparing azelaic acid to clindamycin (RR 1.13, 95% CI 0.92 to 1.38; 1 study, 229 participants; low-quality evidence), but we are uncertain whether there is a difference between azelaic acid and adapalene (1 study, 55 participants; very low-quality evidence). Low-quality evidence indicates there may be no differences in rates of withdrawal for any reason when comparing azelaic acid with benzoyl peroxide (RR 0.88, 95% CI 0.60 to 1.29; 1 study, 351 participants), clindamycin (RR 1.30, 95% CI 0.48 to 3.56; 2 studies, 329 participants), or tretinoin (RR 0.66, 95% CI 0.29 to 1.47; 2 studies, 309 participants), but we are uncertain whether there is a difference between azelaic acid and adapalene (1 study, 55 participants; very low-quality evidence). In terms of total minor adverse events, we are uncertain if there is a difference between azelaic acid compared to adapalene (1 study; 55 participants) or benzoyl peroxide (1 study, 30 participants) (both very low-quality evidence). There may be no difference when comparing azelaic acid to clindamycin (RR 1.50, 95% CI 0.67 to 3.35; 1 study, 100 participants; low-quality evidence). Total minor adverse events were not reported in the comparison of azelaic acid versus tretinoin, but individual application site reactions were reported, such as scaling. Salicylic acid For PGA, there may be little or no difference between salicylic acid and tretinoin (RR 1.00, 95% CI 0.92 to 1.09; 1 study, 46 participants; low-quality evidence); we are not certain whether there is a difference between salicylic acid and pyruvic acid (1 study, 86 participants; very low-quality evidence); and PGA was not measured in the comparison of salicylic acid versus benzoyl peroxide. There may be no difference between groups in withdrawals when comparing salicylic acid and pyruvic acid (RR 0.89, 95% CI 0.53 to 1.50; 1 study, 86 participants); when salicylic acid was compared to tretinoin, neither group had withdrawals (both based on low-quality evidence (2 studies, 74 participants)). We are uncertain whether there is a difference in withdrawals between salicylic acid and benzoyl peroxide (1 study, 41 participants; very low-quality evidence). For total minor adverse events, we are uncertain if there is any difference between salicylic acid and benzoyl peroxide (1 study, 41 participants) or tretinoin (2 studies, 74 participants) (both very low-quality evidence). This outcome was not reported for salicylic acid versus pyruvic acid, but individual application site reactions were reported, such as scaling and redness. Nicotinamide Four studies evaluated nicotinamide against clindamycin or erythromycin, but none measured PGA. Low-quality evidence showed there may be no difference in withdrawals between nicotinamide and clindamycin (RR 1.12, 95% CI 0.49 to 2.60; 3 studies, 216 participants) or erythromycin (RR 1.40, 95% CI 0.46 to 4.22; 1 study, 158 participants), or in total minor adverse events between nicotinamide and clindamycin (RR 1.20, 95% CI 0.73 to 1.99; 3 studies, 216 participants; low-quality evidence). Total minor adverse events were not reported in the nicotinamide versus erythromycin comparison. Alpha-hydroxy (fruit) acid There may be no difference in PGA when comparing glycolic acid peel to salicylic-mandelic acid peel (RR 1.06, 95% CI 0.88 to 1.26; 1 study, 40 participants; low-quality evidence), and we are uncertain if there is a difference in total minor adverse events due to very low-quality evidence (1 study, 44 participants). Neither group had withdrawals (2 studies, 84 participants; low-quality evidence). AUTHORS' CONCLUSIONS: Compared to benzoyl peroxide, azelaic acid probably leads to a worse treatment response, measured using PGA. When compared to tretinoin, azelaic acid probably makes little or no difference to treatment response. For other comparisons and outcomes the quality of evidence was low or very low. Risk of bias and imprecision limit our confidence in the evidence. We encourage the comparison of more methodologically robust head-to-head trials against commonly used active drugs.


Assuntos
Acne Vulgar/tratamento farmacológico , Fármacos Dermatológicos/uso terapêutico , Adapaleno/efeitos adversos , Adapaleno/uso terapêutico , Adolescente , Adulto , Antibacterianos/uso terapêutico , Peróxido de Benzoíla/uso terapêutico , Viés , Criança , Clindamicina/efeitos adversos , Clindamicina/uso terapêutico , Fármacos Dermatológicos/efeitos adversos , Ácidos Dicarboxílicos/efeitos adversos , Ácidos Dicarboxílicos/uso terapêutico , Eritromicina/efeitos adversos , Eritromicina/uso terapêutico , Feminino , Glicolatos/uso terapêutico , Humanos , Ceratolíticos/uso terapêutico , Masculino , Ácidos Mandélicos/uso terapêutico , Niacinamida/efeitos adversos , Niacinamida/uso terapêutico , Pacientes Desistentes do Tratamento/estatística & dados numéricos , Ácido Pirúvico/efeitos adversos , Ácido Pirúvico/uso terapêutico , Qualidade de Vida , Ácido Salicílico/uso terapêutico , Enxofre/uso terapêutico , Tretinoína/uso terapêutico , Adulto Jovem , Zinco/uso terapêutico
11.
J Cosmet Dermatol ; 19(9): 2349-2351, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32250551

RESUMO

BACKGROUND: Many companies capitalized on treatable skin conditions by providing expensive prescription medications or high-end over-the-counter cosmetics. However, patients have become more apprehensive toward these medications in lieu of their often-detrimental side effect profile and reactivity with sensitive skin. AIMS: We developed a serum was created to counteract this budding problem. Our goal was to bring an alternative prescription acne medication that was superior in controlling acne when compared to several OTC and prescription-strength medications. We created a new formulary comprising primarily of all natural glycolic acid and salicylic acid. PATIENTS/METHODS: We designed a prospective study to assess the efficacy of our serum composed of glycolic and salicylic acid for patients suffering from mild to moderate inflammatory and cystic acne, rosacea, folliculitis, and keratosis pilaris. Sixty-six patients were selected ranging in age from 17 to 46. They were asked to apply the wake-up serum at night for 2 weeks. At the follow-up appointment, the patients were asked to fill out a questionnaire regarding the changes they have noticed with their skin. RESULTS: Over 90% of the patients reported they had significant overall improvement in acne with decrease in comedonal and cystic acne. 70%-80% of the patients stated decrease in oiliness, even texture, and smoother looking skin. Physical examination findings were consistent with patient-reported assessment. CONCLUSION: A glycolic and salicylic acid combination serum may be considered an alternative treatment method for patients who wish to opt out of the typical prescription medication treatment.


Assuntos
Acne Vulgar , Ácido Salicílico , Acne Vulgar/tratamento farmacológico , Glicolatos/uso terapêutico , Humanos , Estudos Prospectivos , Ácido Salicílico/uso terapêutico , Resultado do Tratamento
12.
Sci Rep ; 9(1): 2000, 2019 02 13.
Artigo em Inglês | MEDLINE | ID: mdl-30760797

RESUMO

To compare and evaluate the differences of stereoselective activity, the binding affinity, metabolism, transport and molecular docking of phencynonate isomers to muscarinic acetylcholine receptor (mAChR) were investigated in this study. The rotation stimulation and locomotor experiments were used to evaluate anti-motion sickness effects. The competitive affinity with [3H]-QNB and molecular docking were used for studying the interactions between the two isomers and mAChR. The stereoselective mechanism of isomers was investigated by incubation with rat liver microsomes, a protein binding assay and membrane permeability assay across a Caco-2 cell monolayer using a chiral column HPLC method. The results indicated that S-isomer was more effective against motion sickness and had not anxiogenic action at therapeutic doses. S-isomer has the higher affinity and activity for mAChR in cerebral cortex and acted as a competitive mAChR antagonist. The stereoselective elimination of S-isomer was primarily affected by CYP1B1 and 17A1 enzymes, resulting in a higher metabolic stability and slower elimination. Phencynonate S isomer, as a eutomer and central anticholinergic chiral drug, is a novel anti-motion sickness drug with higher efficacy and lower central side effect. Our data assisted the development of a novel drug and eventual use of S-isomer in clinical practice.


Assuntos
Compostos Aza/uso terapêutico , Antagonistas Colinérgicos/uso terapêutico , Glicolatos/uso terapêutico , Enjoo devido ao Movimento/tratamento farmacológico , Enjoo devido ao Movimento/prevenção & controle , Receptores Muscarínicos/efeitos dos fármacos , Animais , Compostos Aza/química , Células CACO-2 , Linhagem Celular Tumoral , Antagonistas Colinérgicos/química , Citocromo P-450 CYP1B1/metabolismo , Glicolatos/química , Humanos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Microssomos Hepáticos/metabolismo , Simulação de Acoplamento Molecular , Ratos , Ratos Sprague-Dawley
13.
Prev Vet Med ; 163: 58-67, 2019 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-30670187

RESUMO

The objective of this study was to evaluate the effect of the implementation of different footbathing practices using a new biocide solution (Pink-Step™, Qalian, France) in the healing and the occurrence of bovine digital dermatitis (bDD) lesions. The investigation was conducted through a controlled within cow clinical trial in which the hind feet of cows from each farm were allocated either to the control group or to a moderate (MR) or (IR) intensive footbath-regimen groups. The trial involved 1036 cows (2072 feet) from 10 dairy farms located in western France where bDD was endemic. Split-footbaths were placed at the exit of the milking parlor of each farm, allowing the biocide to be administered to one side of the cows while using the other empty side as a negative control. The administration frequency for MR was of 2 days/week/1st-month, then 2 days/2 weeks/2nd-month, and then 2 days/month, and for IR was of 2 days/week/1st-2nd months, and then 2 days/2 weeks. Footbaths were administered during 140 days (approx.), and feet were evaluated for the at least once a month in the milking parlor. Nested survival models were used to estimate the relative impact of the footbath regimens and other concomitant risk factors on the time that bDD lesions occurred or healed. No effect of Pink-Step™ was evidenced on the bDD occurrence during the trial. The risk for bDD occurrence was increased by poor feet cleanliness at both the cow (HR 1.69, CI 1.21-2.39) and farm level (HR 2.06, CI 1.44-2.94). Otherwise, the use of Pink-Step™ in an IR was effective in improving the healing of bDD lesions (HR 1.79, CI 1.12-2.88). The time to healing was also improved in inactive lesions (HR 2.19, CI 1.42-3.37). Conversely, the time to healing was delayed in feet receiving hoof-trimming (HR 0.41, CI 0.26-0.62), in cows with a contralateral bDD lesion (HR 0.32, CI 0.22-0.46) or in late lactation (HR 0.61, CI 0.43-0.85), and finally in farms with more than 100 cows (HR 0.48, CI 0.34-0.67). These findings reinforce the crucial role of hygiene in bDD dynamics and highlight the importance of implementing multiple control measures simultaneously, such as hygiene improvements in the barn, early detection and treatment of bDD lesions and the correct usage of individual and collective treatments. The implementation of Pink-Step™ represents a promising strategy for reducing the persistence of bDD lesions in affected herds.


Assuntos
Banhos/veterinária , Doenças dos Bovinos/tratamento farmacológico , Dermatite Digital/tratamento farmacológico , Desinfetantes/uso terapêutico , Higiene da Pele/veterinária , Administração Tópica , Animais , Bovinos , Doenças dos Bovinos/prevenção & controle , Indústria de Laticínios , Dermatite Digital/prevenção & controle , Desinfetantes/administração & dosagem , Feminino , Glicolatos/administração & dosagem , Glicolatos/uso terapêutico , Ácido Láctico/administração & dosagem , Ácido Láctico/uso terapêutico , Resultado do Tratamento
14.
J Cosmet Dermatol ; 18(1): 107-114, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30548170

RESUMO

BACKGROUND: Many methods have been performed to achieve a satisfying outcome in acne scars but some of them were high cost and also were associated with low results and some complications. OBJECTIVES: To evaluate and compare the efficacy and safety therapy of glycolic acid (GA) peel, microneedling with dermapen and a combination of both procedures in treatment of atrophic acne scars. PATENTS AND METHODS: This study was conducted on 30 patients suffering from acne scars. They were randomly assigned into three groups, each group included 10 patients; group I was treated with GA peel, group II treated was with microneedling. Group III received a combination of both procedures. All patients received six sessions with 2-week intervals. The clinical assessment was based on the qualitative global scar grading system before and after treatment, quartile grading scale, and degree of patient satisfaction. RESULTS: There was a statistically significant decrease in acne scars grade after treatment among the studied groups (P = 0.04) but it was higher in group III. There was improvement in boxcar, ice pick, and rolling scars in all groups, respectively (P = 0.03, P = 0.04, P = 0.04). Patients' satisfaction was higher in group III (P = 0.04). CONCLUSION: The combination of dermapen and GA peel is more effective than monotherapy.


Assuntos
Cicatriz/terapia , Técnicas Cosméticas/instrumentação , Glicolatos/uso terapêutico , Ceratolíticos/uso terapêutico , Agulhas , Acne Vulgar/complicações , Adulto , Abrasão Química , Cicatriz/etiologia , Terapia Combinada , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Satisfação do Paciente , Distribuição Aleatória , Índice de Gravidade de Doença , Adulto Jovem
15.
J Am Acad Dermatol ; 81(2): 313-324, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30550830

RESUMO

Chemical peeling, or chemexfoliation, has been used for centuries to improve signs of ultraviolet light-induced sun damage. Over the last 30 years, the science behind chemical peeling has evolved, increasing our understanding of the role of peeling ingredients and treatment indications. The depth of peels is directly related to improved results and to the number of complications that can occur. Key principles for superficial and medium depth peeling are discussed, as well as appropriate indications for these treatments.


Assuntos
Cáusticos/uso terapêutico , Abrasão Química/métodos , Ceratolíticos/uso terapêutico , Dermatopatias/terapia , Abrasão Química/efeitos adversos , Combinação de Medicamentos , Etanol/uso terapêutico , Glicolatos/uso terapêutico , Humanos , Ácido Láctico/uso terapêutico , Fenol/uso terapêutico , Resorcinóis/uso terapêutico , Salicilatos/uso terapêutico , Ácido Salicílico/uso terapêutico , Tretinoína/uso terapêutico , Ácido Tricloroacético/uso terapêutico
16.
Biochem Biophys Res Commun ; 505(3): 898-904, 2018 11 02.
Artigo em Inglês | MEDLINE | ID: mdl-30309657

RESUMO

Major depression is a highly prevalent disorder with no effective medical treatments available. Recent evidence has shown that sirtuins (SIRTs) signaling has been implicated to play an essential in the pathogenesis of depression. Here in this study, we aimed to investigate the potential role of the phencynonate hydrochloride (PHH) in rat models of chronic unpredictable mild stress (CUMS)-induced depression. SIRT6 expression was up-regulated by PHH via increasing NAD+/NADH ratio in the prefrontal cortex. PHH was able to suppress CUMS-induced oxidative stress and enhance the antioxidant capacity and antioxidant proteins activity, such as superoxide dismutase 2 (SOD2) and peroxiredoxin 6 (Prdx6). In vitro study, we found that SIRT6 directly bound to SOD2 and Prdx6 and deacetylated them at Lys68/122 and Lys63/209, which were acetylated by p300/CBP-associated factor (PCAF). Finally, we showed that PHH ameliorated CUMS-induced depressive phenotypes by up-regulating SIRT6 deacetylation activity. In summary, PHH-mediating SIRT6 pathway is required for antidepressant response and PHH can be used as a novel therapeutic to effectively treat depression.


Assuntos
Compostos Aza/farmacologia , Glicolatos/farmacologia , Peroxirredoxina VI/metabolismo , Sirtuínas/metabolismo , Superóxido Dismutase/metabolismo , Acetilação , Animais , Antidepressivos/farmacologia , Compostos Aza/uso terapêutico , Depressão/tratamento farmacológico , Depressão/etiologia , Glicolatos/uso terapêutico , Ratos , Estresse Psicológico/complicações , Estresse Psicológico/tratamento farmacológico
17.
J Cosmet Dermatol ; 17(5): 802-810, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30203434

RESUMO

BACKGROUND: Successful management of acne involves choosing proper medication. Chemical peeling is a well-known option in treatment of acne vulgaris. OBJECTIVE: To evaluate and compare the clinical efficacy and safety of combination chemical peels vs single peel in treatment of mild-to-moderate acne. METHODS: The study included 45 patients with mild-to-moderate acne divided into three equal groups. Group A underwent combination sequential peels with modified Jessner's solution (MJ) followed by trichloro acetic acid (TCA20%) on the right (Rt) side of the face vs TCA 30% on the left (Lt) side. Group B was treated by combination peels of salicylic (20%) mandelic (10%) (SM) mixture on the Rt half vs salicylic acid 30% on the Lt half. Group C underwent combination sequential peeling of MJ and TCA on the Rt side vs SM combination peels on the Lt side. All patients received six sessions with 2-week intervals and followed up for 3 months after the last session. Side effects were reported. RESULTS: Both sides of the face showed significant improvement of acne lesions but improvement was significantly higher and earlier in sides treated by combination peels. Side effects were minimal. CONCLUSION: In conclusion, combination peels achieved a higher and earlier therapeutic response with a reasonable cost that is maintained for a relatively long periods than single peel. Combination sequential peels gave the best results.


Assuntos
Acne Vulgar/diagnóstico , Acne Vulgar/tratamento farmacológico , Abrasão Química/métodos , Ceratolíticos/uso terapêutico , Adulto , Análise de Variância , Combinação de Medicamentos , Quimioterapia Combinada , Etanol/uso terapêutico , Feminino , Glicolatos/uso terapêutico , Humanos , Ácido Láctico/uso terapêutico , Masculino , Análise Multivariada , Prognóstico , Resorcinóis/uso terapêutico , Salicilatos/uso terapêutico , Ácido Salicílico/uso terapêutico , Índice de Gravidade de Doença , Resultado do Tratamento , Ácido Tricloroacético/uso terapêutico , Adulto Jovem
19.
Lasers Med Sci ; 33(7): 1485-1491, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29713841

RESUMO

Pseudo-acanthosis nigricans is a common dermatological disorder that is usually difficult to treat secondary to maceration of the skin from excessive sweating, obesity, or associated with endocrine disorders. Fractional photothermolysis and chemical peeling have been reported to improve the condition. To determine whether fractional CO2 laser resurfacing or glycolic acid peel is more effective and safe option for therapy. Twenty Egyptian patients were included in the study where each patient was subjected to three sessions of both fractional CO2 on the right side of the neck and glycolic acid peel 70% on the left side of the neck. All patients were evaluated by a scoring system Acanthosis Nigricans Area and Severity Index (ANASI) score and three blinded dermatologists before and after treatment. Clinical improvement on the side treated by glycolic acid peel showed 43% improvement while the side treated by fractional CO2 showed 19% improvement. Glycolic acid peel shows superior results to fractional CO2 due to accelerated induced exfoliation, yet still fractional CO2 results are promising due to a presumably long-term improvement of skin texture.


Assuntos
Acantose Nigricans/terapia , Abrasão Química , Glicolatos/uso terapêutico , Lasers de Gás/uso terapêutico , Adulto , Abrasão Química/efeitos adversos , Feminino , Glicolatos/efeitos adversos , Humanos , Lasers de Gás/efeitos adversos , Masculino , Variações Dependentes do Observador , Índice de Gravidade de Doença , Pele/efeitos dos fármacos , Pele/efeitos da radiação
20.
J Dermatolog Treat ; 29(7): 688-693, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29460655

RESUMO

PURPOSE: Washing and over-the-counter cleansers are common interventions in acne vulgaris (AV), but the clinical evidence for their benefit is poorly understood. This systematic review presents clinical studies of washing and cleanser efficacy in acne vulgaris to guide treatment recommendations of dermatologists. MATERIALS AND METHODS: We surveyed English-language articles indexed in MEDLINE (1951-March 2017) and EMBASE (1974-March 2017). Articles were required to be prospective studies of a single over-the-counter cleanser or washing intervention in AV with an objective AV outcome measurement published in a peer-reviewed journal. RESULTS AND CONCLUSIONS: Fourteen prospective studies representing 671 participants were included in this review. Modalities investigated included face washing frequency, true soap/syndet cleansing bars, antiseptic cleansers, alpha and beta-hydroxy (i.e. salicylic) acid cleansers, and several proprietary formulations. Given the low number of well-performed clinical studies of cleansers and washing, it is difficult to formulate reliable recommendations. We hope that our findings highlight the necessity of further investigation in this area.


Assuntos
Acne Vulgar/prevenção & controle , Anti-Infecciosos Locais/uso terapêutico , Detergentes/uso terapêutico , Acne Vulgar/microbiologia , Acne Vulgar/patologia , Anti-Infecciosos Locais/farmacologia , Peróxido de Benzoíla/química , Peróxido de Benzoíla/farmacologia , Peróxido de Benzoíla/uso terapêutico , Detergentes/farmacologia , Face/microbiologia , Face/fisiologia , Glicolatos/farmacologia , Glicolatos/uso terapêutico , Humanos , Propionibacterium acnes/efeitos dos fármacos , Propionibacterium acnes/isolamento & purificação , Ácido Salicílico/farmacologia , Ácido Salicílico/uso terapêutico
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