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1.
J Drugs Dermatol ; 23(6): 410-417, 2024 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-38834229

RESUMEN

INTRODUCTION: Acne vulgaris is a common skin disease prevalent in skin of color patients. Studies have demonstrated that dapsone gel, 7.5% (Aczone) used once daily is effective, safe, and well-tolerated for the treatment of acne in both men and women. However, minimal data are available in skin of color populations. This single-center, open-label clinical study investigated the efficacy and safety of dapsone gel, 7.5% in the treatment of moderate to severe acne vulgaris in patients with Fitzpatrick skin types IV-VI. METHODS: Twenty (20) adult subjects with moderate to severe acne and Fitzpatrick skin types IV-VI were enrolled in this study and treated with dapsone gel, 7.5% once daily for 24 weeks. RESULTS: Dapsone gel, 7.5% applied daily for 24 weeks reduced acne severity, post-inflammatory hyperpigmentation, and decreased new inflammatory and noninflammatory acne lesions in skin of color patients with moderate to severe acne vulgaris. Treatment resulted in improved acne health-related quality of life and patient symptoms related to acne, including patient-reported post-inflammatory hyperpigmentation, especially with a treatment duration of 18 weeks or longer.  Limitations: The sample size was small and underpowered to detect statistically significant changes in some endpoints. CONCLUSION: Dapsone gel 7.5% was safe, well-tolerated, and efficacious in treating acne vulgaris and post-inflammatory hyperpigmentation in skin-of-color patients. Larger studies involving skin-of-color populations with acne vulgaris are warranted. J Drugs Dermatol. 2024;23(6):410-417. doi:10.36849/JDD.7897.


Asunto(s)
Acné Vulgar , Administración Cutánea , Dapsona , Índice de Severidad de la Enfermedad , Adolescente , Adulto , Femenino , Humanos , Masculino , Adulto Joven , Acné Vulgar/tratamiento farmacológico , Dapsona/administración & dosificación , Dapsona/efectos adversos , Geles , Hiperpigmentación/inducido químicamente , Hiperpigmentación/tratamiento farmacológico , Calidad de Vida , Pigmentación de la Piel , Resultado del Tratamiento , Minorías Étnicas y Raciales
2.
J Drugs Dermatol ; 23(6): e151-e153, 2024 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-38834215

RESUMEN

BACKGROUND: Melasma and post-inflammatory hyperpigmentation (PIH) are common cosmetic dermatologic conditions that predominantly affect patients with skin phototypes III-VI. Comparing treatment coverage for these pigmentary disorders to treatment coverage for acne vulgaris may demonstrate disparities in insurance coverage for diseases that primarily affect patients of color. OBJECTIVE: Describe differences in Medicaid coverage for topical tretinoin for melasma and PIH vs. acne vulgaris in all 50 states and the District of Columbia. METHODS: This is a cross-sectional study of Medicaid insurance plans in all 50 states and the District of Columbia conducted between February 1 and 28, 2023. Data was collected from online publicly available preferred drug lists, prior authorization criteria, and email/telephone inquiries. Information was collected regarding coverage restrictions, including age restrictions, diagnostic restrictions, preferred drug status, and prior authorization requirements. RESULTS: Complete coverage data for all three clinical indications was retrieved from 30 (58.8%) states; partial coverage data for acne vulgaris was retrieved from 16 (31.4%) states; no coverage data was retrieved from 5 (9.8%) states. Of states reporting coverage data, topical tretinoin is covered in 45 (97.8%) states for acne vulgaris and 10 (33.3%) states for melasma and post-inflammatory hyperpigmentation. There was decreased Medicaid coverage of topical tretinoin for acne vulgaris compared to melasma and PIH (P<0.05).  Conclusion: There is differential Medicaid coverage for acne vulgaris compared to pigmentary disorders which disproportionately affect patients of color. Greater advocacy is required to ensure equal treatment for conditions that affect racial minority patients. J Drugs Dermatol. 2024;23(6):e151-e153.     doi:10.36849/JDD.8069e  .


Asunto(s)
Acné Vulgar , Cobertura del Seguro , Medicaid , Tretinoina , Humanos , Estados Unidos , Acné Vulgar/tratamiento farmacológico , Tretinoina/administración & dosificación , Tretinoina/economía , Medicaid/estadística & datos numéricos , Estudios Transversales , Cobertura del Seguro/estadística & datos numéricos , Hiperpigmentación/tratamiento farmacológico , Disparidades en Atención de Salud/economía , Femenino , Queratolíticos/administración & dosificación , Queratolíticos/economía , Melanosis/tratamiento farmacológico , Masculino
3.
J Drugs Dermatol ; 23(4): 233-238, 2024 04 01.
Artículo en Inglés | MEDLINE | ID: mdl-38564394

RESUMEN

BACKGROUND: Silymarin is an antioxidant that can protect against free radicals that cause premature signs of aging and oil oxidation that may contribute to breakouts. AIMS: The objective of these studies was to evaluate a silymarin antioxidant serum alone and in combination with a prescription acne treatment regimen in improving facial appearance in blemish-prone skin.  Methods: Two international studies were conducted. A 12-week study in Brazil enrolled 56 subjects to examine the effect of silymarin antioxidant serum on facial acne. Clinical grading on acne lesions, skin tone, clarity, and postinflammatory hyperpigmentation (PIH) were conducted. In addition, consumer self-assessment, analysis for markers of lipid peroxidation, and sebumeter analysis were completed. Another Unites States (US)/German study enrolled 40 subjects who were on topical prescription acne medications to which silymarin antioxidant serum was added. Acne lesion counts, tolerability, and facial appearance assessments were conducted in this study. RESULTS: The Brazilian study demonstrated a 45% reduction in inflammatory lesions and a 43% reduction in noninflammatory lesions after 12 weeks of silymarin antioxidant serum use. In addition, sebumeter testing showed a 16% reduction in oiliness at week 1. The US/German study showed the benefits of the serum in persons already on prescription acne therapy by reducing facial erythema by 60%, dryness by 49%, and scaling by 67%. CONCLUSION: Silymarin is shown in clinical testing to have significant benefits in reducing lipid peroxidation, oiliness, and PIH, and in improving key markers of skin aging. Additionally, the serum can be used alone or as an adjunctive treatment in acne therapy to further benefit aging, acne-prone skin. J Drugs Dermatol. 2024;23(4):     doi:10.36849/JDD.8120.


Asunto(s)
Acné Vulgar , Hiperpigmentación , Silimarina , Humanos , Antioxidantes/uso terapéutico , Silimarina/uso terapéutico , Administración Cutánea , Resultado del Tratamiento , Acné Vulgar/diagnóstico , Acné Vulgar/tratamiento farmacológico , Acné Vulgar/patología , Hiperpigmentación/tratamiento farmacológico
4.
Int J Dermatol ; 63(6): 704-713, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38643368

RESUMEN

Acne, a highly prevalent skin disease, can be particularly bothersome for patients of Asian background because of its impact on self-confidence and social interactions. In addition to active acne lesions, some patients may develop sequelae such as scarring, macular/postinflammatory hyperpigmentation, or erythema. The tendency of Asian skin to develop sequelae because of its increased susceptibility to irritation, cultural preferences for lighter skin phototypes, and differences in skincare regimens may all contribute to the increased burden of acne. Moreover, many Asia-Pacific countries do not have their own guidelines for acne management, and those that do often have no schedule in place for regular updates. In this article, we provide a critical review of the published guidance for the management of acne and its sequelae in the Asia-Pacific region, identifying gaps in current recommendations that could be addressed to enhance standards of acne care in Asia-Pacific countries. Along with highlighting the importance of a comprehensive skincare regimen to increase treatment efficacy and adherence, we discuss topical retinoids and retinoid combination options in the acne armamentarium that may be beneficial for sequelae prevention and management, such as adapalene 0.3% ± benzoyl peroxide 2.5%, tretinoin 0.05%, tazarotene 0.1%, and trifarotene 0.005%. In particular, trifarotene 0.005% has been observed to significantly reduce acne scar counts in a Phase 4 study. The recent data highlight the need to establish up-to-date guidance for acne and acne sequelae management in Asia-Pacific countries to provide optimal care to Asian patients.


Asunto(s)
Acné Vulgar , Fármacos Dermatológicos , Retinoides , Humanos , Acné Vulgar/tratamiento farmacológico , Acné Vulgar/complicaciones , Fármacos Dermatológicos/administración & dosificación , Fármacos Dermatológicos/uso terapéutico , Fármacos Dermatológicos/efectos adversos , Retinoides/administración & dosificación , Retinoides/uso terapéutico , Retinoides/efectos adversos , Asia , Hiperpigmentación/etiología , Hiperpigmentación/tratamiento farmacológico , Administración Cutánea , Cicatriz/etiología , Cicatriz/tratamiento farmacológico , Guías de Práctica Clínica como Asunto , Cuidados de la Piel/métodos , Eritema/tratamiento farmacológico , Eritema/etiología
5.
Int J Dermatol ; 63(6): 806-815, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38685118

RESUMEN

BACKGROUND: Acne-induced hyperpigmentation (AIH) may accompany acne vulgaris (AV) inflammation in all skin phototypes. Trifarotene has shown depigmenting properties in vivo. This study evaluated trifarotene plus skincare because it is increasingly recognized that holistic AV management should include skincare and treatments. METHODS: This is a phase IV double-blind, parallel-group study of patients (13-35 years) with moderate AV and AIH treated with trifarotene (N = 60) or vehicle (N = 63) plus skincare regimen (moisturizer, cleanser, and sunscreen) for 24 weeks. Assessments included the AIH overall disease severity (ODS) score, post-AV hyperpigmentation index (PAHPI), exit interviews, photography, and acne assessments. Standard safety assessments were included. RESULTS: Trifarotene 50 µg/g cream improved significantly from baseline in ODS score versus vehicle (-1.6 vs. -1.1, P = 0.03) at Week 12, but scores were comparable between groups at Week 24 (primary endpoint). Trifarotene had a better reduction in PAHPI score at Week 24 (-18.9% vs. -11.3% vehicle, P < 0.01). Lesion count reductions were higher with trifarotene at Week 12 versus vehicle (P < 0.001) and at Week 24 (P < 0.05), as were IGA success rates versus vehicle at Weeks 12 (P < 0.05) and 24 (P < 0.05). Patients agreed that the skincare regimen contributed to less irritation, making treatment adherence easier. Photography showed improvements in pigmentation and erythema across all skin types. AEs were more common in the vehicle group versus trifarotene (30.2 vs. 16.7%, respectively). CONCLUSIONS: In all skin phototypes, there was more rapid improvement in the ODS and PAHPI scores with trifarotene by Weeks 12 and 24, respectively. The combination of trifarotene and skincare correlated with high patient satisfaction and adherence to the treatment protocol.


Asunto(s)
Acné Vulgar , Hiperpigmentación , Índice de Severidad de la Enfermedad , Cuidados de la Piel , Protectores Solares , Adolescente , Adulto , Femenino , Humanos , Masculino , Adulto Joven , Acné Vulgar/complicaciones , Acné Vulgar/tratamiento farmacológico , Fármacos Dermatológicos/administración & dosificación , Fármacos Dermatológicos/efectos adversos , Método Doble Ciego , Hiperpigmentación/etiología , Hiperpigmentación/tratamiento farmacológico , Hiperpigmentación/prevención & control , Retinoides , Cuidados de la Piel/métodos , Crema para la Piel/administración & dosificación , Pigmentación de la Piel/efectos de los fármacos , Pigmentación de la Piel/efectos de la radiación , Protectores Solares/administración & dosificación , Minorías Étnicas y Raciales
6.
Exp Dermatol ; 33(4): e15069, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38568090

RESUMEN

Topicals and chemical peels are the standard of care for management of facial hyperpigmentation. However, traditional therapies have come under recent scrutiny, such as topical hydroquinone (HQ) has some regulatory restrictions, and high concentration trichloroacetic acid (TCA) peel pose a risk in patients with skin of colour. The objective of our research was to identify, investigate and elucidate the mechanism of action of a novel TCA- and HQ-free professional-use chemical peel to manage common types of facial hyperpigmentation. Using computational modelling and in vitro assays on tyrosinase, we identified proprietary multi-acid synergistic technology (MAST). After a single application on human skin explants, MAST peel was found to be more effective than a commercial HQ peel in inhibiting melanin (histochemical imaging and gene expression). All participants completed the case study (N = 9) without any adverse events. After administration of the MAST peel by a dermatologist, the scoring and VISIA photography reported improvements in hyperpigmentation, texture and erythema, which could be linked to underlying pathophysiological changes in skin after peeling, visualized by non-invasive optical biopsy of face. Using reflectance confocal microscopy (VivaScope®) and multiphoton tomography (MPTflex™), we observed reduction in melanin, increase in metabolic activity of keratinocytes, and no signs of inflammatory cells after peeling. Subsequent swabbing of the cheek skin found no microbiota dysbiosis resulting from the chemical peel. The strong efficacy with minimum downtime and no adverse events could be linked to the synergistic action of the ingredients in the novel HQ- and TCA-free professional peel technology.


Asunto(s)
Hidroquinonas , Hiperpigmentación , Melaninas , Humanos , Hiperpigmentación/tratamiento farmacológico , Piel , Biología Computacional , Biopsia
9.
J Cosmet Dermatol ; 23(6): 2058-2065, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38549196

RESUMEN

BACKGROUND: The diverse causes of hyperpigmentation and complex nature of melanogenesis make it a challenge to manage. Current approaches either fail to deliver effective pigmentation control or have undesirable safety profiles that preclude their long-term use. AIMS: To evaluate the capacity of a cosmetic gel serum comprising tranexamic acid, niacinamide, 4-butylresorcinol, phytic acid, and a mixture of hydroxy acids that was designed to target the biological processes regulating skin melanogenesis to attenuate melanin production in vitro and reduce hyperpigmentation clinically. METHODS: Capacity to reduce melanin production in vitro was determined in melanocyte-containing reconstructed human epidermis (RHEm). Clinical efficacy and skin tolerability following twice daily application were assessed in 35 subjects with slight to moderate facial hyperpigmentation by instrumental (VISIA®-CR, Mexameter®) and clinical (mMASI, clinical score, IGA for hyperpigmentation) evaluation on D14, D28, D56, and D84. Maintenance of pigmentation control was followed up 1 month after cessation of treatment on D112. RESULTS: In RHEm in vitro, melanin production was reduced by 50.0% from baseline (D0) on D14 (p < 0.001) and by 67.0% on D21 (p < 0.001). Clinical reductions from baseline in brown spots count (-9.0%; p < 0.05), brown spots area (-16.7%; p < 0.001), and the melanin index (-11.4%; p < 0.001) were observed within 14 days of use. Statistically significant improvements in all clinical parameters were achieved by D28. By the end of treatment on D84, the number and surface area of brown spots were reduced by 28.4% and 40.3% compared to D0, respectively (p < 0.001, both), the melanin index was reduced by 31.1% (p < 0.001), mMASI was reduced by 63.0% (p < 0.001), and skin luminosity was increased by 79.0% (p < 0.001). IGA was reduced from 2.3 on D0 to 1.3 on D84 (p < 0.001). Improvements to all these parameters were maintained until D112, 1 month after termination of treatment. The product also demonstrated very good skin tolerability. CONCLUSION: A gel serum comprising tranexamic acid, niacinamide, 4-butylresorcinol, and hydroxy acids, designed to target the biological processes regulating skin melanogenesis, demonstrates rapid, robust, and sustained pigmentation control in this cohort.


Asunto(s)
Hiperpigmentación , Melaninas , Melanocitos , Niacinamida , Resorcinoles , Pigmentación de la Piel , Ácido Tranexámico , Adulto , Femenino , Humanos , Masculino , Persona de Mediana Edad , Adulto Joven , Administración Cutánea , Combinación de Medicamentos , Epidermis/efectos de los fármacos , Epidermis/metabolismo , Geles , Hiperpigmentación/tratamiento farmacológico , Melanocitos/efectos de los fármacos , Melanocitos/metabolismo , Melanogénesis , Niacinamida/administración & dosificación , Niacinamida/farmacología , Niacinamida/efectos adversos , Resorcinoles/administración & dosificación , Resorcinoles/efectos adversos , Resorcinoles/farmacología , Preparaciones para Aclaramiento de la Piel/administración & dosificación , Preparaciones para Aclaramiento de la Piel/farmacología , Preparaciones para Aclaramiento de la Piel/efectos adversos , Pigmentación de la Piel/efectos de los fármacos , Ácido Tranexámico/administración & dosificación , Ácido Tranexámico/efectos adversos , Ácido Tranexámico/farmacología , Resultado del Tratamiento
10.
Med Chem ; 20(4): 397-413, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38425108

RESUMEN

INTRODUCTION: Tyrosinase is a versatile, glycosylated copper-containing oxidase enzyme that mainly catalyzes the biosynthesis of melanin in mammals. Its overexpression leads to the formation of excess melanin, resulting in hyperpigmentary skin disorders, such as dark spots, melasma, freckles, etc. Therefore, inhibition of tyrosinase is a therapeutic approach for the treatment of hyperpigmentation. METHODS: The current study focused on evaluating tyrosinase inhibitory activities of triazole derivatives 1-20, bearing different substituents on the phenyl ring. 17 derivatives have shown a potent tyrosinase inhibition with IC50 values between 1.6 to 13 µM, as compared to the standard drug, i.e., kojic acid (IC50 = 24.1 ± 0.5 µM). Particularly, compounds 11 and 15 displayed 12 times more potent inhibitory effects than the kojic acid. RESULTS: The structure-activity relationship revealed that substituting halogens at the C-4 position of the benzene ring renders remarkable anti-tyrosinase activities. Compounds 1-3 and 8 showed a competitive type of inhibition, while compounds 5, 11, and 15 showed a non-competitive mode of inhibition. Next, we performed molecular docking analyses to study the binding modes and interactions between the ligands (inhibitors) and the active site of the tyrosinase enzyme (receptor). Besides this, we have assessed the toxicity profile of inhibitors on the BJ human fibroblast cell line. CONCLUSION: The majority of the newly identified tyrosinase inhibitors were found to be noncytotoxic. The results presented herein form the basis of further studies on triazole derivatives as potential drug leads against tyrosinase-related diseases.


Asunto(s)
Inhibidores Enzimáticos , Hiperpigmentación , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa , Triazoles , Monofenol Monooxigenasa/antagonistas & inhibidores , Monofenol Monooxigenasa/metabolismo , Triazoles/química , Triazoles/farmacología , Triazoles/síntesis química , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/síntesis química , Relación Estructura-Actividad , Hiperpigmentación/tratamiento farmacológico , Humanos , Estructura Molecular , Enfermedades de la Piel/tratamiento farmacológico , Pironas
11.
Pharm Biol ; 62(1): 296-313, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38555860

RESUMEN

CONTEXT: Hyperpigmentation, a common skin condition marked by excessive melanin production, currently has limited effective treatment options. OBJECTIVE: This study explores the effects of Tao-Hong-Si-Wu decoction (THSWD) on hyperpigmentation and to elucidate the underlying mechanisms. MATERIALS AND METHODS: We employed network pharmacology, Mendelian randomization, and molecular docking to identify THSWD's hub targets and mechanisms against hyperpigmentation. The Cell Counting Kit-8 (CCK-8) assay determined suitable THSWD treatment concentrations for PIG1 cells. These cells were exposed to graded concentrations of THSWD-containing serum (2.5%, 5%, 10%, 15%, 20%, 30%, 40%, and 50%) and treated with α-MSH (100 nM) to induce an in vitro hyperpigmentation model. Assessments included melanin content, tyrosinase activity, and Western blotting. RESULTS: ALB, IL6, and MAPK3 emerged as primary targets, while quercetin, apigenin, and luteolin were the core active ingredients. The CCK-8 assay indicated that concentrations between 2.5% and 20% were suitable for PIG1 cells, with a 50% cytotoxicity concentration (CC50) of 32.14%. THSWD treatment significantly reduced melanin content and tyrosinase activity in α-MSH-induced PIG1 cells, along with downregulating MC1R and MITF expression. THSWD increased ALB and p-MAPK3/MAPK3 levels and decreased IL6 expression in the model cells. DISCUSSION AND CONCLUSION: THSWD mitigates hyperpigmentation by targeting ALB, IL6, and MAPK3. This study paves the way for clinical applications of THSWD as a novel treatment for hyperpigmentation and offers new targeted therapeutic strategies.


Asunto(s)
Medicamentos Herbarios Chinos , Hiperpigmentación , Humanos , Análisis de la Aleatorización Mendeliana , Melaninas , Monofenol Monooxigenasa , Simulación del Acoplamiento Molecular , alfa-MSH , Farmacología en Red , Interleucina-6 , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Hiperpigmentación/tratamiento farmacológico
12.
Int J Biol Sci ; 20(5): 1688-1704, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38481807

RESUMEN

Background: Melanocortin 1 receptor (MC1R), a receptor of α-melanocyte-stimulating hormone (α-MSH), is exclusively present in melanocytes where α-MSH/MC1R stimulate melanin pigmentation through microphthalmia-associated transcription factor M (MITF-M). Toll-like receptor 4 (TLR4), a receptor of endotoxin lipopolysaccharide (LPS), is distributed in immune and other cell types including melanocytes where LPS/TLR4 activate transcriptional activity of nuclear factor (NF)-κB to express cytokines in innate immunity. LPS/TLR4 also up-regulate MITF-M-target melanogenic genes in melanocytes. Here, we propose a molecular target of antimelanogenic activity through elucidating inhibitory mechanism on α-MSH-induced melanogenic programs by benzimidazole-2-butanol (BI2B), an inhibitor of LPS/TLR4-activated transcriptional activity of NF-κB. Methods: Ultraviolet B (UV-B)-irradiated skins of HRM-2 hairless mice and α-MSH-activated melanocyte cultures were employed to examine melanogenic programs. Results: Topical treatment with BI2B ameliorated UV-B-irradiated skin hyperpigmentation in mice. BI2B suppressed the protein or mRNA levels of melanogenic markers, such as tyrosinase (TYR), MITF-M and proopiomelanocortin (POMC), in UV-B-exposed and pigmented skin tissues. Moreover, BI2B inhibited melanin pigmentation in UV-B-irradiated co-cultures of keratinocyte and melanocyte cells and that in α-MSH-activated melanocyte cultures. Mechanistically, BI2B inhibited the activation of cAMP response element-binding protein (CREB) in α-MSH-induced melanogenic programs and suppressed the expression of MITF-M at the promoter level. As a molecular target, BI2B primarily inhibited mitogen-activated protein kinase (MAPK) kinase 3 (MKK3)-catalyzed kinase activity on p38MAPK. Subsequently, BI2B interrupted downstream pathway of p38MAPK-mitogen and stress-activated protein kinase-1 (MSK1)-CREB-MITF-M, and suppressed MITF-M-target melanogenic genes, encoding enzymes TYR, TYR-related protein-1 (TRP-1) and dopachrome tautomerase (DCT) in melanin biosynthesis, and encoding proteins PMEL17 and Rab27A in the transfer of pigmented melanosomes to the overlaying keratinocytes in the skin. Conclusion: Targeting the MKK3-p38MAPK-MSK1-CREB-MITF-M pathway was suggested as a rationale to inhibit UV-B- or α-MSH-induced facultative melanogenesis and as a strategy to prevent acquired pigmentary disorders in the skin.


Asunto(s)
Proteína de Unión a Elemento de Respuesta al AMP Cíclico , Hiperpigmentación , Animales , Ratones , Proteína de Unión a Elemento de Respuesta al AMP Cíclico/metabolismo , Melaninas/metabolismo , Receptor Toll-Like 4/genética , Receptor Toll-Like 4/metabolismo , Proteínas Quinasas p38 Activadas por Mitógenos/metabolismo , alfa-MSH/farmacología , alfa-MSH/metabolismo , Factor de Transcripción Asociado a Microftalmía/genética , Factor de Transcripción Asociado a Microftalmía/metabolismo , Lipopolisacáridos/toxicidad , Melanocitos/metabolismo , Hiperpigmentación/tratamiento farmacológico , Hiperpigmentación/metabolismo , Monofenol Monooxigenasa/metabolismo , Línea Celular Tumoral
14.
J Biomater Sci Polym Ed ; 35(7): 967-988, 2024 05.
Artículo en Inglés | MEDLINE | ID: mdl-38340313

RESUMEN

The possibility of controlling periorbital hyperpigmentation disorders is one of the most important research goals in cosmetic preparations. In the current investigation, 1% vitamin K (Vit K) was incorporated into a Chitosan/alginate hydrogel which aimed to increase the dermal delivery and anti-pigmentation effect. The Vit K-hydrogel was evaluated using several different tests, including volume expansion/contraction analysis, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), ultraviolet (UV) absorbance spectroscopy, and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. Vit K hydrogel's drug release profile showed a steady increase over time. Furthermore, the modified Vit K hydrogel formulations showed no harmful effects in an in vitro cytotoxicity study. The Vit K hydrogel was tested for dermal irritation on Wistar rats, and the hydrogel was found to be non-irritating. Furthermore, Vit K-hydrogel inhibited melanin formation (31.76 ± 1.14%) and was remarkably higher than free Vit K. In addition, Vit K-hydrogel inhibited L-dopa auto-oxidation to a greater extent (94.80 ± 2.41%) in comparison with Vit K solution (73.95 ± 1.62%). Vit K-hydrogel enhanced percutaneous transport of Vit K, according to in vitro percutaneous absorption findings, suggesting that this innovative formulation may provide new therapeutic options for periorbital hyperpigmentation.


Asunto(s)
Alginatos , Quitosano , Hidrogeles , Hiperpigmentación , Ratas Wistar , Quitosano/química , Animales , Alginatos/química , Hidrogeles/química , Hidrogeles/farmacología , Hiperpigmentación/tratamiento farmacológico , Ratas , Liberación de Fármacos , Portadores de Fármacos/química , Vitamina K 1/química , Vitamina K 1/administración & dosificación , Vitamina K 1/farmacología , Melaninas/química , Piel/efectos de los fármacos , Piel/metabolismo , Humanos , Masculino
15.
Trop Med Int Health ; 29(4): 327-333, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38348585

RESUMEN

OBJECTIVES: Cutaneous hyperpigmentation is one of the main adverse effects encountered in patients undergoing leprosy treatment with multidrug therapy (WHO-MDT). This adverse effect has been described as intolerable and capable of contributing to social stigma. The objectives of this study were to quantify the variation in skin colour induced by clofazimine during and after treatment and to assess the related stigma. METHODS: This observational cross-sectional study objectively measured skin colour in 51 patients by reading the individual typology angle (ITA°) with a spectrophotometer, followed by the application of the Stigma Scale of the Explanatory Model Interview Catalogue (EMIC). RESULTS: Skin hyperpigmentation was observed in 100% of the individuals. They showed more negative ITA° values in lesion areas than non-lesion areas, particularly in sun-exposed regions. Clofazimine-induced cutaneous hyperpigmentation was not homogeneous and seemed to follow the lesion locations. The mean EMIC score was 18.8 points. CONCLUSION: All patients presented skin hyperpigmentation caused by clofazimine, detectable through spectrophotometry. Hyperpigmentation strongly impacted the social domain, indicating the intersectionality of disease and skin colour stigma, contributing to the social isolation of these patients. Health authorities should consider the negative impact of clofazimine on treatment adherence.


Asunto(s)
Hiperpigmentación , Lepra , Humanos , Clofazimina/efectos adversos , Leprostáticos/efectos adversos , Estudios Transversales , Estigma Social , Quimioterapia Combinada , Lepra/tratamiento farmacológico , Lepra/etiología , Hiperpigmentación/inducido químicamente , Hiperpigmentación/tratamiento farmacológico , Hiperpigmentación/patología
16.
J Cosmet Dermatol ; 23(6): 2145-2155, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38415395

RESUMEN

BACKGROUND: The emulgel, a novel drug delivery system, merges emulsion and gel, offering advantages like enhanced stability, precise control over drug release kinetics, and increased drug absorption compared to emulsions alone. Kojic acid (KA) demonstrates potent inhibition of the tyrosinase enzyme, a crucial player in the melanin synthesis pathway. AIMS: The main objective of this experimental study is to formulate KA within an emulgel framework and assess its stability under various environmental conditions. METHODS: One percent of KA emulgel and 1% simple gel, serving as the control product, were supplemented with varying concentrations of sodium metabisulfite (SMBS) for its antioxidant properties. The formulations were segregated into four groups and subjected to diverse maintenance and stress conditions over a three-month period. Monthly evaluations of physicochemical alterations were conducted, initially employing digital photography, followed by the extraction of KA and subsequent quantification of its concentration through high performance liquid chromatography (HPLC). RESULTS: The best formulations for retaining KA among the prepared ones were the 0.25% SMBS KA emulgel and the 0.1% SMBS KA simple gel, capable of retaining 86% and 76% of the initial KA content under stress conditions, respectively (p < 0.0001). CONCLUSIONS: Regarding to this study, ideal storage condition for KA emulgel and simple gel is in the refrigerator temperatures. Moreover, optimal SMBS concentrations for stability enhancement are 0.25% for emulgel and 0.1% for the simple gel. A significant statistical difference was observed between refrigerated emulgel and simple gel in the retention of KA in the presence of optimum concentration of antioxidants (p < 0.0001).


Asunto(s)
Estabilidad de Medicamentos , Emulsiones , Geles , Pironas , Pironas/administración & dosificación , Pironas/farmacocinética , Pironas/farmacología , Emulsiones/química , Antioxidantes/administración & dosificación , Antioxidantes/farmacología , Hiperpigmentación/tratamiento farmacológico , Humanos , Almacenaje de Medicamentos , Sistemas de Liberación de Medicamentos/métodos , Administración Cutánea , Composición de Medicamentos/métodos , Sulfitos/química , Sulfitos/administración & dosificación , Preparaciones para Aclaramiento de la Piel/administración & dosificación , Preparaciones para Aclaramiento de la Piel/química , Preparaciones para Aclaramiento de la Piel/farmacología
17.
J Cosmet Dermatol ; 23(5): 1726-1733, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38288515

RESUMEN

BACKGROUND: Facial hyperpigmentation can negatively affect an individual's emotional and psychosocial well-being. AIMS: Assess safety and tolerability of a combination of microdermabrasion (DG) procedures using a novel brightening pro-infusion serum (EC-DG) with a targeted at-home treatment regimen in subjects with mild to severe facial hyperpigmentation, including melasma, post-inflammatory hyperpigmentation, and dark spots. PATIENTS/METHODS: This 12-week, open-label study enrolled 18 subjects (Fitzpatrick skin types I-IV) who underwent 6 in-office DG procedures with EC-DG (one procedure administered biweekly), along with daily topical application of a brightening treatment serum and dark spot cream. End points included change from baseline across multiple skin quality attributes and the Melasma Area and Severity Index (MASI), self-assessment questionnaires, and tolerability assessments. RESULTS: The combination treatment was well tolerated and resulted in significant (p ≤ 0.05) improvements from baseline in radiance, tactile roughness, and moisturization/hydration immediately after the first treatment, in MASI score at day 3, and in overall hyperpigmentation at week 4. Most (94.1%) subjects were satisfied with treatment. CONCLUSIONS: DG procedures using EC-DG combined with a targeted at-home skincare regimen are effective and tolerable for treating facial hyperpigmentation across a broad range of skin types.


Asunto(s)
Dermabrasión , Hiperpigmentación , Índice de Severidad de la Enfermedad , Humanos , Femenino , Adulto , Persona de Mediana Edad , Hiperpigmentación/etiología , Hiperpigmentación/tratamiento farmacológico , Dermabrasión/efectos adversos , Dermabrasión/métodos , Dermabrasión/instrumentación , Masculino , Resultado del Tratamiento , Melanosis/terapia , Melanosis/tratamiento farmacológico , Melanosis/diagnóstico , Terapia Combinada/efectos adversos , Terapia Combinada/métodos , Administración Cutánea , Preparaciones para Aclaramiento de la Piel/administración & dosificación , Preparaciones para Aclaramiento de la Piel/efectos adversos , Adulto Joven , Dermatosis Facial/tratamiento farmacológico , Dermatosis Facial/terapia , Cara
18.
J Drugs Dermatol ; 23(1): 1260-1265, 2024 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-38206158

RESUMEN

Dyschromia is the result of irregular facial pigmentation. These cutaneous manifestations can have a significant impact on the quality of life of those affected, especially among females and skin of color. In this randomized, double-blinded, two-cell, single-center, 16-week clinical study, all subjects had moderate to severe (scores 4-9 on the modified Griffiths Scale) hyperpigmentation and skin unevenness of the face such that approximately 20% of subjects had post-inflammatory hyperpigmentation (PIH), 40% had overall mottled hyperpigmentation, and 40% had superficial melasma (Superficial Melasma was determined by Wood's Lamp Assessment). Study participants received either Product A (proprietary new formulation - Cysteamine HSA) or Product B (current marketed product - Cyspera®) and used the test product either in the morning or at night, beginning with every other day application, and then advanced to every day, or as tolerated. The results revealed that both Product A (Cysteamine HSA) and Product B (Cyspera®) had statistically significant improvement in facial hyperpigmentation and skin unevenness, however, Product A (Cysteamine HSA) had better tolerability results for scaling, peeling, burning, stinging, erythema, and dryness, indicating that Product A (Cysteamine HSA) outperformed Product B (Cyspera®). J Drugs Dermatol. 2024;23(1):1260-1265.     doi:10.36849/JDD.7584.


Asunto(s)
Hiperpigmentación , Melanosis , Femenino , Humanos , Cisteamina , Hiperpigmentación/diagnóstico , Hiperpigmentación/tratamiento farmacológico , Melanosis/diagnóstico , Melanosis/tratamiento farmacológico , Calidad de Vida , Piel , Método Doble Ciego
19.
Photodermatol Photoimmunol Photomed ; 40(1): e12945, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38288772

RESUMEN

BACKGROUND: Photoprotection is crucial in preventing the development and progression of various skin diseases. However, patients with skin disease have limited awareness of photoprotection. We evaluated the knowledge and behavioral patterns of photoprotection among Koreans with skin diseases. METHODS: A cross-sectional study was conducted in 11 general hospitals across South Korea. The study population consisted of patients aged 19 years or older who visited dermatologic clinics for their skin diseases. A self-administered questionnaire was used to collect patient demographics, knowledge of photoprotection, and photoprotective habits. RESULTS: In this study, 1173 patients with skin cancer, hyperpigmentary disorders, hypopigmentary disorders, or other skin diseases participated. Females scored significantly higher in knowledge of photoprotection compared to males (mean score 8.4 vs. 7.8; p < .001), and younger patients (<50 years) scored higher than older patients (mean score 8.7 vs. 7.5; p < .001). Males also reported longer sun exposure times and lower usage of photoprotective measures (both p < .001). Patients with skin cancer had the lowest mean knowledge score (7.1 ± 2.6) and were less likely to use photoprotective measures compared to other groups (p < .001). In contrast, patients with hyperpigmentation actively avoided sun exposure compared with other groups (p < 0.001). CONCLUSIONS: Knowledge of photoprotection among Korean patients with skin diseases varied depending on the gender, age, and type of skin disease. Their photoprotective behaviors were inadequate, especially among males and those with skin cancer. These findings emphasize the importance of educating and tailoring photoprotection strategies for patients with skin diseases.


Asunto(s)
Hiperpigmentación , Neoplasias Cutáneas , Masculino , Femenino , Humanos , Rayos Ultravioleta/efectos adversos , Protectores Solares/uso terapéutico , Estudios Transversales , Neoplasias Cutáneas/tratamiento farmacológico , Hábitos , Hiperpigmentación/tratamiento farmacológico
20.
J Cosmet Dermatol ; 23(1): 215-226, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-37381171

RESUMEN

BACKGROUND: The excessive production and accumulation of melanin in the epidermal skin layer can result in skin hyperpigmentation and darkening. Current technologies for regulating melanin are based on inhibiting melanin biosynthesis. They have low effectiveness and safety issues. AIMS: This study aimed to evaluate the potential role of Pediococcus acidilactici PMC48 as a probiotic strain in medicines and cosmetics for skin treatment. MATERIALS AND METHODS: Meanwhile, our research team has reported that P. acidilactici PMC48 strain isolated from sesame leaf kimchi can directly decompose the already synthesized melanin. It can also inhibit melanin biosynthesis. In the present study, we investigated the skin-whitening effect of this strain by arranging an 8-week clinical trial with 22 participants. PMC48 was applied to each participant's artificially UV-induced tanned skin in the clinical trial. Its whitening effect was investigated based on visual evaluation, skin brightness, and melanin index. RESULTS: PMC48 showed a significant effect on the artificially induced pigmented skin. The color intensity of the tanned skin was decreased by 47.647%, and skin brightness was increased by 8.098% after the treatment period. PMC48 also significantly decreased the melanin index by 11.818%, indicating its tyrosinase inhibition capacity. Also, PMC48 improved skin moisture content level by 20.943%. Additionally, 16S rRNA-based amplicon sequencing analysis showed a distinct increase in Lactobacillaceae in the skin by up to 11.2% at the family level without affecting other skin microbiota. Furthermore, it showed no toxicity in in vitro or in vivo analyses. DISCUSSION: These results indicate that P. acidilactici PMC48 is a promising probiotic strain that can be used to develop medicines and cosmetic products to solve skin-related problems. CONCLUSIONS: These results demonstrate that P. acidilactici PMC48 can be a potential probiotic for the cosmetic industry against different skin disorders.


Asunto(s)
Cosméticos , Hiperpigmentación , Pediococcus acidilactici , Humanos , Pediococcus acidilactici/genética , Melaninas , ARN Ribosómico 16S , Piel , Hiperpigmentación/tratamiento farmacológico , Cosméticos/farmacología
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