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Journal of Drugs in Dermatology : JDD Aug 2019BACKGROUND: Topical corticosteroids are efficacious treatment options for multiple dermatoses. However, ointments and cream corticosteroid vehicles can be cumbersome to... (Review)
Review
BACKGROUND: Topical corticosteroids are efficacious treatment options for multiple dermatoses. However, ointments and cream corticosteroid vehicles can be cumbersome to patients and may act as a barrier to adherence. Foam vehicles may be preferred by some patients. OBJECTIVE: To evaluate the efficacy and safety of topical corticosteroid foams. METHODS: A literature review was conducted using the keywords “clobetasol,” “betamethasone,” “propionate,” “valerate,” “topical,” “foam,” “vehicles,” “desonide,” and “clinical trial.” Thirty-seven articles were chosen. RESULTS: For moderate plaque-type psoriasis, 68% of subjects using clobetasol propionate foam achieved a Physician Static Global Assessment score of 0 or 1 at week 2 compared with 21% in the control group (P<0.0001). For betamethasone valerate (BMV) foam, a 12-week regimen for alopecia areata yielded a mean Investigator Global Assessment score of 2.9 compared with placebo (4.6; P<0.001) and achieved ≥75% hair regrowth in 42.86% of subjects. Furthermore, BMV foam cleared or almost cleared 72% of scalp psoriasis subjects compared with BMV lotion (P≤0.005%). For calcipotriol plus betamethasone dipropionate foam, 38.3% of psoriasis subjects achieved treatment success compared with placebo (22.5%; P<0.001). Desonide 0.05% foam was superior to vehicle foam in pediatric atopic dermatitis subjects. CONCLUSION: Topical corticosteroid foams can be used for a variety of corticosteroid-responsive dermatoses. Topical corticosteroid foams are generally easy to apply and may improve patient adherence and, therefore, clinical outcome in patients who prefer a convenient and less messy topical therapy.
Topics: Administration, Cutaneous; Clinical Trials as Topic; Glucocorticoids; Medication Adherence; Patient Preference; Pharmaceutical Vehicles; Skin Diseases; Treatment Outcome
PubMed: 31424707
DOI: No ID Found -
Current Drug Delivery 2023When administered transdermally, desonide is ineffective due to its poor solubility. As a new transdermal delivery system, nanoemulsion gel has demonstrated significant...
BACKGROUND
When administered transdermally, desonide is ineffective due to its poor solubility. As a new transdermal delivery system, nanoemulsion gel has demonstrated significant advantages for drug delivery over conventional formulations. We have established desonide nanoemulsion gel (DES NE gel) for better transdermal absorption, but its efficacy and safety still need to be evaluated. This study aims to provide additional evidence demonstrating the improved pharmacodynamics and safety of transdermal delivery of Desonide via nanoemulsion gel.
METHODS
Pharmacodynamics and safety of Desonide nanoemulsion gel were evaluated using Desonate as the reference formulation. To assess the difference in curative effect between DES NE gel and Desonate and to ensure safety, atopic dermatitis (AD) models in KM mice were developed using 2,4-dinitrofluorobenzene (DNFB). The degree of ear swelling, ear mass difference, thymus, spleen index, and HE conventional pathology of mice were used as pharmacodynamic evaluation indexes, and the irritation was predicted by the New Zealand rabbit epidermal stimulation assay.
RESULTS
Nanoemulsion gels may facilitate transdermal penetration of drugs by influencing the skin condition. Medium and high doses of DES NE gel significantly ameliorated the inflammation and swelling of the ear caused by dermatitis/eczema in mice. In addition, compared with DES gel, skin irritation extent did not increase.
CONCLUSION
Nanoemulsion gel can be applied to improve the efficacy of drugs with low potency or poor solubility. DES NE gel provides a higher transdermal potential than other delivery systems. In this study, it was found that nanoemulsion gel is a promising percutaneous carrier of DES. DES NE-GEL has a significant curative effect on dermatitis/eczema in a mouse model and is expected to provide a new, efficient, and low toxic preparation for clinical treatment of dermatitis/eczema through the percutaneous system.
Topics: Mice; Animals; Rabbits; Skin Absorption; Skin; Desonide; Administration, Cutaneous; Eczema; Emulsions; Gels
PubMed: 35986531
DOI: 10.2174/1567201819666220819110128 -
Drug Development and Industrial Pharmacy Jan 2016Our group previously reported the photoinstability of some desonide topical commercial formulations under direct exposure to UVA radiation.
CONTEXT
Our group previously reported the photoinstability of some desonide topical commercial formulations under direct exposure to UVA radiation.
OBJECTIVE
This study aimed to prepare and characterize a gel-cream containing desonide, with greater photostability than the commercial gel-cream (C-GC). Benzophenone-3 (BP-3) was used as a photostabilizing agent.
METHODS
The gel-cream developed (D-GC) containing BP-3 at 0.1% was prepared and characterized regarding its pH, drug content, spreadability, viscosity, in vitro drug release and in vitro permeation. The in vivo anti-inflammatory effect was assessed by ear edema measurement, croton oil-induced acute skin inflammation and myeloperoxidase assay.
RESULTS AND DISCUSSION
D-GC presented characteristics compatible with topical application, appropriate drug content and good spreadability, and non-Newtonian behavior with pseudoplastic flow. D-GC showed a good photostability profile, presenting a desonide content of 95.70% after 48 h of exposure to UVA radiation, and stability under room conditions during 60 days. The amount of desonide released from D-GC and C-GC was 57.8 and 51.7 µg/cm, respectively, measured using the vertical Franz cell. The in vitro skin permeation showed that desonide reached the site of action of the topical corticosteroids, from both formulations; however, the desonide amount retained in the dermis was lower with D-GC. The in vivo evaluation of topical anti-inflammatory activity indicated that D-GC presented the same biological effect as C-GC.
CONCLUSION
D-GC represents a promising approach to treat dermatological disorders, since it presented satisfactory physicochemical characteristics, the same biological activity as C-GC and superior photostability, conferred by the addition of BP-3 at 0.1%.
Topics: Animals; Anti-Inflammatory Agents; Benzophenones; Chemistry, Pharmaceutical; Croton Oil; Dermatitis, Contact; Dermatologic Agents; Desonide; Disease Models, Animal; Ear; Gels; Glucocorticoids; Humans; Male; Mice; Skin; Skin Cream; Ultraviolet Rays
PubMed: 25775013
DOI: 10.3109/03639045.2015.1022554 -
American Journal of Clinical Dermatology Apr 2017Facial seborrheic dermatitis (SD), a chronic inflammatory skin condition, can impact quality of life, and relapses can be frequent. Three broad categories of agents are... (Review)
Review
BACKGROUND
Facial seborrheic dermatitis (SD), a chronic inflammatory skin condition, can impact quality of life, and relapses can be frequent. Three broad categories of agents are used to treat SD: antifungal agents, keratolytics, and corticosteroids. Topical therapies are the first line of defense in treating this condition.
OBJECTIVE
Our objective was to critically review the published literature on topical treatments for facial SD.
METHODS
We searched PubMed, Scopus, Clinicaltrials.gov, MEDLINE, Embase, and Cochrane library databases for original clinical studies evaluating topical treatments for SD. We then conducted both a critical analysis of the selected studies by grading the evidence and a qualitative comparison of results among and within studies.
RESULTS
A total of 32 studies were eligible for inclusion, encompassing 18 topical treatments for facial SD. Pimecrolimus, the focus of seven of the 32 eligible studies, was the most commonly studied topical treatment.
CONCLUSION
Promiseb, desonide, mometasone furoate, and pimecrolimus were found to be effective topical treatments for facial SD, as they had the lowest recurrence rate, highest clearance rate, and the lowest severity scores (e.g., erythema, scaling, and pruritus), respectively. Ciclopirox olamine, ketoconazole, lithium (gluconate and succinate), and tacrolimus are also strongly recommended (level A recommendations) topical treatments for facial SD, as they are consistently effective across high-quality trials (randomized controlled trials).
Topics: Administration, Cutaneous; Anti-Inflammatory Agents; Antifungal Agents; Calcineurin Inhibitors; Ciclopirox; Dermatitis, Seborrheic; Dermatologic Agents; Desonide; Facial Dermatoses; Humans; Ketoconazole; Malassezia; Mometasone Furoate; Plant Preparations; Practice Guidelines as Topic; Pyridones; Quality of Life; Randomized Controlled Trials as Topic; Tacrolimus; Treatment Outcome; Vitamins
PubMed: 27804089
DOI: 10.1007/s40257-016-0232-2 -
AAPS PharmSciTech May 2021This research aimed to develop a novel drug delivery system to improve treatment of skin disorders. The system is comprised of a Carbopol 980-based nanoemulgel (NE-gel)...
This research aimed to develop a novel drug delivery system to improve treatment of skin disorders. The system is comprised of a Carbopol 980-based nanoemulgel (NE-gel) containing a desonide (DES; 0.05%, w/w) nanoemulsion (NE), which has a small particle size, high encapsulation efficiency, good thermodynamic stability, good permeation ability, and high skin retention. DES-loaded NE (DES-NE) was prepared by high-pressure homogenization. The developed formulation was characterized by differential scanning calorimetry (DSC), X-ray diffraction, drug release, skin permeation, and drug retention. DES in vitro release and skin permeation studies with different formulations of artificial membrane and rat abdominal skin were performed with the Franz diffusion cell system. Confocal laser scanning microscopy (CLSM) was used to detect the localization and permeation pathways of drugs in the skin. Compared with commercially available gel (CA-gel) and NE, the NE-gel release process conformed to the Higuchi release model (R = 0.9813). NE-gel prolonged the drug release time and allowed for reduced administration dose and frequency. The unit cumulative permeation of NE and NE-gel through the skin for 12 h was 63.13 ± 2.78 and 42.53 ± 2.06 μg/cm, respectively, values significantly higher (p < 0.01) than that of the CA-gel (30.65 ± 1.25 μg/cm) and CA-cream (15.21 ± 0.97 μg/cm). The DES-NE and DES NE-gel skin drug retention was significantly higher than commercially available formulations (p < 0.01). Hence, the prepared NE-gel is a potential vehicle for improved topical DES delivery for better treatment of skin disorders.
Topics: Administration, Topical; Animals; Colloids; Desonide; Drug Delivery Systems; Emulsions; Excipients; Microscopy, Confocal; Nanogels; Particle Size; Rats; Skin; Skin Absorption
PubMed: 34031790
DOI: 10.1208/s12249-021-02035-5 -
AAPS PharmSciTech Oct 2014Desonide is a topical corticoid used in the treatment of skin diseases and is marketed in different pharmaceutical dosage forms. Recently, the poor photostability of a...
Desonide is a topical corticoid used in the treatment of skin diseases and is marketed in different pharmaceutical dosage forms. Recently, the poor photostability of a commercially available hair solution after direct exposure to UVA light was verified. In this study, we investigated the ability of the antioxidants ascorbic acid, butylhydroxyanisole (BHA), butylhydroxytoluene (BHT), α-tocopherol, and the UV filter benzophenone-3 (BP-3) to prevent the photodegradation of desonide in hair solution (desonide 0.1%) and the stability of the proposed formulation under environmental conditions. The tested antioxidants were not able to prevent the photolysis of desonide, whereas the addition of 0.3% BP-3 enhanced the photostability of the drug. After 15 h of direct exposure to UVA radiation, the desonide remaining content in the hair solution with BP-3 was approximately 98%. Higher photostability was also verified under UVC radiation. Additionally, the results indicated that the formulation was stable under accelerated and room temperature conditions for 70 days, corresponding to the total period of the study.
Topics: Antioxidants; Benzophenones; Chemistry, Pharmaceutical; Dermatologic Agents; Desonide; Excipients; Photochemistry; Spectrophotometry, Ultraviolet; Temperature; Ultraviolet Rays
PubMed: 24871554
DOI: 10.1208/s12249-014-0149-0 -
The Medical Letter on Drugs and... Jun 2020
Topics: Administration, Cutaneous; Administration, Oral; Animals; Dermatitis, Atopic; Dermatologic Agents; Humans; Injections
PubMed: 32555122
DOI: No ID Found -
Proceedings of the National Academy of... Mar 2022Identifying inhibitors of pathogenic proteins is the major strategy of targeted drug discoveries. This strategy meets challenges in targeting neurodegenerative disorders...
Identifying inhibitors of pathogenic proteins is the major strategy of targeted drug discoveries. This strategy meets challenges in targeting neurodegenerative disorders such as Huntington’s disease (HD), which is mainly caused by the mutant huntingtin protein (mHTT), an “undruggable” pathogenic protein with unknown functions. We hypothesized that some of the chemical binders of mHTT may change its conformation and/or stability to suppress its downstream toxicity, functioning similarly to an “inhibitor” under a broader definition. We identified 21 potential mHTT selective binders through a small-molecule microarray–based screening. We further tested these compounds using secondary phenotypic screens for their effects on mHTT-induced toxicity and revealed four potential mHTT-binding compounds that may rescue HD-relevant phenotypes. Among them, a Food and Drug Administration–approved drug, desonide, was capable of suppressing mHTT toxicity in HD cellular and animal models by destabilizing mHTT through enhancing its polyubiquitination at the K6 site. Our study reveals the therapeutic potential of desonide for HD treatment and provides the proof of principle for a drug discovery pipeline: target-binder screens followed by phenotypic validation and mechanistic studies.
Topics: Animals; Desonide; Disease Models, Animal; Huntingtin Protein; Huntington Disease; Mice; Mice, Transgenic; Mutation; Protein Stability
PubMed: 35238684
DOI: 10.1073/pnas.2114303119 -
The Journal of Dermatological Treatment Dec 2024Dupilumab is a novel treatment agent for moderate to severe atopic dermatitis (AD) with few adverse effects. Drug-induced psoriasiform lesions are rare. We report a...
Dupilumab is a novel treatment agent for moderate to severe atopic dermatitis (AD) with few adverse effects. Drug-induced psoriasiform lesions are rare. We report a 4-year-old boy with AD who developed pustular psoriasis during treatment with dupilumab. Pustular psoriasis appeared within 1 week of treatment and worsened in the second week. After stopping dupilumab administration, topical corticosteroids (desonide and mometasone furoate creams) and oral desloratadine without relief. Pustular psoriasis was confirmed by pathological examination, and thiamphenicol was administered. After 2 weeks of treatment, the lesions nearly resolved without recurrence in 1-year follow-up. Dupilumab-induced pustular psoriasis is rare in children.
Topics: Humans; Male; Psoriasis; Antibodies, Monoclonal, Humanized; Child, Preschool; Dermatitis, Atopic; Mometasone Furoate; Dermatologic Agents
PubMed: 38839072
DOI: 10.1080/09546634.2024.2333016