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The Journal of Investigative Dermatology Nov 1977Corticosteroid-induced dermal atrophy has been studied in the rat using daily application of ethanolic solutions to small areas of flank skin. After 12 days of...
Corticosteroid-induced dermal atrophy has been studied in the rat using daily application of ethanolic solutions to small areas of flank skin. After 12 days of treatment, the degree of atrophy was determined by comparing the weights of skin plugs (16 mm diameter) taken from the treated areas with contralaterally paired control areas. Doses can be adjusted so that systemic effects are minimized and only local effects are observed. Hydrocortisone, hydrocortisone butyrate, dexamethasone, betamethasone, desonide and triamcinolone acetonide all produce atrophy in the rat, and the degree of thinning is dose dependent. Potencies in the dermal atrophy assay compare directly with topical anti-inflammatory potencies in the rat, and the presence of fluorine in the steroid molecule is not a determining factor in the production of atrophy.
Topics: Administration, Topical; Animals; Anti-Inflammatory Agents; Atrophy; Betamethasone; Desonide; Dexamethasone; Hydrocortisone; Male; Rats; Skin; Triamcinolone Acetonide
PubMed: 908845
DOI: 10.1111/1523-1747.ep12511301 -
BioMed Research International 2022A topological index is a real number derived from the structure of a chemical graph. It is helpful to determine the physicochemical and biological properties of a wide...
A topological index is a real number derived from the structure of a chemical graph. It is helpful to determine the physicochemical and biological properties of a wide range of drugs, and it better reflects the theoretical properties of organic compounds. This is accomplished using degree-based topological indices. Vitiligo is a common, acquired skin pigmentation disorder that significantly impacts the quality of life. It frequently embodies a therapeutic challenge, resulting in interest in alternative treatments based on vitamin and herbal supplements. In this article, azathioprine, clobetasol, desonide, hydrocortisone valerate, and other drugs utilized to cure vitiligo have discoursed, and the goal of QSPR revision is to determine the mathematical relationship between properties under investigation (e.g., polarity and enthalpy) and diverse descriptors associated with the drugs' molecule. The QSPR model will help to predict physical properties. In this study, topological indices (TIs) imposed on said drugs were found to have a good correlation with physicochemical properties in this course. Finally, this work can be helpful to design and synthesize new vitiligo treatments and other disease drugs.
Topics: Humans; Vitiligo; Quantitative Structure-Activity Relationship; Quality of Life; Autoimmune Diseases; Restraint, Physical
PubMed: 36425334
DOI: 10.1155/2022/6045066 -
Se Pu = Chinese Journal of... Dec 2023Glucocorticoids, which are a class of steroidal hormones secreted by the adrenal cortex, have significant anti-inflammatory, immunosuppressive, and anti-allergic...
Glucocorticoids, which are a class of steroidal hormones secreted by the adrenal cortex, have significant anti-inflammatory, immunosuppressive, and anti-allergic effects. Thus, these compounds are widely used in clinical practice. However, the long-term use of cosmetics containing glucocorticoids can lead to serious consequences, such as hormone-dependent dermatitis, hypertension, and other serious injuries. The Safety and Technical Specification for Cosmetics (2015 edition) and Regulation (EC) No. 1223/2009 of the European Parliament and Council on cosmetic products list glucocorticoids as prohibited raw materials. According to the National Medical Products Administration, reports on the illegal addition of glucocorticoids to cosmetics by manufacturers have increased in recent years. Therefore, establishing high-throughput screening methods to ensure the quality and safety of cosmetics is imperative. In this study, a comprehensive analytical method based on ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was developed for the rapid screening of 83 glucocorticoids in cosmetics. A series of conditions were optimized using three matrices that are commonly used in cosmetics: water, lotion, and cream (o/w-type). Four mobile-phase systems and three chromatographic columns were then optimized to achieve the best separation effects. Various MS parameters, such as the capillary voltages, cone voltages, desolvation gas flow rates, and collision energies of the ion pairs of the target compounds, were also optimized. Furthermore, pretreatment was essential for glucocorticoid determination owing to the complex matrix effects of cosmetics. The analytes were divided into two groups, with lg =4 as the limit, to compare the effects of the extraction solvent on recoveries. The extraction recoveries of target analytes with six extraction methods, namely, extraction with acetonitrile, extraction with acetone, extraction with ethyl acetate, dispersion in saturated sodium chloride solution followed by extraction with acetonitrile, dispersion in saturated sodium chloride solution followed by extraction with acetone, and dispersion in saturated sodium chloride solution followed by extraction with ethyl acetate, were compared. The recoveries from QuEChERS and solid-phase extraction (SPE) purification were also compared. Based on the experimental results, the final sample pretreatment method included acetonitrile vortex dispersion, ultrasonic extraction, and sample loading after filtration. The 83 target compounds were separated on a Thermo Accucore PFP column (100 mm×2.1 mm, 2.6 μm) with 0.1% (v/v) acetic acid in acetonitrile and 0.1% (v/v) acetic acid in water as the mobile phases. The analytes were determined by dynamic multiple-reaction monitoring (MRM) in electrospray positive ionization mode (ESI) and quantified using the external standard method. Matrix standard curves were used to reduce matrix effects. The calibration curves of the 83 target compounds were linear in the mass concentration range of 2-200 μg/L (>0.995). At three levels of addition, the recoveries were 74.5%-112.4%, and the relative standard deviations (RSDs, =6) were 0.8%-9.9%. The limits of detection (LODs, ≥3) were 0.001-0.023 μg/g, and the limits of quantification (LOQs, ≥10) were 0.002-0.076 μg/g. The developed method was used to detect glucocorticoids in 41 cosmetic samples. Fluocinolone acetonide, beclomethasone dipropionate, desonide 21-acetate, and desonide were detected in four samples. The content range of glucocorticoids in the positive samples was 0.53-634.27 μg/g. Notably, desonide 21-acetate, which is not included in the scope of the statutory detection method, was detected in two batches of samples. In conclusion, the proposed method is simple, sensitive, reliable, and suitable for the high-throughput analysis of the 83 glucocorticoids in cosmetics with different matrices. This method could provide reliable technical support for the daily supervision of cosmetics and serve as a supplement to current glucocorticoid standards.
Topics: Glucocorticoids; Acetone; Chromatography, High Pressure Liquid; Chromatography, Liquid; Desonide; Sodium Chloride; Tandem Mass Spectrometry; Acetic Acid; Acetonitriles; Water; Cosmetics; Solid Phase Extraction
PubMed: 38093538
DOI: 10.3724/SP.J.1123.2023.04009 -
Chemical & Pharmaceutical Bulletin Jun 2006The photochemistry of anti-inflammatory drug desonide (De, 1) was studied in aerobic as well as in anaerobic condition with different irradiation wavelengths (254, 310...
The photochemistry of anti-inflammatory drug desonide (De, 1) was studied in aerobic as well as in anaerobic condition with different irradiation wavelengths (254, 310 nm) in acetonitrile and 2-propanol. All photoproducts obtained were isolated and characterized on the basis of IR, (1)H-, (13)C-NMR spectroscopy and elemental analysis study. The products were: 11beta,21-dihydroxy-16alpha,17alpha-(1-methylethylidenedioxy)-1,5-cyclopregn-3-ene-2,20-dione 2 (254 nm), 11beta-hydroxy-16alpha,17alpha-(1-methylethylidenedioxy)androsta-1,4-diene-3-one 3 (310 nm/2-propanol), 17beta-hydroperoxy-11beta-hydroxy-16alpha,17alpha-(1-methylethylidenedioxy)androsta-1,4-diene-3-one 4 (310 nm/O(2)/2-propanol). Cyclohexadienone moiety in ring A and keto group at C(17) were found to be deeply modified by UV light therefore, loss of biological activity both during storage and in vivo can not be ruled out.
Topics: 2-Propanol; Acetonitriles; Animals; Anti-Inflammatory Agents, Non-Steroidal; Desonide; Drug Stability; Molecular Structure; Oxygen; Photochemistry
PubMed: 16755054
DOI: 10.1248/cpb.54.836 -
Contact Dermatitis Aug 2020
Topics: Anti-Inflammatory Agents; Betacoronavirus; COVID-19; Coronavirus Infections; Dermatitis, Allergic Contact; Desonide; Facial Dermatoses; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Isocyanates; Loratadine; Masks; Pandemics; Patch Tests; Pneumonia, Viral; SARS-CoV-2; Young Adult
PubMed: 32390190
DOI: 10.1111/cod.13599 -
Annales de Dermatologie Et de... 2000Systemic side effects of local corticosteroid therapy may occur when treating chronic inflammatory dermatoses in children. We compared the effect of micronized desonide... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
[Comparative study of efficacy and effect on plasma cortisol levels of micronised desonide cream 0.1 p. 100 versus betamethasone dipropionate cream 0.05 p. 100 In the treatment of childhood atopic dermatitis].
OBJECTIVE
Systemic side effects of local corticosteroid therapy may occur when treating chronic inflammatory dermatoses in children. We compared the effect of micronized desonide cream 0.1 p.100 versus betamethasone dipropionate cream 0.5 p.100.
PATIENTS AND METHODS
A randomized double-blind trial was conducted to assess the efficacy of micronized desonide cream 0.1 p.100 (group 1) versus bethamethasone cream dipropionate 0.05 p.100 (group 2) in children treated for atopic dermatitis and to compare their effects on serum cortisol levels 8 hours after administration. Twenty-nine patients, mean age 13.8 months were included (15 in group 1 and 14 in group 2). The creams were applied twice a day from day 1 to 5 then once a day from day 6 to 7 and finally once every two days to day 15.
RESULTS
The two treatments were effective with a decrease in body surface area involved and an improvement in lesion score from day 5 to day 20. Cortisolemia fell off significantly for both treatments between day 0 and day 5 (group 1: Deltad5=-4.74 mg/ml, p=0.01; group 2: Deltad5=-13.06 mg/ml, p<0.0001), only for group 2 between day 0 and day 20 (Deltad20=-7.38 mg/ml, p=0.02) and to a lesser degree between day 0 and day 30 (Deltad30=-3.18 mg/ml, p=0.06). The decrease was greater in group 2 than in group 1 on day 5 (p=0.01) and to a lesser degree at day 20 (p=0.06).
CONCLUSIONS
Micronized desonide cream 0.1 p.100 has less potential for suppressing the adrenal cortisol axis than betamethasone dipropionate cream 0.05 p.100 while the therapeutic effect on childhood atopic dermatitis is the same.
Topics: Administration, Topical; Anti-Inflammatory Agents; Betamethasone; Child, Preschool; Dermatitis, Atopic; Desonide; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Female; Humans; Hydrocortisone; Infant; Male; Ointments; Treatment Outcome
PubMed: 10930856
DOI: No ID Found -
Indian Journal of Dermatology 2020A 50-year-old woman had suffered from chronic pruritic plaque located on right retroauricular area for around 16 years, which was diagnosed as lichen simplex chronicus....
A 50-year-old woman had suffered from chronic pruritic plaque located on right retroauricular area for around 16 years, which was diagnosed as lichen simplex chronicus. Seventeen years ago, patient had multiple scalded areas distributed throughout the body and underwent autologous skin flap transplantation for the right retroauricular wound. After the wound healed, patient started experiencing paresthesia continuously on the skin grafted area and could not resist scratching. To our knowledge, this is the first reported case of lichen simplex chronicus secondary to scald injury and skin flap transplantation. We successfully treated this patient with dyclonine hydrochloride cream 1% and desonide cream 0.05%.
PubMed: 32029940
DOI: 10.4103/ijd.IJD_88_19 -
Dermatology and Therapy Jun 2018Medical device repairing emollient creams (MDRECs) are designed to repair and protect the skin barrier. In this study, we examined the added clinical benefit and...
Efficacy and Tolerability of a Medical Device Repairing Emollient Cream Associated with a Topical Corticosteroid in Adults with Atopic Dermatitis: An Open-label, Intra-individual Randomized Controlled Study.
INTRODUCTION
Medical device repairing emollient creams (MDRECs) are designed to repair and protect the skin barrier. In this study, we examined the added clinical benefit and tolerability of a MDREC when used in association with a moderately potent topical corticosteroid (TCS) for adults with atopic dermatitis (AD).
METHODS
This was an intra-individual randomized controlled trial in adults with moderate to severe AD (EudraCT no. 2014-002,194-10). Symmetrical lesions on each arm of the subjects were randomized to treatment for 10 days with twice-daily TCS (desonide) cream alone or with combined TCS + MDREC. Subjects were then included in a following 2-week maintenance phase if the AD on at least one test area had sufficiently improved so that the treatment was no longer needed. During the maintenance phase, treatment with the TCS cream was stopped, but twice-daily application of the MDREC was continued on the same test area previously assigned to receive it. The primary outcome measure was the change in local Scoring Atopic Dermatitis (SCORAD) index between day 1 and 3 based on investigators' assessment. Secondary measures of lesion severity included changes in the local patient-oriented SCORAD index, pruritus intensity according to subjects' assessments, and global assessments by subjects and investigators.
RESULTS
The study included 54 subjects. The change in investigator-observed local SCORAD index between day 1 and 3 was - 14.4% with TCS alone and - 24.5% for TCS + MDREC (p = 0.0005). Between baseline and the end of the treatment phase, all secondary measures of lesion severity decreased more with the combined TCS + MDREC treatment than with the TCS cream alone. The MDREC also reduced the relapse of AD lesions during the maintenance phase. Tolerability was very good, and the product was well accepted by subjects.
CONCLUSION
These results support using the MDREC in association with TCS during AD flares and as a maintenance therapy after treatment with TCS has stopped.
FUNDING
Laboratoires Dermatologiques Ducray, Pierre Fabre.
PubMed: 29511936
DOI: 10.1007/s13555-018-0228-3 -
Canadian Medical Association Journal Jan 1973Desonide, a non-fluorinated topical corticosteroid (16-alpha-hydroxyprednisolone acetonide), is compared with its fluorinated analogue, triamcinolone acetonide, as to... (Comparative Study)
Comparative Study
Desonide, a non-fluorinated topical corticosteroid (16-alpha-hydroxyprednisolone acetonide), is compared with its fluorinated analogue, triamcinolone acetonide, as to vasoconstriction ability and epidermal penetration rate. Clinical effectiveness of desonide is further assessed by means of a double-blind paired comparison with an accepted potent fluorinated steroid, betamethasone 17-valerate. It is demonstrated that fluorination of the steroid molecule is not necessary to achieve potent topical anti-inflammatory effect. Vasoconstriction and epidermal penetration are not enhanced by fluorination in the drugs studied.
Topics: Abdomen; Administration, Topical; Adult; Anti-Inflammatory Agents; Betamethasone; Cadaver; Dermatitis, Atopic; Dermatitis, Contact; Humans; Middle Aged; Prednisolone; Psoriasis; Skin Absorption; Triamcinolone Acetonide; Vascular Resistance
PubMed: 4682636
DOI: No ID Found -
Indian Journal of Microbiology Dec 2017Present study demonstrated the expression of cloned RSE163 keratinase gene and in silico binding affinities of deduced protein with psoriasis topical drugs for systemic...
Present study demonstrated the expression of cloned RSE163 keratinase gene and in silico binding affinities of deduced protein with psoriasis topical drugs for systemic absorption and permeation through skin. The gene expressed in showed significantly higher keratinase activity 450 ± 10.43 U representing 1342 bp nucleotides encoding 447 amino acids with molecular weight of 46 kDa. The modeled structure was validated using ramachandran's plot showing 305 residues (84.3%) in most favoured region. Docking studies using extra precision (XP) method of Glide showed optimum binding affinities with the drugs Acitretin (- 39.62 kcal/mol), Clobetasol propionate (- 37.90 kcal/mol), Fluticasone (- 38.53 kcal/mol), Desonide (- 32.23 kcal/mol), Anthralin (- 38.04 kcal/mol), Calcipotreine (- 21.55 kcal/mol) and Mometasone (- 28.40 kcal/mol) in comparison to other psoriasis drugs. The results can further be correlated with in vitro enzymatic experiments using keratinase as an effective drug mediator through skin to serve the unmet need of industries.
PubMed: 29151650
DOI: 10.1007/s12088-017-0677-x