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Zhongguo Dang Dai Er Ke Za Zhi =... Mar 2024To investigate the effects of different concentrations of adapalene on the morphology and functions of neuroblastoma cell line SH-SY5Y, as well as its role in inducing...
OBJECTIVES
To investigate the effects of different concentrations of adapalene on the morphology and functions of neuroblastoma cell line SH-SY5Y, as well as its role in inducing cell differentiation and apoptosis.
METHODS
SH-SY5Y cells were divided into control group, low concentration (0.1 μM and 1 μM) adapalene groups, and high concentration (10 μM) adapalene group. Time-lapse microscopy was used to observe the morphological changes of SH-SY5Y cells. Immunofluorescence staining was performed to detect the expression of neuronal specific marker βIII-tubulin and mature neuronal marker neurofilament heavy polypeptide (NFH). Multi-electrode array was used to record the electrophysiological features of SH-SY5Y cells. Cell apoptosis was evaluated using a cell apoptosis detection kit.
RESULTS
Low concentrations of adapalene promoted the formation of neurite outgrowth in SH-SY5Y cells, with the neurites interconnected to form a network. Spontaneous discharge activity was observed in SH-SY5Y cells treated with low concentrations of adapalene. Compared to the control group, the expression of βIII-tubulin and NFH increased in the 1 μM adapalene group, while the level of cell apoptosis increased in the high concentration adapalene group (<0.05).
CONCLUSIONS
Low concentrations of adapalene can induce differentiation of SH-SY5Y cells into mature functional neurons, while high concentrations of adapalene can induce apoptosis in SH-SY5Y cells.
Topics: Humans; Tubulin; Neuroblastoma; Neurons; Cell Differentiation; Apoptosis; Cell Line, Tumor
PubMed: 38557381
DOI: 10.7499/j.issn.1008-8830.2310100 -
CMAJ : Canadian Medical Association... Dec 2012
Topics: Adapalene; Adult; Carcinoma, Squamous Cell; Dermatologic Agents; Facial Dermatoses; Humans; Male; Mouth Neoplasms; Naphthalenes; Radiotherapy
PubMed: 22690005
DOI: 10.1503/cmaj.112098 -
JAAD International Mar 2021Real-life data on topical treatments in daily practice in patients with moderate acne are poorly characterized.
BACKGROUND
Real-life data on topical treatments in daily practice in patients with moderate acne are poorly characterized.
OBJECTIVE
To investigate the drug survival of topical treatments administered to patients with moderate acne in a daily practice.
METHODS
Survival analysis was performed on subjects (Belgian university hospital and private practice outpatient dermatology patients) with moderate acne who received topical therapies according to the current published guidelines.
RESULTS
A total of 1160 treatment series (1029 patients) were included, including benzoyl peroxide (BPO, n = 93), azelaic acid (n = 246), adapalene (n = 254), a fixed combination of adapalene 0.1% and BPO 2.5% (A/BPO, n = 264), and a fixed combination of clindamycin 1.2% and tretinoin 0.025% gel (Clin-RA, n = 303). The calculated overall median treatment duration of all drugs was 2 months. The probability of treatment discontinuation after only 3 months was 50%. Overall, the drugs were discontinued for the following reasons: controlled acne (9%), side effects (9%), ineffectiveness (52%), combination of side effects and ineffectiveness (3%), and other reasons (1%). Overall, 27% patients were lost to follow-up.
LIMITATIONS
The post hoc study design and generalizability limit interpretation of the data.
CONCLUSION
Overall, the median treatment duration of topical anti-acne therapies was short (2 months). The main reason for discontinuation was ineffectiveness.
PubMed: 34409359
DOI: 10.1016/j.jdin.2020.12.006 -
Dermatology and Therapy Mar 2017Adapalene 0.1%/benzoyl peroxide 2.5% (0.1% A/BPO) and adapalene 0.3%/BPO 2.5% (0.3% A/BPO) gels are fixed-combination options for the topical treatment of acne. However,...
Fixed-Combination Gels of Adapalene and Benzoyl Peroxide Provide Optimal Percutaneous Absorption Compared to Monad Formulations of These Compounds: Results from Two In Vitro Studies.
INTRODUCTION
Adapalene 0.1%/benzoyl peroxide 2.5% (0.1% A/BPO) and adapalene 0.3%/BPO 2.5% (0.3% A/BPO) gels are fixed-combination options for the topical treatment of acne. However, the active compounds of these combinations are also available as monads, to be used in association or as monotherapy. These two in vitro studies determined the effect of different treatment regimens on the percutaneous absorption of adapalene (0.1% and 0.3%) gels and BPO 2.5% gel in ex vivo human skin.
METHODS
In vitro percutaneous absorption studies were conducted using full-thickness human skin from six donors. Treatment regimens included the application of 0.1% A/BPO, 0.3% A/BPO, or four free-combination regimens of the monads. Skin samples were incubated for 24 h. Concentrations of adapalene and BPO equivalent (BPO-eq) (i.e. benzoic acid after chemical transformation of BPO) were measured using high-performance liquid chromatography. Comparison of regimens was performed using a bioequivalence criterion (estimated ratio bewteen 0.8 and 1.25).
RESULTS
The fixed combination 0.3% A/BPO regimen demonstrated more than three times higher absorption of adapalene versus the fixed-combination 0.1% A/BPO. Based on the bioequivalence acceptance criterion, all four free-combination regimens were different from 0.1% A/BPO and 0.3% A/BPO, with higher adapalene release delivered by the fixed combinations versus the free combinations. For BPO-eq, the results showed that the free-combination regimens where adapalene 0.1% was applied first were different from 0.1% A/BPO, with lower BPO-eq release delivered by these regimens compared to the fixed combination. The regimen adapalene 0.3% for 10 h followed by BPO 2.5% delivered lower BPO-eq release compared to the fixed combination.
CONCLUSION
The fixed-combination A/BPO gels provide optimal percutaneous absorption of the active compounds compared to free combinations of adapalene 0.1%, adapalene 0.3%, and BPO 2.5%. The higher concentration of adapalene in the 0.3% A/BPO gel and the resulting higher absorption may explain higher clinical efficacy.
PubMed: 27900658
DOI: 10.1007/s13555-016-0159-9 -
Scientific Reports Oct 2022CD271 (also referred to as nerve growth factor receptor or p75) is expressed on cancer stem cells in hypopharyngeal cancer (HPC) and regulates cell proliferation....
CD271 (also referred to as nerve growth factor receptor or p75) is expressed on cancer stem cells in hypopharyngeal cancer (HPC) and regulates cell proliferation. Because elevated expression of CD271 increases cancer malignancy and correlates with poor prognosis, CD271 could be a promising therapeutic target; however, little is known about the induction of CD271 expression and especially its promoter activity. In this study, we screened transcription factors and found that RELA (p65), a subunit of nuclear factor kappaB (NF-κB), is critical for CD271 transcription in cancer cells. Specifically, we found that RELA promoted CD271 transcription in squamous cell carcinoma cell lines but not in normal epithelium and neuroblastoma cell lines. Within the CD271 promoter sequence, region + 957 to + 1138 was important for RELA binding, and cells harboring deletions in proximity to the + 1045 region decreased CD271 expression and sphere-formation activity. Additionally, we found that clinical tissue samples showing elevated CD271 expression were enriched in RELA-binding sites and that HPC tissues showed elevated levels of both CD271 and phosphorylated RELA. These data suggested that RELA increases CD271 expression and that inhibition of RELA binding to the CD271 promoter could be an effective therapeutic target.
Topics: Humans; Adapalene; Cell Proliferation; Hypopharyngeal Neoplasms; NF-kappa B; Receptors, Nerve Growth Factor; Transcription Factor RelA
PubMed: 36273237
DOI: 10.1038/s41598-022-22736-6 -
Crystal Growth & Design Jun 2024Lipophilic aggregation using adamantanes is a widely exploited molecular property in medicinal and materials chemistry. Adamantanes are traditionally installed to...
Lipophilic aggregation using adamantanes is a widely exploited molecular property in medicinal and materials chemistry. Adamantanes are traditionally installed to molecular units via covalent bonds. However, the noncovalent installation of adamantanes has been relatively underexplored and presents the potential to bring properties associated with adamantanes to molecules without affecting their intrinsic properties (e.g., pharmacophores). Here, we systematically study a series of adamantanecarboxylic acids with varying substitution levels of methyl groups and their cocrystals with bipyridines. Specifically, single-crystal X-ray diffraction shows that while the directionality of single-component adamantanes is notably sensitive to changes in methyl substitution, hydrogen-bonded cocrystals with bipyridines show consistent and robust packing due to π-stacking predominance. Our observations are supported by Hirshfeld surface and energy framework analyses. The applicability of cocrystal formation of adamantanes bearing carboxylic acids was used to generate the first cocrystals of adapalene, an adamantane-bearing retinoid used for treating acne vulgaris. We envisage our study to inspire noncovalent (i.e., cocrystal) installation of adamantanes to generate lipophilic aggregation in multicomponent systems.
PubMed: 38911135
DOI: 10.1021/acs.cgd.4c00457 -
Clinical, Cosmetic and Investigational... 2019Acne vulgaris is a common and chronic disease that impacts on physical and psychological perceptions. Cosmeceutical products are widely used as adjunct therapy to...
The efficacy of glycolic acid, salicylic acid, gluconolactone, and licochalcone A combined with 0.1% adapalene vs adapalene monotherapy in mild-to-moderate acne vulgaris: a double-blinded within-person comparative study.
BACKGROUND
Acne vulgaris is a common and chronic disease that impacts on physical and psychological perceptions. Cosmeceutical products are widely used as adjunct therapy to standard treatments.
OBJECTIVE
To evaluate the efficacy of cosmeceutical products comprising glycolic acid, salicylic acid, gluconolactone, and licochalcone A as adjunct therapy to adapalene in mild-to-moderate acne vulgaris.
MATERIALS AND METHODS
A 28-day, double-blind, within-person comparative study was conducted with a total of 25 subjects. Each participant received two products, consisting of (1) a cosmeceutical product mixed with 0.1% adapalene, and (2) 0.1% adapalene, and was asked to apply them separately on each hemi-side once nightly for 28 days. The number of acne lesions, severity of acne vulgaris, physician's and patient's global assessment of acne severity, visual analog scale of radiance, skin biophysics, safety assessment, and VISIA camera system were evaluated. The primary efficacy outcome was to compare the reduction of inflammatory lesions between two treatments at day 7 by using non-inferiority comparison.
RESULTS
The mean differences of inflammatory lesions reduction at day 7 between the two groups was 0.391 (90% CI = 0.253-0.530). The differences between two groups fell within our acceptable margin for the 90% CI. The spot score from VISIA showed higher statistically significant improvement in the combination side.
CONCLUSION
The results showed no hindrance of using a cosmeceutical combined with standard treatment. Nevertheless, this cosmeceutical product showed some benefits in reducing complications from acne.
CLINICAL TRIAL REGISTRATION
Thai Clinical Trials Registry (primary site), no. TCTR20171031005.
PubMed: 30858720
DOI: 10.2147/CCID.S193730 -
The Journal of Clinical and Aesthetic... Jul 2016To evaluate the efficacy and safety of adapalene 0.1% benzoyl peroxide 2.5% gel in women aged 25 years or older via subgroup analysis of existing Phase 2 and 3 study...
To evaluate the efficacy and safety of adapalene 0.1% benzoyl peroxide 2.5% gel in women aged 25 years or older via subgroup analysis of existing Phase 2 and 3 study data. Meta-analysis of pooled data from three multicenter, randomized, double-blind, vehicle-controlled, parallel-group, clinical trials compared results of treatment with either adapalene 0.1% benzoyl peroxide 2.5% gel or vehicle gel in adult females and teen-aged females. Efficacy assessments included investigator's global assessment and median percent change in acne lesions. Safety assessments included skin tolerability and adverse events. Two hundred fifty-four adult females and 488 teen-aged females were included in the analyses, and baseline characteristics were comparable between subjects receiving adapalene 0.1% benzoyl peroxide 2.5% or vehicle. Both adult females and teen-aged females in the adapalene 0.1% benzoyl peroxide 2.5% arm were significantly more often rated clear/almost clear compared with those in the vehicle arm at Weeks 8 (=0.016) and 12 (<0.001); at endpoint, success was achieved in 39.2 percent with adapalene 0.1% benzoyl peroxide 2.5% and 18.5 percent with vehicle. Comparison of the amount of difference between active and vehicle reductions in investigator's global assessment showed that efficacy was similar for adult females versus teen-aged females (20.7% vs. 19.9%, respectively). Adapalene 0.1% benzoyl peroxide 2.5% had a rapid onset of action, with statistically significant reductions in all acne lesion types versus vehicle observed by Week 1. Adapalene 0.1% benzoyl peroxide 2.5% was safe and well-tolerated by adult females with a tolerability profile consistent with that seen in teen-aged females. The once-daily fixed-dose combination product adapalene 0.1% benzoyl peroxide 2.5% is an efficacious, safe, and well-tolerated treatment for adult female acne, with a profile similar to that in teen-aged females.
PubMed: 28331557
DOI: No ID Found -
PloS One 2019Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and...
Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, some topical adverse effects such as erythema, dryness, and scaling have been reported with its commercial formula. In this sense, the microencapsulation of this drug using polyesters can circumvent its topical side effects and can lead to the enhancement of drug delivery into sebaceous glands. The goal of this work was to obtain ADAP-loaded poly(ε-caprolactone) (PCL) microparticles prepared by a simple emulsion/solvent evaporation method. Formulations containing 10 and 20% of ADAP were successfully obtained and characterized by morphological, spectroscopic, and thermal studies. Microparticles presented encapsulation efficiency of ADAP above 98% and showed a smooth surface and spherical shape. Fourier transform infrared spectroscopy (FTIR) results presented no drug-polymer chemical bond, and a differential scanning calorimetry (DSC) technique showed a partial amorphization of the drug. ADAP permeation in the Strat-M membrane for transdermal diffusion testing was evaluated by photoacoustic spectroscopy (PAS) in the spectral region between 225 and 400 nm after 15 min and 3 h from the application of ADAP-loaded PCL formulations. PAS was successfully used for investigating the penetration of polymeric microparticles. In addition, microencapsulation decreased the in vitro transmembrane diffusion of ADAP.
Topics: Adapalene; Calorimetry, Differential Scanning; Diffusion; Drug Carriers; Drug Delivery Systems; Emulsions; Membranes, Artificial; Microscopy, Electron, Scanning; Microspheres; Particle Size; Photoacoustic Techniques; Polyesters; Solvents; Spectrophotometry; Spectroscopy, Fourier Transform Infrared; Water
PubMed: 30897170
DOI: 10.1371/journal.pone.0213625 -
Italian Journal of Dermatology and... Feb 2021CD10, CD271 and Nestin, which are proteins associated with tumor-initiating properties and/or progression potential, have not been specifically studied on malignant...
BACKGROUND
CD10, CD271 and Nestin, which are proteins associated with tumor-initiating properties and/or progression potential, have not been specifically studied on malignant melanoma (MM) with cutaneous recurrences.
METHODS
We evaluated the expression of CD10, CD271 and Nestin in 27 tumor samples from 16 patients. These tumor samples corresponded to 6 primary melanomas which developed 11 ITM and 10 primary melanomas without recurrences at 10-year follow-up from specimens obtained from surgical excisions of patients referred to the Unit of Dermatology, Department of Medical-Surgical and Transplant Physiopathology, University of Milan, between 2006 and 2016.
RESULTS
We demonstrated a higher expression of CD271 and Nestin in primary tumors which recurred than control population, Nestin was expressed with significantly higher percentages in primary tumors than recurrences, and CD10 expression was statistically significant correlated with disease-free survival: cases with a lower score recurred lately than cases with higher scores.
CONCLUSIONS
Our preliminary results suggested that CD271 and Nestin can be considered early biomarkers for the development of ITM, Nesting can be useful in differentiating primary MM from cutaneous recurrences and CD10 is associated with a rapid disease progression and may be considered a potential prognostic marker.
Topics: Adapalene; Biomarkers, Tumor; Humans; Melanoma; Neoplasm Recurrence, Local; Neprilysin; Nerve Tissue Proteins; Nestin; Prognosis; Receptors, Nerve Growth Factor; Skin Neoplasms
PubMed: 30251808
DOI: 10.23736/S2784-8671.18.06145-X