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JPMA. the Journal of the Pakistan... Oct 2023
Topics: Humans; Adapalene; Acne Vulgaris; Anti-Inflammatory Agents, Non-Steroidal; Melanoma; Gels; Treatment Outcome; Dermatologic Agents
PubMed: 37876097
DOI: 10.47391/JPMA.8438 -
Drug Safety Mar 2024In refining drug safety signals, defining the object of study is crucial. While research has explored the effect of different event definitions, drug definition is often...
INTRODUCTION
In refining drug safety signals, defining the object of study is crucial. While research has explored the effect of different event definitions, drug definition is often overlooked. The US FDA Adverse Event Reporting System (FAERS) records drug names as free text, necessitating mapping to active ingredients. Although pre-mapped databases exist, the subjectivity and lack of transparency of the mapping process lead to a loss of control over the object of study.
OBJECTIVE
We implemented the DiAna dictionary, systematically mapping individual free-text instances to their corresponding active ingredients and linking them to the World Health Organization Anatomical Therapeutic Chemical (WHO-ATC) classification.
METHODS
We retrieved all drug names reported to the FAERS (2004-December 2022). Using existing vocabularies and string editing, we automatically mapped free text to ingredients. We manually revised the mapping and linked it to the ATC classification.
RESULTS
We retrieved 18,151,842 reports, with 74,143,411 drug entries. We manually checked the first 14,832 terms, up to terms occurring over 200 times (96.88% of total drug entries), to 6282 unique active ingredients. Automatic unchecked translations extend the standardization to 346,854 terms (98.94%). The DiAna dictionary showed a higher sensitivity compared with RxNorm alone, particularly for specific drugs (e.g., rimegepant, adapalene, drospirenone, umeclidinium). The most prominent drug classes in the FAERS were immunomodulating (37.40%) and neurologic drugs (29.19%).
CONCLUSION
The DiAna dictionary, as a dynamic open-source tool, provides transparency and flexibility, enabling researchers to actively shape drug definitions during the mapping phase. This empowerment enhances accuracy, reproducibility, and interpretability of results.
Topics: United States; Humans; Adverse Drug Reaction Reporting Systems; Drug-Related Side Effects and Adverse Reactions; Reproducibility of Results; Software; United States Food and Drug Administration
PubMed: 38175395
DOI: 10.1007/s40264-023-01391-4 -
Theranostics 2024Spinal cord injury (SCI) results in neural tissue damage. However, the limited regenerative capacity of adult mammals' axons upon SCI leads to persistent neurological...
Exosomes derived from CD271CD56 bone marrow mesenchymal stem cell subpopoulation identified by single-cell RNA sequencing promote axon regeneration after spinal cord injury.
Spinal cord injury (SCI) results in neural tissue damage. However, the limited regenerative capacity of adult mammals' axons upon SCI leads to persistent neurological dysfunction. Thus, exploring the pathways that can enhance axon regeneration in injured spinal cord is of great significance. Through the utilization of single-cell RNA sequencing in this research, a distinct subpopulation of bone marrow mesenchymal stem cells (BMSCs) that exhibits the capacity to facilitate axon regeneration has been discovered. Subsequently, the CD271CD56 BMSCs subpopulation was isolated using flow cytometry, and the exosomes derived from this subpopulation (CD271CD56 BMSC-Exos) were extracted and incorporated into a hydrogel to create a sustained release system. The aim was to investigate the therapeutic effects of CD271CD56 BMSC-Exos and elucidate the underlying mechanisms involved in promoting axon regeneration and neural function recovery. The findings indicate that CD271CD56 BMSC-Exos share similar physical and chemical properties with conventional exosomes. Importantly, in an SCI model, in situ implantation of CD271CD56 BMSC-Exos hydrogel resulted in increased expression of NF and synaptophysin, markers associated with axon regeneration and synapse formation, respectively. This intervention also contributed to improved neural function recovery. In vitro experiments demonstrated that CD271CD56 BMSC-Exos treatment significantly enhanced axon extension distance and increased the number of branches in dorsal root ganglion axons. Moreover, further investigation into the molecular mechanisms underlying CD271CD56 BMSC-Exos-mediated axon regeneration revealed the crucial involvement of the miR-431-3p/RGMA axis. In summary, the implantation of CD271CD56 BMSC-Exos hydrogel presents a promising and effective therapeutic approach for SCI.
Topics: Adult; Animals; Humans; Axons; Exosomes; Adapalene; Nerve Regeneration; Mesenchymal Stem Cells; Spinal Cord Injuries; Hydrogels; Sequence Analysis, RNA; Mammals
PubMed: 38169566
DOI: 10.7150/thno.89008 -
Indian Journal of Dermatology Jul 2014A combination of topical retinoid and antibacterial therapy is often advocated for acne to enhance therapeutic efficacy.
Efficacy and tolerability of topical fixed combination of nadifloxacin 1% and adapalene 0.1% in the treatment of mild to moderate acne vulgaris in Indian patients: a multicenter, open-labelled, prospective study.
BACKGROUND
A combination of topical retinoid and antibacterial therapy is often advocated for acne to enhance therapeutic efficacy.
AIMS
A preliminary study to evaluate the efficacy and tolerability of a topical fixed combination of nadifloxacin (1%) and adapalene (0.1%) in the treatment of mild to moderate acne in Indian patients.
MATERIALS AND METHODS
This was an open-labeled, phase 3 non-randomized, non-comparative study conducted at five centers (Ahmedabad, Nagpur, Thane, Bangalore, and Mumbai) across India. Of 119 enrolled patients with mild to moderate acne, 117 patients were evaluated at the end of the study for efficacy parameters. A fixed combination of nadifloxacin (1%) and adapalene (0.1%) topical gel was applied at the affected area once at night for a period of 8 weeks. Reduction in the total, inflammatory and non-inflammatory lesion counts from the baseline, investigator global assessment (IGA) and reduction in the severity of acne as per combined acne severity classification were the primary efficacy variables measured at 2 weeks, 4 weeks, and 8 weeks.
RESULTS
Overall, 98.3% patients showed a statistically significant progressive reduction in non-inflammatory lesion counts, inflammatory lesion counts, and total lesion counts over the study duration. By the end of 8 weeks, 75% of the patients had their global assessment scores approaching to normal healthy skin score. The adverse events were mild to moderate in severity.
CONCLUSION
This preliminary study shows that a fixed combination of 1% nadifloxacin and 0.1% adapalene topical gel could be an effective and well-tolerated option for the treatment of mild to moderate acne vulgaris. However, further well-controlled, randomized and comparative evaluation of this combination is necessary.
PubMed: 25071260
DOI: 10.4103/0019-5154.135492 -
Molecular Diversity Feb 2023Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been significantly paralyzing the societies, economies and health care systems around the globe. The...
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been significantly paralyzing the societies, economies and health care systems around the globe. The mutations on the genome of SARS-CoV-2 led to the emergence of new variants, some of which are classified as "variant of concern" due to their increased transmissibility and better viral fitness. The Omicron variant, as the latest variant of concern, dominated the current COVID-19 cases all around the world. Unlike the previous variants of concern, the Omicron variant has 15 mutations on the receptor-binding domain of spike protein and the changes in the key amino acid residues of S protein can enhance the binding ability of the virus to hACE2, resulting in a significant increase in the infectivity of the Omicron variant. Therefore, there is still an urgent need for treatment and prevention of variants of concern, particularly for the Omicron variant. In this study, an in silico drug repurposing was conducted through the molecular docking of 2890 FDA-approved drugs against the mutant S protein of SARS-CoV-2 for Omicron variant. We discovered promising drug candidates for the inhibition of alarming Omicron variant such as quinestrol, adapalene, tamibarotene, and dihydrotachysterol. The stability of ligands complexed with the mutant S protein was confirmed using MD simulations. The lead compounds were further evaluated for their potential use and side effects based on the current literature. Particularly, adapalene, dihydrotachysterol, levocabastine and bexarotene came into prominence due to their non-interference with the normal physiological processes. Therefore, this study suggests that these approved drugs can be considered as drug candidates for further in vitro and in vivo studies to develop new treatment options for the Omicron variant of SARS-CoV-2.
Topics: Humans; Antiviral Agents; SARS-CoV-2; Dihydrotachysterol; Adapalene; COVID-19; Drug Repositioning; Molecular Docking Simulation
PubMed: 35507211
DOI: 10.1007/s11030-022-10440-6 -
American Family Physician Jan 2000Acne is a common problem in adolescents and young adults. The disorder is caused by abnormal desquamation of follicular epithelium that results in obstruction of the... (Review)
Review
Acne is a common problem in adolescents and young adults. The disorder is caused by abnormal desquamation of follicular epithelium that results in obstruction of the pilosebaceous canal. This obstruction leads to the formation of comedones, which can become inflamed because of overgrowth of Propionibacterium acnes. Topical retinoids such as tretinoin or adapalene are effective in many patients with comedonal acne. Patients with inflammatory lesions benefit from treatment with benzoyl peroxide, azelaic acid or topical antibiotics. Frequently, the use of comedonal and antibacterial agents is required.
Topics: Acne Vulgaris; Administration, Topical; Adolescent; Adult; Anti-Bacterial Agents; Anti-Infective Agents, Local; Benzoyl Peroxide; Dermatologic Agents; Dicarboxylic Acids; Drug Therapy, Combination; Humans; Keratolytic Agents; Patient Education as Topic; Pharmaceutical Vehicles; Retinoids; Salicylic Acid; Sulfacetamide
PubMed: 10670502
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Apr 2023Acne vulgaris is a complex skin disease involving infection by Cutibacterium acnes, inflammation, and hyperkeratinization. We evaluated the activity of the retinoid...
Acne vulgaris is a complex skin disease involving infection by Cutibacterium acnes, inflammation, and hyperkeratinization. We evaluated the activity of the retinoid 6-[3-(adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid (CD437) and 16 other retinoid analogs as potential anti- compounds and found that CD437 displayed the highest antimicrobial activity with an MIC against (ATCC 6919 and HM-513) of 1 μg/mL. CD437 demonstrated an MBC of 2 μg/mL compared to up to 64 μg/mL for the retinoid adapalene and up to 16 μg/mL for tetracycline, which are commonly used clinically to treat acne. Membrane permeability assays demonstrated that exposure of ATCC 6919 to CD437 damaged the integrity of ATCC 6919 bacterial membranes, and this finding was confirmed with scanning electron microscopy. Additionally, CD437 downregulated the expression of ATCC 6919 virulence factors, including the genes encoding Christie-Atkins-Munch-Petersen factor 1 (CAMP1), CAMP2, glycerol-ester hydrolase B (GehB), sialidase B, and neuraminidase. In a mouse skin infection model of ATCC 6919, topical treatment with CD437 ameliorated skin lesions and reduced the bacterial burden ( < 0.001). In human NHEK primary cells, CD437 reduced the transcriptional levels of the coding genes for inflammatory cytokines (interleukin-1α, ~10-fold; interleukin-6, ~20-fold; interleukin-8, ~30-fold; and tumor necrosis factor-alpha, ~6-fold) and downregulated the transcriptional levels of (~10-fold), (~4-fold), and (~2-fold), indicating that CD437 can diminish inflammation and hyperkeratinization. In summary, CD437 deserves further attention for its dual function as a potential acne therapeutic that potentially acts on both the pathogen and the host.
Topics: Mice; Animals; Humans; Retinoids; Acne Vulgaris; Cytokines; Anti-Bacterial Agents; Inflammation; Propionibacterium acnes
PubMed: 36943064
DOI: 10.1128/aac.01679-22 -
Indian Journal of Dermatology,... 2012Acne vulgaris is a very common skin disease with a significant detrimental effect on the quality of life of the patients. (Randomized Controlled Trial)
Randomized Controlled Trial
Efficacy and safety of a nano-emulsion gel formulation of adapalene 0.1% and clindamycin 1% combination in acne vulgaris: a randomized, open label, active-controlled, multicentric, phase IV clinical trial.
BACKGROUND
Acne vulgaris is a very common skin disease with a significant detrimental effect on the quality of life of the patients.
AIMS
To assess the comparative efficacy and safety of a nano-emulsion gel formulation of adapalene and clindamycin combination with its conventional formulation in the treatment of acne vulgaris of the face. It was a prospective, randomized, open label, active-controlled, multicentric, clinical trial.
METHODS
Eligible patients suffering from acne vulgaris of the face were randomized to receive once-daily treatment with a nano-emulsion gel or conventional gel formulation of adapalene 0.1% and clindamycin (as phosphate) 1% combination for 12 weeks. Total, inflammatory and noninflammatory lesion counts, with grading of acne severity were carried out on a monthly basis. Safety assessments were done to determine the comparative local and systemic tolerability. Two-tailed significance testing was carried out with appropriate statistical tests, and P-values < 0.05 were considered as significant.
RESULTS
209/212 patients enrolled in the study were eligible for efficacy and safety assessments in both nano-emulsion gel (118/119 patients) and conventional gel (91/93 patients) groups. Significantly better reductions in total (79.7% vs. 62.7%), inflammatory (88.7% vs. 71.4%) and noninflammatory (74.9% vs. 58.4%) lesions were reported with the nano-emulsion gel as compared to the conventional gel (P < 0.001 for all). Mean acne severity score also reduced significantly more with the nano-emulsion formulation (1.9 ± 0.9 vs. 1.4 ± 1.0; P < 0.001) than the comparator. Significantly lower incidence and lesser intensity of adverse events like local irritation (4.2% vs. 19.8%; P < 0.05) and erythema (0.8% vs. 9.9%; P < 0.05) were recorded with the nano-emulsion gel.
CONCLUSIONS
The nano-emulsion gel formulation of adapalene and clindamycin combination appears to be more efficacious and better tolerated than the conventional formulation for the treatment of acne vulgaris in Indian patients. Further studies can elucidate the comparative treatment benefits of this nano-emulsion gel formulation.
Topics: Acne Vulgaris; Adapalene; Adolescent; Adult; Anti-Bacterial Agents; Clindamycin; Dermatologic Agents; Drug Combinations; Emulsions; Female; Gels; Humans; Male; Nanotechnology; Naphthalenes; Treatment Outcome; Young Adult
PubMed: 22772617
DOI: 10.4103/0378-6323.98077 -
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