Evaluation of effectiveness of combined use of COC and topical preparation containing azelaic acid for acne

The article presents the results of evaluating the effectiveness of the combined use of combined oral contraceptives (COC) and Skinoren cream in severe papular-pustular and moderate nodular-cystic acne.Material and methods. Patients of the first group (n = 11) used COC and an external antibacterial drug two times a day for the treatment of acne. Patients of the second group (n = 12) used COC and an external drug containing azelaic acid (Skinoren) for the treatment of acne two times a day. The duration of follow-up was 6 months. The efficiency assessment was carried out taking into account the dynamics of the indicators of the IGA (Investors Global Assessment) scale. The Manchester Scar Scale (MSS) was used to assess the effectiveness of post-acne correction. In addition, the effectiveness was evaluated based on the results of the mexametry.Results. When evaluating IGA in the comparison groups in patients with severe papulopustular acne and moderate nodular cystic acne, comparable efficacy was noted, but the best results were recorded in the COC + Skinoren group (p < 0.05). No effect and deterioration of the condition were observed in any group. When assessing MSS, the most pronounced changes were observed in patients of group 2, where the combination of COC + Skinoren was used. So, in group 1, the severity of scars decreased by 42.3 %, in group 2 by 48.2 % (p < 0.05). The evaluation of the results of the mexametry showed a more pronounced decrease in the amount of pigment in patients from group 2. When studying the results of the severity of erythema, the dynamics similar to the severity of the pigment was obtained. The best result was registered in group 2 (COC + Skinoren) (p < 0.05).Conclusions. The combined use of COC and Skinoren cream for severe papular-pustular and moderate nodular-cystic acne has proven to be an effective method both in relation to the number of inflammatory and retention elements, and in relation to hyperpigmentation.

Azelaic Acid Esters as Pluripotent Immunomodulatory Molecules: Nutritional Supplements or Drugs

Azelaic acid and its esters, the azelates, occur naturally in organisms ranging from plants to humans. We have shown that diethyl azelate (DEA) exhibits a broad range of immunomodulatory activities in vitro and in vivo, and mitigates insulin resistance. To further investigate the therapeutic utility of DEA, we evaluated its mutagenicity in Salmonella typhimurium strains, examined metabolism of DEA in rat, dog, monkey and human primary hepatocytes and in human saliva, determined pharmacokinetics of DEA after an oral dose in rats, and queried its physicochemical properties for drug-like characteristics. DEA was not mutagenic in bacterial strains ± rat liver metabolic activation system S-9. It was chemically unstable in hepatocyte culture medium with a half-life of <1 h and was depleted by the hepatocytes in <5 min, suggesting rapid hepatic metabolism. DEA was also quickly degraded by human saliva in vitro. After an oral administration of DEA to rats, the di- and monoester were undetectable in plasma while the levels of azelaic acid increased over time, reached maximum at <2 h, and declined rapidly thereafter. The observed pharmacological properties of DEA suggest that it has value both as a drug or a nutritional supplement.

Comparative Study of Combination of Oral Tranexamic Acid with Modified Kligman’s Formula Versus Oral Tranexamic Acid with Azelaic Acid 15% in the Treatment of Melasma

Background: Melasma refers to acquired hyper-pigmentary condition effecting skin. Owing to its multifactorial causation and chronicity, there is an increased need for new multimodality therapies to treat melasma more effectively and to prevent the side effects seen with the conventional modalities of treatment. Objectives: Compare efficacy of combining oral Tranexamic Acid and Azelaic Acid 15% with that of Oral Tranexamic Acid (TA) and Modified Kligman’s Formula. Also, to record any adverse effects of combining these agents. Methods: Patients having Melasma who will be coming to Dermatology OPD, AVBRH, Sawangi, Wardha, will be enrolled after considering the various inclusion and exclusion criteria. A detailed history will be asked, which will be followed by a cutaneous examination that includes the calculation of MASI (Melasma Area and Severity Index). One Group (A) - participants will receive - Oral 500 mg Tranexamic acid OD plus Modified Kligman’s Formula (fluocinolone acetonide 0.01%, tretinoin 0.05%, and hydroquinone 2%) cream one time at night only. Second Group (B)- participants will receive - Oral 500 mg Tranexamic Acid OD plus Azelaic Acid 15% gel once daily at night only. Both groups will also receive Broad-spectrum sunscreen SPF-30 daily (3 hourly). Patients will be called for regular follow up at 4 weeks and 8 weeks (for early results). Clinical photos will be clicked at every follow-up visit and MASI score shall be doocumented. Expected Results: To analyze efficacy of combining Oral TA along with Azelaic Acid 15% and if it provides better results, we can avoid the undesirable side effects that are seen on prescribing the Modified Klingman’s Formula, in Melasma patients. Conclusion: This study will help us in analyzing efficacy of combining Oral TA with Azelaic Acid 15%, therefore will provide a newer treatment modality with lesser side effects and maybe better results than the gold standard- Modified Klingman’s Formula.

The Abnormal Metabolites in Tongue Coating of Chronic Gastritis Patients Reflect the Changes in Indexes of Gastroscopic Observation and Gastric Mucosal Pathology

ObjectiveIn this study, we analyzed the correlation between different metabolites in the tongue coating of patients with chronic gastritis, gastroscopy and pathological indexes, and discussed the metabolic mechanism at different pathological stages in the development of chronic gastritis.MethodsWe used GC-TOF-MS and UHPLC-QE-MS metabonomics to detect the distribution of metabolites in the tongue coating of patients with chronic gastritis, and analyzed the correlation between different metabolites in the tongue coating of patients with chronic gastritis and gastroscopy and pathological indexes.ResultsCompared with 50 healthy people, 54 metabolites were upregulated and 47 metabolites were downregulated in 350 patients with chronic gastritis. The main differential metabolites were Lipids and lipid-like molecules, which contain 47 metabolites. The best diagnostic model was composed of 5 metabolites, with an accuracy of 95.4%, a specificity of 87.4% and a sensitivity of 88.0%. These 5 metabolites were 1-methyladenosine, Sphinganine 1-phosphate, 3-Hydroxycapric acid, 4-Ipomeanol, and Nervonic acid. Compared with healthy people, Sphinganine 1-phosphate, 4-Ipomeanol, and Nervonic acid were significantly upregulated in chronic gastritis patients, and 1-methyladenosine and 3-Hydroxycapric acid were significantly downregulated in chronic gastritis patients. After correlation analysis between differential metabolites in tongue coatings and gastroscopic indexes, we found that Trimethylaminoacetone, Sphinganine1-phosphate, alpha-Carboxy-delta-decalactone, and 5,6-Dihydroxyindole were positively correlated with intestinal metaplasia. Conduritol-beta-expoxide, Tetracosanoic acid, Lactosylceramide(d18:1/26:0), Chondrillasterol 3-[glucosyl-(1->4)-glucoside], Azelaic acid, and 1-Methyladenosine were negatively correlated with intestinal metaplasia. Sphinganine1-phosphate, alpha-Carboxy-delta-decalactone, and 5,6-Dihydroxyindole were positively correlated with atrophic. Octadecanol, conduritol-beta-expoxide, Tetracosanoic acid, Smilanippin A, Lactosylceramide(d18:1/26:0), Chondrillasterol 3-[glucosyl-(1->4)-glucoside], and Azelaic acid were negatively correlated with atrophic. 6-deoxyglucitol was negatively correlated with bile reflux, methylmaleic acid, 4-methylcatechol, and 2,4-dichloro-1-(2-chloroethenyl)-benzene were negatively correlated with Hp, 3-benzoyloxy-11-oxo-12-ursen-28-oic acid was negatively correlated with gastric mucosal erosion. From the change trend of different metabolites in different pathological stages, we found that the content of conduritol-beta-expoxide decreased significantly in mild atrophic compared with moderate atrophic and the content of conduritol-beta-expoxide decreased significantly in mild intestinal metaplasia compared with moderate intestinal metaplasia.ConclusionsWe found that Lipids and lipid-like molecules were the main abnormal metabolites in patients with chronic gastritis. Among them, Sphinganine 1-phosphate, which was significantly positively correlated with the aggravation of atrophic and intestinal metaplasia, could be used as one of the diagnostic model markers for chronic gastritis. Additionally, the amount of conduritol-beta-expoxide significantly decreased with the aggravation of atrophic and intestinal metaplasia. We believe that these differential markers in tongue coating may help us to establish a noninvasive and convenient auxiliary detection method for gastritis and gastric precancerous lesion in the future.

Azelaic acid and Melaleuca alternifolia essential oil co-loaded vesicular carrier for combinational therapy of acne

Aim: Azelaic acid (AzA), a comedolytic, antibacterial, anti-inflammatory anti-melanogenic agent, prescribed against acne vulgaris is safe on skin. Its combination with another widely used anti-acne agent, tea tree oil (EO) whose delivery is limited by volatility, instability and lipophilicity constraints was attempted. Method: Solvent injection was used to prepare AzA-EO integrated ethosomes. Result: Ethosomes were transformed into carbopol hydrogel, which exhibited pseudo-plastic properties with appreciable firmness, work of shear, stickiness and work of adhesion. The hydrogel showed better permeation and retention characteristics vis-a-vis commercial formulation (AzidermTM), when evaluated in Wistar rat skin. Further, ethosome hydrogel composite was better tolerated with no side effects. Conclusion: The findings suggests that the aforementioned strategy could be a potential treatment used for acne management.

Azelaic Acid: A Bio-Based Building Block for Biodegradable Polymers

Azelaic acid is a dicarboxylic acid containing nine C atoms, industrially obtained from oleic acid. Besides its important properties and pharmacological applications, as an individual compound, azelaic acid has proved to be a valuable bio-based monomer for the synthesis of biodegradable and sustainable polymers, plasticizers and lubricants. This review discusses the studies and the state of the art in the field of the production of azelaic acid from oleic acid, the chemical and enzymatic synthesis of bio-based oligo and polyester and their properties, including biodegradability and biocompostability.

Hydrogel composite containing azelaic acid and tea tree essential oil as a therapeutic strategy for Propionibacterium and testosterone-induced acne

Azelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (−1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris. Graphical abstract