{"title":"Combinatorial Approach of Polymeric Patches and Solid Microneedles for Improved Transdermal Delivery of Valsartan: A Proof-of-Concept Study","authors":"","doi":"10.33263/briac134.314","DOIUrl":"https://doi.org/10.33263/briac134.314","url":null,"abstract":"Valsartan (VALS) is a first-line therapy for hypertension that belong to the Angiotensin II Receptor Blockers class. VALS is currently administered orally, but it is associated with its low bioavailability. The transdermal route can be an alternative to overcome this problem. However, this route has low permeation caused by the presence of stratum corneum on the skin. The use of permeation enhancers is needed. This study aims to determine the effect of PEG 400 concentration on physical characteristics and release of VALS from transdermal patch preparations and determine the effect of solid microneedles on VALS permeation. The transdermal patch formula was made using HPMC as a base and PEG 400 as a permeation enhancer with various concentrations. The patches were evaluated for their physical appearance, weight uniformity, thickness, moisture content, folding endurance, drug content, in vitro drug release, in vitro drug permeation, and ex vivo permeation test. The results showed that all formulations showed good characteristics for transdermal administration, and the use of PEG 400 could increase the permeation of VALS. Importantly, when combined with solid microneedles, the permeation of VALS was significantly improved. To conclude, the combination of VALS patch transdermal and MNs can increase the amount of VALS permeated.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44250343","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Concomitant Production of α-Amylase and Protease by Bacillus Aerius Strain FPWSHA Isolated from Food Wastes","authors":"","doi":"10.33263/briac134.310","DOIUrl":"https://doi.org/10.33263/briac134.310","url":null,"abstract":"Amylase and protease are enzymes that have potential applications in the food industry, detergent formulation, pharmaceuticals, waste degradation, and the dehairing process in the leather-making industry. In the current study, fifty-six bacteria were isolated from food wastes and screened for amylase and protease production. Biochemical tests and 16S rRNA gene sequencing were used to characterize and identify bacterial strains. Ten potential isolates with high extracellular enzyme secretion were selected. Among ten isolates, strain FPWSHA was ideal for α-amylase and protease production based on its larger hydrolytic zone of clearance under casein and starch agar than other isolates. This strain was identified as Bacillus aerius FPWSHA (Accession number in GenBank: OM258619) and utilized to produce protease and α-amylase enzymes using potato peels powder (PPP) waste as a cheap substrate under submerged fermentation. Under culture conditions optimization, 16.9 U/mL amylase and 12.3 U/mL proteases were achieved within 48 h of fermentation. Bacillus aerius was isolated from food wastes for the first time to produce α-amylase and protease enzymes. In the future, the bacterial strain described here should be improved for hydrolytic enzyme production in commercial and biotechnological applications.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48472373","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Genetic Variants and Biochemical Parameters Associated with the Risk for Venous Thromboembolism in a Romanian Cohort","authors":"","doi":"10.33263/briac134.308","DOIUrl":"https://doi.org/10.33263/briac134.308","url":null,"abstract":"Thrombophilia can be defined as a predisposition to form clots inappropriately. We studied the carrier status for thrombophilia-related genetic variants in a cohort of 237 Romanian patients who were referred to Synevo Romania between January 2021 and April 2021. Two groups of patients consisting of 117 subjects were evaluated for the underlying causes of a VTE (venous thromboembolism) - group A and group B, consisting of 120 patients with no thromboembolic events. All patients were screened for PC, PC, AT-III, FVL, FII, and MTHFR. The presence of thrombophilia was compared between groups. Out of the 117 patients in group A, 113 (96.58 %), revealed at least one of the analyzed mutations, while just 4 (3.41 %) there were no identified mutations; in comparison, the mutation carrier/non-carrier ratio in group B was 104 patients (86.67%) and 16 (13.33%), respectively. The prevalence of FVL and FII mutation in group A, 21/117 (17.94%) heterozygous and 17/117 (14.53%) heterozygous, respectively, was notably higher when compared to 10/120 (8.33%) FVL heterozygous and 6/120 (5%) FII heterozygous in group B (p=0.034 and p=0.0156). The prevalence of inherited natural anticoagulants was comparable between groups with no statistically significant difference (p=0.6592, p= 0.0992, p= 0.6809).","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46675726","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Cryoprotective Effect of Pyrano-[2,3-C]-Pyrazoles on H2O2 Induced Damage in Tetrahymena thermophila","authors":"","doi":"10.33263/briac134.305","DOIUrl":"https://doi.org/10.33263/briac134.305","url":null,"abstract":"Antioxidants are developed to assist the immune system and overcome oxidative stress, break the auto-oxidative chain reaction, quench oxygen singlets (O2-), and inhibit peroxidase formation. The main objective of this study was to search for potent antioxidant supplements to protect our cells against diseases associated with oxidative stress. We chose four pyrano-[2,3-c]-pyrazole derivatives to test their antioxidant properties in vivo using \"Tetrahymena spp\" as a cellular model. Then, we measured the activity of some antioxidant and biochemical biomarkers such as CAT, SOD, GAPDH, SDH, Gr, and MDA. Also, the fragmentation of DNA has been investigated. The current study demonstrated that the three compounds (5a, b, and c) have potent antioxidant activity, characterized by increased activity of some antioxidant enzymes, inhibiting lipid peroxidation and DNA damage. These findings suggest for the first time that Pyrano-[2,3-c]-Pyrazoles is a promising source of synthetic antioxidants that could offer protection against H2O2-induced- stress and provide us with a new challenge to design a library of pharmaceutical compounds with high activity and low toxicity.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44913111","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Review on Computer-Aided Drug Design (CADD) Technique in Drug Discovery Researches and Solvent-Free Synthesis of 3,4-Dihydropyrimidin-2-(1H)-Ones/Thiones Catalyzed by Camphor Sulfonic Acid","authors":"","doi":"10.33263/briac134.303","DOIUrl":"https://doi.org/10.33263/briac134.303","url":null,"abstract":"Combined with various computational and theoretical approaches, computer-aided drug design (CADD) is one of the contemporary approaches to drug discovery. Furthermore, this study briefly assesses the literature on computer-assisted drug design (CADD) techniques used in drug discovery research. An environmentally friendly synthetic route was developed for the convenient Biginelli synthesis of 3,4-dihydropyridine-2-(1H)-ones/thiones when no solvents are involved in the reaction using aromatic derivatives, urea/thiourea, and ethyl/methyl acetoacetate as catalysts in combination with camphor sulfonic acid (CSA). All reactions proceeded rapidly, and good product yields were obtained. Green synthesis in this study has many advantages over conventional synthesis, including a clean and environmentally friendly synthesis, easy operation, the elimination of hazardous organic solvents, a purification step free of chromatography, and the use of a non-corrosive and non-volatile catalyst. Furthermore, the method can be applied to single-tank reactions in a solvent-free environment.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45117319","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Analysis of Distance 2 Topological Models of Alkanes","authors":"","doi":"10.33263/briac134.307","DOIUrl":"https://doi.org/10.33263/briac134.307","url":null,"abstract":"Topological Indices serve as mathematical models for the QSPR/QSAR study, which provides the optimum theoretical analysis for expensive practical drug discovery experiments. In this paper, some of the degree-based topological indices concerning the vertices at distance 2 are obtained for alkane groups. And then, some physiochemical properties of Alkanes are analyzed using linear and double regression models.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44255175","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Quantitative Structure-Property Relationship Analysis on Priority PAHs Using Certain Closed Neighbourhood Topological Indices","authors":"","doi":"10.33263/briac134.306","DOIUrl":"https://doi.org/10.33263/briac134.306","url":null,"abstract":"Molecular structures and their physicochemical properties are related harmoniously. Having the potential uses in our everyday life, graph theory has become one of the most iconic and discussed areas of applied mathematics. Chemical graph theory (CGT) is a branch of graph theory that incorporates chemical aspects. The topological index (TI) is a well-defined graph-theoretical tool that offers a mathematical relationship with molecular structures and also characterizes their topology. TI has real-time applications such as isomer discrimination, drug design, QSPR, and QSAR studies in various domains of chemistry, including nanotechnology and biochemistry. Herein, seven closed neighborhood TIs are investigated. Using QSPR regression analysis, the chemical signature of the indices in predicting the physicochemical properties of priority polycyclic aromatic hydrocarbons (PAHs) is explored. These Tis exhibited a strong correlation with certain properties of priority PAHs. Certain statistical aspects of these indices are discussed, and the significant results have also been represented graphically.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42612536","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Interactive Performance of Wheat Nitrogen Fertilization and Inoculation with Growth-Promoting Bacteria","authors":"","doi":"10.33263/briac134.304","DOIUrl":"https://doi.org/10.33263/briac134.304","url":null,"abstract":"The exploitation of plant growth-promoting rhizobacteria (PGPR) emerges as an important strategy for fixing atmospheric nitrogen (N) and making it available to plants. Correspondingly, the purpose of this study was to evaluate the inoculation with Azospirillum brasilense via foliar with distinct N doses (40, 20, and 0 kg/ha) for different wheat cultivars (Sossego, Toruk, and Quartzo). The experiment was conducted during the 2020 harvest at the State University of Rio Grande do Sul, Cachoeira do Sul, Brazil. A completely randomized design (CRD) in a 3x6 factorial scheme with four replications was applied. Yield components and grain yield were established. Furthermore, the physicochemical characterization of wheat siliqua biomass was executed based on subcritical water hydrolysis (SWH). Gluten and mass analysis was established. Appropriately, the grain yield was up to 3197.05 kg/ ha for the Sossego cultivar with the N dose of 40 kg/ ha. Up to 0.84 g reducing sugars/ 100 g wheat siliqua was obtained based on the SWH. Finally, this study promoted N management as a key factor in increasing grain yield. This scenario reports the importance of the association of PGPRs as a fundamental promoter of N for plants to express their maximum potential.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45979045","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Molecular Docking, ADMET Prediction, and Quantum Computational on 2-Methoxy Benzoyl Hydrazone Compounds as Potential Antileishmanial Inhibitors","authors":"","doi":"10.33263/briac134.302","DOIUrl":"https://doi.org/10.33263/briac134.302","url":null,"abstract":"Leishmaniasis is a neglected disease that affects about one million people a year worldwide and is present in over 90 countries. This illness is a serious public health issue since it can result in mutilation, incapacity, and even death. The drugs currently used for treatment are highly toxic, ineffective, expensive, and may cause antiparasitic resistance. A series of twenty-five 2-methoxy benzoyl hydrazone derivatives have recently been identified as promising antileishmanial inhibitors and was addressed using a molecular docking approach. All docked compounds interacted well within the active pocket of the receptor. Compounds M12, M15, M16, and M20 show a good binding energy value of -9.40, -8.90, -9.00, and -9.20 Kcal/mol, respectively, compared to pentamidine (-8.20 Kcal/mol), used as reference drug. These molecules also present many types and numbers of interactions with the studied receptor. The studied molecules were evaluated for their pharmacokinetic properties using ADMET prediction. They showed good bioavailability, particularly the molecules M12, M15, and M16 which were found to be non-toxic. Quantum calculations using the DFT approach were performed on the four selected compounds to determine the most electrophilic and nucleophilic of them. These findings would be very helpful in the search for new antileishmanial inhibitors.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44844109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Investigation of the Antibiofilm Activity of Some Spices and Medicinal Plants Essential Oils","authors":"","doi":"10.33263/briac134.301","DOIUrl":"https://doi.org/10.33263/briac134.301","url":null,"abstract":"Biofilms are the structure microbial that attach to different surfaces and enclave microorganisms in a matrix composed, protecting them from harsh conditions, including immune effectors and antibiotics. Therefore, this study aimed to assess the anti-biofilm activity of lavender, cloves, eucalyptus, rosemary, thyme, and oregano commercial essential oils, known for their biocidal properties against Gram-positive and Gram-negative ESKAPE isolates, exhibiting multiple drug resistance. The most efficient proved to be the oregano, thyme, and clove essential oils, which exhibited the lowest minimal biofilm eradication concentrations values against all bacterial species. Although lavender, eucalyptus, and rosemary had a weaker effect than the first three oils, they have also inhibited biofilm development at concentrations low enough to be considered effective. This experimental approach may open new perspectives for developing efficient strategies to combat the emergent threat of antibiotic resistance and to control the formation of microbial biofilms, being also a valuable source of bioactive compounds and new anti-biofilm drugs.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45234414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}