scholarly journals Comparative evaluation of hydrophilic bases for improved delivery of Benzoic acid and Salicylic acid in antimicrobial ointment

2021 ◽  
Vol 22 (1) ◽  
pp. 74-87
Author(s):  
A.O. Oyedele ◽  
E.O. Akinkunmi

Background: Benzoic acid (BA) and salicylic acid (SA) combined are used as choice topical treatment for fungal and bacterial infections but their delivery is affected by ointment vehicle, among other factors. With aim to achieve improved release and antimicrobial activity in ointment formulation of these medicaments through selection of more efficient vehicle(s), this study comparatively evaluated prospective alternatives to thecompendium-specified base for delivery potential and relevant physical properties.Methodology: Water-sorption capacity, rheological characteristics and heat-tolerance limits of six hydrophilic bases [hydrous ointment (HO), hydrous sheabutter (HS), neat sheabutter (NS), lanolin anhydrous (LA), lanolin hydrous (LH), and emulsifying ointment (EO)] and their ointment products containing 1, 2, 3, or 6% w/w of BA or SA were determined. Drug delivery propensity of the products was evaluated by agar diffusion colorimetric assay, while their antimicrobial activities were determined by hole-in-plate agar diffusion assay against selected type organisms (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Candida pseudotropicalis).Results: BA was released in relatively larger quantity and demonstrated greater antimicrobial activity than SA in most bases. The released quantities of each medicament correlated directly with concentration and antimicrobial activities. The rates and extents of drug release followed a similar trend in different vehicles namely, HO > HS > NS ≥ EO > LA ≈ LH. Water number of base, ointment preparation method, viscosity, or heat-tolerance showed no influence on drug release or antimicrobial activity.Conclusion: HO and HS are better vehicles for delivery of BA and SA in ointment than EO which is the prototypical base. Keywords: Benzoic acid, Salicylic acid, Antimicrobial activity, Ointment base, Delivery factors French Title: Évaluation comparative des bases hydrophiles pour une meilleure administration d'acide benzoïque et d'acide salicylique dans une pommade antimicrobienne Contexte: L'acide benzoïque (BA) et l'acide salicylique (SA) combinés sont utilisés comme traitement topique de choix pour les infections fongiques et bactériennes, mais leur administration est affectée par le véhicule de la pommade, entre autres facteurs. Dans le but d'améliorer la libération et l'activité antimicrobienne dans la  formulation de pommade de ces médicaments grâce à la sélection de véhicules plus efficaces, cette étude a évalué comparativement des alternatives potentielles à la base spécifiée dans le compendium pour le potentiel d'administration et les propriétés physiques pertinentes.Méthodologie: Capacité de sorption de l'eau, caractéristiques rhéologiques et limites de tolérance à la chaleur de six bases hydrophiles [pommade hydratée (HO), beurre de karité hydraté (HS), beurre de karité pur (NS), lanoline anhydre (LA), lanoline hydratée (LH), et onguent émulsifiant (EO)] et leurs produits de pommade contenant 1, 2, 3 ou 6% p/p de BA ou SA ont été déterminés. La propension à l'administration de médicaments des produits a été évaluée par un essai colorimétrique de diffusion sur gélose, tandis que leurs activités antimicrobiennes ont été déterminées par un essai de diffusion sur gélose en plaque contre des organismes de type sélectionné (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans et Candida pseudotropicalis).Résultats: BA a été libéré en quantité relativement plus grande et a démontré une plus grande activité antimicrobienne que SA dans la plupart des bases. Les quantités libérées de chaque médicament étaient directement liées à la concentration et aux activités antimicrobiennes. Les taux et l'étendue de la libération de médicaments ont suivi une tendance similaire dans différents véhicules, à savoir HO> HS> NS ≥ EO> LA ≈ LH. Le nombre d'eau de base, la méthode de préparation de la pommade, la viscosité ou la tolérance à la chaleur n'ont montré aucune influence sur la libération du médicament ou l'activité antimicrobienne.Conclusion: HO et HS sont de meilleurs véhicules pour la livraison de BA et SA en onguent que EO qui est la base prototypique. Mots-clés: acide benzoïque, acide salicylique, activité antimicrobienne, base de pommade, facteurs de délivrance  

2012 ◽  
Vol 61 (3) ◽  
pp. 223-225
Author(s):  
MUHAMMAD JAWWAD SAIF ◽  
MOHAMMED ZUBER ◽  
JAMIL ANWAR ◽  
MUNAWAR ALI MUNAWAR

The antimicrobial activity of two new series of bis-piperidinium compounds with alkyl chains of different lengths against bacterial (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis) and fungal strains (Aspergillus flavus, Aspergillus niger, Rhodolorula rubera, Lipomyces lopofera and Candida albicans), are described. Antimicrobial activities of the synthesized compounds were compared to that of dodecyltrimethylammonium chloride. Bis-piperidinium salts possessing 12-16 carbon side chains showed better antimicrobial properties as compared to the standard dodecyltrimethylammonium chloride.


2018 ◽  
Vol 13 (4) ◽  
pp. 1934578X1801300
Author(s):  
Daniyar Sadyrbekov ◽  
Timur Saliev ◽  
Yuri Gatilov ◽  
Ivan Kulakov ◽  
Roza Seidakhmetova ◽  
...  

A cyclopropane derivative of limonene, (1 S, 4 S, 6 R)-7,7-dichloro-4-[(1 S)-2,2-dichloro-1-methylcyclopropyl]-1-methylbicyclo [4.1.0] heptane (compound 2), was synthesized and its structure was determined by NMR and X-ray crystallographic methods. In addition, an antimicrobial activity of the compound against Gram-positive ( Staphylococcus aureus, Bacillus subtilis) and Gram-negative ( Escherichia coli, Pseudomonas aeruginosa) bacterial strains was also scrutinized.


Medicina ◽  
2008 ◽  
Vol 44 (12) ◽  
pp. 977 ◽  
Author(s):  
Alvydas Pavilonis ◽  
Algirdas Baranauskas ◽  
Ligita Puidokaitė ◽  
Žaneta Maželienė ◽  
Arūnas Savickas ◽  
...  

Objective. To evaluate the antimicrobial activity of soft and purified propolis extracts. Study object and methods. Antimicrobial activity of soft and purified propolis extracts was determined with reference cultures of Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 33499, Pseudomonas aeruginosa ATCC 27853, Proteus mirabilis ATCC 12459, Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 8035, and fungus Candida albicans ATCC 60193. Microbiological tests were performed under aseptic conditions. Minimum inhibitory concentration (MIC) – the highest dilution of preparation (the lowest concentration of preparation) that suppresses growth of reference microorganisms – was determined. Results. Concentration of phenolic compounds in soft propolis extract that possesses antimicrobial activity against gram-positive (Staphylococcus aureus, Enterococcus faecalis) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis) is 0.587±0.054 mg and 0.587±0.054–0.394±0.022 mg (P>0.05) and in purified propolis extract – 0.427±0.044 mg and 0.256±0.02 mg (P>0.05). Klebsiella pneumoniae is most resistant to soft propolis extract when the concentration of phenolic compounds is 1.119± 0.152 mg and to purified propolis extract when the concentration of phenolic compounds is 1.013±0.189 mg (P>0.05). Spore-forming Bacillus subtilis bacteria are more sensitive to soft and purified propolis extracts when the concentration of phenolic compounds is 0.134±0.002 mg and 0.075±0.025 mg, respectively, and Bacillus cereus – when the concentration is 0.394±0.022 mg and 0.256±0.02 mg (P>0.05). Sensitivity of fungus Candida albicans to soft and purified propolis extracts is the same as Bacillus subtilis. Encapsulated bacterium Klebsiella pneumoniae is most resistant to antimicrobial action of soft and purified propolis extracts as compared with gram-positive Staphylococcus aureus and Enterococcus faecalis bacteria (P<0.05), gram-negative Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis (P<0.05), sporeforming Bacillus subtilis and Bacillus cereus bacteria (P<0.05), and fungus Candida albicans (P<0.05). There is no statistically significant difference between antimicrobial effect of soft propolis extract and purified propolis extract on gram-positive bacteria, gram-negative bacteria, spore-forming bacteria, encapsulated bacteria, and Candida fungus. Conclusions. Soft and purified propolis extracts possess antimicrobial activity. They could be recommended as natural preservatives in the manufacture of pharmaceutical products.


2012 ◽  
Vol 65 (4) ◽  
pp. 343 ◽  
Author(s):  
Mei Zhang ◽  
Dong-Mei Xian ◽  
Hai-Hua Li ◽  
Ji-Cai Zhang ◽  
Zhong-Lu You

A series of new halo-substituted aroylhydrazones have been prepared and structurally characterized by elemental analysis, 1H NMR, 13C NMR, and IR spectra, and single crystal X-ray diffraction. The compounds were evaluated for their antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence) and antifungal (Candida albicans and Aspergillus niger) activities by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method. Among the tested compounds, N′-(2-chloro-5-nitrobenzylidene)-2-fluorobenzohydrazide showed the most effective antimicrobial activity with minimum inhibitory concentration values of 0.82, 2.5, 1.7, 15.2, and 37.5 μg mL–1 against B. subtilis, S. aureus, E. coli, P. fluorescence, and C. albicans, respectively. The biological assay indicated that the presence of the electron-withdrawing groups in the aroylhydrazones improved their antimicrobial activities.


Medicina ◽  
2011 ◽  
Vol 47 (3) ◽  
pp. 24 ◽  
Author(s):  
Vilma Jurkštienė ◽  
Alvydas Pavilonis ◽  
Daiva Garšvienė ◽  
Algirdas Juozulynas ◽  
Laimutė Samsonienė ◽  
...  

The aim of the study was to determine antimicrobial activity of rhaponticum and shrubby cinquefoil extracts. Material and Methods. Ethanol extract from the leaves of rhaponticum (Rhaponticum carthamoides D.C. Iljin) and shrubby cinquefoil (Potentilla fruticosa L.) was produced at the Department of Food Technology, Kaunas University of Technology. The antimicrobial activity of the viscous extract or rhaponticum and shrubby cinquefoil was evaluated using standard microorganism cultures (bacteria Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 33499, Pseudomonas aeruginosa ATCC 27853, Proteus mirabilis ATCC 12459, Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 8035 and fungi Candida albicans ATCC 60193). The minimum inhibitory concentration (MIC) of the examined preparations was determined. Results. Both studied preparations – rhaponticum (Rhaponticum carthamoides D.C. Iljin) and shrubby cinquefoil (Potentilla fruticosa L.) – demonstrated similar antimicrobial activity. The highest sensitivity to the studied preparations was observed in microbes with eukaryotic cell structure: Candida albicans, which is a fungus, and a spore-forming prokaryotic bacterium, Bacillus cereus. The highest resistance was observed in Escherichia coli and Klebsiella pneumoniae. Conclusions. The studied preparations – viscous extracts of rhaponticum and shrubby cinquefoil – are substances with antimicrobial activity against gram-positive (Staphylococcus aureus and Enterococcus faecalis) and gram-negative (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis) bacteria, spore-forming bacteria (Bacillus subtilis and Bacillus cereus), and fungi (Candida albicans).


2003 ◽  
Vol 58 (11-12) ◽  
pp. 850-854 ◽  
Author(s):  
Ayşen Özdemir Türk ◽  
Meral Yılmaz ◽  
Merih Kıvanç ◽  
Hayrettin Türk

Abstract In this study, the antimicrobial activity of the acetone, diethyl ether and ethanol extracts of the lichen Cetraria aculeata has been investigated. The extracts were tested against twelve bacteria and eight fungi and found active against Escherichia coli, Staphylococcus aureus, Aeromonas hydrophila, Proteus vulgaris, Streptococcus faecalis, Bacillus cereus, Bacillus subtilis, Pseudomonas aeruginosa, Listeria monocytogenes. No antimicrobial activity against the fungi was detected. It was determined that only one substance in the extracts has antimicrobial activity and it was characterized as protolichesterinic acid. The MICs of the extracts and protolichesterinic acid were also determined.


2021 ◽  
Vol 47 (3) ◽  
pp. 1296-1302
Author(s):  
Oluwaseyi B. Ovonramwen ◽  
Bodunde J. Owolabi ◽  
Abiodun Falodun

A new 1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide was synthesized from methyl-1-[(5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl]pyrrolidine-2-carboxylate and ethylamine. The compound methyl-1-[(5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl]pyrrolidine-2-carboxylate was synthesized from methyl pyrrolidine-2-carboxylate and 5-chloro-4-chlorosulfonyl-1-ethyl-2-methyl-imidazole. The compounds were characterized based on FTIR, 1H, 13C NMR, and DEPT 135 analysis. Antimicrobial activities of the 1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide against Gram-positive (methicillin-susceptible Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, and Bacillus subtilis), Gram-negative (Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae), and Candida albicans were carried out using the standard microbiological method. The newly synthesized 1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide had no activities against the tested organisms. Keywords:    1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide; methyl-1-[(5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl]pyrrolidine-2-carboxylate; L-proline; ethylamine.


Author(s):  
Powar Priyatama V ◽  
Powar Trupti A

The growing phenomenon of antibiotic resistance, particularly to pathogenic microorganisms, in current medicine, has directed the concern of scientists for finding novel antimicrobial agents from plant origin with negligible side effect. The present study was aimed to phytochemical investigation and antimicrobial activity of seed extract of Datura stramonium in sequentially with different organic solvents. For this, antimicrobial properties were tested against bacteria Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumonia and Bacillus subtilis by cup plate method. Among the tested bacterial Klebsiella pneumoniae was the most inhibited majorly with the chloroform extract. Datura stramonium chloroform seed extract produced maximum zone of inhibition 26 mm against Klebsiella pneumoniae and 12 mm against Bacillus subtilis and 13 mm against Escherichia coli. Datura Stramonium methanol seed extract produced maximum zone of inhibition 27 mm against Pseudomonas aeruginosa and 15 mm against Bacillus subtilis, 14 mm against Staphylococcus aureus and 19 mm against Escherichia coli. Datura stramonium petroleum ether seed extract produced 16 mm zone of inhibition against Escherichia coli. Datura stramonium aqueous seed extract exhibits 24 mm zone of inhibition against Bacillus subtilis. All the experienced solvent extracts showed potential antimicrobial activity Index against various tested microorganisms. Owning to the results, it can be concluded that the extracts of the Datura stramonium can be used to design different herbal antimicrobial agents.


2021 ◽  
Vol 68 (3) ◽  
pp. 541-547
Author(s):  
Fu-Ming Wang ◽  
Li-Jie Li ◽  
Guo-Wei Zang ◽  
Tong-Tong Deng ◽  
Zhong-Lu You

A series of five new fluoro-substituted aroylhydrazones were prepared and structurally characterized by elemental analysis, IR, UV-Vis and 1H NMR spectroscopy, as well as single crystal X-ray diffraction. The compounds were evaluated for their antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence) and antifungal (Candida albicans and Aspergillus niger) activities by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method. The biological assay indicated that the presence of the electron-withdrawing groups in the aroylhydrazones improved their antimicrobial activities.


2006 ◽  
Vol 61 (1-2) ◽  
pp. 47-51 ◽  
Author(s):  
Demet Cansaran ◽  
Demet Çetin ◽  
M. Gökhan Halıcı ◽  
Orhan Atakol

Abstract Three species of lichens, Rhizoplaca chrysoleuca (Sm.) Zopf, Rhizoplaca melanopthalma (DC.) Leuckert & Poelt and Rhizoplaca peltata Ramonds Leuckert, were collected from middle Anatolia, Erciyes Mountain (Kayseri) in Turkey. Their usnic acid amounts were determined by HPLC in acetone extracts. In addition, antimicrobial activities of these extracts were determined against Escherichia coli (ATCC 35218), Enterococcus faecalis (RSKK 508), Proteus mirabilis (Pasteur Ens. 235), Staphylococcus aureus, Bacillus subtilis, Bacillus megaterium and Pseudomonas aeruginosa. It was shown that, as the usnic acid amount increased, the antimicrobial activities increased too. The usnic acid contents of Rhizoplaca species varied between 0.19-4.0% dry weight


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