• Title/Summary/Keyword: Antifungal drug

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Screening of nanoemulgels for physicochemical stability and antifungal efficacy

  • Andleeb Fatima;Muhammad Naeem Aamir;Shahiq-Uz-Zaman;Masood-Ur-Rehman;Zeeshan Javaid;Keng Wooi Ng;Hina Hussain;Muhammad Asif
    • Advances in nano research
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    • v.16 no.6
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    • pp.593-600
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    • 2024
  • The nanoemulgel was prepared to induce a synergistic effect along with higher efficacy. Nine sets of macroemulsion were made in which liquid paraffin was stabilized by the two non-ionic surfactants, Tween® 80 and Span® 80. Comparative stability analysis of the macroemulsions was used to determine the effective surfactant concentrations that gave the most stable systems (NE 2, NE3, NE4, NE5). High-speed homogenization was then applied. The final formulation was evaluated for globule size and polydispersablity index, physical properties (color, homogeneity, consistency, syneresis), pH, viscosity, spreadability with 200 g and 500 g weight, conductivity, drug content, stability, skin irritation, antifungal efficacy. Zeta size analysis confirmed the nanosize of the droplets in NE2 (284.8 nm), NE3 (79.89 nm), NE4 (194 nm) but not NE5 (632.8 nm), which was outside the nanoemulsion range. The antifungal assay exhibited zone of inhibition for NE3 (43±1.0 mm) and NE4 (42±1.7 mm), a marketed cream (33±1 mm), fluconazole alone (35±1 mm) and terbinafine alone (35.0±1.7 mm). The zone of inhibition of nanoemulgels increased compared with the drugs when used individually and when compared a placebo.

Antiviral Effect of Amphotericin B on Japanese Encephalitis Virus Replication

  • Kim, Hun;Kim, Seong-Jun;Park, Sue-Nie;Oh, Jong-Won
    • Journal of Microbiology and Biotechnology
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    • v.14 no.1
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    • pp.121-127
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    • 2004
  • Amphotericin B (AmB), an amphipathic polyene macrolide, is an antifungal drug produced by Streptomyces nodosus. Recently, AmB has been shown to exert antiviral activity against rubella virus and human immunodeficiency virus by different mechanisms. In this study, we evaluated the antiviral effect of AmB against Japanese encephalitis virus (JEV) and investigated which step of the viral life cycle was inhibited by AmB to understand the mechanism of antiviral action of AmB. AmB reduced both plaque size and number in the infected cells in a dose-dependent manner. In addition, a 200-fold reduction of infectious virus titer was observed by treatment of infected cells with $5\mug/ml$ of AmB. AmB acted at the post virus-infection step, but not during adsorption of virus to host cells. Western blot analysis revealed that the accumulated level of JEV envelope protein dramatically decreased in the infected cells by treatment with $5-10\mug/ml$ of AmB. Our results indicate that AmB inhibits the replication of JEV at the postinfection step by interfering with viral replication and/or by inhibiting the synthesis of viral proteins.

Bioactive Constituents of Marine Sponges of the Genus Spongosorites

  • Bao, Baoquan;Hong, Jongki;Lee, Chong-O.;Cho, Hee Young;Jung, Jee H.
    • Journal of Marine Bioscience and Biotechnology
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    • v.1 no.3
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    • pp.144-155
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    • 2006
  • This report reviews the literatures on chemical constituents of marine sponges of the genus Spongosorites and also highlights our own research. Specific biological activities of the metabolites from these sponges include: cytotoxic, antitumor, antibacterial, antifungal, antiviral, anti-inflammatory, and other pharmacological activities.

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Drug susceptibility of bacteria and M pachydermatis isolated from canine external ear canals (개 외이도에서 분리한 세균 및 M pachydermatis의 약제감수성에 대하여)

  • Kim, Ki-hyang;Choi, Won-phil;Yeo, Sang-geon
    • Korean Journal of Veterinary Research
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    • v.39 no.3
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    • pp.560-565
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    • 1999
  • The present work was conducted to investigate the drug susceptibility of microorganisms isolated from canine external ear canals. Antifungal susceptibility test of M pachydermatis (17 strains) was perfomed by agar dilution method, using 11 antifungal drugs including amphotericin B(A), nystatin(N), pimaricin(P), griseofulvin(G), bifonazole(B), clotrimazole(C), miconazole(M), econazole(E), ketoconazole(K), tolnaftate(T), 5-fluorocytosine(F). All isolates were highly sensitive to K, M, T(geometric mean MIC ; GM $MIC{\leq}0.16{\mu}g/ml$) but they weren't sensitive to P, F and G(GM $MIC{\geq}92.37{\mu}g/ml{\sim}{\geq}128{\mu}g/ml$). Antibacterial susceptibility test against 119 isolates of bacteria was performed by agar dilution method, using 9 antibacterial drugs including erythromycin(ET), chloramphenicol(CP), gentamycin(G), vancomycin(V), ampicillin(AP), amoxacillin(AX), chlortetracycline(CT), ciprofloxacin(CF), enrofloxacin(EF). All isolates of Staphylococcus spp(101 strains) were highly sensitive to EF, CF, G(GM MIC $0.33{\sim}1.47{\mu}g/ml$). In other gram positive cocci(4 strains), they were highly sensitive to EF, CF, V(GM MIC $1{\sim}4.76{\mu}g/ml$) and CT(GM MIC 1 UFL unit/ml). In gram positive rods(13 strains), they were highly sensitive to EF, CF, G(GM $MIC{\leq}0.19{\sim}1{\mu}g/ml$). In Pseudomonas aeruginosa(1 strain), it was highly sensitive to AX, EF, ET, CF(GM MIC $0.06{\sim}1{\mu}g/ml$) and CT(GM MIC 1 UFL unit/ml). All isolates weren't sensitive to AP(GM MIC 16~>$32{\mu}g/ml$).

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Hypericum source of natural antimicrobials

  • Mukherjee, Pulok K.;Wahile, Atul;Ahamed, KFH Nazeer;Rajan, S.
    • Advances in Traditional Medicine
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    • v.3 no.3
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    • pp.111-122
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    • 2003
  • Plants of the genus Hypericum (Family - Hypericaceae) are herbs, shrubs or small trees and are distributed chiefly in the temperate regions of the world. About 400 different species of Hypericum are available throughout the globe and 20 species occur in India, including a few cultivated in gardens. Almost all plants of the genus Hypericum are widely used in folk medicine. Several potent phytoconstituents from different Hypericum species have led to the isolation of antibacterial, antifungal and cytotoxic compounds. With the development of resistance and cross resistance with different microorganisms and the evolution of so many deadly diseases the screening and evaluation of the phytoconstituents so much so the development of varied phytoconstituents for the drug development for these deadly diseases is utmost essential in every aspects. The present review on the antimicrobial use of different Hypericum reports the findings from and extensive literature search on the Hypericum species around the globe that have been assessed for antimicrobial and antiviral activity. An attempt has been made through this review to summarize the information in this aspect in order to highlight the promising species of this genus which are worthy for further investigation as leads for drug development. Over 31 different Hypericum species have been reported to possess such activities with their varied number of phytoconstituents. Sixteen different constituents of six different classes of phytoconstituents have been reported to be present in different varieties of Hypericum, which may be considered responsible for this activity.

Preparation of Micro- and Submicron-Particles of a Poorly Water-Soluble Antifungal Drug Using Supercritical Fluid Process (초임계유체공정을 이용한 난용성 항진균제의 미세입자 제조)

  • Kim, Seok-Yun;Lee, Jung-Min;Won, Byoung- Hyun;Jung, In-Il;Ryu, Jong-Hoon;Lim, Gio-Bin
    • Clean Technology
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    • v.16 no.2
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    • pp.80-87
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    • 2010
  • In this study, micro- and submicron particles of itraconazole, a poorly water-soluble antifungal drug, were prepared for improving its aqueous solubility using an ultrasound-assisted supercritical fluid technique, called SAS-EM. The SAS-EM process used in our experiments was different from the conventional SAS-EM in that the ultrasound was applied directly to the spray nozzle. The effect of the ultrasonic power, temperature, and solvent on the formation of itraconazole particles were investigated. Smaller particles were obtained through our SAS-EM process compared with the ASES process, and the mean particle size decreased as the ultrasonic power increased. Our experimental results confirmed that the ultrasound-assisted supercritical fluid process is an efficient method for producing ultrafine particles.

Computational Evaluation on the Interactions of an Opaque-Phase ABC Transporter Associated with Fluconazole Resistance in Candida albicans, by the Psidium guajava Bio-Active Compounds

  • Mithil Vora;Smiline Girija Aseervatham Selvi;Shoba Gunasekaran;Vijayashree Priyadharsini Jayaseelan
    • Journal of Pharmacopuncture
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    • v.27 no.2
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    • pp.91-100
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    • 2024
  • Objectives: Candida albicans is an opportunistic pathogen that occurs as harmless commensals in the intestine, urogenital tract, and skin. It has been influenced by a variety of host conditions and has now evolved as a resistant strain. The aim of this study was thus detect the fluconazole resistant C. albicans from the root caries specimens and to computationally evaluate the interactions of an opaque-phase ABC transporter protein with the Psidium guajava bio-active compounds. Methods: 20 carious scrapings were collected from patients with root caries and processed for the isolation of C. albicans and was screened for fluconazole resistance. Genomic DNA was extracted and molecular characterization of Cdrp1 and Cdrp2 was done by PCR amplification. P. guajava methanolic extract was checked for the antifungal efficacy against the resistant strain of C. albicans. Further in-silico docking involves retrieval of ABC transporter protein and ligand optimization, molinspiration assessment on drug likeness, docking simulations and visualizations. Results: 65% of the samples showed the presence of C.albicans and 2 strains were fluconazole resistant. Crude methanolic extract of P. guajava was found to be promising against the fluconazole resistant strains of C. albicans. In-silico docking analysis showed that Myricetin was a promising candidate with a high docking score and other drug ligand interaction scores. Conclusion: The current study emphasizes that bioactive compounds from Psidium guajava to be a promising candidate for treating candidiasis in fluconazole resistant strains of C. albicans However, further in-vivo studies have to be implemented for the experimental validation of the same in improving the oral health and hygiene.

The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies (이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구)

  • Cho, Young-Ho;Lee, Jong-Hwa;Kim, Hak-Hyung;Lee, Gye-Won
    • KSBB Journal
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    • v.26 no.3
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    • pp.217-222
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    • 2011
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.

Formulation Design and Evaluation of Niosome Containing Itraconazole for Dermal Delivery System (니오좀 시스템을 이용한 이트라코나졸 외용제의 제제 설계 및 평가)

  • Cho, Hye-Jung;Kyong, Kee-Yeol;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.165-171
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    • 2005
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. However, it is difficult for itraconazloe to be delivered by topical system due to its poor aqueous solubility. First, niosomes containing drug were prepared with span 60, cholesterol. tocopherol and poloxamer 407 as vesicle forming agents in an effort to increase solubility of itraconazole. And then prepared niosomes were dispersed in O/W creams (containing xanthan gum, glycerin, vaseline, glyceryl monostearate and $Cerix^{\circledR}-5$) or gels (containing xanthan gum and poloxamer 407). Both creams and gels were evaluated with respect to their rheological properties, in vitro permeation through excised skin of hairless mouse. Creams or gels containing niosome showed pseudoplastic flow and hysteresis loop. For both creams and gels, viscosity was increased with increasing the content of glycerine or vaseline and the content of gel forming polymer, respectively. In creams, the permeability of drug to skin was decreased with increasing the viscosity of cream. The permeability of drug was affected by pH as well as viscosity of gel. In vitro permeation test results demonstrated that cream formulations showed better permeability than gels. In conclusion, these results suggest that creams formulation containing niosome can be useful for the topical delivery of intraconazole.

Genomic Tandem Quadruplication is Associated with Ketoconazole Resistance in Malassezia pachydermatis

  • Kim, Minchul;Cho, Yong-Joon;Park, Minji;Choi, Yoojeong;Hwang, Sun Young;Jung, Won Hee
    • Journal of Microbiology and Biotechnology
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    • v.28 no.11
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    • pp.1937-1945
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    • 2018
  • Malassezia pachydermatis is a commensal yeast found on the skin of dogs. However, M. pachydermatis is also considered an opportunistic pathogen and is associated with various canine skin diseases including otitis externa and atopic dermatitis, which usually require treatment using an azole antifungal drug, such as ketoconazole. In this study, we isolated a ketoconazole-resistant strain of M. pachydermatis, designated "KCTC 27587," from the external ear canal of a dog with otitis externa and analyzed its resistance mechanism. To understand the mechanism underlying ketoconazole resistance of the clinical isolate M. pachydermatis KCTC 27587, the whole genome of the yeast was sequenced using the PacBio platform and was compared with M. pachydermatis type strain CBS 1879. We found that a ~84-kb region in chromosome 4 of M. pachydermatis KCTC 27587 was tandemly quadruplicated. The quadruplicated region contains 52 protein coding genes, including the homologs of ERG4 and ERG11, whose overexpression is known to be associated with azole resistance. Our data suggest that the quadruplication of the ~84-kb region may be the cause of the ketoconazole resistance in M. pachydermatis KCTC 27587.