scholarly journals New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 75
Author(s):  
Lavinia Vlaia ◽  
Ioana Olariu ◽  
Ana Maria Muţ ◽  
Georgeta Coneac ◽  
Vicenţiu Vlaia ◽  
...  

Biocompatible gel microemulsions containing natural origin excipients are promising nanocarrier systems for the safe and effective topical application of hydrophobic drugs, including antifungals. Recently, to improve fluconazole skin permeation, tolerability and therapeutic efficacy, we developed topical biocompatible microemulsions based on cinnamon, oregano or clove essential oil (CIN, ORG or CLV) as the oil phase and sucrose laurate (D1216) or sucrose palmitate (D1616) as surfactants, excipients also possessing intrinsic antifungal activity. To follow up this research, this study aimed to improve the adhesiveness of respective fluconazole microemulsions using chitosan (a biopolymer with intrinsic antifungal activity) as gellator and to evaluate the formulation variables’ effect (composition and concentration of essential oil, sucrose ester structure) on the gel microemulsions’ (MEGELs) properties. All MEGELs were evaluated for drug content, pH, rheological behavior, viscosity, spreadability, in vitro drug release and skin permeation and antifungal activity. The results showed that formulation variables determined distinctive changes in the MEGELs’ properties, which were nevertheless in accordance with official requirements for semisolid preparations. The highest flux and release rate values and large diameters of the fungal growth inhibition zone were produced by formulations MEGEL-FZ-D1616-CIN 10%, MEGEL-FZ-D1216-CIN 10% and MEGEL-FZ-D1616-ORG 10%. In conclusion, these MEGELs were demonstrated to be effective platforms for fluconazole topical delivery.

2015 ◽  
Vol 3 (3) ◽  
pp. 374-379 ◽  
Author(s):  
Neveen Helmy Abou El-Soud ◽  
Mohamed Deabes ◽  
Lamia Abou El-Kassem ◽  
Mona Khalil

BACKGROUND: The leaves of Ocimum basilicum L. (basil) are used in traditional cuisine as spices; its essential oil has found a wide application in perfumery, dental products as well as antifungal agents.AIM: To assess the chemical composition as well as the in vitro antifungal activity of O. basilicum L. essential oil against Aspergillus flavus fungal growth and aflatoxin B1 production.MATERIAL AND METHODS: The essential oil of O. basilicum was obtained by hydrodistillation and analysed using gas chromatography (GC) and GC coupled with mass spectrometry (GC/MS). The essential oil was tested for its effects on Aspergillus flavus (A. flavus) mycelial growth and aflatoxin B1 production in Yeast Extract Sucrose (YES) growth media. Aflatoxin B1 production was determined by high performance liquid chromatography (HPLC).RESULTS: Nineteen compounds, representing 96.7% of the total oil were identified. The main components were as follows: linalool (48.4%), 1,8-cineol (12.2%), eugenol (6.6%), methyl cinnamate (6.2%), α-cubebene (5.7%), caryophyllene (2.5%), β-ocimene (2.1%) and α-farnesene (2.0%).The tested oil showed significant antifungal activity that was dependent on the used oil concentration. The complete inhibition of A. flavus growth was observed at 1000 ppm oil concentration, while marked inhibition of aflatoxin B1 production was observed at all oil concentrations tested (500, 750 and 1000 ppm).CONCLUSION: These results confirm the antifungal activities of O. basilicum L. oil and its potential use to cure mycotic infections and act as pharmaceutical preservative against A. flavus growth and aflatoxin B1 production.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2818 ◽  
Author(s):  
Emira Noumi ◽  
Mejdi Snoussi ◽  
Mousa Alreshidi ◽  
Punchappady-Devasya Rekha ◽  
Kanekar Saptami ◽  
...  

To highlight the importance of the spices in the Mediterranean diet, the aim of the paper was to study the essential oil compositions and to clarify the potential differences in the biological activities of the three cardamom species. In the study, we compared the phytochemical profiles and biological activities of essential oils from Elettaria cardamomum, Aframomum corrorima and Amomum subulatum. The oils were analyzed using the GC and GC/MS techniques and were mainly constituted of the oxygenated monoterpenes which represents 71.4%, 63.0%, and 51.0% of all compounds detected in E. cardamomum, A. corrorima and A. subulatum essential oils, respectively, 1,8-cineole was the main common compound between the tree tested volatile oil. The essential oils showed significant antimicrobial activity against Gram-positive and Gram-negative microorganisms tested especially the fungal strains. The Ethiopian cardamom was the most active essential oil with fungal growth inhibition zone ranging from 12.67 to 34.33 mm, MICs values ranging from 0.048 to 0.19 mg/mL, and MBCs values from 0.19 to 1.75 mg/mL. The three tested essential oils and their main component (1,8-cineole) significantly increased the production of elastase and protease production, and motility in P. aeruginosa PAO1 in a dose dependent manner. In fact, at 10 mg/mL concentration, the three essential oils showed more than 50% of inhibition of elastolytic and proteolytic activities in P. aeruginosa PAO1. The same oils inhibited also the violacein production in C. violaceum strain. It was also noticed that at high concentrations, the A. corrorima essential oil significantly inhibited the germination of radish. A thorough knowledge of the biological and safety profiles of essential oils can produce applications of economic importance.


2020 ◽  
Vol 19 (1) ◽  
pp. 34-42
Author(s):  
Phanin Sintawarak ◽  
◽  
Suwimon Uthairatsamee ◽  
Tharnrat Keawgrajang ◽  
◽  
...  

Cylindrocladium reteaudii (Bugnic.) Boesew. is a severe pathogen which can cause leaf blight disease in Eucalyptus seedlings in tropical countries. This study investigated the antifungal activity of essential oils extracted from Acorus calamus L. rhizomes in inhibiting the growth of C. reteaudii, both in in vitro and in vivo experiments. The extraction of essential oils from rhizomes was carried out by hydro-distillation technique and the in vitro antifungal testing was done by using the poisoned food technique. The results indicated that an essential oil concentration of 2,000 ppm can completely inhibit the fungal growth with a 50% inhibitory concentration value of 54.76 ppm. For the in vivo experiment, it was found that an essential oil concentration of 500 ppm and Captan® of 1,000 ppm were not significantly different in inhibiting the growth of C. reteaudii. However, these two treatments significantly inhibited the fungal growth (p<0.05) when compared with the control treatments. Physiological and anatomical characteristics were investigated to check for the antifungal activity after the application of essential oils. Results showed that essential oil spraying had no effect on the leaf transpiration rate and temperature of the Eucalyptus seedlings, but the incident disease ratio was high when an essential oil concentration of more than 1,500 ppm was applied. Therefore, it can be inferred that the essential oils from A. calamus rhizomes at an optimum concentration can be an efficient antifungal compound with a potential to control leaf and shoot blight diseases in Eucalyptus seedlings in a nursery.


2006 ◽  
Vol 50 (8) ◽  
pp. 2797-2805 ◽  
Author(s):  
Jingsong Zhu ◽  
Paul W. Luther ◽  
Qixin Leng ◽  
A. James Mixson

ABSTRACT A family of histidine-rich peptides, histatins, is secreted by the parotid gland in mammals and exhibits marked inhibitory activity against a number of Candida species. We were particularly interested in the mechanism by which histidine-rich peptides inhibit fungal growth, because our laboratory has synthesized a variety of such peptides for drug and nucleic acid delivery. In contrast to naturally occurring peptides that are linear, peptides made on synthesizers can be varied with respect to their degrees of branching. Using this technology, we explored whether histidine-lysine (HK) polymers of different complexities and degrees of branching affect the growth of several species of Candida. Polymers with higher degrees of branching were progressively more effective against Candida albicans, with the four-branched polymer, H2K4b, most effective. Furthermore, H2K4b accumulated efficiently in C. albicans, which may indicate its ability to transport other antifungal agents intracellularly. Although H2K4b had greater antifungal activity than histatin 5, their mechanisms were similar. Toxicity in C. albicans induced by histatin 5 or branched HK peptides was markedly reduced by 4,4′-diisothiocyanato-stilbene-2,2′-disulfonate, an inhibitor of anion channels. We also determined that bafilomycin A1, an inhibitor of endosomal acidification, significantly decreased the antifungal activity of H2K4b. This suggests that the pH-buffering and subsequent endosomal-disrupting properties of histidine-rich peptides have a role in their antifungal activity. Moreover, the ability of the histidine component of these peptides to disrupt endosomes, which allows their escape from the lysosomal pathway, may explain why these peptides are both effective antifungal agents and nucleic acid delivery carriers.


2018 ◽  
Vol 49 (4) ◽  
pp. 929-935 ◽  
Author(s):  
Carolina M. Bedoya-Serna ◽  
Gustavo C. Dacanal ◽  
Andrezza M. Fernandes ◽  
Samantha C. Pinho

2018 ◽  
Vol 73 (7-8) ◽  
pp. 313-318 ◽  
Author(s):  
Rose Vanessa Bandeira Reidel ◽  
Simona Nardoni ◽  
Francesca Mancianti ◽  
Claudia Anedda ◽  
Abd El-Nasser G. El Gendy ◽  
...  

Abstract The objective of the present paper was the assessment of the chemical composition of the essential oils from four Asteraceae species with a considerable food, medicinal, and agricultural value, collected in Egypt, together with their in vitro inhibitory activity against molds and yeasts. The essential oil of Launaea cornuta flowers was also evaluated for the first time, but because of its very low yield (<0.01%), no antifungal test was performed.


2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Tamirat Bekele Beressa ◽  
Serawit Deyno ◽  
Paul E. Alele

Background. Echinops kebericho is an endemic medicinal plant in Ethiopia widely used in the treatment of infectious and noninfectious diseases. Essential oils are known for their antibacterial, antifungal, antiviral, insecticidal, and antioxidant properties. This study evaluated the antifungal activity of essential oil from E. kebericho against four common pathogenic fungi and two standard strains. Methods. The essential oil was obtained by hydrodistillation. The antifungal screening was done by agar well diffusion method. Minimal inhibitory concentrations (MICs) were determined by broth microdilution. Minimal fungicidal concentrations (MFCs) were determined by subculturing fungal strains with no visible growth onto a Sabouraud dextrose agar (SDA) plate. Results. Candida albicans and Cryptococcus neoformans were highly sensitive while Aspergillus flavus did not show sensitivity up to 1 mg/ml of essential oil; MICs ranged from 0.083 mg/ml to 0.208 mg/ml. Concentration and fungal species showed significant dose-dependent associations ( p < 0.0001 ) with antifungal activity. The MICs of essential oil were comparable to those of the standard drug (fluconazole) against C. glabrata and C. krusei. The lowest MFC of the essential oil was observed against Candida parapsilosis (0.145 mg/ml) while the highest MFC was against Candida krusei (0.667 mg/ml). Conclusion. Echinops kebericho essential oil showed noteworthy antifungal activity against Cryptococcus neoformans, Candida albicans, and Candida glabrata and could be a potential candidate for further antifungal drug development.


2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Mária Pl'uchtová ◽  
Teresa Gervasi ◽  
Qada Benameur ◽  
Vito Pellizzeri ◽  
Daniela Grul'ová ◽  
...  

Genus Mentha presents group of plants which are the most studied in family Lamiaceae. Aboveground parts are used for different purposes in pharmacy, food industry or confectionery. Most important is natural product extracted from leaves - essential oil (EO). The aim of presented experiment was to demonstrate different chemotype and compare antibacterial activity of two Mentha species EO. Plant samples were obtained from various environments – from Slovakia and from Italy. Dominant compounds were determined by GC/MS. The results showed high amount of menthol and menthone in tested Slovak peppermint EO. On the other hand, carvone and 1,8-cineole were determinate as dominant compounds in Italian spearmint EO. The antimicrobial activity of the EO was investigated by disc diffusion and broth micro dilution methods. EO was evaluated for their antibacterial activity against 7 microorganisms: Enterobacter cloacae, Salmonella spp., Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Streptococcus pyogenes. The determination results of antibacterial activity by agar disk diffusion method ranged from 7 to 14 mm of the growth inhibition zone. MIC of tested mint EO varied from 0.625 to 2.5 μg/mL. In addition, both EO showed relatively the same antibacterial activity against the selected Gram-negative bacteria. However, there is a variation in the antibacterial activity against Gram-positive bacteria.


2008 ◽  
Vol 3 (9) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Mehrdad Iranshahi ◽  
Abdolmajid Fata ◽  
Bahareh Emami ◽  
Bibi Mohadeseh Jalalzadeh Shahri ◽  
Bibi Sedigheh Fazly Bazzaz

The increase in dermatophytoses and the fact that some patients do not respond well to therapy make it necessary to find new antifungal agents. As part of our ongoing studies on medicinal plants from Iran, we studied antidermatophytic activities of Ferula latisecta essential oil, which had shown considerable antifungal activity in preliminary antimicrobial screening. Antifungal activity was evaluated by determination of MIC values using the agar dilution method on type strains of Candida albicans and dermatophytes. The composition of the oil was characterized by GC and GC/MS analyses. The essential oil was rich in polysulfides (75.2%) and exhibited good activity against Trichophyton rubrum and T. verrucosom for about three weeks, with a MIC value 96 μg/mL. The oil showed antifungal activity, especially against dermatophytes, and the activity is probably related to the sulfur-containing components of the oil. This study has identified that the polysulfides-rich essential oil of Ferula latisecta fruits has activity against a range of human pathogenic dermatophytes, justifying future clinical trials to validate its use as a therapeutic alternative for dermatophytosis.


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