The objective of the study was to develop, optimize and evaluate a nanoemulsion (NE) of Amphotericin B (AmB) using excipients with inherent antifungal activities (Candida albicans and Aspergillus niger) for topical delivery. AmB-loaded NE was prepared using Capmul PG8 (CPG8), labrasol and polyethylene glycol-400 by spontaneous titration method and evaluated for mean particle size, polydispersity index, zeta potential and zone of inhibition (ZOI). NE6 composed of CPG8 (15%w/w), S mix (24%w/w) and water (61%w/w) was finally selected as optimized NE. AmB-NE6 was studied for improved in vitro release, ex vivo skin permeation and deposition using the Franz diffusion cell across the rat skin followed with drug penetration using confocal laser scanning microscopy (CLSM) as compared to drug solution (DS) and commercial Fungisome Õ . The results of in vitro studies exhibited the maximum ZOI value of NE6 as 19.1 ± 1.4 and 22.8 ± 2.0 mm against A. niger and C. albicans, respectively, along with desired globular size (49.5 ± 1.5 nm), zeta potential (À24.59 mV) and spherical morphology. AmB-NE6 revealed slow and sustained release of AmB as compared to DS in buffer solution (pH 7.4). Furthermore, AmB-NE6 elicited the highest flux rate (22.88 ± 1.7 mg/cm 2 /h) as compared to DS (2.7 ± 0.02 mg/cm 2 /h) and Fungisome Õ (11.5 ± 1.0 mg/cm 2 /h). Moreover, the enhancement ratio and drug deposition were found to be highest in AmB-NE6 than DS across the stratum corneum barrier. Finally, CLSM results corroborated enhanced penetration of the AmB-NE6 across the skin as compared to Fungisome Õ and DS suggesting an efficient, stable and sustained topical delivery.
Triazoles and triazoles with different substituent groups are found to possess diverse application in the field of medicine and industry. A series of 4-(substituted) ethanoylamino-3-mercapto-5-(4-substituted) phenyl-1,2,4-triazoles were synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical structures of these newly synthesized compounds were elucidated by IR, 1 H NMR, 13 C NMR, FAB + -mass spectral data and elemental analyses. The antimicrobial activity of title compounds were examined against two gram positive bacteria (Staphylococcus aureus, Bacillus subtilis), two gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and three fungi (Candida albicans, Aspergillus niger and Fusarium oxysporum) using disc diffusion method. Some of the compounds bearing methoxy group exhibited moderate to good antibacterial and antifungal activities.
Background:
Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities.
Objective:
The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities.
Methods:
Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay.
Results:
Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities.
Conclusion:
Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.
The enantioselective separation of racemic mixtures is highly important in the pharmaceutical, food and agrochemical sector. Metal-organic frameworks, as a class of highly porous materials are emerging as highly efficient and selective platforms for chiral recognition and separation owing to their ultrahigh porosities, functionalized pore walls, controllable pore chemistry and presence of highly ordered chiral recognition sites. In this review, we summarize the progress made in the synthesis of chiral MOFs via direct and indirect methods, followed by their applications in some important chiral separations of alcohols, drugs, amino acids, biologically relevant molecules and important chiral organic mixtures. The developments in chiral MOF membranes as thin films for practical industrial use are also explored. Finally, the outlook for the MOFs as emerging platforms for enantioseparation and the future directions are discussed.
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