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Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents.

ABSTRACT: Among different Candida species triggering vaginal candidiasis, Candida albicans is the most predominant yeast. It is commonly treated using azole drugs such as Tioconazole (TIO) and Econazole (ECO). However, their low water solubility may affect their therapeutic efficiency. Therefore, the aim of this research was to produce a novel chitosan nanocapsule based delivery system comprising of TIO or ECO and to study their suitability in vaginal application. These systems were characterized by their physicochemical properties, encapsulation efficiency, in vitro release, storage stability, cytotoxicity, and in vitro biological activity. Both nanocapsules loaded with TIO (average hydrodynamic size of 146.8 ± 0.8 nm, zeta potential of +24.7 ± 1.1 mV) or ECO (average hydrodynamic size of 127.1 ± 1.5 nm, zeta potential of +33.0 ± 1.0 mV) showed excellent association efficiency (99% for TIO and 87% for ECO). The analysis of size, polydispersity index, and zeta potential of the systems at 4, 25, and 37 °C (over a period of two months) showed the stability of the systems. Finally, the developed nanosystems presented fungicidal activity against C. albicans at non-toxic concentrations (studied on model human skin cells). The results obtained from this study are the first step in the development of a pharmaceutical dosage form suitable for the treatment of vaginal candidiasis.

SUBMITTER: Calvo NL

PROVIDER: S-EPMC6695956 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature

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Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents.

Calvo Natalia L NL Sreekumar Sruthi S Svetaz Laura A LA Lamas María C MC Moerschbacher Bruno M BM Leonardi Darío D

International journal of molecular sciences 20190727 15

Among different Candida species triggering vaginal candidiasis, <i>Candida albicans</i> is the most predominant yeast. It is commonly treated using azole drugs such as Tioconazole (TIO) and Econazole (ECO). However, their low water solubility may affect their therapeutic efficiency. Therefore, the aim of this research was to produce a novel chitosan nanocapsule based delivery system comprising of TIO or ECO and to study their suitability in vaginal application. These systems were characterized b ...[more]

PMID: 31357647

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Project description:Developing and creating novel antibiotics is one of the most important targets in treating infectious diseases. Novel coumarins were synthesized and characterized using different spectroscopic techniques such as Fourier Transform Infrared (FTIR), Nuclear magnetic resonance1H and 13C and mass spectroscopy (MS). All of the synthesized compounds have been tested for activity and sensitivity against the microbial strains of B. subtilis, S. aureus, E. coli, P. aeruginosa, S. typhi, and C. albicans. All compounds showed substantial results against the tested microbes except S. typhi, which was not affected in any way by these coumarins. Exceptional results were shown by compounds 4, 6d, and 8b, which made them the best candidates for loading to the vicinity of nanostructure lipid carrier and coated by chitosan nanocapsule (NLC-Cs). Transmission electron microscope (TEM) confirmed spherical morphology with particles size less than 500 nm. Also, dynamic light scattering (DLS) were utilized to measure the average particle size (between 100 and 200 nm) and the stability assessed by zeta potential were found to be more positive confirming the chitosan encapsulation. Antimicrobial activity assessments were performed for both synthetic compounds and their NLCs analogues. The nanoformulation of 4-NLC-Cs, 6d-NLC-Cs, and 8b-NLC-Cs manifested unique biological results, especially 8b-NLC-Cs, which revealed powerful effects over all the tested organisms including S. typhi. The increasing biological effect of the drugs in their nanoscale form is reflected in the increasing value of inhibition zone diameter and suppressing the value of MIC to reach record levels like 8b-NLC-Cs disclosed MIC = 0.48 and 0.24 µg/ml against S. aureus and C. albicans, respectively, by the mean 8b-NLC-Cs nanoformulation suppressed the MIC by 65 folds of its initial value before nano. In continuation, it was proven that the compounds 4, 6d and 8b were found to make noticeable changes on the DNA-Gyrase levels with reduced IC50 values particularly 8b showed excellent inhibitory effect with IC50 = 4.56 µM. TEM was used to pursue the morphological changes that occur in bacterial cells of P. aeruginosa. The weakness of the cell wall in most bacterial cells treated with nanomaterials, 8b-NLC-Cs, has reached the point of the cell wall rupture and the cell components spilling out of the cells causing necrotic cell death.

Project description:Introduction:In the last years, the utilization of phytomedicines has increased given their good therapeutic activity and fewer side effects compared to allopathic medicines. However, concerns associated with the biocompatibility and toxicity of natural compounds, limit the phytochemical therapeutic action, opening the opportunity to develop new systems that will be able to effectively deliver these substances. This study has developed a nanocomposite of chitosan (CS) functionalized with graphene oxide (GO) for the delivery of proanthocyanidins (PAs), obtained from a grape seed extract (Ext.). Methods:The GO-CS nanocomposite was covalently bonded and was characterized by Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), atomic force microscopy (AFM) and by dynamic light scattering (DLS). The loading and release of Ext. from the GO-CS nanocomposite were performed in simulated physiological, and the cytotoxicity of the raw materials (GO and Ext.) and nanocomposites (GO-CS and GO-CS-Ext.) was determined using a human kidney cell line (HEK 293). Results:The chemical characterization indicated that the covalent union was successfully achieved between the GO and CS, with 44 wt. % CS in the nanocomposite. The GO-CS nanocomposite was thermostable and presented an average diameter of 480 nm (by DLS). The Ext. loading capacity was approximately 20 wt. %, and under simulated physiological conditions, 28.4 wt.% Ext. (g) was released per g of the nanocomposite. GO-CS-Ext. was noncytotoxic, presenting a 97% survival rate compared with 11% for the raw extract and 48% for the GO-CS nanocomposite at a concentration of 500 µg mL-1 after 24 hrs. Conclusion:Due to ?-? stacking and hydrophilic interactions, GO-CS was reasonably efficient in binding Ext., with high loading capacity and Ext. release from the nanocomposite. The GO-CS nanocomposite also increased the biocompatibility of PAs-rich Ext., representing a new platform for the sustained release of phytodrugs.

Dataset Information

Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents.

Publications

Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents.

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