Current Techniques of Water Solubility Improvement for Antioxidant Compounds and Their Correlation with Its Activity: Molecular Pharmaceutics

Budiman, Arif; Rusdin, Agus; Aulifa, Diah Lia

doi:10.3390/antiox12020378

Cited by 16 publications

(5 citation statements)

References 137 publications

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“…This facilitates in vitro testing by eliminating the need for potentially harmful solvents. Moreover, water-soluble compounds are generally more suitable for medical applications, reducing risks and enhancing patient safety [17]; (b) Antimicrobial Activity: As indicated in Table 1, the MIC values of ED matched the MBC values, suggesting that ED not only inhibits but also kills the tested microor-ganisms. Such antimicrobial activity, as opposed to a bacteriostatic mode of action, is essential for topical treatment of wound infections [18]; (c) Gram-Positive Susceptibility: Gram-positive pathogens were more susceptible to the ED agent than Gram-negative bacteria and fungi.…”

Section: Discussionmentioning

confidence: 81%

Antimicrobial and Cytotoxic Activities of Water-Soluble Isoxazole-Linked 1,3,4-Oxadiazole with Delocalized Charge: In Vitro and In Vivo Results

Dudek,

Bąchor,

Drozd-Szczygieł

et al. 2023

IJMS

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The distinct structure of cationic organic compounds plays a pivotal role in enhancing their water solubility, which in turn influences their bioavailability. A representative of these compounds, which contains a delocalized charge, is 5-amino-2-(5-amino-3-methyl-1,2-oxazol-4-yl)-3-methyl-2,3-dihydro-1,3,4-oxadiazol-2-ylium bromide (ED). The high-water solubility of ED obviates the need for potentially harmful solvents during in vitro testing. The antibacterial and antifungal activities of the ED compound were assessed in vitro using the microtiter plate method and a biocellulose-based biofilm model. Additionally, its cytotoxic effects on wound bed fibroblasts and keratinocytes were examined. The antistaphylococcal activity of ED was also evaluated using an in vivo larvae model of Galleria mellonella. Results indicated that ED was more effective against Gram-positive bacteria than Gram-negative ones, exhibiting bactericidal properties. Furthermore, ED demonstrated greater efficacy against biofilms formed by Gram-positive bacteria. At bactericidal concentrations, ED was non-cytotoxic to fibroblasts and keratinocytes. In in vivo tests, ED was non-toxic to the larvae. When co-injected with a high load of S. aureus, it reduced the average larval mortality by approximately 40%. These findings suggest that ED holds promise for further evaluation as a potential treatment for biofilm-based wound infections, especially those caused by Gram-positive pathogens like S. aureus.

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Section: Discussionmentioning

confidence: 81%

Antimicrobial and Cytotoxic Activities of Water-Soluble Isoxazole-Linked 1,3,4-Oxadiazole with Delocalized Charge: In Vitro and In Vivo Results

Dudek,

Bąchor,

Drozd-Szczygieł

et al. 2023

IJMS

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“…It can be concluded that the preparation conditions of the NE-4-CUR sample were able to disperse the CUR more homogeneously in the nanodroplets, preventing its crystallization and allowing the CUR to remain in its amorphous and strongly encapsulated form. This fact makes the NE-4-CUR more interesting to release CUR in the medium, since actives in their amorphous form are more soluble than in their crystalline form (Budiman et al 2023 ).…”

Section: Discussionmentioning

confidence: 99%

Olive oil nanoemulsion containing curcumin: antimicrobial agent against multidrug-resistant bacteria

Confessor,

Agreles,

Campos

et al. 2024

Appl Microbiol Biotechnol

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The present work aimed to develop, characterize, and evaluate the antibacterial and antibiofilm activity of two nanoemulsions (NEs) containing 500 µg/mL of curcumin from Curcuma longa (CUR). These NEs, produced with heating, contain olive oil (5%) and the surfactants tween 80 (5%) and span 80 (2.5%), water q.s. 100 mL, and were stable for 120 days. NE-2-CUR presented Ø of 165.40 ± 2.56 nm, PDI of 0.254, ζ of − 33.20 ± 1.35 mV, pH of 6.49, and Entrapment Drug Efficiency (EE) of 99%. The NE-4-CUR showed a Ø of 105.70 ± 4.13 nm, PDI of 0.459, ζ of − 32.10 ± 1.45 mV, pH of 6.40 and EE of 99.29%. Structural characterization was performed using DRX and FTIR, thermal characterization using DSC and TG, and morphological characterization using SEM, suggesting that there is no significant change in the CUR present in the NEs and that they remain stable. The MIC was performed by the broth microdilution method for nine gram-positive and gram-negative bacteria, as well as Klebsiella pneumoniae clinical isolates resistant to antibiotics and biofilm and efflux pump producers. The NEs mostly showed a bacteriostatic profile. The MIC varied between 125 and 250 µg/mL. The most sensitive bacteria were Staphylococcus aureus and Enterococcus faecalis, for which NE-2-CUR showed a MIC of 125 µg/mL. The NEs and ceftazidime (CAZ) interaction was also evaluated against the K. pneumoniae resistant clinical isolates using the Checkerboard method. NE-2-CUR and NE-4-CUR showed a synergistic or additive profile; there was a reduction in CAZ MICs between 256 times (K26-A2) and 2 times (K29-A2). Furthermore, the NEs inhibited these isolates biofilms formation. The NEs showed a MBIC ranging from 15.625 to 250 µg/mL. Thus, the NEs showed physicochemical characteristics suitable for future clinical trials, enhancing the CAZ antibacterial and antibiofilm activity, thus becoming a promising strategy for the treatment of bacterial infections caused by multidrug-resistant K. pneumoniae. Key points • The NEs showed physicochemical characteristics suitable for future clinical trials. • The NEs showed a synergistic/additive profile, when associated with ceftazidime. • The NEs inhibited biofilm formation of clinical isolates.

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“…Due to its small size, the surface area, surface free energy, and surface-to-volume ratios are significantly enhanced, which may improve the solubility and dissolution rate of poorly water-soluble drugs. 31 As mentioned earlier, physcion has shown potential antitumor effects against different cell lines, including hepatocellular, breast, and colorectal cancer; however, its biological applications are greatly hindered due to its poor aqueous solubility and oral bioavailability. 19,20,32 The purpose of the present study is to prepare physcion NPs using the APSP method in order to improve the oral bioavailability of physcion.…”

Section: Introductionmentioning

confidence: 98%

Preparation, Characterization, and Evaluation of Physcion Nanoparticles for Enhanced Oral Bioavailability: An Attempt to Improve Its Antioxidant and Anticancer Potential

Khuda,

Zahir,

Khalil

et al. 2023

ACS Omega

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This study aims to enhance the dissolution rate of a poorly water-soluble drug physcion by producing its nanoparticles (NPs) using an antisolvent precipitation with a syringe pump (APSP) method and to assess its antioxidant and cytotoxic potential. The NPs were prepared using a simple and cost-effective APSP method and subsequently characterized by different analytical techniques including dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and X-ray powder diffractometry (XRD). They were also subjected to solubility and dissolution studies, and different parameters such as dissolution efficiency (DE), mean dissolution time (MDT), and difference (f 1) and similarity factors (f 2) were determined. Furthermore, physcion and its NPs were investigated for antioxidant and cytotoxic effects using various in vitro assays. SEM and DLS analysis indicated that the average size of physcion NPs was 110 and 195 ± 5.6 nm, respectively. The average ζ-potential and polydispersibility index (PDI) of the prepared NPs were −22.5 mV and 0.18, respectively, showing excellent dispersibility. XRD confirmed the amorphous nature of physcion NPs. The solubility and dissolution rates of NPs were significantly higher than those of the original powder. The antioxidant potential studied by the (DPPH), FRAP, and H2O2 assays was greater for physcion NPs than that for the raw powder. The IC50 values of physcion NPs against the aforementioned models were 57.56, 22.30, and 22.68 μg/mL, respectively. Likewise, the cytotoxic potential investigated through the MTT assay showed that physcion NPs were more cytotoxic to cancer cell lines A549 (IC50 4.12 μg/mL), HepG2 (IC50 2.84 μg/mL), and MDA-MB-231 (IC50 2.97 μg/mL), while it had less effect on HPAEpiC (IC50 8.68 μg/mL) and HRPTEpiC (IC50 10.71 μg/mL) normal human epithelial cells. These findings have proved that the APSP method successfully produced physcion NPs with enhanced solubility, dissolution rate, and antioxidant and cytotoxic activities.

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Current Techniques of Water Solubility Improvement for Antioxidant Compounds and Their Correlation with Its Activity: Molecular Pharmaceutics

Cited by 16 publications

References 137 publications

Antimicrobial and Cytotoxic Activities of Water-Soluble Isoxazole-Linked 1,3,4-Oxadiazole with Delocalized Charge: In Vitro and In Vivo Results

Antimicrobial and Cytotoxic Activities of Water-Soluble Isoxazole-Linked 1,3,4-Oxadiazole with Delocalized Charge: In Vitro and In Vivo Results

Olive oil nanoemulsion containing curcumin: antimicrobial agent against multidrug-resistant bacteria

Preparation, Characterization, and Evaluation of Physcion Nanoparticles for Enhanced Oral Bioavailability: An Attempt to Improve Its Antioxidant and Anticancer Potential

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