Cyclodextrin modulates the cytotoxic effects of chlorhexidine on microrganisms and cells<i>in vitro</i>

Teixeira, Karina Imaculada Rosa; Denadai, Ângelo Márcio Leite; Sinisterra, Rubén D.; Cortés, María Esperanza

doi:10.3109/10717544.2013.879679

Cited by 21 publications

(15 citation statements)

References 70 publications

(98 reference statements)

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“…Also, PEGylated MNPs can be decorated with functional groups such as CD, resulting in enhanced drug delivery. Hosting of CDs is an effective strategy for stabilizing the guest molecules against aggregation, thermal denaturation, or degradation (Sun et al 2008, Teixeira et al 2014). In recent decades, NP delivery systems based on CDs are considered as interesting agents to enhance drug solubility and loading.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of host–guest system to enhance the tamoxifen efficiency

Majd

Akbarzadeh

Sargazi

2016

Artificial Cells, Nanomedicine, and Biotechnology

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Hydrophobic drugs can absorb as guest molecules inside the cavity of cyclodextrins as host sites. So, forming the drug-cyclodextrin complex can exert a profound effect on the physicochemical and biological properties of the drugs. According to these advantages, in this study, we synthesized the tamoxifen (TMX) loaded cyclodextrin (CD)-conjugated MNPs to evaluate simultaneously the cytotoxicity and sustained release as well as hepatoprotective effect of this nanomedicine. The average size of FeO-DPA-PEG-CD-TMX NPs was approximately 31 nm. By energy-dispersive X-ray spectroscopy (EDS), it was revealed that FeO constitutes 14.34% of the composition of modified MNPs. In the other words, nearly 85% of FeO-DPA-PEG-CD NPs are made of dopamine (DPA), polyethylene glycol (PEG) and β-cyclodextrin (β-CD). The TMX loaded MNPs (with entrapment efficiency of 33 mg TMX per unit CD (mg) and loading efficiency of 87.5%) showed sustained liberation of TMX molecules (with 91% release in 120 h). Cytotoxicity assay and apoptosis assay by TUNEL analysis revealed that the engineered FeO-DPA-PEG-CD-TMX NPs were able to significantly inhibit the MCF-7 breast cancer cells. According to effect of CD on TMX sustained release, it was found that CD can decrease the hepatotoxicity induced by TMX nearly 30%. Based upon these findings, we suggest the FeO-DPA-PEG-CD-TMX NPs as an effective multifunctional nanomedicine with simultaneous therapeutic and hepatoprotective effects.

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Section: Discussionmentioning

confidence: 99%

Evaluation of host–guest system to enhance the tamoxifen efficiency

Majd

Akbarzadeh

Sargazi

2016

Artificial Cells, Nanomedicine, and Biotechnology

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“…63 Together these reports indicate a concentration dependence to ocular toxicity although they do not provide information as to the levels of chlorhexidine delivered to the cornea, which will be formulation-dependent. Interestingly, Teixeira et al (2015) reported that α-CD, β-CD and HP-β-CD increased the antimicrobial activity of chlorhexidine, but decreased its cytotoxic effects on mammalian fibroblasts and osteoblasts. 64 Some Acanthamoeba and fungal keratitis infections are considered untreatable with current drug therapies, including 0.02% to 0.06% chlorhexidine eyedrops.…”

Section: Potential Clinical Relevancecytotoxicitymentioning

confidence: 99%

“…Interestingly, Teixeira et al (2015) reported that α-CD, β-CD and HP-β-CD increased the antimicrobial activity of chlorhexidine, but decreased its cytotoxic effects on mammalian fibroblasts and osteoblasts. 64 Some Acanthamoeba and fungal keratitis infections are considered untreatable with current drug therapies, including 0.02% to 0.06% chlorhexidine eyedrops. Therefore, higher concentrations of chlorhexidine may be justified since the risk of vision loss in these cases is very high.…”

Section: Potential Clinical Relevancecytotoxicitymentioning

confidence: 99%

In Vitro Topical Delivery of Chlorhexidine to the Cornea: Enhancement Using Drug-Loaded Contact Lenses and β-Cyclodextrin Complexation, and the Importance of Simulating Tear Irrigation

et al. 2020

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Microbial keratitis is a severe, sight threatening condition caused by various pathogens. Eyedrops are the standard delivery modality for treating these disorders; however, blinking reflex, elevated tear production and nasolacrimal drainage eliminate much of the instilled dose within a few seconds. Therefore, eye drops must be applied repeatedly for prolonged periods. The present study aimed to probe more effective ocular delivery of chlorhexidine based upon drug-loaded hydrogel contact lenses and β-cyclodextrin (β-CD), whilst also determining the effect of constant irrigation with simulated tear fluid (STF) in in vitro experiments. Chlorhexidine digluconate (as 0.2 and 2.0% solution, β-CD inclusion complexes and loaded hydrogel contact lenses) were applied to enucleated porcine eyes as single or multiple 10 µL doses, or as drug-loaded contact lenses, with and without β-CD. The corneas were then excised and drug extracted quantified by HPLC. The effect of constant irrigation by STF was evaluated to test the effect of increased tear production on corneal delivery. Potential antimicrobial activity of delivered drug was also assessed. Results showed that drug-loaded contact lenses delivered the greatest amount of chlorhexidine into the cornea over a 24 h period, whilst the eyedrop solution comparator delivered the least. The β-CD significantly enhanced chlorhexidine delivery to the cornea from eyedrop solution, although contact lenses loaded with chlorhexidine-β-CD failed to enhance delivery. β-CD within the hydrogel matrix impeded drug release. Constant irrigation with STF significantly reduced the amount of drug delivered to the cornea in all cases. Chlorhexidine retained antimicrobial activity in all delivery methods. Hydrogel contact lenses loaded with chlorhexidine delivered significantly higher levels to the cornea compared to eyedrops, either multiple hourly doses or a single dose. They also offer reduced application, in particular to a non-ulcerated corneal infection. Finally, the importance of fully accounting for tear production in in vitro ocular delivery experiments was highlighted.

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“…From the perspective of development of new formulations, the strategy of preparing controlled release systems for environmental purposes, via host/guest interactions, have been proposed [12]. In this context, complexation of insecticides with cyclodextrins (CDs) could be an important strategy to improvement of current formulations [13, 14, 15].…”

Section: Introductionmentioning

confidence: 99%

Hydrophobic nanoprecipitates formed by benzoylphenylureas and β-cyclodextrin inclusion compounds: synthesis, characterization and toxicity against aedes aegypti larvae

Bittencourt

Moreira

Silva

et al. 2019

Heliyon

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The aim of this work was to synthesize and characterize the inclusion compounds formed by the complexation of β-cyclodextrin (βCD) with insecticides from the class of benzoylphenylureas (BPUs), named novaluron (NOV) and diflubenzuron (DIF), beyond evaluate their larvicidal activity against Aedes aegypti larvae. Solid state characterization by FTIR showed changes in the main peaks of BPUs and βCD, suggesting the formation of inclusion compounds in solid phase. DTA and TGA thermal analysis showed changes in temperatures of BPUs decomposition as result of molecular interactions. 1 H NMR experiments allowed to observe the occurrence of interactions in solution through changes in chemical shifts of BPUs aromatic hydrogens. However, the presence of H–H intermolecular correlations in 2D ROESY was found only for the DIF/βCD complex, suggesting different topology for each complex. Such hypothesis was corroborated by thermodynamic analysis using ITC, which showed different profile of titration curves, beyond endothermic and exothermic interactions for NOV/βCD and DIF/βCD complexes, respectively. DLS titrations of BPUs or BPUs/βCD DMSO solutions in aqueous solution demonstrated that the spontaneously formed hydrophobic nanoprecipitates (HNPs) have different profile of sizes depending on the BPU/βCD system, corroborating also with the hypothesis about the existence of different topologies for each complex. Finally, the HNPs of inclusion compounds showed to be more efficient than free BPUs, allowing proposing a new insecticide formulation.

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Cyclodextrin modulates the cytotoxic effects of chlorhexidine on microrganisms and cellsin vitro

Cited by 21 publications

References 70 publications

Evaluation of host–guest system to enhance the tamoxifen efficiency

Evaluation of host–guest system to enhance the tamoxifen efficiency

In Vitro Topical Delivery of Chlorhexidine to the Cornea: Enhancement Using Drug-Loaded Contact Lenses and β-Cyclodextrin Complexation, and the Importance of Simulating Tear Irrigation

Hydrophobic nanoprecipitates formed by benzoylphenylureas and β-cyclodextrin inclusion compounds: synthesis, characterization and toxicity against aedes aegypti larvae

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