Search Results (1,451)

Introduction. Larvae of the insect Hermetia illucens can represent an alternative source for low-molecular-weight chitosan (CS) production compared with CS from crustaceans (CS_crustac), making it appealing in terms of pharmaceutical applications. Hence, the performances of CS_larvae and CS_crustac were compared herein by investigating the in vitro features of nanoparticles (NPs) made from each polysaccharide and administered with the antioxidant quercetin (QUE). Methods. X-ray diffraction and FT-IR spectroscopy enabled the identification of each type of CS. Following the ionic gelation technique and using sulfobutylether-β-cyclodextrin as a cross-linking agent, NPs were easily obtained. Results. Physicochemical data, release studies in PBS, and the evaluation of antioxidant effects via the 1,1-diphenyl-2-picrylhydrazyl (DPPH) test were studied for both CS_larvae and CS_crustac. QUE-loaded NP sizes ranged from 180 to 547 nm, and zeta potential values were between +7.5 and +39.3 mV. In vitro QUE release in PBS was faster from QUE-CS_larvae NPs than from CS_crustac, and high antioxidant activity—according to the DPPH test—was observed for all tested NP formulations. Discussion. The agar diffusion assay, referring to Escherichia coli and Micrococcus flavus, as well as the microdilution assay, showed the best performance as antimicrobial formulations in the case of QUE-CS_larvae NPs. QUE-CS_larvae NPs can represent a promising vehicle for QUE, releasing it in a sustained manner, and, relevantly, the synergism noticed between QUE and CS_larvae resulted in a final antimicrobial product. Conclusions. New perspectives for low-molecular-weight CS are disclosed by adopting renewable sources from insects instead of the commercial CS_crustac. Full article

The high incidence of melanoma leading to a poor prognosis rate endorses the development of alternative and innovative approaches in the treatment of melanoma. Therefore, the present study aims to develop and characterize, in terms of physicochemical features and biological impact, an aqueous suspension of magnetite (Fe₃O₄) coated with β-cyclodextrin (Fe₃O₄@β-CD) as a potential innovative alternative nanosystem for melanoma therapy. The nanosystem exhibited physicochemical characteristics suitable for biological applications, revealing a successful complexation of Fe₃O₄ NPs with β-CD and an average size of 18.1 ± 2.1 nm. In addition, the in vitro evaluations revealed that the newly developed nanosystem presented high biocompatibility on a human keratinocyte (HaCaT) monolayer and selective antiproliferative activity on amelanotic human melanoma (A375) cells, inducing early apoptosis features when concentrations of 10, 15, and 20 μg/mL were employed for 48 h and 72 h. Collectively, the Fe₃O₄@β-CD nanosystem reveals promising features for an adjuvant approach in melanoma treatment, mainly due to its β-cyclodextrin coating, thus endorsing a potential co-loading of therapeutic drugs. Furthermore, the intrinsic magnetic core of Fe₃O₄ NPs supports the magnetically based cancer treatment strategies. Full article

This study investigates the self-assembly and host–guest complexation behaviour of novel resveratrol-based lipophenols (LipoResv)—resveratrol-4′-linoleate (Resv-4′-LA) and resveratrol-4′-docosahexaenoate (Resv-4′-DHA)—with hydroxypropyl-β-cyclodextrins (HP-β-CDs). These amphiphilic molecules display surfactant-like properties, forming micellar aggregates in aqueous media. Fluorescence spectroscopy was used to determine the critical micelle concentration (CMC), revealing that LipoResv exhibit significantly lower CMC values than their free fatty acids, indicating higher hydrophobicity. The formation of inclusion complexes with HP-β-CDs was evaluated based on changes in CMC values and further confirmed by dynamic light scattering (DLS) and molecular modelling analyses. Resv-4′-LA formed 1:1 complexes (Kc = 720 M⁻¹), while Resv-4′-DHA demonstrated a 1:2 stoichiometry with lower affinity constants (K₁ = 17 M⁻¹, K₂ = 0.18 M⁻¹). Environmental parameters (pH, temperature, and ionic strength) significantly modulated CMC and binding constants. Computational docking and molecular dynamics simulations supported the experimental findings by revealing the key structural determinants of the host–guest affinity and micelle stabilization. Ligand efficiency (LE) analysis further aligned with the experimental data, favouring the unmodified fatty acids. These results highlight the versatile encapsulation capacity of HP-β-CDs for bioactive amphiphile molecules and support their potential applications in drug delivery and functional food systems. Full article

Cetraria islandica (L.) Ach. (CI) is a lichen from the Parmeliaceaea family used in medicine. However, the low solubility of CI secondary metabolites in water limits the application of lichen extract and compounds. It prompted us to study the systems of cyclodextrins (CDs) (β-CD, γ-CD, HP-β-CD, and HP-γ-CD) with the CI acetone or CI methanol extracts prepared using grinding and solvent evaporation methods. The content of fumarprotocetraric acid (FPCA), a key CI metabolite, was quantified using HPLC. CD–extract systems were characterized by X-ray powder diffraction (XRPD) and Fourier-transform infrared (FTIR) spectroscopy. Biological activity was evaluated using cell-free assays: a Folin–Ciocalteu analysis, DPPH test, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitions. Dissolution profiles were also assessed. The best biological and physicochemical results were obtained for systems prepared with HP-β-CD and HP-γ-CD via solvent evaporation, showing higher activity and enhanced FPCA release compared to the pure extracts. To the best of our knowledge, this is the first study to report the preparation and characterization of CD-based systems with CI extracts. The obtained results encourage us to continue our research on CI to improve the physicochemical properties of its active compounds. Full article

Cynara cardunculus L. subsp. cardunculus (Cynara cardunculus L. var. sylvestris (Lam.) Fiori), the wild cardoon, is known for its culinary applications and potential health benefits. Due to this, and given the growing interest in circular economies, deepening our under-standing of the effects of wild cardoon leaf waste on angiogenesis and collagenase activity represents a valuable opportunity to valorise agricultural byproducts as health-promoting ingredients. In this study, the waste product of wild cardoon leaves was extracted to examine its chemical composition and biological activities. Analytical techniques identified several bioactive compounds, including flavonoids, hydroxycinnamic acids such as dicaffeoyl-succinoylquinic acids, and luteolin-7-O-rutinoside. In vivo tests in zebrafish embryos and the chick chorioallantoic membrane demonstrated dose-dependent antiangiogenic effects, particularly enhanced by the complexation with hydroxypropyl-β-cyclodextrin (HP-β-CD). Considering the link between angiogenesis and collagenase, the potential effects of the extract on collagenase activity was investigated. The extract alone inhibited collagenase with an IC₅₀ value comparable to that of the standard inhibitor while its complexed form exhibited a 4.5-fold greater inhibitory activity. A molecular docking study examined the interaction between the main compounds and collagenase. In conclusion, wild cardoon leaves can represent a valuable source of bioactive compounds. This study demonstrated that the complexation of the extract with cyclodextrin determines an increase in its biological activity. Full article

The increasing demand for sustainable and safer alternatives in the cosmetic industry has driven the search for multifunctional natural ingredients. Essential oils (EOs), known for their antimicrobial and antioxidant activities, are promising candidates with which to replace synthetic preservatives and antioxidants. This study aimed to evaluate the preservative and antioxidant potential of Lippia origanoides Kunth essential oil, in pure and encapsulated in β-cyclodextrin form, for cosmetic applications. The EO exhibited strong antioxidant activity, with low IC₅₀ values in DPPH and ABTS assays, and demonstrated antimicrobial efficacy, particularly against Escherichia coli and Staphylococcus aureus. Six cosmetic cream formulations were developed and tested for physicochemical and microbiological stability. Formulations with pure EO maintained high antioxidant performance and remained free of bacterial and fungal contamination over time, outperforming the commercial preservatives. In contrast, formulations with encapsulated EO exhibited delayed antioxidant and antimicrobial activity, indicating gradual release. Overall, Lippia origanoides EO proved to be an effective natural alternative to synthetic preservatives and antioxidants. This approach aligns with the current trend of eco-friendly formulations, offering a sustainable solution by incorporating plant-derived bioactives into cosmetic products. Full article

Nepafenac is an anti-inflammatory drug used in ophthalmology, marketed as a suspension due to its low aqueous solubility. A solution formulation could provide better bioavailability than suspension and facilitate single unit doses, avoiding the use of preservatives which are required to maintain sterility in multidose packaging. In this study, solubilization of nepafenac was achieved in the presence of randomly methylated β-cyclodextrin (RAMEB) and the actual complexation was assessed by NMR and phase-solubility studies. It was also found that the addition of hydrophilic polymers plays an important role in allowing increased solubilization of nepafenac at the same cyclodextrin concentration. Compared to complexes of nepafenac with other cyclodextrins, only 5% RAMEB was sufficient to solubilize 0.3% (w/v) nepafenac, enabling for the first time the development of an ophthalmic solution that proved chemically and physically stable for 12 months at 25 °C. The formulated solutions of nepafenac were tested for cytotoxicity on human corneal epithelial cells (HCE-2) and the results suggest their potential as a valuable and safe alternative to the commercially available 0.3% (w/v) suspension of the drug. Full article

Cyclodextrins (CDs) have been widely employed as natural host molecules to form inclusion complexes with bioactive molecules such as antioxidants. Their particular spatial configuration, in the form of truncated cones formed through α(1–4) ether linkages of glucopyranose units, makes them very appropriate for the formation of host–guest complexes, modifying their physicochemical properties and their location in multiphasic systems. Here, we investigated the effects of 2-hydroxypropyl-β-cyclodextrin (HPCD) on the efficiency of a series of gallic acid derivatives (propyl (PG), butyl (BG), octyl (OG), and lauryl (LG) gallates) in inhibiting the oxidation of soybean oil-in-water emulsions. For this purpose, we investigated the effects of HPCD on both the kinetics of lipid oxidation and the distribution of antioxidants in the same intact emulsions. The results show that in an aqueous solution, the antioxidants form 1:1 inclusion complexes with HPCD, with inclusion constants ranging from 383 M⁻¹ (PG) to 1946 M⁻¹ (OG). The results also show that the addition of HPCD to emulsions containing antioxidants does not lead to significant changes in their antioxidant effectiveness, with their efficiency being similar to that when no HPCD molecules are present. The results are interpreted in terms of the blocking effect exerted by the Tween 20 molecules, which act as effective guest competitors capable of removing the antioxidants from the HPCD cavity. The Tween 20 surfactant molecules need to be employed to stabilize the emulsions kinetically. This blocking effect, as a primary consequence, indicates that the interfacial concentration of the antioxidants, which is the region where the inhibition reaction takes place, remains constant; thus, their efficiency is not altered. Full article

Resveratrol is one of the most extensively studied natural products due to its pleiotropic health benefits. However, its low water solubility and limited stability hinder its application in the nutraceutical, cosmetic, and pharmaceutical sectors. In this work, we investigated the ability of a cationic mono-choline-β-cyclodextrin derivative to complex trans-resveratrol. The complex was prepared using a phase solubility method without using organic solvents and was found to be stable after freeze-drying. The complex was characterized by a phase solubility study, NMR spectroscopy, and molecular modeling simulations, which revealed a 1:1 stoichiometry, a stability constant of 2051 M⁻¹ (K_C), and structural details. Complexation improved resveratrol’s solubility and dissolution rate, reduced its photoinduced trans-to-cis isomerization, and preserved its radical scavenging activity. The wound-healing activity of the complex was demonstrated via in vitro experiments on human keratinocyte cells. Full article

This work represents the first use of a phosphonium salt-functionalized β-Cyclodextrin polymer (β-CDP) as a highly selective sensing membrane for monitoring the safety of drinking water against perchlorate ions (ClO₄⁻) using electrochemical impedance spectroscopy (EIS). Structural confirmation via ¹H NMR, ¹³C NMR, ³¹P NMR, and FT-IR spectroscopies combined with AFM and contact angle measurements demonstrate how the enhanced solubility of modified cyclodextrin improves thin film quality. The innovation lies in the synergistic combination of two detection mechanisms: the “Host-Guest” inclusion in the cyclodextrin cavity and anionic exchange between the bromide ions of the phosphonium groups and perchlorate anions. Under optimized functionalization conditions, EIS reveals high sensitivity and selectivity, achieving a record-low detection limit (LOD) of ~10⁻¹² M and a wide linear range of detection (10⁻¹¹ M–10⁻⁴ M). Sensing mechanisms at the functionalized transducer interfaces are examined through numerical fitting of Cole-Cole impedance spectra via a single relaxation equivalent circuit. Real water sample analysis confirms the sensor’s practical applicability, with recoveries between 96.9% and 109.8% and RSDs of 2.4–4.8%. Finally, a comparative study with reported membrane sensors shows that β-CDP offers superior performance, wider range, higher sensitivity, lower LOD, and simpler synthesis. Full article

Per- and polyfluoroalkyl substances (PFASs) are synthetic chemicals widely used in industrial applications and have become persistent environmental contaminants due to their chemical stability. Water-soluble PFASs with fewer than ten carbon atoms, such as perfluorooctanoic acid (PFOA), are particularly concerning because of their high solubility in water, environmental mobility, and resistance to degradation. In this work, we present an eco-friendly Fe₃O₄ magnetic nanoparticle (MNP)-based platform for the detection and removal of PFOA from water. The synthesized iron oxide MNPs exhibit rapid and strong magnetic responsiveness, enabling efficient magnetic separation for both PFOA detection and removal. To optimize surface affinity for PFOA, we functionalized the MNPs with distinctive ligands, including polyethylene glycol (PEG), β-cyclodextrin (βCD), and dopamine (DA). Among these, PEG and DA showed notable binding affinity toward PFOA, as confirmed by infrared spectroscopy and colorimetric assays. After incubation with the functionalized MNPs followed by magnetic retrieval, we achieved over 90% PFOA removal efficiencies, demonstrating the potential for future research in PFAS remediation technologies. Importantly, the system was validated using deionized, tap, and lake water, all of which yielded comparable and promising results. This study provides a promising, eco-friendly, and recyclable nanomaterial platform for investigating the crucial role of surface chemistry in nanoparticle–PFAS interactions through ligand-mediated magnetic separation. Full article

In this work, a glassy carbon electrode (GCE) modified with reduced graphene oxide and β-cyclodextrin (rGO/β-CD) nanocomposite was developed for the electrochemical detection of nitrofurantoin (NFT). The structural and morphological characteristics of the synthesized nanocomposite were determined using scanning electron microscopy (SEM), Raman spectroscopy, X-ray diffraction (XRD), and X-ray photoelectron spectroscopy (XPS). Moreover, the electrochemical behavior of the modified electrodes was thoroughly examined using cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS), with the rGO/β-CD-modified glassy carbon electrode (GCE) demonstrating superior electron transfer capability. Key experimental parameters, including scan rate, material loading, and solution pH, were systematically optimized. After optimizing the experimental conditions, the modified sensor showed excellent electrocatalytic performance and selectivity toward NFT, achieving a broad linear detection range from 0.5 to 120 μM, a low limit of detection (LOD) of 0.048 μM, and a high sensitivity of 12.1 µA µM^–1 cm^–2 using differential pulse voltammetry (DPV). Furthermore, the fabricated electrode exhibited good anti-interference ability, stability, precision, and real-time applicability for NFT detection in a wastewater sample. These results highlight the potential of the rGO/β-CD nanocomposite as a high-performance platform for electrochemical sensing applications. Full article

Background/Objectives: In order to enhance the biological activity, novel complexes of N-(2-bromo-phenyl)-2-hydroxy-benzamide derivatives and β-cyclodextrin were obtained. Methods: The inclusion complexes were characterized using spectral and thermal analyses. The antimicrobial activity was determined using the disk diffusion agar method, and completed with the minimum inhibitory concentration (MIC) values obtained by the broth microdilution method. The in vitro anti-inflammatory activity was evaluated using the protease inhibition assay. Results: The computed supramolecular architectures of the inclusion complexes showed that the most stable molecular arrangements correspond to the models in which the N-(2-bromo-phenyl)-2-hydroxy-benzamide derivatives are partially included in the cyclodextrin cavity. The antimicrobial screening showed that the compounds were active against Gram-positive bacteria (MIC = 2.5–5.0 mg/mL). Also, the evaluation of the proteinase inhibitory activity showed that the IC₅₀ values of the title compounds (0.04–0.07 mg/mL) were much lower than that of the acetylsalicylic acid (0.4051 ± 0.0026 mg/mL) used as positive control, proving their superior efficiency in inhibiting trypsin activity. Conclusions: The complexation proved to be beneficial for both antimicrobial and anti-inflammatory effects. Full article

Clove essential oil (Eugenia caryophyllata essential oil, ECEO) is known for its high eugenol content and notable antimicrobial properties. However, the volatility and instability of its active compounds hinder broader pharmaceutical applications. Methods: This study characterised the chemical composition of ECEO and comparatively evaluated four β-cyclodextrin (β-CD) encapsulation methods: kneading, co-precipitation, lyophilisation, and co-precipitation–lyophilisation for eugenol, eucalyptol, and ECEO. Encapsulation efficiency, physicochemical properties, and antimicrobial potential were assessed. Analytical techniques included Gas Chromatography–Mass Spectrometry (GC-MS), Headspace GC-MS (HS-GC-MS), Differential Scanning Calorimetry (DSC), Job’s method, and Dynamic Light Scattering (DLS). Results: GC-MS identified eugenol (90.67%), eugenyl acetate (4.77%), and (E)–β-caryophyllene (3.98%) as major components of ECEO, while HS-GC-MS indicated a slightly reduced eugenol content (86.46%). The kneading method yielded the highest encapsulation efficiency for eugenol, whereas the co-precipitation–lyophilisation method was optimal for eucalyptol. DSC thermograms confirmed complex formation, and DLS analysis revealed nanostructures averaging 186.4 nm in diameter (PDI = 0.298). Antimicrobial assays showed MIC values ranging from 0.039 mg/mL to 10,000 mg/mL. Notably, ECEO and its β-CD complex displayed enhanced efficacy against Escherichia coli (0.039 mg/mL), surpassing the reference antibiotic gentamicin (0.049 mg/mL). Conclusions: β-Cyclodextrin encapsulation significantly enhances the stability and bioactivity of volatile antimicrobial compounds, thereby supporting their potential integration into advanced essential oil-based pharmaceutical formulations. Full article

Background/Objectives: Early diagnosis and oral or, in severe cases, intravenous antibiotics are usually effective for Lyme disease, but some patients have persistent symptoms unresponsive to standards of care, requiring alternative therapies. Disulfiram (DIS), a drug for alcoholism, is under investigation as a potential adjunctive treatment, but its low bioavailability, rapid metabolism, and safety concerns urge the development of improved formulations for clinical translation. Methods: Screening dissolution and permeation studies were investigated for vehicle and excipient selection, following the pharmacopeia perspectives to develop and optimize the low-dose DIS rectal suppository intended for application in post-treatment Lyme disease syndrome (PTLDS). Further characterizations were carried out by differential scanning calorimetry, X-ray diffraction, and infrared spectroscopy. Results: Cyclodextrin (CD) encapsulation was investigated to improve the aqueous solubility of the hydrophobic drug. The dissolution of DIS from fatty base suppository was very slow; it was remarkably improved by the molecular encapsulation of the drug with CDs. The dissolution of DIS from a water-soluble base was more favorable, but incomplete. In the polyethylene glycol (PEG) based suppositories, the addition of CDs already in a physical mixture ensured the dissolution of the drug. The presented drug delivery system relates to a novel preparation for rectal administration comprising a low-dose disulfiram with improved solubility and permeability by the PEG and hydroxypropyl-β-cyclodextrin (HPBCD) synergistic matrix. Conclusions: The rectal dosage form containing the drug and CD in the physical mixture is advantageous, avoiding the hepatic first-pass effect, minimizing dose-limiting toxicity, simplifying production, and fasting the availability of the repositioned drug. Full article