Search Results (738)

Gene delivery/administration and, in particular, small interfering RNA (siRNA) delivery represent a therapeutic challenge, though very effective carriers have yet to be identified. Cyclodextrins (CDs) are cyclic oligosaccharides with unique host–guest inclusion capabilities, widely recognized in the pharmaceutical field for their ability to enhance drug solubility and bioavailability. Their excellent biocompatibility and chemical versatility make them powerful building blocks for the design of supramolecular nanovectors (NVs). Thanks to their facility of functionalization, CDs are highly versatile and have found numerous applications across various fields. In this context, CD-based NVs are currently explored as non-viral agents to transport and release siRNA. Recent studies suggest that self-assembled NVs based on CDs can improve the transfection and safety of siRNA delivery. This review provides a comprehensive overview of the most recent advances in the design of NVs based on CDs and their use for siRNA delivery, discussing the role played by structural differences and chemical functionalization in the context of encapsulation and release. Full article

Isoflavones are plant-derived polyphenols with broad biological activity; however, their application in topical formulations is limited by poor aqueous solubility. The aim of this study was to enhance the aqueous solubility of formononetin using a solvent-free hot-melt extrusion (HME) approach and to enable its incorporation into a hydrogel formulation suitable for skin delivery. Amorphous formononetin-based systems were prepared by HME using polymeric carriers and hydroxypropyl-β-cyclodextrin, with and without prior inclusion complex formation. The resulting formulations were characterized using XRPD, DSC, and FT-IR/ATR to assess amorphization and intermolecular interactions. Aqueous solubility and skin permeability were evaluated using solubility testing, PAMPA, and Franz diffusion cells. The optimized amorphous system exhibited a substantial increase in apparent aqueous solubility compared to crystalline formononetin while maintaining comparable permeability. Cyclodextrin–formononetin interactions were effectively generated during the extrusion process, rendering pre-inclusion unnecessary. The selected system was successfully incorporated into a hydrogel matrix. This study demonstrates that solvent-free HME combined with cyclodextrins is an effective strategy for improving formononetin solubility and enabling its application in hydrogel-based topical delivery systems. Full article

This study focused on the incorporation of Piper betle L. essential oil (EO) into β-cyclodextrin (β-CD) and the subsequent incorporation of this complex into chitosan-based films with a beeswax coating. The objective of this study was to develop a hydrophobic, antibacterial bio-based film suitable for preservation applications. A total of four formulations were prepared: (1) chitosan film with no EO or β-CD, (2) chitosan film with β-CD only, (3) chitosan film with EO only, and (4) chitosan film with both EO and β-CD. The EO concentration was varied between 0, 0.5 and 1% (v/v) in the formulation, while β-CD was used at a concentration of 5% (w/v). The films were characterized using FTIR to analyze functional groups, SEM for surface morphology, contact angle to assess hydrophobicity, and tensile tests for mechanical properties. The results indicated significant changes in functional group characteristics and surface morphology across the different formulations. Beeswax coating enhanced the water impermeability and increased the hydrophobicity of the films, improving the contact angle from 59.93 ± 1.79° to 97.84 ± 0.77° and the mechanical strength from 0.28 ± 0.07 MPa to 24.49 ± 0.04 MPa. The antibacterial activity, assessed using the Kirby–Bauer method, showed that the EO concentration significantly inhibited the growth of Escherichia coli, with a maximum inhibition zone of 7.43 ± 0.60 mm observed at the highest EO concentration. These findings demonstrate that chitosan-based film modifications, incorporating both EO and β-CD, significantly improve the material properties and antibacterial activity, indicating its potential for food preservation applications. Full article

To meet the challenge of microbial contamination of food, smart packaging materials with active controlled-release functions have become a research hotspot. In this study, a humidity-responsive antimicrobial composite film was constructed by introducing cinnamaldehyde@β-cyclodextrin inclusion complexes (CIN@β-CD ICs) into a konjac glucomannan/polyvinyl alcohol/lithium chloride (KGM/PVA/LiCl) matrix. Characterization results showed that the CIN@β-CD ICs formed a dense structure through hydrogen bonding, which enhanced the thermal stability, mechanical strength (tensile strength: 20.83 MPa) and surface hydrophilicity (water contact angle < 60°) of the film. The film acted as a humidity-triggered release system for CIN, enabling controlled antimicrobial delivery: at high humidity (98% RH), the film rapidly swelled and accelerated the release of CIN, with a cumulative release rate of 87.29% over 7 days, whereas the release slowed significantly at low humidity (43% RH). The antimicrobial activity of the released CIN was strongly influenced by ambient humidity, with the effect enhanced under high humidity conditions. It is noteworthy that the film containing 0.2% ICs exhibited the optimal antimicrobial performance among the formulations studied. This study elucidates a mechanism for humidity-triggered release through multicomponent synergism, which provides a feasible strategy for the design of environmentally friendly, smart packaging materials with high antimicrobial activity. Full article

Background: Chitosan-based hydrogels exhibit excellent temperature-sensitive properties and are widely used as skin dressings. However, several challenges remain, such as long gelation times and difficulties releasing insoluble drugs, which limit their application in skin wound healing. In this study, we developed a novel sulfobutyl-β-cyclodextrin/quercetin@chitosan/hyaluronic acid hydrogel (Qe/SBE@CS/HA Gel). In this gel, SBE not only encapsulates Qe to form inclusion complexes, thereby enhancing the solubility of Qe, but also shortens the gelation time of thermosensitive gels through electrostatic adsorption with chitosan. Methods: Qe/SBE was prepared using the saturated solution method, while Qe/SBE@CS/HA gel was fabricated via electrostatic adsorption. The performance of the gels was evaluated using antibacterial, antioxidant, compatibility, and skin infection damage models. Results: The Qe/SBE@CS/HA Gel exhibits both thermosensitivity and acid sensitivity, releasing 91.9% of Qe in a medium with a pH of 5.0. This gel displays notable antibacterial activity and antioxidant characteristics. Furthermore, it shows excellent biocompatibility, as evidenced by hemolytic and in vivo degradation tests. The gel has the capacity to modulate chronic inflammation and facilitate angiogenesis and collagen synthesis, thereby significantly accelerating wound healing in wound and infection models. Conclusions: This multi-responsive and multifunctional gel shows potential as a therapeutic strategy for bacterial infection wounds. Full article

Cyclodextrins (CyDs) are cyclic oligosaccharides that form inclusion complexes that allow organic compounds and other substances to be incorporated into their cavities. Hydroxypropyl-β-cyclodextrin (HP-β-CyD) is frequently used to improve the formulation properties of poorly water-soluble drugs because of its aqueous solubility and biocompatibility. Previous studies have demonstrated that the solubility and biocompatibility of poorly water-soluble anti-cancer agents can be improved by complexation with HP-β-CyD, which in some cases enhances their anticancer activity relative to the unmodified drugs. Advances in formulation strategies have enabled more efficient intracellular delivery, improved tissue and cell selectivity, and controlled release. HP-β-CyD has also been investigated as an active pharmaceutical ingredient, with demonstrated efficiency in treating leukemia and breast cancer. For example, folate-conjugated HP-β-CyD exhibits high selectivity for folate receptor-expressing cells and more potent anti-cancer activity than unmodified HP-β-CyD. Autophagy has been suggested to be involved in this mechanism. The continued development of drug-delivery systems that integrate advanced technologies and materials based on HP-β-CyD holds promise for further advances in cancer therapy. These findings indicate a paradigm shift in the role of HP-β-CyD from a formulation additive to an active pharmaceutical ingredient, suggesting broader applications for HP-β-CyD in anticancer treatments. Full article

The aim of this study was to prepare curcumin/2-hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complex, evaluate the antioxidant and antimicrobial activities of curcumin and curcumin in inclusion complex, as well as to examine the effect of curcumin and curcumin inclusion complex on the textural properties of Carbopol^® gel mixture. Curcumin/2-hydroxypropyl-β-cyclodextrin inclusion complex was prepared using the co-precipitation method in a molar ratio of 1:1. The antioxidant activity of curcumin and curcumin in inclusion complex was determined using DPPH, ABTS, and FRAP methods. The micro-dilution method was used to examine in vitro the antimicrobial activity of curcumin and curcumin in inclusion complex. The textural, rheological, and morphological properties of the samples (Gel 1- Carbopol^® gel; Gel 2- Carbopol^® gel with dispersed curcumin inclusion complex; Gel 3- Carbopol^® gel with dispersed curcumin) were examined. The textural properties were evaluated using a texturometer CT3 Texture Analyzer by means of a Texture Profile Analysis (TPA) test. The results showed that curcumin in inclusion complex had higher antioxidant and antimicrobial activity. The SEM confirms the presence of curcumin and inclusion complex in Carbopol^® gel. The rheological analysis confirmed that the structural integrity of Carbopol^® gel was preserved. The highest swelling degree is achieved by Gel 3 formulation. The in vitro release of curcumin from Gel 2 and Gel 3 occurs at the rates of 0.414 µg/h·g_gel and 0.376 µg/h·g_gel, respectively. The textural analysis showed that adding curcumin or its inclusion complex did not significantly change the properties of Carbopol^® gel, indicating potential for topical use. Full article

Background/Objectives: Essential oils (EOs) from plants of the genus Cinnamomum have been widely used based on their antimicrobial, antioxidant, and anti-inflammatory properties. However, their elevated volatility and limited aqueous solubility restrict their use in pharmaceutical and food formulations. Cyclodextrins (CDs) have emerged as a promising strategy to overcome these limitations through the formation of inclusion complexes. Methods: In this study, inclusion complexes of essential oil from C. camphora L. (EOCNM) with β-cyclodextrin (β-CD) were developed using physical mixing (PM), ultrasonic treatment (US), and freeze-drying (FD). The inclusion complexes were physicochemically characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TG/DTG), X-ray diffraction (XRD), and scanning electron microscopy (SEM) to evaluate their physicochemical interactions and complexation efficiency. Results: Our results demonstrated successful complex formation, with the FD and US methods showing greater amorphization and stronger inclusion characteristics compared to the PM method. Thermal analysis confirmed improved physicochemical stability of the essential oil when complexed with β-CD. Furthermore, the cytotoxicity assay of the complexes was assessed using the MTT assay and J774 macrophage cells. The complexes exhibited low cytotoxicity, indicating their potential biocompatibility for biomedical and food applications. Conclusions: Overall, β-CD encapsulation effectively enhanced the physicochemical stability and safety profile of C. camphora essential oil, providing a promising strategy for its controlled delivery and protection against degradation. Full article

Organic and inorganic peroxides can induce intracellular redox homeostasis. In this study, a γ-cyclodextrin/genistein inclusion complex (γ-CD/GEN) was constructed to systematically elucidate the molecular mechanism by which it catalyzes GPx4-mediated peroxide reduction. The results indicate that the incorporation of γ-CD effectively disrupts the aggregated state of GEN, achieving an encapsulation efficiency (EE) exceeding 40%. Surface-enhanced Raman spectroscopy (SERS) analysis reveals significant differences in the catalytic behavior of γ-CD/GEN toward cumene hydroperoxide (CHP) and hydrogen peroxide (H₂O₂): the reduction efficiency of CHP depends on both the concentration of γ-CD/GEN and GPx4, whereas the reduction of H₂O₂ is primarily regulated by the concentration of γ-CD/GEN. Isotope effect studies demonstrate that the reduction of CHP relies more on radical-initiated reactions, while the reduction of H₂O₂ involves proton transfer, with the differences in reduction rates correlating with their respective redox mechanisms. Molecular docking and molecular dynamics simulations further confirm that γ-CD/GEN can stably bind to the Sec (Cys)-46 site in the active center of GPx4, thereby enhancing its catalytic activity. This study provides a theoretical basis for the development of antioxidant strategies based on the precise regulation of enzyme activity. Full article

Water-soluble poly-β-cyclodextrins (PCDs), crosslinked with ethylenediaminetetraacetic acid dianhydride (EDTADA), were synthesized at varying β-CD:EDTADA molar ratios (1:6, 1:9, 1:12, 1:15) to develop multifunctional nanocarriers with the ability to complex drugs, polymers, and ions. All PCDs exhibited nanometric particle sizes (14 to 28 nm), negative zeta potential (−18 to −27 mV), and adjustable content of free carboxyl groups controlled by crosslinker ratio. Functional evaluations demonstrated effective Ca²⁺ chelation and a linear inclusion complexation profile with acyclovir, but not with naproxen, highlighting pH-dependent solubility effects. Additionally, PCDs successfully formed polyelectrolyte complexes with poly-L-lysine, indicating their potential as components of advanced drug delivery systems. Among the analyzed variants, PCD 1:6 showed reduced yields, fewer reactive groups, and diminished ion-binding capacity compared to formulations with higher crosslinker content. These findings underscore the importance of crosslinking density in modulating physicochemical and functional properties and support the potential of EDTA-crosslinked PCDs as versatile platforms for advanced, ion-sensitive biomedical applications. Full article

The selective removal of trace heteroatomic contaminants from fuel remains a critical challenge for clean combustion and refinery upgrading, particularly due to the chemical stability and structural similarity of sulfur- and nitrogen-containing aromatics. Herein, a surface-engineered graphene oxide aerogel functionalized with cyclodextrin (β-CD-CONH-GO) is developed via covalent grafting to introduce well-defined host–guest recognition sites within a porous framework. Spectroscopic and microscopic characterizations confirm successful functionalization, preserved aerogel morphology, and accessible hybrid interfaces. The removal process for monocyclic, bicyclic, and tricyclic impurities is governed by synergistic molecular inclusion within the cyclodextrin cavity, interfacial hydrogen bonding, and secondary confinement provided by the aerogel porosity. Thus, the β-CD-CONH-GO exhibits efficient adsorption toward representative bicyclic impurities, and the removal performance follows the order of indole > quinoline > benzothiophene. Kinetic analysis demonstrates pseudo-second-order adsorption behavior, indicating chemisorption dominated by cooperative host–guest recognition and hydrogen bonding. It possesses removal selectivity even in mixed systems containing structurally similar aliphatic and aromatic competitors and maintains > 95% efficiency after five regeneration cycles via ethanol extraction, confirming superb durability. This study demonstrates a feasible pathway to design adsorbents for deep fuel refining and highlights cyclodextrin-based graphene hybrid aerogels as promising candidates for separations. Full article

Background: Arterial hypertension (AH) remains a global health concern due to its multifactorial etiology, limited therapeutic success, and high cardiovascular risk. In this context, plant-derived compounds such as essential oils have gained attention as alternative strategies. The monoterpene (-)-linalool (LIN) demonstrates antihypertensive effects. However, its clinical application is hampered by poor solubility and low bioavailability. Methods: This study aimed to investigate the chronic cardiovascular effects of free LIN and its inclusion complex with β-cyclodextrin (LIN/β-CD) in spontaneously hypertensive rats (SHR) and normotensive Wistar rats. Results: Pharmacokinetic analysis showed that complexation with β-CD markedly improved LIN plasma exposure, increasing systemic bioavailability by approximately 20-fold and prolonging its circulation time. In acute assays, intravenous LIN and LIN/β-CD (50 mg/kg) reduced blood pressure in SHR, LIN induced bradycardia, and LIN/β-CD elicited a mild, non-significant tachycardia. Orally administered LIN/β-CD exerted superior antihypertensive effects compared to free LIN. In a 60-day chronic regimen, LIN/β-CD consistently maintained reduced arterial pressure, achieving levels comparable to normotensive controls, while free LIN produced transient effects. LIN/β-CD also significantly reduced the cardiac mass index in SHR, suggesting attenuation of hypertrophic remodeling. Vascular reactivity assays revealed enhanced endothelium-dependent and -independent relaxation and diminished vasoconstriction in LIN/β-CD-treated animals, indicating improved endothelial and smooth muscle function. Histological analyses confirmed the absence of cardiac or vascular injury in both treatment groups. Conclusions: In conclusion, the LIN/β-CD complex improves the pharmacokinetic profile and enhances the arterial morphology, antihypertensive and cardioprotective effects of linalool. These findings support its translational potential as a safe and effective oral formulation for the long-term management of hypertension and associated cardiovascular dysfunction. Full article

An important aspect of food technology is that vitamin compounds can be used for a variety of purposes, such as developing methods to enhance the nutritional value of foods. This paper discusses the synthesis and properties of β-cyclodextrin (β-CD)-functionalized silver nanoparticles, and the use of the resulting β-CD-AgNP inclusion complex when loading vitamin D₃ (cholecalciferol, VD₃) molecules. β-Cyclodextrin was used as a reducing agent and a stabilizer in the production of silver nanoparticles. The preparation of VD₃-β-CD-AgNP nanocompositions was confirmed by UV spectroscopy, transmission electron microscopy, and X-ray diffraction spectroscopy. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) revealed that the resulting β-CD-VD₃-AgNP nanocomposite was well dispersed with particle sizes ranging from 6 to 15 nm. ¹H-, ¹³C-NMR and FTIR spectroscopy showed the reduction of silver ions and the formation of β-CD-encapsulated AgNPs. The kinetic parameters of the thermal decomposition reaction of the VD₃-β-CD-AgNP nanocomposition have been determined under nonisothermal conditions that ensure the preservation of the kinetic triplet and a more accurate description of the process. The nanocomposition of VD₃ with silver nanoparticles demonstrated antibacterial activity against the used bacteria. Full article

Dacarbazine (DTIC) is a clinically important anticancer drug whose photosensitivity poses challenges for its stability and interactions with supramolecular hosts. Here, we investigate its complexation with the host 1,10-N,N′-bis-(β-D-ureidocellobiosyl)-4,7,13,16-tetraoxa-1,10-diazacyclooctadecane (TN), a hybrid urea–carbohydrate–diazacrown system, using combined experimental and computational approaches. While TN has been studied as a host molecule, its specific interactions with DTIC and the associated thermodynamic characteristics had not been characterized. Computational results (obtained at the density functional theory level (DFT)) indicate that TN primarily forms non-inclusion complexes, with DTIC engaging in hydrogen bonding with sugar units, urea bridges, and diazacrown ether moieties. Experimental ¹H NMR studies in D₂O confirmed these interaction patterns, showing notable chemical shifts for sugar protons. Conductometric measurements between 293 and 313 K allowed for the determination of formation constants and thermodynamic parameters. The results demonstrate that TN:DTIC complexation is spontaneous, exothermic, and enthalpy-driven, accompanied by decreased system entropy. Comparison with previous studies on cyclodextrin complexes shows that TN forms strong associations with DTIC, owing to its abundant donor–acceptor groups, which facilitate extensive hydrogen-bonding networks. These findings provide new insights into DTIC stabilization and highlight TN’s potential as a multifunctional platform for drug delivery. Full article

The effect of active packaging on maintaining the quality of cherry tomatoes and kale during storage was investigated. The active packaging consisted of kraft paper sheets coated with thymol/eugenol (50:50) encapsulated in β-cyclodextrin. Cherry tomatoes were stored at 10, 15, and 22 °C for 15, 14, and 8 days, respectively, while kale was stored at 2, 8, 15, and 22 °C for 21, 16, 9, and 7 days. Physicochemical (pH, total soluble solids, titratable acidity, colour, and firmness), microbiological (mesophilic, psychrophilic, enterobacteria, moulds, and yeasts) and pigment/bioactive/nutritional (chlorophylls, carotenoids, total phenolic content, vitamin C, and total antioxidant capacity) characteristics were analysed. Active packaging significantly reduced microbial growth, particularly enterobacteria and moulds, in cherry tomatoes and psychrophiles and moulds in kale, without negatively affecting the physicochemical quality. The microbial kinetics were successfully described using the Baranyi–Ratkowsky predictive model, which quantified the effects of temperature and active packaging on microbial growth parameters. This modelling approach revealed that active packaging increased the minimum growth temperature and reduced the specific growth rate of key microbial groups, confirming its inhibitory action under different storage conditions. The use of active packaging slowed colour degradation in kale by reducing chlorophyll loss up to 50% at 22 °C and maintained tomato firmness and colour during storage. Furthermore, a strong correlation (R² = 0.87) between colour index and carotenoid content was found, enabling the non-destructive prediction of ripening in tomatoes. Overall, active packaging enhanced microbial stability, delayed visual deterioration, and sustainably extended the shelf life and post-harvest quality of perishable products, offering a promising alternative to conventional preservation methods. Full article