Search Results (1,979)

Folic acid (FA) and its structural analog, anticancer medicine methotrexate (MTX), are known to form host/guest complexes with native cyclodextrins, of which the most stable are formed with the medium-sized β-cyclodextrin. Based on our research, proving that simple sugars (D-glucose, D-galactose, and D-mannose) can form adducts with folic acid, we envisioned that combining these two types of molecular receptors (cyclodextrin and simple carbohydrates) into one may be beneficial for the complexation of FA and MTX. We designed and obtained host/guest inclusion complexes of FA and MTX with two monoderivatives of β-cyclodextrin—substituted at position 6 with monosaccharide (glucose, G-β-CD) and disaccharide (maltose, Ma-β-CD). The complexation was proved by experimental (NMR, UV-vis, IR, TG, DSC) and theoretical methods. We proved that derivatization of β-cyclodextrin with glucose and maltose has a significant impact on the complexation with FA and MTX, as the addition of one glucose subunit to the structure of the receptor significantly increases the value of association constant for both FA/G-β-CD and MTX/G-β-CD, while further extending a pendant chain (incorporation of maltose subunit) results in no additional changes. Full article

Most chemotherapeutic agents are poorly soluble in water, have low selectivity, and cannot reach the tumor in the desired therapeutic concentration. On the other hand, sensitive hydrophilic therapeutics like nucleic acids and proteins suffer from poor bioavailability and cell internalization. To solve this problem, new types of controlled release systems based on nano-sized self-assemblies of cyclodextrins able to control the speed, timing, and location of therapeutic release are being developed. Cyclodextrins are macrocyclic oligosaccharides characterized by a high synthetic plasticity and potential for derivatization. Introduction of new hydrophobic and/or hydrophilic domains and/or formation of nano-assemblies with therapeutic load extends the use of CDs beyond the tried-and-tested CD-drug host–guest inclusion complexes. The recent advances in nano drug delivery have indicated the benefits of the hybrid amphiphilic CD nanosystems over individual CD and polymer components. This review provides a comprehensive overview of the most recent advances in the design of CDs self-assemblies and their use for delivery of a wide range of therapeutic molecules. It aims to offer a valuable insight into the many roles of CDs within this class of drug nanocarriers as well as current challenges and future perspectives. Full article

Cyclodextrins are ring-shaped sugars used as additives in medications to improve solubility, stability, and sensory characteristics. Despite being widespread, Chagas disease is neglected because of the limitations of available medications. This study aims to review the compounds used in the formation of inclusion complexes for the treatment of Chagas disease, analyzing the incorporated compounds and advancements in related studies. The databases consulted include Scielo, Scopus, ScienceDirect, PubMed, LILACS, and Embase. The keywords used were “cyclodextrin AND Chagas AND disease” and “cyclodextrin complex against Trypanosoma cruzi”. Additionally, a statistical analysis of studies on Chagas disease over the last five years was conducted, highlighting the importance of research in this area. This review focused on articles that emphasize how cyclodextrins can improve the bioavailability, therapeutic action, toxicity, and solubility of medications. Initially, 380 articles were identified with the keyword “cyclodextrin AND Chagas disease”; 356 were excluded for not being directly related to the topic, using the keyword “cyclodextrin complex against Trypanosoma cruzi”. Over the last five years, a total of 13,075 studies on Chagas disease treatment were found in our literature analysis. The studies also showed interest in molecules derived from natural products and vegetable oils. Research on cyclodextrins, particularly in the context of Chagas disease treatment, has advanced significantly, with studies highlighting the efficacy of molecules in cyclodextrin complexes and indicating promising advances in disease treatment. Full article

The use of cyclodextrins in textiles for the development of biofunctional fabrics represents an interesting alternative for the advancement of dental, medical, and hospital materials. Cyclodextrins can interact with the chemical groups present in cotton fibers, leading to the formation of a nanostructured surface with specific functional properties, including antibacterial activity. Although there are numerous antibacterial textile finishes, the use of methylene blue as a cyclodextrin host molecule for photodynamic applications in textile materials remains to be investigated. This is because methylene blue is a photosensitive dye capable of generating singlet oxygen (¹O₂) when illuminated, which inactivates the pathogenic microorganisms that may be present in wounds. The objective of this study was to develop a biofunctionalized and photoactivatable cotton fabric with antimicrobial properties for use in the cosmetic or medical industries. The materials obtained were characterized via scanning electron microscopy (SEM), Fourier transform infrared spectroscopy with attenuated total reflection (FTIR-ATR), the determination of cotton fabric functionalization dyeing variables, colorimetry, UV-VIS spectrophotometry, degradation of 9,10-anthracenediyl-bis(methylene)dimalonic acid (ABDA), photodegradation tests, and microbiological analysis. The results showed that the textile was functionalized with β-cyclodextrin, mainly evidenced by the appearance of the band at 1730 cm⁻¹, indicating the formation of the ester group. Thus, when exposed to light, the non-functionalized material showed greater photobleaching, about 60%, compared to the material treated with cyclodextrin. This result was also reflected in the ABDA degradation kinetics, with the treated material showing 592.00% (first phase) and 966.20% (second phase) higher degradation than the untreated sample. Finally, the photodynamic activity was determined based on the antimicrobial properties of the textile, showing a reduction of more than 99% without exposure to light and 100% when exposed to light. It is believed that this study could open avenues for future research and the development of antimicrobial fabrics, as well as demonstrate the efficiency of the treatment with cyclodextrin in relation to photobleaching. Full article

Anemia is a global health problem that affects both adults and children, but treatment is hampered by serious side effects, primarily associated with the gastrointestinal tract with oral administration of drugs. In this study, we aimed to develop an oral form of iron compounds using polymethylsilsesquioxane hydrogels. To boost loading efficiency and prolong release, the iron compounds (FeCl₃ and ferrous D-Gluconate) are incorporated into a guest–host complex with 2-hydroxypropyl-beta-cyclodextrin. We used PRXD, SEM, EDX mapping, and FTIR to investigate the complex formation, as well as the incorporation of such complexes into hydrogels. The optimal system underlines a combination of ferrous D-Gluconate and HPCD in a 1:1 molar ratio, embedded into a hydrogel with a modest quantity of silicate crosslinks. We demonstrated the slowing of iron release in a gastric media. Mathematical investigation revealed that the Higuchi mechanism releases iron from the hydrogel. Full article

Inhalable formulations with cyclodextrins (CDs) as solubility and absorption enhancers show promise for pulmonary delivery. Thiolated hydroxypropyl-β-cyclodextrin (HP-β-CD-SH) has mucoadhesive properties, enhancing drug absorption. Moreover, it has self-aggregation capability, which could further improve absorption and drug stability, as well as reduce irritation. This study aims to stabilize CD nanoaggregates using bifunctional cross-linkers and evaluate their benefits for lung drug delivery compared to pristine HP-β-CD-SH. Methods: The effectiveness of cross-linked HP-β-CD-SH nanoparticles (HP-β-CD-SH-NP) was compared to transient nanoaggregates in enhancing the activity of dexamethasone (DMS) and olive leaf extracts (OLE). DMS, a poorly soluble drug commonly used in lung treatments, and OLE, known for its antioxidant properties, were chosen. Drug-loaded HP-β-CD-SH-NP were prepared and nebulized onto a lung epithelial Air–Liquid Interface (ALI) model, assessing drug permeation and activity. Results: HP-β-CD-SH with 25% thiolation was synthesized via microwave reaction, forming 150 nm nanoaggregates and stabilized 400 nm HP-β-CD-SH-NP. All carriers showed good complexing ability with DMS and OLE and were biocompatible in the lung ALI model. HP-β-CD-SH promoted DMS absorption, while stabilized HP-β-CD-SH-NP protected against oxidative stress. Conclusion: HP-β-CD-SH is promising for lung delivery, especially as stabilized nanoaggregates, offering versatile administration for labile molecules like natural extracts. Full article

Background: The need for efficient and simplified techniques for seafood traceability is growing. This study proposes the Biolog EcoPlate assay as an innovative method for assessing wild and farmed Sparus aurata traceability, offering advantages over other molecular techniques in terms of technical simplicity. Methods: The Biolog EcoPlate assay, known for its high-throughput capabilities in microbial ecology, was utilized to evaluate the functional diversity of microbial communities from various organs of S. aurata (seabream) from the Mediterranean area. Samples were taken from the anterior and posterior gut, cloaca swabs and gills to distinguish between farmed and wild-caught individuals. The analysis focused on color development in OmniLog Units for specific carbon sources at 48 h. Results: Gills provided the most accurate clusterization of sample origin. The assay monitored the development of color for carbon sources such as α-cyclodextrin, D-cellobiose, glycogen, α-D-lactose, L-threonine and L-phenylalanine. A mock experiment using principal component analysis (PCA) successfully identified the origin of a blind sample. Shannon and Simpson indexes were used to statistically assess the diversity, reflecting the clusterization of different organ samples; Conclusions: The Biolog EcoPlate assay proves to be a quick, cost-effective method for discriminate S. aurata traceability (wild vs. farmed), demonstrating reliable reproducibility and effective differentiation between farmed and wild-caught seabream. Full article

A novel ophthalmic delivery system utilizing levofloxacin-loaded, preservative-free, nanofiber-based inserts was investigated. Polyvinyl alcohol (PVA) and Poloxamer 407 (Polox)were employed as matrix materials, while hydroxypropyl-beta-cyclodextrin (HP-β-CD) was a solubilizer. The formulations were prepared via electrospinning and characterized for fiber morphology, drug dissolution, cytotoxicity, and antimicrobial activity. Scanning electron microscopy confirmed uniform fibrous structures. Fourier Transform Infrared spectroscopy and X-ray diffraction analyses demonstrated the amorphous state of levofloxacin within the fibers. In vitro dissolution studies revealed a rapid (within 2 min) and complete drug release, with higher HP-β-CD levels slightly delaying the release. Cytotoxicity tests showed increased HP-β-CD concentrations induced irritation, that was mitigated by sodium hyaluronate. The antimicrobial efficacy of the nanofibers was comparable to conventional eye drops, with lower minimum inhibitory concentrations for most tested strains. The nanofibrous formulation prepared from a PVA–Polox-based viscous solution of the drug:CD 1:1 mol ratio, containing 0.4% (w/w) sodium hyaluronate) was identified as a particularly promising alternative formulation due to its rapid and complete dissolution, good biocompatibility, and effective antimicrobial properties. Its gelling properties indicate that the residence time on the eye surface can be increased, potentially reducing discomfort and enhancing therapeutic outcomes. The nanofibrous formulations enhanced antimicrobial efficacy, providing a preservative-free alternative that minimizes the potential eye irritation that might occur because of the preservative agent and reduces the administrated dose frequency by extending the drug’s retention time on the eye’s surface. Subsequently, it improves patients’ adherence, which would reflect positively on the bioavailability. The levofloxacin-HP-β-CD nanofibers demonstrate promise as an alternative to traditional eye drops, offering advantages in solubility, stability, and patient compliance for ocular infection treatment. Full article

Immunoglobulin A (IgA) is a major gut antibody that coats commensal gut bacteria and contributes to shaping a stable gut bacterial composition. Although previous studies have shown that cyclic oligosaccharides, including cyclic nigerosyl-1,6-nigerose (CNN) and cyclodextrins (CDs, including αCD, βCD, and γCD), alter the gut bacterial composition, it remains unclear whether cyclic oligosaccharides modify the IgA coating of gut bacteria, which relates to cyclic oligosaccharide-induced alteration of the gut bacterial composition. To address this issue, mice were maintained for 12 weeks on diets containing CNN, αCD, βCD, or γCD; the animals’ feces were evaluated for their bacterial composition and the IgA coating index (ICI), a measure of the degree of IgA coating of bacteria. We observed that the intake of each cyclic oligosaccharide altered the gut bacterial composition, with changes in the ICI found at both the phylum and genus levels. The ICI for Bacillota, Lachnospiraceae NK4A136 group, UC Lachnospiraceae, and Tuzzerella were significantly and positively correlated with the relative abundance (RA) in total bacteria for these bacteria; in contrast, significant correlations were not seen for other phyla and genera. Our observations suggest that cyclic oligosaccharide-induced modulation of the IgA coating of gut bacteria may partly relate to changes in the community structure of the gut bacteria. Full article

In this study, a novel oral formulation of berberine hydrochloride (BBH) hydrogel was successfully synthesized through physical cross-linking using chitosan (CS) and carboxymethyl-β-cyclodextrin (CMCD). The characterization results confirmed the successful synthesis of the CS/CMCD hydrogel and the subsequent loading of BBH into this composite (CS/CMCD/BBH) was effectively accomplished. The BBH was used as a model drug and the resulting hydrogel demonstrated a sustained drug release profile. In addition to its improved solubility and sustained release characteristics, the hydrogel exhibited excellent antibacterial activity against common pathogens such as Escherichia coli (E. coli), Staphylococcus aureus (S. aureus), and Candida albicans (C. albicans). Additionally, in vitro studies indicated that the hydrogel was not cytotoxic to NIH3T3 and HaCaT cells, suggesting its safety for biomedical applications. This lack of cytotoxic effects, combined with the mechanical strength, solubility improvements, and antibacterial properties of the hydrogel, positions the CS/CMCD/BBH hydrogel as a promising candidate for the effective oral delivery of BBH. By addressing the solubility and delivery challenges of BBH, this hydrogel offers a viable solution for the oral administration of BBH, with potential applications in various biomedical fields. Full article

Efficient delivery of therapeutic agents to the lesion site or specific cells is an important way to achieve “toxicity reduction and efficacy enhancement”. Macrocycles have always provided many novel ideas for drug or gene loading and delivery processes. Specifically, macrocycles represented by crown ethers, cyclodextrins, cucurbit[n]urils, calix[n]arenes, and pillar[n]arenes have unique properties, which are different cavity structures, good biocompatibility, and good stability. Benefited from these diverse properties, a variety of supramolecular drug delivery systems can be designed and constructed to effectively improve the physical and chemical properties of guest molecules as needed. This review provides an outlook on the current application status and main limitations of macrocycles in supramolecular drug delivery systems. Full article

Cilostazol is a phosphodiesterase III inhibitor characterized by poor solubility. This limitation can be overcome by using a drug carrier capable of delivering the drug to the target site. Cyclodextrins are essential as drug carriers because of their outstanding complexation abilities and their capacity to improve drug bioavailability. This study comprises two stages: The first involves verifying different cyclodextrins and their complexation abilities towards cilostazol. This was accomplished using molecular docking simulations (MDS) and density functional theory (DFT). Both techniques indicate that the largest Sulfobutyl Ether-β-Cyclodextrin forms the most stable complex with cilostazol. Additionally, other important parameters of the complex are described, including binding sites, dominant interactions, and thermodynamic parameters such as complexation enthalpy, Gibbs free energy, and Gibbs free energy of solvation. The second stage involves a binding study between cilostazol and Phosphodiesterse3 (PDE3). This study was conducted using molecular docking simulations, and the most important energetic parameters are detailed. This is the first such report, and we believe that the results of our predictions will pave the way for future drug development efforts using cyclodextrin–cilostazol complexes as potential therapeutics. Full article

The diversity of cyclodextrins and their derivatives is increasing with continuous research. In addition to monomolecular cyclodextrins with different branched chains, cyclodextrin-based polymers have emerged. The aim of this review is to summarize these innovations, with a special focus on the study of applications of cyclodextrins and their derivatives in nano-delivery systems. The areas covered include nanospheres, nano-sponges, nanogels, cyclodextrin metal–organic frameworks, liposomes, and emulsions, providing a comprehensive and in-depth understanding of the design and development of nano-delivery systems. Full article

The aim of this study was to develop functional composite edible films or coatings for fruit preservation by the addition of bioactive components in combinations that have not yet been thoroughly studied, according to the relevant literature. Edible films were initially composed of (i) chitosan (CH), cellulose nanocrystals (CNC) and beta-cyclodextrin (CD) (50%-37.5%-12.5% ratio), and (ii) hydroxypropyl methylcellulose (HPMC), cellulose nanocrystals (CNC) and beta-cyclodextrin (CD) (50%-37.5%-12.5% ratio). The bioactive components incorporated (5, 10 and 15% v/v) were as follows: (i) pomace oil-based nanoemulsion (NE) aiming to enhance barrier properties, and (ii) caffeine (C), aiming to enhance the antioxidant activity of films, respectively. Indeed, NE addition led to very high barrier properties (low oxygen and water vapor permeability), increased flexibility and reduced color. Furthermore, the contribution of these coatings to fresh strawberries’ preservation under cold storage was investigated, with very promising results concerning weight loss, color difference, and preservation of fruit moisture and quantity of O₂ and CO₂ inside the packages. Additionally, C addition led to very high antioxidant activity, reduced color and improved barrier properties. Finally, the contribution of these coatings to avocado’s preservation under cold storage was investigated, with very encouraging results for color difference, hardness and peroxide value of the fruit samples. Full article

In order to enhance the quality of hot air drying for Tartary buckwheat sprouts and minimize the loss of active substances, this research explored the impact of Color Protection(CP), Osmosis(OM), Blanching (BC), β-cyclodextrin (β-CD), and Ultrasound (US) in conjunction with hot air drying on the color, nutritional value, antioxidant properties, and other attributes of Tartary buckwheat sprouts. The findings revealed that as the drying temperature increased from 50 °C to 70 °C, the drying duration for Tartary buckwheat sprouts decreased across all treatment groups, leading to a higher dehydration rate. Treatments involving CP, US, and BC effectively reduced the drying time of Tartary buckwheat sprouts. Sprouts subjected to CP, β-CD, and US treatments exhibited elevated L* values and decreased a* values and displayed a more vibrant green color. When exposed to a hot air setting of 60 °C, the total flavonoid content in the CP, OM, β-CD, and US groups increased by 8.76%, 6.76%, 12.34%, and 4.25%, respectively, compared to the Control Group (CK). The application of the CP, OM, β-CD, and US treatments enhanced the sprouts’ ability to combat ABTS and DPPH free radicals. Notably, under hot air conditions of 60 °C, the β-CD treatment demonstrated the most effective quality preservation during the hot air drying process for sprouts. This study provides valuable insights into the drying behavior of Tartary buckwheat sprouts and offers guidance for optimizing the drying procedures in industrial settings. Tartary buckwheat sprouts contain a variety of polyphenols and have a high water content. The study of changes in active components such as polyphenols and their alteration mechanisms in Tartary buckwheat sprouts under different processing methods is particularly important for the development of sprout processing. Full article