Methyl-Beta-Cyclodextrin

Ding Y, et al. Journal of Molecular Structure, 2025, 1321, 140105.

In the aqueous solution method, trimethoprim dissolved in glacial acetic acid was combined with an aqueous solution of M-β-CD at 60 °C under vigorous stirring (900 rpm) for 6 hours. After cooling and sequential processing steps-filtration, freezing at –20 °C, and lyophilization-a dry powder complex was obtained, demonstrating the ability of M-β-CD to form host–guest complexes under mild thermal conditions.

In the ultrasonic-assisted approach, the same reactants were subjected to ultrasound at 80% power for 1 hour. This technique significantly enhanced molecular interaction through acoustic cavitation, promoting rapid inclusion and uniform encapsulation. Post-treatment involved refrigeration, removal of the acetic acid, filtration, freezing, and freeze-drying to isolate the complex.

In the microwave-assisted synthesis, M-β-CD and trimethoprim were reacted under intermittent microwave irradiation (10 min heating and 5 min interval cycles) for 30 minutes, enabling efficient energy transfer and expedited complexation. The final product was similarly processed by filtration, freezing, and lyophilization.

Liu C, et al. Carbohydrate Polymer Technologies and Applications, 2025, 9, 100636.

Methyl-beta-cyclodextrin (M-β-CD) was utilized to improve the solubility and stability of Urolithin B (UB) through the formation of an inclusion complex. The UB–M-β-CD inclusion complex was synthesized using a modified solution-stirring method. M-β-CD (45 g) was dissolved in 300 mL of heated distilled water, followed by the gradual addition of UB (2.443 g) dissolved in acetone. Stirring at 800 rpm for 8 hours at 85°C ensured effective interaction and encapsulation. The acetone was evaporated, and unencapsulated UB was removed via filtration through a 0.45-µm membrane. The complex was then frozen at −80°C and lyophilized at −50°C under vacuum, yielding 42.006 g of lyophilized powder (88.54% yield).

Jadhav K, et al. Journal of Controlled Release, 2025, 378, 671-686.

Methyl-beta-cyclodextrin (M-β-CD) was employed as a key excipient in the development of nasal powder formulations for isoniazid (INH) and rifampicin (RIF), two essential anti-tubercular drugs. A phase solubility study confirmed the inclusion complex formation between M-β-CD and RIF, enhancing its solubility and stability. INH- and RIF-loaded microparticles (INH-MP and RIF-MP) were synthesized via spray drying, where M-β-CD served as a polymeric carrier. For INH-MP, 100 mg of M-β-CD was dissolved in water, followed by the addition of 20 mg INH. RIF-MP preparation involved dissolving RIF in isopropyl alcohol before introducing it into an aqueous M-β-CD solution under continuous mechanical stirring. Both formulations maintained a 1:5 drug-to-polymer ratio (w/w) and a total solid content of 2% (w/v). Spray drying was conducted at an inlet temperature of 100–150 °C, with optimized flow rates ensuring the formation of stable microparticles.

Xu M, et al. Molecular Pharmaceutics, 2024, 21(12), 6109-6122.

Methyl-β-cyclodextrin (MβCD) significantly enhances the intracellular accumulation of α-linolenic acid-paclitaxel conjugate nanoparticles (ALA-PTX NPs) by modulating membrane dynamics and lysosomal stability. Through plasma membrane cholesterol depletion, MβCD increases membrane fluidity, facilitating clathrin-mediated endocytosis and promoting the uptake of ALA-PTX NPs by HepG2 tumor cells. Additionally, MβCD disrupts lysosomal integrity, reducing ALA-PTX NP degradation and ensuring greater cytosolic drug release. In vivo studies in tumor-bearing mice demonstrated that MβCD markedly improves the antitumor activity of ALA-PTX NPs, highlighting its potential as a nanomedicine enhancer. Notably, MβCD selectively enhances the uptake of polyunsaturated fatty acid (PUFA)-conjugated paclitaxel nanoparticles, a property not observed in traditional paclitaxel liposomes unless co-administered with ALA-PTX NPs. These findings suggest that MβCD, in combination with PUFA-conjugated nanomedicines, offers a promising strategy for optimizing intracellular drug delivery and improving therapeutic outcomes in cancer treatment.

Zhang Y, et al. Industrial Crops and Products, 2024, 209, 117974.

Methyl-beta-cyclodextrin (MβCD) enhances the solubility and processability of betulin by forming an inclusion complex. In this study, a 200% (w/v) aqueous MβCD solution was prepared by dissolving 2 g of MβCD in 1 mL of ultrapure water. Betulin was incorporated at a 1:2 molar ratio (betulin:MβCD), and the mixture was stirred for 12 hours at 25°C to form a Betulin/MβCD inclusion complex (Betulin/MβCD-IC). The Betulin/MβCD-IC solution was then utilized for electrospinning to fabricate nanofibers. Under controlled environmental conditions (25°C, 18% relative humidity), the electrospinning process was conducted using a 17 kV applied voltage, a 0.5 mL/h solution injection rate, and a 17 cm needle-to-collector distance. The resultant Betulin/MβCD-IC nanofibers (Betulin/MβCD-IC-NF) were successfully collected and sealed for further applications. This study underscores the role of MβCD in improving the aqueous dispersibility of hydrophobic bioactives like betulin, enabling their integration into electrospun nanofiber systems for biomedical and pharmaceutical applications.