Overview
Sulfobutylether-β-Cyclodextrin (SBE-β-CD) is a sulfobutyl ether derivative of β-cyclodextrin, engineered to enhance the solubility and stability of poorly water-soluble drugs. Developed as a safer alternative to earlier cyclodextrins, it is commercially known as Captisol® and is widely adopted in FDA-approved injectable formulations. Its anionic nature and high solubility (unlike native β-cyclodextrin) make it ideal for complexing hydrophobic active pharmaceutical ingredients (APIs), enabling higher drug loading and reduced toxicity. The degree of substitution (DS) typically ranges between 6.2–6.9 sulfobutyl groups per cyclodextrin molecule, ensuring optimal performance.
Physical and Chemical Properties
SBE-β-CD exhibits exceptional water solubility (>50 g/100 mL at 25°C), attributed to the sulfobutyl groups that disrupt its crystalline structure. This property is critical for parenteral formulations where high concentrations are required. The compound is stable under physiological pH (2–10) and resists enzymatic degradation. Thermogravimetric analysis shows decomposition above 250°C without a distinct melting point. Its solubilization capacity stems from a hydrophobic cavity (7.8 Å diameter) that encapsulates nonpolar drug molecules, while the sulfobutyl exterior enhances aqueous compatibility. Nuclear magnetic resonance (NMR) studies confirm its amorphous powder form.
Main Applications
In pharmaceuticals, SBE-β-CD is pivotal for solubilizing antivirals (e.g., remdesivir), antifungals, and oncology drugs. It forms non-covalent inclusion complexes, improving bioavailability and reducing injection-site irritation. Over 10 FDA-approved therapies utilize Captisol®, including Vyxeos® (daunorubicin/cytarabine) and Nexterone® (amiodarone). Beyond drug delivery, it stabilizes proteins in biopharmaceuticals and masks unpleasant tastes in oral formulations. Cosmetic applications include fragrance encapsulation and skin permeation enhancement. Research explores its use in gene delivery and diagnostic imaging contrast agents.
Safety and Storage
SBE-β-CD is classified as GRAS (Generally Recognized As Safe) for oral and intravenous use, with LD50 values >2 g/kg in rodents. Unlike β-cyclodextrin, it causes negligible hemolysis or nephrotoxicity due to its anionic charge and rapid renal excretion. Storage requires protection from humidity (hygroscopic) and temperatures exceeding 25°C to prevent clumping. Bulk packaging should use double-layer polyethylene bags with desiccants. Occupational exposure limits are not established, but dust control measures (e.g., PPE, ventilation) are recommended during handling.
B2B Procurement Guide
Pharmaceutical-grade SBE-β-CD must meet USP/NF or EP monographs, with certificates of analysis (CoA) specifying substitution degree (DS), residual solvents, and endotoxin levels. Drug master files (DMFs) are available for regulatory support. Pricing varies by DS (higher DS increases cost) and order volume. Contract manufacturing organizations (CMOs) often provide custom DS optimization. Key suppliers include Ligand Pharmaceuticals (Captisol®), CycloLab, and Wuhan Yuancheng. For injectables, prioritize suppliers with cGMP certification and ISO 13485 compliance.
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