The application of Betadex Sulfobutyl ether sodium (SEβCD)

What is Sulfobutyl ether beta-cyclodextrin (SEβCD)?

Sulfobutyl ether beta-cyclodextrin (SEβCD) is a Cyclodextrin derivative synthesized by β-Cyclodextrin and 1,4-BS(1,4-Butane Sultone) (CAS 182410-00-0. Sulfobutylether-β-cyclodextrin (SBE-β-CD) is a derivative of cyclodextrin. It is a white to off-white, practically odorless, crystalline powder. SBE-β-CD is widely used in the pharmaceutical and other industries due to its solubilizing and stabilizing properties. With its unique structure, SBE-β-CD forms inclusion complexes with various molecules, enhancing their solubility and bioavailability.

Due to the low solubility of β-Cyclodextrin, long-term storage may lead to drug precipitation; and it is nephrotoxic and lacks flexibility in the application of parenteral administration, so it was modified to Sulfobutyl ether beta-cyclodextrin (SEβCD), effectively reduces the nephrotoxicity of β-Cyclodextrin and improves the solubility and blood compatibility, which promotes its excellent bioavailability and good tolerance in clinical use. It has also been approved for use in a number of pharmaceutical excipients by the United States Pharmacopoeia and the European Pharmacopoeia.

Sulfobutyl ether beta-cyclodextrin (SEβCD) has excellent stability, permeability, solubility, low toxicity, and bioavailability. In addition, it can control the release time of the drug by placing drug molecules in the inner cavity, so that Sulfobutyl ether beta-cyclodextrin(SEβCD) is widely used in oral medicines, eye drops, nasal sprays, pulmonary drug delivery (PDD), intravenous injection, and topical skin medicine. The following will summarize the performance and the application of Sulfobutyl ether beta-cyclodextrin (SEβCD) in clinical drug:

Intravenous injection: 

• There are many FDA-approved injections on the market that contain SβECD, which is mainly used as a solubilizer.[1]
• It has been used in antiviral injection: Remdesivir (REM), as a solubilizer.[1]

Topical medication:

• It has been used in an iontophoresis drug-propofol, which can increase the passive permeation flux of propofol.[2]
• Acyclovir, a vaginal drug used to treat herpes simplex virus type 2 (HSV-2), is used to improve antiviral efficacy.[3]

Sulfobutyl ether beta-cyclodextrin sodium (SBECD) has been used in several medications, including:

1. Itraconazole Injection: This antifungal medication benefits from SBECD as a solubilizing agent.
2. Voriconazole Injection: Another antifungal medication utilizing SBECD for solubility enhancement.
3. Pimavanserin Tablets: Used to treat Parkinson's disease-related psychosis, SBECD is employed to improve solubility in this medication.
4. Droperidol Injection: Used to prevent postoperative nausea and vomiting, SBECD is also included in the formulation of this medication.

It's important to note that the application of Sulfobutyl ether beta-cyclodextrin sodium in medications can vary based on the specific characteristics of the drug and its formulation. Additionally, as time progresses, there may be additional medications utilizing SBECD to enhance solubility and bioavailability.

Application Overview:

Pharmaceutical Industry:

SBE-β-CD is extensively used in pharmaceutical formulations to improve the solubility and stability of poorly soluble drugs.

It aids in enhancing the bioavailability of active pharmaceutical ingredients (APIs) through the formation of inclusion complexes, thereby improving drug delivery and efficacy.

SBE-β-CD is employed in various dosage forms such as oral solutions, injections, and nasal sprays.

[1] Sulfobutylether-beta-cyclodextrin-enabled antiviral remdesivir: Characterization of electrospun- and lyophilized formulations https://www.sciencedirect.com/science/article/pii/S0144861721003982#bib0075

[2] Transdermal iontophoretic delivery of a liquid lipophilic drug by complexation with an anionic cyclodextrin https://www.sciencedirect.com/science/article/abs/pii/S0168365914004131

[3] Acyclovir-loaded sulfobutyl ether-β-cyclodextrin decorated chitosan nanodroplets for the local treatment of HSV-2 infections https://www.sciencedirect.com/science/article/abs/pii/S0378517320306608