The application of Sulfobutyl ether beta-cyclodextrin (SEβCD)

Market trend Cyclodextrin 1,4-BS (1,4-Butane Sultone) Pharmaceutical manufacturer solubility

 

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 1633-83-6). 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:

Oral medication:

  • It has been used in Famotidine, a medicine used to treat stomach diseases, to increase water solubility and mask the bitter taste of Famotidine. [2]
  • It has been used to increase the solubility of steroid drugs in water and increase the bioavailability of these hydrophobic APIs. [3]
  • It has been used in the hormone drug raloxifene (Raloxifene (RXF)) to increase water solubility and overcome absorption barriers.[4]
  • It has been used in pharmaceutical formulations containing Diminazene Aceturate (DA) to overcome the rate of degradation in gastric acid.[13]
  • It has been used in the second-generation antipsychotic iloperidone (ILO) to improve its solubility.[14]

Eye drop:

  • It has been used in a prodrug for the treatment of glaucoma-Pilocarpine rue eye drops to improve eye tolerance.[6]
  • It has been proven to extend the residence time of the drug in the cornea and improve bioavailability.[7]

Nasal sprays:

  • It has been used in thalidomide nasal powder, a medicine for the treatment of nasal mucosal microvascular diseases, to improve the solubility of thalidomide nasal powder in the nasal mucosa.[8]

Pulmonary drug delivery:

  • It has been used as a therapeutic drug for pulmonary inhalation to improve the stability and water solubility of resveratrol.[9]

Intravenous injection:

  • There are many FDA-approved injections on the market that contain SβECD, which is mainly used as a solubilizer.[10]
  • It has been used in antiviral injection: Remdesivir (REM), as a solubilizer.[10]

Topical medication:

  • It has been used in an iontophoresis drug-propofol, which can increase the passive permeation flux of propofol.[11]
  • Acyclovir, a vaginal drug used to treat herpes simplex virus type 2 (HSV-2), is used to improve antiviral efficacy.[12]

Further reading:What is Cyclodextrin

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Reference:

[1]Utility of Sulfobutyl Ether beta-Cyclodextrin Inclusion Complexes in Drug Delivery: A Review https://www.ijpsonline.com/articles/utility-of-sulfobutyl-ether-betacyclodextrin-inclusion-complexes-in-drug-delivery-a-review-3659.html

[2]Enhancement of the Aqueous Solubility and Masking the Bitter Taste of Famotidine Using Drug/SBE-β-CyD/Povidone K30 Complexation Approach https://jpharmsci.org/article/S0022-3549(15)32460-6/abstract

[3]Solubilizing steroidal drugs by β-cyclodextrin derivatives https://pubmed.ncbi.nlm.nih.gov/28743551/

[4]Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement https://www.mdpi.com/1999-4923/10/3/76

[5]Cyclodextrins as Drug Carrier Molecule: A Review https://www.mdpi.com/2218-0532/76/4/567

[6]Sulfobutyl Ether β-Cyclodextrin (SBE-β-CD) in Eyedrops Improves the Tolerability of a Topically Applied Pilocarpine Prodrug in Rabbits https://www.liebertpub.com/doi/abs/10.1089/jop.1995.11.95

[7]Chloramphenicol/sulfobutyl ether-β-cyclodextrin complexes in an ophthalmic delivery system: prolonged residence time and enhanced bioavailability in the conjunctival sac https://www.tandfonline.com/doi/abs/10.1080/17425247.2019.1609447

[8]Role of New Antifungal Agents in the Treatment of Invasive Fungal Infections in Transplant Recipients: Isavuconazole and New Posaconazole Formulations https://www.mdpi.com/2309-608X/1/3/345/htm

[9]Cyclodextrin Complexation for Enhanced Stability and Non-invasive Pulmonary Delivery of Resveratrol—Applications in Non-small Cell Lung Cancer Treatment https://link.springer.com/article/10.1208/s12249-020-01724-x

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

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

[12]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

[13]β-Cyclodextrin as a Functional Excipient Used for Enhancing the Diminazene Aceturate Bioavailability https://doi.org/10.3390/pharmaceutics11060295

[14]Inclusion Complex of Iloperidone with Sulfobutyl Ether Beta-Cyclodextrin: Characterization and Dissolution Studies https://www.mdpi.com/2504-3900/78/1/22

Release date：2021.05.10

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