Cyclodextrin-Mediated Drug Products

Integral BioSystems scientists have worked on cyclodextrin-containing products for multiple products, including intravenous and ocular injectables as well as ophthalmic eye-drops for hydrophobic, water-insoluble products. Contact us for a fee-for-service collaboration to develop an injectable or an eye-drop. 

“Both α-CD (Alphadex) and β-CD (Betadex) are listed in the European Pharmacopoeia (Ph.Eur.) and γ-CD is referenced in the Japanese Pharmaceutical Codex (JPC) and will be included in the Ph.Eur. A monograph for HP-β-CD (Hydroxypropyl-betadex) is available in the Ph.Eur. In 2000-2004, α-CD, β-CD and γ-CD were introduced into the generally regarded as safe (GRAS) list of the FDA for use as a food additive. Alpha- and beta-CD are approved as novel food ingredients by the Commission. Beta-CD is approved in Europe as a food additive (E 459) with an ADI (acceptable daily intake) of 5 mg/kg/day. SBE-β-CD and HP-β-CD are cited in the FDA’s list of Inactive Pharmaceutical Ingredient”, excerpt from European Medicines Agency, 9 October 2017, EMA/CHMP/ 333892/2013, Committee for Human Medicinal Products.

Cyclodextrin-Mediated Drug Products
Cyclodextrin-Mediated Drug Products formula

In the example below, use of cyclodextrins solubilized and stabilized a highly hydrophobic drug to achieve its target solubility of 25 mg/mL. In aqueous solutions, the drug was soluble to < 100 micrograms/mL. 

API in cyclodextrin T0 and T5 days
cyclodextrin solubility data
  • Can solubilize to high concentrations of API
  • 1:10 weight ratio of API : SBEβCD solubilizes and protects
  • pH of solution is ~3.4 (unbuffered) after 5 days
  • NO CHANGE IN 5 DAYS AT 25℃ with 1:10 API/SBEβCD weight ratio

 

To date, Integral has developed injectable dose forms of 5 hydrophobic drugs, as 505b2, NCE and 505b3 (generic) products. Additionally, Integral has developed eye-drop formulations containing HPβCD and SBβCD.

 

Collaborate with Our Experts in Cyclodextrin-Mediated Drug Products

Ready to harness the power of cyclodextrin-mediated drug  products to enhance solubility and stability for your hydrophobic drugs? Contact Integral BioSystems today for a fee-for-service collaboration to develop injectables or eye-drops tailored to your specific needs. Let’s leverage our expertise to bring your drug formulations to the next level, ensuring efficacy and compliance. Take the next step towards innovative drug delivery solutions with Integral BioSystems as your trusted partner!