Cyclodextrins as reliable solubilizationtools for BCS class II and IV drugs

Title : Cyclodextrins as reliable solubilizationtools for BCS class II and IV drugs

Abstract:

In recent years, formulator’s attention was focusing on cyclodextrins as a solubilizing tool for their stubborn APIs (BCS class II and IV)). The reason is obvious: easy to scale up and a successful presence of APIs solubilized with cyclodextrins as both liquid and solid dosage form, on the market. This presentation is centered on a coherent approach of insoluble APIs solubilization by cyclodextrincomplexation in liquid phase and as solid dispersions (by kneading, spray drying, lyophilization and physical mix) through case studies (carbamazepine, danazol, albendazole, furosemide, zotepine, zaleplon, lorazepam, NSAIDs, etc.). Based on physical and chemical properties of your API , specifically : how many atoms (C, P, S, and N ) the skeleton of the drug molecule holds, how many condensed rings, water solubility ,melting point temperature, molecular weight ,electrostatic charge, log P, pKa, stability issues (chemical, photo, etc.) it is easy to decide if cyclodextrins are the answer to its solubilization. If solubilization optimization is not needed for a good performance of your API and you still wonder “why cyclodextrincomplexation?“ you should to not forget that they can additionally offer: increased stability (physical, chemical), masked taste /odor, convert liquid forms into amorphous powders, new formulation, new routs of administration, patent extension increased shelf life, etc. Cyclodextrins in biotechnology are a very efficient tool in preparation of widespread use of serum-free and chemically defined (CD) media by replacing FBS (fetal bovine serum) by solubilizing cholesterol and fatty acids for supplementation of cell culture.
Takeaway Notes
•Based on physical and chemical properties of your API, dose and route of administration you can decide even in preformulation stage if cyclodextrins can solubilize your API
•Identify the type of cyclodextrin and the most efficient process suitable for your API formulation
•Summarize the advantages and cyclodextrin flexibility in liquid and solid dispersions formulation and scaling up processes

Biography:

Dr. Carmen Popescu got her B.S. degree in Physics and Ph.D. in Biophysics at University of Bucharest, Romania. She is a Senior Project Coordinator at Roquette America Inc., located in Geneva, Illinois. She came to USA in 1999, as an Associate Professor with University of Illinois at Chicago, College of Pharmacy where she is still an Adjunct Associate Professor. In her career, she focused on the development of classic dosage forms (liquid, semi-solid and solid dosage forms formulation) as well as drug delivery systems (microparticles, nanoparticles, liposomes, niozome) for small and large molecules. She has published over 120 research papers, book chapters and presentations. You can find her publications on: https://www.researchgate.net/profile/Carmen_Popescu3

She is also an Adjunct Associate Professor with Roosevelt University and University of Tennessee. She is teaching in “Tablets & Capsules Hands-on Short Course” at Univ. of Maryland and “Hands-on Tablet Technology Course “at Univ. of Mississippi.