Improving Bioavailability & Solubility

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Drug Development & delivery published on the virtual 2020 Global Drug Bioavailability Enhancement Summit, which this past December showcased novel technologies and platforms aimed at addressing bioavailability and solubility challenges. These included techniques like elec­trospinning, mesoporous silica technology, physiochemical optimization, amorphous nanoparticle engineering, pharmacokinetic modeling and cyclodextrin complexation. And the end goal is the same: Save time and money while accelerating formulation devel­opment.

The cyclodextrin technology is introduced by István Puskás, research chemist at CycloLab. In addition to solubility enhancement, cyclodextrins are also applied to replace some outdated, toxic, irritative inactive in­gredients. “For example, SBECD-con­taining busulfan formulation does not contain toxic excipient N,N-dimethy­lacetamide and allergizing polyethyl­ene glycol, which are both present in the traditional marketed product,” he says. “SBECD can replace irritating polysorbate 80 in docetaxel prepara­tions. Cyclodextrins may prevent the formation of toxic degradation products compared to classical solubilizing agents, ensuring a higher patient safety profile. Melphalan in SBECD complex shows superior chemical sta­bility over its traditional propylene gly­col-based formulation, and similarly due to the presence of SBECD, fos­phenytoin owns significantly longer shelf life as well.”

In a current project, Recipharm is supporting a cus­tomer with a formulation for safety studies. By applying its own screening platform, Recipharm has been able to rap­idly develop an appropriately optimized formulation solu­tion, combining pH adjustment and complexation by cyclodextrin – says Torkel Gren, Senior Director, Technology Officer & Strategic Investments at Recipharm.

SPECIAL FEATURE – Improving Bioavailability & Solubility: Each Molecule Is Unique. Drug Development & delivery, March 2021


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