New pharmaceutical manufacturing process improves bioavailability of poorly soluble drugs
Solubility of pharmaceuticals is crucial to absorption by the human intestine and, ultimately, efficacy of the drug. Over 90% of new chemical entities being considered for drug development have low solubility. Amorphous solid dispersions (ASDs) are a common way to enhance solubility of compounds for drugs. Current methods for forming ASDs require a high ratio of polymer to drug which decreases disintegration time and limits the amount of drug that can be loaded into a single pill.
The Williams Lab at The University of Texas at Austin has designed a new method for making ASDs that can enhance solubility and achieve high drug loading. This technique incorporates of highly porous carriers without the use of solvents. The resulting novel formulations have high drug loading, enhanced solubility, and favorable dissolution. This technique makes it possible to formulate orally available dosages of BCS class 2 and 4 drugs that are normally insoluble in water. Many BCS class 2 and 4 drugs have promising therapeutic potential if an effective dose can be delivered. For practical oral administration, these drugs need high drug loading and must be able to rapidly dissolve in the gut. As proof of concept, the research team has demonstrated the ability to formulate small-size tablets with an ideal dissolution profiles for poorly soluble drugs indomethacin1 and itraconazole2. The Williams lab is looking for industry partnerships to improve drug delivery of other poorly soluble compounds in development.
1. Hanada, M. et al., J Pharm Sci, 2018 Jan;107(1):362-371. https://doi.org/10.1016/j.xphs.2017.09.025
2. Hanada, M. et al., Mol. Pharmaceutics, 2021, 18, 1, 198-213. https://doi.org/10.1021/acs.molpharmaceut.0c00811