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Researchers develop novel method to enhance hydrophobic drug

MIT researchers have devised an innovative method to enhance the efficiency of processing and delivering hydrophobic drugs, which often pose challenges due to their poor solubility in water. Published in the journal Advanced Healthcare Materials, the approach involves initially processing drugs in a liquid solution instead of a solid form. This streamlining process aims to improve the bioavailability of hydrophobic drugs, addressing a significant hurdle in their oral administration. As up to 90% of pharmaceutical candidates fall into this category, the impact on could be substantial.

The current drug processing pathway involves a series of sequential steps. The MIT team, led by Professor Patrick Doyle and graduate student Lucas Attia, proposes a more efficient approach by combining these steps and leveraging insights from soft matter and self-assembly processes. Hydrogels, sponge-like gel materials capable of retaining water and holding in place, play a crucial role in the new process. This approach contrasts with conventional methods that mechanically grind crystals to improve solubility, a time-consuming and costly process with limited control over size distribution.

In the novel process, the drug is dissolved in a carrier solution, forming nanodroplets dispersed in a solution (nanoemulsion). This nanoemulsion is then transformed into a hydrogel through a syringe, maintaining the nanodroplets in place as the carrier evaporates. The result is uniform drug nanocrystals with precise control over their size. The hydrogel acts as a safeguard against the merging of droplets, preventing irregularities in particle size.

The process yields a dual-component structure: a core containing active molecules surrounded by a hydrogel shell. This shell, made of hydrogel, enables control over the timing of drug release into the body. The researchers demonstrated precise control over drug release, both in terms of delay and rate. This capability is particularly valuable for drugs targeting specific regions of the digestive system, allowing for controlled release in the lower intestine or colon.

This breakthrough presents a significant advancement, as it represents the first approach capable of forming core-shell composite particles and structuring drugs in distinct polymeric layers in a single processing step. While the researchers anticipate scalability, further testing on a variety of drug molecules is essential. Despite potential scalability challenges, the materials used in the process are recognized as safe for medical use, simplifying the approval process. The researchers are optimistic that this method could be implemented within a few years, offering a promising solution to the challenges posed by hydrophobic drugs in pharmaceutical development.

Source: Massachusetts Institute of Technology

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