 Over-the-counter non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin and ibuprofen are commonly used for reducing pain and fever owing to their distinct anti-inflammatory, analgesic, and antipyretic functions. However, NSAIDs normally have low water-solubility, which leads to a large dosage in medication. After a long-term use, they often develop side effects like gastrointestinal bleeding and ulcers. NSAIDs also need to be taken daily, even for multiple times a day, to maintain the therapeutic level of the drugs inside the body. This work develops a novel strategy enhancing the solubility of NSAIDs and reducing their dependence on patient's compliance in treatment. Multiple NSAIDs are incorporated via biocompatible and biodegradable links into different layers (or generations) of a dendrimer structure to form a drug-tree, which can potentially release the drugs in a sustained manner. To make the dendrimer more water-soluble, hydrophilic carbohydrates are covalently attached to the surface of the dendrimer. This research specifically incorporates salicylic acid into a poly(glycerol-succinic acid) (PGLSA) dendrimer, and sugars including glucose, galactose, and mannose are conjugated onto the termini of the dendrimer to increase the solubility. Such 'sweet' salicylic acid drugtrees can have a well-defined drug capacity, which depends on the generation of the dendrimer, or drugtree, to be synthesized thus the delivery of the drugs can be more controllable for future applications. This novel synthetic strategy can also be applied to make drugtrees from other drugs.

Novel "sweet" water-soluble drugtrees for high efficient slow-released NSAIDs

248th National Meeting (2014)

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