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D-amino acids boost the selectivity and confer supramolecular hydrogels of a nonsteroidal anti-inflammatory drug (NSAID).

Journal of the American Chemical Society (2012-11-10)
Jiayang Li, Yi Kuang, Yuan Gao, Xuewen Du, Junfeng Shi, Bing Xu
RESUMEN

As systemically used therapeutics for treating acute or chronic pains or inflammations, nonsteroidal anti-inflammatory drugs (NSAIDs) also associate with the adverse gastrointestinal and renal effects and cardiovascular risks. Thus, it is beneficial to develop topical gels that selectively inhibit cyclooxygenase-2 (COX-2) for the management of local inflammation. In this work, we demonstrate that the covalent conjugation of d-amino acids to naproxen (i.e., a NSAID) not only affords supramolecular hydrogelators for the topical gels but also unexpectedly and significantly elevates the selectivity toward COX-2 about 20× at little expense of the activity of naproxen. This work illustrates a previously unexplored approach that employs d-amino acids for the development of functional molecules that have dual or multiple roles and exceptional biostability, which offers a new class of molecular hydrogels of therapeutic agents.

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Naproxen, 98%
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Naproxen, Pharmaceutical Secondary Standard; Certified Reference Material
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Naproxen solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material, Cerilliant®
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Naproxen, meets USP testing specifications
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Naproxen, European Pharmacopoeia (EP) Reference Standard
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Naproxene, VETRANAL®, analytical standard
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