Oral nanoparticles

Researchers from Brigham and Women's Hospital and the Massachusetts Institute of Technology have developed targeted nanoparticles that could enable the oral delivery of biologics such as insulin.1 The clinical translation of the approach will require identifying a suitable therapeutic payload and fine-tuning the pharmacology of the system.

Poor intestinal absorption prevents the oral delivery of many compounds and virtually all biologics. Factors that affect oral bioavailability include stability and size, as peptide therapeutics generally are degraded in the GI tract and large molecules cannot be passively absorbed through the intestinal epithelium.

Several companies have tried to develop oral delivery methods for biologics. In 2006, an oral insulin tablet from Emisphere Technologies Inc.

failed in a Phase II trial in type 2 diabetes. In 2011, Emisphere and partners Nordic Bioscience A/S and Novartis AG discontinued development of the oral salmon calcitonin biologic SMC021 after it failed several Phase III trials in osteoarthritis and osteoporosis.

Emisphere is now using its Eligen oral drug delivery platform, which consists of binding small molecules to the therapeutic of interest to

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