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4.4: Transportation Dilemmas

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    211481
  • Scientists are solving the dilemma of drug delivery with a variety of other clever techniques. Many of the techniques are geared toward sneaking through the cellular gate-keeping systems' membranes. The challenge is a chemistry problem—most drugs are water-soluble, but membranes are oily. Water and oil don't mix, and thus many drugs can't enter the cell. To make matters worse, size matters too. Membranes are usually constructed to permit the entry of only small nutrients and hormones, often through private cellular alleyways called transporters.

    Many pharmacologists are working hard to devise ways to work not against, but with nature, by learning how to hijack molecular transporters to shuttle drugs into cells. Gordon Amidon, a pharmaceutical chemist at the University of Michigan-Ann Arbor, has been studying one particular transporter in mucosal membranes lining the digestive tract. The transporter, called hPEPT1, normally serves the body by ferrying small, electrically charged particles and small protein pieces called peptides into and out of the intestines.

    Amidon and other researchers discovered that certain medicines, such as the antibiotic penicillin and certain types of drugs used to treat high blood pressure and heart failure, also travel into the intestines via hPEPT1. Recent experiments revealed that the herpes drug Valtrex® and the AIDS drug Retrovir® also hitch a ride into intestinal cells using the hPEPT1 transporter. Amidon wants to extend this list by synthesizing hundreds of different molecules and testing them for their ability to use hPEPT1 and other similar transporters. Recent advances in molecular biology, genomics, and bioinformatics have sped the search for molecules that Amidon and other researchers can test.

    Scientists are also trying to slip molecules through membranes by cloaking them in disguise. Steven Regen of Lehigh University in Bethlehem, Pennsylvania, has manufactured miniature chemical umbrellas that close around and shield a molecule when it encounters a fatty membrane and then spread open in the watery environment inside a cell. So far, Regen has only used test molecules, not actual drugs, but he has succeeded in getting molecules that resemble small segments of DNA across membranes. The ability to do this in humans could be a crucial step in successfully delivering therapeutic molecules to cells via gene therapy.

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