Nanoparticles could help smuggle1 drugs into the gut2(内脏,肠子) , according to a study published this month in the International Journal of Nanotechnology. There are several drugs that would have more beneficial therapeutic3 effects if they could be targeted at absorption by the lower intestine4(肠) . However, in order to target the colon5 for treating colon cancer for instance, medication delivered by mouth must surmount6(克服,战胜) several barriers including stomach acidity7, binding8 to mucus(黏液) layers, rapid clearance9 from the gut, and premature10 uptake by cells higher up the gastrointestinal tract11(胃肠道) . Being able to deliver a drug by mouth has several benefits over injection or suppository: ease of dosing, for instance, and better patient compliance12.
Various methods have been tried, including coating drug molecules14 with a polymer shell. However, Kevin P. O'Donnell and Robert O. Williams III of the Division of Pharmaceutics15, at The University of Texas at Austin, have reviewed the various techniques on offer and suggest that encapsulating a drug molecule13 within nanoparticles offers the best option for controlling drug delivery and targeting the colon.
The Texas team has reviewed the state of the art in nanotechnology for delivery of therapeutic agents to the colon. They explain that advances in particle engineering techniques have recently made it possible to made drug products on the nanoscale. Techniques such as spray drying, antisolvent methods, dialysis methods, emulsion(乳剂) methods and cryogenic(冷冻的) methods are all now available for drug formulation. Converting a drug powder into nanoparticles can often render a compound that is poorly soluble16 in water soluble or increase bioavailability simply through an increase in the surface area to volume ratio. Smaller particles mean a bigger surface area to interact with absorbing surfaces in the gastrointestinal tract. Indeed, fatty but solid nanoparticles of the compound quercetin (a health supplement) are absorbed almost 6 times more effectively by the gut in nanoparticle form than the common drug suspension formulation.
The researchers explain that nanoparticle drug delivery could be particularly beneficial for patients suffering from inflammatory bowel17 diseases including Crohn's Disease, ulcerative colitis(溃疡性结肠炎) and irritable18 bowel syndrome19, all which often require long-term treatment. However, they also add that because there are no digestive enzymes20 in the colon and its neutral pH it is a prime target for the delivery of therapeutic proteins, peptides(多肽类,缩氨酸) , viral vectors, and nucleotides(核苷酸) for a wide range of disease not simply those associated with the colon.