Abstract
BackgroundThe use of drug nanocarriers to encapsulate drugs for oral administration may become an important strategy in addressing the challenging oral absorption of some drugs. In this study—with the premise of controlling single variables—we prepared model nanoparticles with different particle sizes, surface charges, and surface hydrophobicity/hydrophilicity. The two key stages of intestinal nanoparticles (NPs) absorption—the intestinal mucus layer penetration stage and the trans-intestinal epithelial cell stage—were decoupled and analyzed. The intestinal absorption of each group of model NPs was then investigated.ResultsDifferences in the behavioral trends of NPs in each stage of intestinal absorption were found to result from differences in particle properties. Small size, low-magnitude negative charge, and moderate hydrophilicity helped NPs pass through the small intestinal mucus layer more easily. Once through the mucus layer, an appropriate size, positive surface charge, and hydrophobic properties helped NPs complete the process of transintestinal epithelial cell transport.ConclusionsTo achieve high drug bioavailability, the basic properties of the delivery system must be suitable for overcoming the physiological barrier of the gastrointestinal tract.
Highlights
The use of drug nanocarriers to encapsulate drugs for oral administration may become an important strategy in addressing the challenging oral absorption of some drugs
Extensive clinical studies have been conducted on nanoparticle delivery systems, and many particle-based formulations and technologies have been introduced into the clinic
Characterization of model NPs In this study, polystyrene nanoparticles, water-soluble chitosan nanoparticles, and (PEG-)Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were used as model NPs representing the particle size group, zeta potential group, and surface hydrophobicity/ hydrophilicity group, respectively
Summary
The use of drug nanocarriers to encapsulate drugs for oral administration may become an important strategy in addressing the challenging oral absorption of some drugs. Various nano preparations, including polymer nanoparticles, have been used in drug delivery research to improve bioavailability, solubility, and drug retention time, as well as to reduce drug side effects, such as toxicity. Extensive clinical studies have been conducted on nanoparticle delivery systems, and many particle-based formulations and technologies have been introduced into the clinic. Local, topical, and systemic (such as intravenous) administration are all approved by the US Food and Drug Administration (FDA) for delivery of nanoparticles/microparticles [4]. More than 50 nano pharmaceutical preparations have been approved for clinical use, and more than 400 are expected to become new clinical solutions alone or in combination with other key enabling technologies [5,6,7,8,9]
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