The biological challenges and pharmacological opportunities of orally administered nanomedicine delivery

Abstract

Nano-scale formulations are being developed to improve the delivery of orally administered medicines, and the interactions between nanoformulations and the gastrointestinal luminal, mucosal and epithelial environment is currently being investigated. The mucosal surface of the gastrointestinal tract is capable of trapping and eliminating large particles and pathogens as part of the natural defences of the body, it is becoming clearer that nanoformulation properties such as particle size, charge, and shape, as well as mucous properties such as viscoelasticity, thickness, density, and turn-over time are all relevant to these interactions. However, progress has been slow to utilise this information to produce effective mucous-penetrating particles. Areas covered: This review focuses on delivery method of nanomedicines both into and across the gastrointestinal mucosal surface, and aims to summarise the biological barriers that exist to successful oral nanomedicine delivery and how these barriers may be investigated and overcome. Expert commentary: Despite successes in the laboratory, no nanotechnology-enabled products are currently in clinical use which either specifically target the intestinal mucous surface or cross the epithelial barrier intact. New nanomedicine-based treatments of local diseases (intestinal cancer, inflammation, infection) and systemic diseases are advancing towards clinical use, and offer genuine opportunities to improve therapy.

Advances in Oral Drug Delivery for Regional Targeting in the Gastrointestinal Tract - Influence of Physiological, Pathophysiological and Pharmaceutical Factors

“…Nanoparticles have a larger surface-area-to-volume ratio, which provides a greater surface area for interaction with the mucosal surface and for the solubilization of drugs. Nanoparticulate dosage forms have shown the following advantages for gastrointestinal drug delivery, owing to their smaller size: (i) easier transport through the GI tract; (ii) more uniform distribution and drug release; (iii) increase in residence time of particles in the GI tract, even when colonic motility is increased in diarrhea; (iv) improved uptake into mucosal tissues and cells; and (v) specific accumulation to the site of disease, such as inflamed tissues (Hua et al, 2015;Moss et al, 2018;Reinholz et al, 2018). Nanoparticles generally undergo cellular uptake via the transcellular pathway in the GI tract (Yu et al, 2016;Reinholz et al, 2018).…”

Gold nanoparticles (GNPs) in biomedical and clinical applications: A review

“…[321,322] Oral drugs based nanocarriers or nanomaterials can be designed for cell-specific absorption, increasing the rate of absorption from the absorption site to the bloodstream, evading biological barriers (e.g., brainblood barriers), and targeted delivery to a specific cell from the bloodstream (Figure 21). [323][324][325][326] GNPs that are administered orally can be designed with a specific gastrointestinal (GI) tract area in mind (i.e., stomach, small intestine, intestinal lymphatic system and colon). [327] Drugs can be conjugated to the surfaces of GNPs through ionic or covalent bonding and delivered via control release via biological stimuli or external light activation via SPR properties.…”

Nanodelivery of Natural Antioxidants: An Anti-aging Perspective

“…Among the most important features of orally administered nanomedicines, it is their capability to overcome the chemical and physical barriers in the gut such as the acidic pH of the stomach, intestinal mucosal lining and selectively permeable membranes of enterocytes (Moss et al, 2018). Physico-chemical characteristics of nanoparticles such as their metabolism, absorption, distribution and excretion depend on their size, hydrophobicity and charge.…”