Drug targeting systems for inflammatory disease: One for all, all for one

Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

“…So, in inflammation sites the permeability of the vasculature is increased allowing the penetration to the interstitial site of particles that normally wouldn't be able to pass through the vasculature [77,78]. This process is generally known as the Enhanced Permeability and Retention (EPR) effect [77,79].…”

“…For this, the drug system size is an important factor and must be between approximately 50 kDa and 200 nm in order to pass through the vessels by the EPR effect and also avoiding glomerular filtration [79]. The circulation time of these systems is also important since long circulation times will increase its accumulation on the inflammation site [79].…”

“…Particles that are too big to be cleared renally will be fagocyted in the liver and spleen, however the therapeutic consequences of this are more complex when we talk of macrophage passive targeting since particles with sizes superior to 200 nm are taken up by macrophages [77,79].…”

Recent progress in nanomedicine: therapeutic, diagnostic and theranostic applications

“…Regarding the former, it is important to note that in recent years, increasing numbers of efforts have been initiated in which therapeutic nanomedicines are used for drug targeting to non-cancerous disorders, including e.g. rheumatoid arthritis and atherosclerosis [12,14,[21][22][23]. As mentioned above, also inflammatory diseases are characterized by leaky blood vessels, and the accumulation of long-circulating nanotherapeutics within such lesions (via 'site-specific drug delivery'), together with their ability to attenuate localization in healthy non-target tissues ('site-avoidance drug delivery'), enables the use of potent anti-inflammatory agents, such as corticosteroids, at much higher i.v.…”

Targeted therapeutics in inflammatory atherosclerosis

“…These "flaring" molecules drive lesion remodeling, invasiveness (and metastasis in the case of cancer), and can induce a phenotypical change in preexisting macrophages and other cells [230][231][232]. Thus, preventing macrophage activation and dampening local inflammation by using nanomedicines to deliver anti-inflammatory drugs can induce a favorable phenotype [233]. Glucocorticoids are potent anti-inflammatory drugs, which, however, generally come with severe side effects upon prolonged use [234].…”