Innovative Formulations for the Controlled and Site-specific Delivery of Antiinflammatory Drugs

Abstract

Pharmaceutical technology has introduced a promising pathway in the future of medicinein particular nanotechnological innovations have provided the opportunity to design and develop efficient drug delivery systems able to target and treat several diseases, including those mediated by inflammation. The engineering of drug delivery systems can be used to target tissues involved in the pathology under treatment, to avoid early drug biological environmental degradation and to modulate drug pharmacokinetics. Glucocorticoids and non-steroidal anti-inflammatory drugs are the most commonly prescribed drug categories worldwide for the treatment of disorders associated with inflammation.Although glucocorticoids can be highly effective in treating inflammation, their systemic application is limited due to the high incidence of serious adverse effects, mainly in long-term treatment. Non-steroidal anti-inflammatory drugs are a heterogeneous group of compounds and most of them have unfavorable pharmacokinetics and pharmacodynamics, leading to adverse effects, such as gastrointestinal disorders. Therefore, the need for drug delivery systems for long term administration of anti-inflammatory drugs witha well-controlled release profile is evident. The aim of this review is to assess innovative colloidal drugs carriers, in particular liposomes and nanoparticles, with special focus on site-specific delivery for particularly problematic tissues such as the gastrointestinal tract, joints and eyes.3

Solid lipid nanoparticles delivering anti-inflammatory drugs to treat inflammatory bowel disease: Effects in anin vivomodel

“…Thanks to pharmaceutical technology, we had the opportunity to develop an efficient drug delivery system able to improve the treatment of such a disease mediated by inflammation[11,46]. The use of a nanoparticulate drug carrier is useful to prevent early drug biological environmental degradation, to modulate drug pharmacokinetics, but also to enhance the treatment selectivity by targeting.…”

“…The use of a nanoparticulate drug carrier is useful to prevent early drug biological environmental degradation, to modulate drug pharmacokinetics, but also to enhance the treatment selectivity by targeting. Indeed, nanoparticles depending on their physico-chemical properties can preferentially accumulate in areas of intestinal inflammation when delivered orally[11,12]. They are particularly well-suited to the treatment of IBD through the local delivery of drugs to areas of inflammation, allowing site-specific delivery and minimizing side effects in other organs.…”

“…Since drugs encounter a harmful environment after oral administration, high doses and/or frequent administration are usual to counter the degradation by stomach acidic pH or small intestine digestive enzymes; on the other hand, the occurrence of side effects are more likely[11,47]. In particular, SLN have been one of most studied carriers worldwide for drug delivery, since this nanosystem is mainly composed of solid lipid core and lecithin, has very low toxicity profile, good affinity for biological membrane, ability to facilitate up-taking/overcoming, and capacity to improve drug pharmacokinetics[48,49].…”

“…Recent advances in nanotechnology have enabled the development of new corticosteroid formulations with a nanometric approach to ameliorate pharmacological properties, resulting in increased efficacy and reduction of side effects[11]. Different from the MMX strategy, the nanoparticle drug delivery strategy relies on the nanosize as the cardinal property for interaction with biological systems.…”

“…It is well-known that nanoparticles are efficiently taken up by immunocompetent cells, so that nanoparticulate drug carriers may be useful in targeting the inflamed regions. Indeed, in the presence of IBD there is a strong cellular immunoresponse from the inflamed regions, and the nanoparticle passive targeting may allow for the accumulation of the drug loaded into the nanoparticulate carrier in the inflamed area[11]. …”