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

Abstract

AIMTo improve anti-inflammatory activity while reducing drug doses, we developed a nanoformulation carrying dexamethasone and butyrate.METHODSDexamethasone cholesteryl butyrate-solid lipid nanoparticles (DxCb-SLN) were obtained with the warm microemulsion method. The anti-inflammatory activity of this novel nanoformulation has been investigated in vitro (cell adhesion to human vascular endothelial cells and pro-inflammatory cytokine release by lipopolysaccharide-induced polymorphonuclear cells) and in vivo (disease activity index and cytokine plasma concentrations in a dextran sulfate sodium-induced mouse colitis) models. Each drug was also administered separately to compare its effects with those induced by their co-administration in SLN at the same concentrations.RESULTSDxCb-SLN at the lowest concentration tested (Dx 2.5 nmol/L and Cb 0.1 μmol/L) were able to exert a more than additive effect compared to the sum of the individual effects of each drug, inducing a significant in vitro inhibition of cell adhesion and a significant decrease of pro-inflammatory cytokine (IL-1β and TNF-α) in both in vitro and in vivo models. Notably, only the DxCb nanoformulation administration was able to achieve a significant cytokine decrease compared to the cytokine plasma concentration of the untreated mice with dextran sulfate sodium-induced colitis. Specifically, DxCb-SLN induced a IL-1β plasma concentration of 61.77% ± 3.19%, whereas Dx or Cb used separately induced a concentration of 90.0% ± 2.8% and 91.40% ± 7.5%, respectively; DxCb-SLN induced a TNF-α plasma concentration of 30.8% ± 8.9%, whereas Dx or Cb used separately induced ones of 99.5% ± 4.9% and 71.1% ± 10.9%, respectively.CONCLUSIONOur results indicate that the co-administration of dexamethasone and butyrate by nanoparticles may be beneficial for inflammatory bowel disease treatment.

Improved uptake and therapeutic intervention of curcumin via designing binary lipid nanoparticulate formulation for oral delivery in inflammatory bowel disorder

“…pH and ionic strength of GIT fluid destabilizes nanoparticulate formulations and potentially leads to aggregation after oral administration of formulations. The perspectives of binary lipid nanoparticulate formulations like higher lymphatic uptake, sustained drug release and drug protection are linked to their nanosize [26][27][28]. Thus, evaluation of nanoparticulate formulation for particle size, zeta potential and dispersibility in simulated GIT environment is imperative.…”

“…They are colloidal carriers socializing the benefits of polymeric nanoparticles, emulsions and liposomes. SLNs encompasses the fundamental benefits like excellent biocompatibility, high drug loading potential, controlled release, biodegradability, improved pharmacokinetic profile, physical stability and scalability [25][26][27][28]. Nano size range and lipid composition of SLNs contribute to their higher uptake from Peyer's patches [29].…”

“…Nano size range and lipid composition of SLNs contribute to their higher uptake from Peyer's patches [29]. SLNs loaded with various therapeutically active molecules had displayed significant reduction in induction and penetration of immune-related cells during IBD compared to drug alone [25,27,30]. However, characteristic features of SLNs like drug pay load efficacy, physical stability and release behaviour are governed by crystallinity and polymorphic behaviour of lipid.…”

Topical Solid Lipid Nanoparticles Based Gel of Lavender Essential Oil for Anti‑inflammatory Activity

“…The size of nanoparticles was counted using PixelPro software. The particle size was checked in a triplicate manner [12,13].…”

Effect of Mn3O4 Nanoparticles on Lipopolysaccharide-Induced Inflammatory Factors in the Human Tendon Cells and Its Mechanism

“…International Journal of Polymer Science tendon collagen [9]. In recent years, with the in-depth study of nanoparticles, its important role in the treatment of inflammation-related diseases has also been confirmed [10]. Mn 3 O 4 NPs, as nanomaterials with enzyme-like activity, display good therapeutic potential in the treatment of inflammatory diseases.…”