Mannose-decorated ginsenoside Rb1 albumin nanoparticles for targeted anti-inflammatory therapy

Abstract

Ginsenoside Rb1 is a potential anti-inflammatory natural molecule, but its therapeutic efficacy was tremendously hampered by the low solubility and non-targeted delivery. In this study, we innovatively developed a mannose (Man)-modified albumin bovine serum albumin carrier (Man-BSA) to overcome the previously mentioned dilemmas of Rb1. The constructed Man-BSA@Rb1 NPs could improve the solubility and increase the cellular uptake of Rb1, finally leading to the enhanced anti-inflammatory effects. The robust therapeutics of Man-BSA@Rb1 NPs were measured in terms of nitrite, tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6) levels, which might be achieved by potently inhibiting nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways in lipopolysaccharide (LPS)-induced Raw264.7 cells. Moreover, the therapeutic efficacy of Man-BSA@Rb1 NPs was further confirmed in the d-Gal/LPS-induced liver injury model. The results indicated that Man-BSA may offer a promising system to improve the anti-inflammatory therapy of Rb1.

Inflammation-Targeted Drug Delivery Strategies via Albumin-Based Systems

“…Man modified BSA (Man-BSA) has been developed to overcome the dilemma of Rb1. The constructed Man-BSA@Rb1 NPs can increase the solubility of Rb1, increase the uptake of Rb1 by cells, and ultimately enhance its anti-inflammatory effect . Methotrexate (MTX) was loaded into mannose-modified human serum albumin (MTX-M-NPs) nanoparticles to target neutrophils.…”

“…The constructed Man-BSA@Rb1 NPs can increase the solubility of Rb1, increase the uptake of Rb1 by cells, and ultimately enhance its anti-inflammatory effect. 101 Methotrexate (MTX) was loaded into mannose-modified human serum albumin (MTX-M-NPs) nanoparticles to target neutrophils. The absorption of MTX-M-NPs by neutrophils was significantly better than that of the same nanoparticles without mannose.…”

Development of nanoparticle‐based drug delivery system for inflammation treatment and diagnosis

“…To attain an inflammatory targeting effect, ligands of pro‐inflammatory macrophage derived receptors including hyaluronic acid to bind with the CD44 receptor and mannose to recognize mannose receptor will improve the anti‐inflammatory therapy of the vectors 76,105 . Macrophages play an important role in the formation of atherosclerotic plaque and phosphatidylserine (PtdSer) mediates the engulfment of foreign matters by macrophages through the classical “eat me” signaling 106 .…”

“…To attain an inflammatory targeting effect, ligands of pro-inflammatory macrophage derived receptors including hyaluronic acid to bind with the CD44 receptor and mannose to recognize mannose receptor will improve the anti-inflammatory therapy of the vectors. 76,105 Macrophages play an important role in the formation of atherosclerotic plaque and phosphatidylserine (PtdSer) mediates the engulfment of foreign matters by macrophages through the classical "eat me" signaling. 106 PtdSer-decorated liposomes loaded with a peroxisome proliferator-activated receptor γ agonist were synthesized to suppress macrophage function, and these liposomes effectively targeted to atherosclerotic plaques and impeded the progression of atherosclerosis relative to the nontargeted control.…”

Preparation, characterization and in vivo pharmacokinetic study of ginsenoside Rb1-PLGA nanoparticles

“…The hydrophilic sugar moieties form the external surface, interacting with the surrounding solvent to establish the aggregates, while the hydrophobic segments remain sequestered internally, resulting in the formation of nanoparticles (NPs). This arrangement enhances the water solubility of GRb1, facilitating its transport within the body 20 , 21 .…”