Modulation of Macrophages M1/M2 Polarization Using Carbohydrate-Functionalized Polymeric Nanoparticles

Abstract

Exploiting surface endocytosis receptors using carbohydrate-conjugated nanocarriers brings outstanding approaches to an efficient delivery towards a specific target. Macrophages are cells of innate immunity found throughout the body. Plasticity of macrophages is evidenced by alterations in phenotypic polarization in response to stimuli, and is associated with changes in effector molecules, receptor expression, and cytokine profile. M1-polarized macrophages are involved in pro-inflammatory responses while M2 macrophages are capable of anti-inflammatory response and tissue repair. Modulation of macrophages’ activation state is an effective approach for several disease therapies, mediated by carbohydrate-coated nanocarriers. In this review, polymeric nanocarriers targeting macrophages are described in terms of production methods and conjugation strategies, highlighting the role of mannose receptor in the polarization of macrophages, and targeting approaches for infectious diseases, cancer immunotherapy, and prevention. Translation of this nanomedicine approach still requires further elucidation of the interaction mechanism between nanocarriers and macrophages towards clinical applications.

Hyaluronated and PEGylated Liposomes as a Potential Drug-Delivery Strategy to Specifically Target Liver Cancer and Inflammatory Cells

“…In contrast with some literature [ 27 , 28 ] and with the results obtained in liver cancer cells, we observed a rapid internalization of PEGylated liposomes in THP-1 cells, with a plateau being reached after 1 h of incubation (approximately 85%), compared with the other formulations ( Figure 5 A). In addition, the presence of PEG seems to improve the cellular uptake efficiency of HA 4800 liposomes ( Figure 5 A), suggesting that the addition of PEG to liposomes can modify their properties, making them more visible to phagocytic cells.…”

“…In fact, when evaluating liposomes that were conjugated with either HA or PEG (5%) with human and murine macrophage cell lines, we observed a significant difference between the uptake of HA-modified liposomes and PEGylated liposomes, with there being a rapid increase in the internalization of PEG-coated liposomes in THP-1 and RAW264.7. Although our data are in conflict with literature data reporting that PEG chains reduce the internalization of liposomes by the mononuclear phagocytic system [ 27 , 28 ], they seem to be potentially relevant. In fact, limited PEGylated-liposome internalization was observed in HepG2 cells ( Supplementary Figure S1 , which is why it was not further investigated in cancer cells), meaning that the selective targeting of multiple cellular targets for drug delivery is a real possibility.…”

Fluorescent PLGA Nanocarriers for Pulmonary Administration: Influence of the Surface Charge

“…The formation of aggregates has been shown to alter the behavior of the NPs and have an impact on their cellular uptake [ 21 , 22 ], biodistribution [ 23 ], or toxicity [ 24 ]. NPs’ aggregation and flocculation in complex biological media is mainly due to the presence of ionic salts and biomolecules, which can adsorb on the NPs’ surface and induce clustering [ 25 ]. Particle aggregation can be overcome by introducing either steric hindrance or electrostatic repulsion between the NPs.…”

Defining Endocytic Pathways of Fucoidan-Coated PIBCA Nanoparticles from the Design of their Surface Architecture

“…At present, incomplete understanding of the influence of the nanoparticle properties on their interactions with cells is a bottleneck to improving the design of carriers so that they can deliver their cargo to the desired intracellular compartment. Although this is a challenging subject, a better understanding on how the endocytic pathways of a nanomaterial can be manipulated by its properties would certainly open up tremendous perspectives towards achieving more efficient and precise intracellular delivery of drugs ( 3 , 5 , 14 , 15 ).…”