PLGA Based Nanospheres as a Potent Macrophage-Specific Drug Delivery System

Abstract

Macrophages possess an innate ability to scavenge heterogenous objects from the systemic circulation and to regulate inflammatory diseases in various organs via cytokine production. That makes them attractive targets for nanomedicine-based therapeutic approaches to inflammatory diseases. In the present study, we have prepared several different poly(lactic-co-glycolic acid) (PLGA) polymer nanospheres for macrophage-targeted drug delivery using both nanoprecipitation and emulsification solvent evaporation methods. Two experimental linear PLGA polymers with relatively low molar weight, one experimental branched PLGA with unique star-like molecular architecture, and a commercially available PLGA, were used for nanosphere formulation and compared to their macrophage uptake capacity. The nanosphere formulations labelled with loaded fluorescent dye Rhodamine B were further tested in mouse bone marrow-derived macrophages and in hepatocyte cell lines AML-12, HepG2. We found that nanospheres larger than 100 nm prepared using nanoprecipitation significantly enhanced distribution of fluorescent dye selectively into macrophages. No effects of nanospheres on cellular viability were observed. Additionally, no significant proinflammatory effect after macrophage exposure to nanospheres was detected as assessed by a determination of proinflammatory cytokines Il-1β and Tnfα mRNA. All experimental PLGA nanoformulations surpassed the nanospheres obtained with the commercially available polymer taken as a control in their capacity as macrophage-specific carriers.

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

“…The organic phase was added drop wisely to 10 mL of aqueous phase containing various concentrations of PVA (%w/v) ( Table 1 ) under intense sonication using an ultrasonic probe (Cole-Parmer Model 50 Cp T 4710 Series, USA) for 2 minutes followed by cooling in ice bath. 19 The formulated o/w emulsions were gently stirred for 2–3 hrs of solvent evaporation. GPS-PLGA NSs pellets were then collected by centrifugation (Hettich Microliter Centrifuge MIKRO 220, Germany) at 15,000 rpm and - 4°C for 20 minutes.…”

“…GPS-PLGA NSs pellets were then collected by centrifugation (Hettich Microliter Centrifuge MIKRO 220, Germany) at 15,000 rpm and - 4°C for 20 minutes. Two additional centrifugation cycles were performed after the dispersion of the collected pellets in 10 mL of purified water to remove residuals of PVA and then NSs pellets were finally redispersed 19 for further characterization. Unloaded placebo NSs were similarly prepared without the addition of GPS in the organic phase ( Table 1 ).…”

Broad-Spectrum Theranostics and Biomedical Application of Functionalized Nanomaterials

“…They are prepared using several methods including emulsification–evaporation, nanoprecipitation, etc., using biodegradable polymer materials including chitosan, gelatin and PLA. They are spherical matrices where the biological active compounds are distributed evenly and released to the environment with the help of the diffusion process [ 102 ]. They are important tools for drug delivery, with a high loading capacity for hydrophobic drugs, and they effectively protect the drugs from enzymatic and chemical degradation.…”

Stimuli-Responsive Polymeric Nanoplatforms for Cancer Therapy

“…Most have relatively narrow size distributions with diameters ranging from 10 to 200 nm. Boltnarova et al have prepared polymer nanospheres based on PLGA with low molar weight for macrophage-targeted drug delivery using both nanoprecipitation and emulsification solvent evaporation methods, which serves as a compelling, biodegradable and biocompatible drug delivery platform for macrophages (Boltnarova et al, 2021).…”