Preparation, Characterization and In vitro Biological activity of 5-Fluorouracil Loaded onto poly (D, L-lactic-co-glycolic acid) Nanoparticles

Abstract

Nanoscale devices offer a lot of potential in drug delivery because of their small size. The goal of this work was to increase the oral bioavailability of the anti-cancer hydrophilic drug as 5-fluorouracil (5-FU) by incorporating it into poly (D, L-lactide-co-glycolide) nanoparticles (PLGNPs) using the double emulsion process, 5-FU- PLGNPs nanoparticles were created. Various factors, such as drug, polymer, and stabilizer concentrations, were investigated for assembly in order to arrive at the most effective formulation of 5-FU-PLGNPs. PLGNPs had a drug encapsulation efficiency of 9.75 to 24.8%. The prepared nanoparticles had a spherical shape and an average size of 212.3–285 nm, as shown by TEM. The dispersion of the drug into the prepared PLGNPs was confirmed by XRPD and FTIR. The optimized nanoparticles (F225) had high encapsulation efficiency 24.8 ± 0.21%, low particles size 212.3 ± 48.2 nm with an appropriate PDI value of 0.448, and ZP of − 48.3 ± 2.7 mV. The molecular dispersion of the medication within the system was validated by thermal behavior studies (DSC). In vitro drug release from the best-selected formulations revealed a sustained release of nanoparticles, with slower release reported when lower PVA concentrations were utilized. Three 5-FU-PLGNPs formulations were tested for anticancer efficacy against cell cultures of HCT-116 (human colorectal carcinoma), MCF-7 (human breast carcinoma), and HepG2 (human hepatocellular carcinoma). The created formulations were examined for in vitro cytotoxic activity, revealing that they appeared to be promising effective anticancer formulations when compared to the positive controlled (doxorubicin).

Fabrication and Evaluation of Poloxamer Facilitated, Glyceryl Monooleate based 5-Fluorouracil Cubosomes

“…It is clear that the DSC thermogram of 5-Fluorouracil shows a single sharp endothermic peak at 280-285°C, which is related to a study reported previously. 34,[39][40][41] GMO and poloxamer have shown endotherms at around 30-35 and 55-60°C. Furthermore, the thermogram of 5-Fluorouracil loaded cubosomes has shown a border peak between 30-60°C, that night has shown the presence of both GMO and poloxamer, however, the sharp characteristic endotherm 5-FU has been converted into a broader peak, confirming that drug now, has been captured by the cubosomes of GMO, assisted by poloxamer 407.…”

“…Thus, confirming the crystalline nature of the drug. 34 The intense peaks were greatly diffused and their intensity has been reduced to a great extent, hence indicating the encapsulation of the drug in cubosomes. Few less intense peaks could be due to the presence of some un-entrapped drug molecules that might be present on the surface (Figure 6).…”

In-vitro cytotoxic studies of 1-hexylcarbamoyl-5-fluorouracil encapsulated nanogels in BMG-1 cells

“…Coating with polysorbate80 enhances the uptake of nanoparticles encapsulating various drugs by brain tissue as compared to the control group of uncoated nanoparticles. 19,20 At the moment we speculate that the coating of nanoparticles with polysorbate80 leads to the specific alteration of the surface properties. 16 This new surface then seems to adsorb certain substances from blood that, in turn, induce endocytotic uptake by brain endothelial cells.…”