Preparation andin vitroevaluation of 5-fluorouracil-loaded PCL nanoparticles for colon cancer treatment

Abstract

Nanoparticles loaded with 5-fluorouracil (5-FU) for colon cancer therapies were prepared using the solvent evaporation technique, which involved lyophilization by freeze-drying. Formulations produced a substantially high encapsulation efficiency of approximately 93%. A positive correlation was seen when increasing polycaprolactone (PCL) and/or PVA concentrations and the size of nanoparticles produced. Increasing PCL concentration had a considerable influence on PDI while increasing PVA concentration had a lesser effect. All nanoparticles possessed a negative zeta potential, particularly in formulations with low polymer and polymer emulsifier concentrations. The formulation with the lowest PCL and PVA concentration was characterized by the most optimal properties; which accounts for the desirable delayed release profile of the active drug in dissolution testing indicating an improved targeting capability and enhanced bioavailability at the action site. Cytotoxicity studies showed that 5-FU loaded PCL nanoparticles had higher antiproliferative effect than free 5-FU on Caco-2 cell line (p < 0.05). The encouraging results obtained offer reasons for optimism regarding the future of 5-FU nanoparticles as a promising drug delivery system which could be further improved by including either enteric coating or encapsulating the nanoparticles onto microparticles to overcome unanticipated degradation.

<p>Green synthesis of multifunctional PEG-carboxylate &pi; back-bonded gold nanoconjugates for breast cancer treatment</p>

“…[2][3][4][5] The anticancer drug 5-fluorouracil (5FU) is one of the most commonly used drugs for treating breast cancer, and various folate (FA)-based controlled drug delivery systems (DDSs) have been developed to deliver 5FU to MCF-7 breast cancer cells. 6,7 Several biodegradable polymer-based materials, including gellan gum, 8 poly(D,Llactic-co-glycolic acid), 9 polycaprolactone, 10 and L-lysinemodified hyperbranched polyester, 11 have been developed as 5FU delivery platforms to enhance the anticancer activity of 5FU. However, the size of these polymeric platforms is a major concern with regard to cell internalization of drugincorporated carriers.…”

Fabrication of chitosan/collagen/hydroxyapatite scaffolds with encapsulated Cissus quadrangularis extract

“…A reduction in encapsulation efficiency observed in higher PVA concentrations might be due to an increase in aqueous solubility of drug . However, increasing PCL concentrations did not significantly affect the encapsulation efficiency . Taken together of particle size and encapsulation efficiency results, the CQ‐PCL NPs that fabricated using 20 mg/mL PCL and 0.5% w/v PVA, had the smallest particle size (334.22 ± 43.21 nm), good uniformity of size distribution (PDI = 0.13 ± 0.05) with high encapsulation efficiency of 95.54 ± 1.49%.…”

Eco-Friendly Route for Encapsulation of 5-Fluorouracil Into Polycaprolactone Nanoparticles

“…The measurements were performed with reference to the supernatant of the drug-free nanoparticles as blank. The amount of encapsulated 5-FU was determined by subtracting the amount of free drug in the collected supernatant aftercentrifugation from the added amount in the beginning of the preparation using the following equation [14].…”