Caffeic Acid Phenethyl Ester Loaded PLGA Nanoparticles: Effect of Various Process Parameters on Reaction Yield, Encapsulation Efficiency, and Particle Size

Abstract

CAPE loaded PLGA nanoparticles were prepared using the oil in water (o/w) single emulsion solvent evaporation methods. Five different processing parameters including initial CAPE amount, initial PLGA amount, PVA concentration in aqueous phase, PVA volume, and solvent type were screened systematically to improve encapsulation of hydrophobic CAPE molecule, simultaneously minimize particle size, and raise the reaction yield. Obtained results showed that the encapsulation efficiency of the nanoparticles significantly increased with the increase of the initial CAPE amount (p<0.05) and particle size (p<0.05). Furthermore, the particle size is significantly influenced by initial polymer amount (p<0.05) and surfactant concentration (p<0.05). By the optimization of process parameters, the nanoparticles produced70±6% reaction yield,89±3% encapsulation efficiency,-34.4±2.5 mV zeta potential, and163±2 nm particle size with low polydispersity index0.119±0.002. The particle size and surface morphology of optimized nanoparticles were studied and analyses showed that the nanoparticles have uniform size distribution, smooth surface, and spherical shape. Lyophilized nanoparticles with different CAPE and PLGA concentration in formulation were examined forin vitrorelease at physiological pH. Interestingly, the optimized nanoparticles showed a high (83.08%) and sustained CAPE release (lasting for 16 days) compared to nonoptimized nanoparticle.

Polymeric Nano-Encapsulation of Curcumin Enhances its Anti-Cancer Activity in Breast (MDA-MB231) and Lung (A549) Cancer Cells Through Reduction in Expression of HIF-1α and Nuclear p65 (Rel A)

“…Entrapment efficiency increased significantly, as the ratio of PLGA increased 270 ( Figure 1C). Similar results were reported by Derman et al 49 . It is proposed that the increase 271 in PLGA in the organic phase increases the viscosity and reduces diffusivity to the water phase 272 41,50 .…”

Comparative evaluation of hesperetin loaded nanoparticles for anticancer activity against C6 glioma cancer cells

“…Functional groups present in the surface of nanoparticles were analysed by Fourier-transform infrared spectroscopy in universal attenuation total reflectance (ATR) mode [27]. The FTIR spectra of free hesperetin, free nanoparticle and HspNPs were obtained with 16 scans per sample and 4 cm À1 resolution in the region of 650-4000 cm À1 .…”

A novel nanoparticle loaded with methyl caffeate and caffeic acid phenethyl ester against Ralstonia solanacearum—a plant pathogenic bacteria

“…19 Due to their potential ability to inhibit bacteria, our attention has been focused on caffeic acid-a naturally sourced compound-and its derivatives. Among them, caffeic acid phenethyl ester (CAPE), which is considered to be one of the most popular compounds for the development of new drugs 20 and has been the main active ingredient isolated from propolis residues, has shown toxic effects toward R. solanacearum. 21 Methyl caffeate (MC) has many pharmacological activities, and it is a synthetic intermediate of many natural drugs and food additives, such as propyl caffeate (PC); CAPE can be prepared by the transesterication of MC with the corresponding alcohol.…”

“…21 Methyl caffeate (MC) has many pharmacological activities, and it is a synthetic intermediate of many natural drugs and food additives, such as propyl caffeate (PC); CAPE can be prepared by the transesterication of MC with the corresponding alcohol. 22 Recently, PLGA particles loaded with CAPE were successfully prepared, 20 which demonstrated the feasibility of fabricating PLGA particles loaded with caffeic acid and its derivatives. Many studies have focused on the preparation process as well as the lack of research on the mechanism of bacteriostatic action of the prepared nanoparticles.…”