Mucoadhesive chitosan-coated PLGA nanoparticles for oral delivery of ferulic acid

Abstract

This paper describes the development and in vitro evaluation of poly(lactic-co-glycolic acid) (PLGA) nanoparticles coated with chitosan (CS) for oral delivery of ferulic acid (FA). Nanoparticles were obtained by an emulsion evaporation technique and characterized. Furthermore, we evaluated the scavenging activity over hypochlorous acid (HOCl), the cytotoxicity over tumour cells and the in vitro intestinal permeability. Nanoparticles were spherical with a mean diameter of 242 nm, positive zeta potential and 50% of encapsulation efficiency. The in vitro release in phosphate buffered saline (PBS) (pH 7.4) demonstrated a prolonged and biphasic profile diffusion-controlled. In simulated gastrointestinal fluids, about 15% of FA was released in gastric fluid and a negligible release was observed in the intestinal fluid. In the HOCl scavenging activity and cytotoxicity over B16-F10 and HeLa cells, FA-loaded nanoparticles presented the same efficacy of the free drug. Besides, in the antioxidant and cytotoxic assay, CS contributed to FA effects. In the intestinal permeability study, FA-loaded nanoparticles exhibited a permeation of 6% through the Caco-2 monolayer and 20% through the Caco-2/HT29-MTX/Raji B co-culture. CS-coated PLGA nanoparticles are promising carriers for oral delivery of FA.

Repurposing Itraconazole Loaded PLGA Nanoparticles for Improved Antitumor Efficacy in Non-Small Cell Lung Cancers

“…The increase in particle size of CS-ITR-PLGA NPs compared with PLGA NPs and ITR-PLGA NPs is due to increased viscosity of the chitosan-added aqueous phase; this lowers the shear stress during ultrasonication of the emulsion, and results in a larger particle size [18]. This agrees with the previous observations of Lima et al [19], who developed ferulic acid-loaded PLGA nanoparticles with a chitosan coating. A small particle size is important in determining a better biodistribution, increased systemic stability, and enhanced permeability and retention [16].…”

“…The entrapment efficiency of ITR-PLGA NPs and CS-ITR-PLGA NPs was found to be 79.68% ± 7.30% and 80.18% ± 8.12%, respectively, with respective drug loadings of 15.93% ± 1.46% and 16.03% ± 1.62%; thus, addition of the CS coating did not significantly alter the drug loading and entrapment efficiency ( Table 1; p > 0.05). This was not in agreement with previous findings [19,21], which showed that CS-coated PLGA nanoparticles loaded with paclitaxel and ferulic acid increased the hydrophilicity of the system, resulting in decreased entrapment of hydrophobic drugs [19,21]. As shown using TEM, the particles were perfectly spherical, with the CS coating uniformly distributed on the surface ( Figure 3A).…”

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

“…The pharmaceutical strategies in developing ferulic acid nanoformulation have been found to mitigate physicochemical, biopharmaceutical, and pharmacokinetic incompetence of ferulic acid. Ferulic-acid-assembled chitosan-coated PLGA nanoparticles have been found to improve intestinal permeability, gastrointestinal stability, biological half-life, and oral bioavailability of ferulic acid [301]. The mucoadhesive property of ferulic-acid-chitosan-PLGA nanoparticles allowed their greater association with the intestinal epithelium [301].…”

Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity

“…Chitosan (CHIT) is a natural alkaline polysaccharide derived from chitin, characterized by its non-toxic, biocompatible, hypoallergenic, antibacterial, and biodegradable properties. Most of the properties that render chitosan a desirable carrier for the preparation of drug-loaded NPs are attributable to the primary amine group, which, among many features, is also responsible for chitosan's cationic nature, controlled drug release, and adhesion to mucosal surfaces [4,5]. As recently highlighted, chitosan-based microparticles (MPs) formulations can release several anti-tumor agents that increase drug internalization into targeted cells and enhance therapeutic effects paralleled by reduced adverse effects [6][7][8].…”