Mucoadhesive nanostructured polyelectrolytes complexes modulate the intestinal permeability of methotrexate

Abstract

Nanostructured polyelectrolytes complexes (nano PECs) loaded with methotrexate (MTX) were obtained by the polyelectrolyte complexation of chitosan (CS) and hyaluronic acid (HA), further incorporating hypromellose phthalate (HP). The mean diameter of nano PECs ranged from 325 to 458nm, with a narrow size distribution. Zeta potential was close to +30mV, decreasing to +21mV after the incorporation of HP, a range of values that favour the physical stability of system as the interaction with cationic biological membranes. The electrostatic interactions between the different components were indicated by the FTIR data. The mucoadhesiveness of nano PECs was demonstrated and MTX and HP influenced this property. The cell viability assays showed the biosafety of the isolated polymers and nano PECs in intestinal HT29-MTX and Caco-2 cell lines at 4h of test. The permeability values of MTX loaded in CS/HA nano PECs were 7.6 and 4-fold higher than those of CS/HA/HP nano PECS and free drug, respectively, in the Caco-2 monoculture. In mucus secreting co-culture cell model these values were 3 and 6.5 fold, respectively. Such features indicate that nano PECs developed in this work can be promising carriers for MTX in the treatment of local or systemic diseases.

Effect of glutaraldehyde/glycerol ratios on the properties of chitosan films

“…The band at 1,630 cm ‐1 is related to a primary amide (López‐Pérez et al., 2007). Bands at 2,856 and 3,247 cm ‐1 are related to the vibration of CH 2 and the O‐H bonds (Boni et al., 2018; Doshi et al., 2018; Jamal et al., 2018; Liu et al., 2019). The enlargement of the O‐H band for samples CG10, CG20, and CG30 suggests the increase of the amount of hydroxyl group due to adding glycerol according to Martínez‐Camacho et al.…”

Polymeric Nanoparticle Associated with Ceftriaxone and Extract of Schinopsis Brasiliensis Engler against Multiresistant Enterobacteria

“…Polymeric nanoparticles (PN) were developed according to the polyelectrolytic complexation methodology, using a cationic charge polymer (chitosan (CS)) and an anionic charge polymer (HPMC) according to Boni et al [30], CS was dispersed in 0.1 mol L −1 acetic acid, while HPMC was dispersed in distilled water obtaining in both, a final concentration of 2 mg mL −1 . The pH of the solutions were obtained with the aid of a pHmeter Mylabor (OA210A) brand and the adjustment was performed by dripping an alkaline solution of NaOH 1M, to obtain a final pH of 5.5.…”

“…To obtain PN by polyelectrolytic complexation, Boni et al [30] used the positive charge polymers chitosan and the negative charge, hyaluronic acid, and HPMC. The PN obtained with and without API showed sizes ranging between 325.7 and 450.5, and zeta potential ranging between ±20.9 and ±33.1, which is similar to the results found in the formulations named PN-1, PN-2, PN-3, and PN-4.…”

Exploiting supramolecular interactions to produce bevacizumab-loaded nanoparticles for potential mucosal delivery

“…Generally, different materials and systems are able to establish supramolecular interactions with mucosal components, such as mucin chains, because of the presence of reactive functional groups at the polymer chains, which facilitate adhesion to the mucus. On the other hand, to design mucus penetrating systems, the opposite logic must be used in order to open paths, facilitating system permeation [19,[25][26][27].…”