Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability

Abstract

Chitosan (CS) is a polymer extensively used in drug delivery formulations mainly due to its biocompatibility and low toxicity. In the present study, chitosan was used for nanoencapsulation of a budesonide (BUD) drug via the well-established ionic gelation technique and a slight modification of it, using also poly(vinyl alcohol) (PVA) as a surfactant. Scanning electron microscopy (SEM) micrographs revealed that spherical nanoparticles were successfully prepared with average sizes range between 363 and 543 nm, as were measured by dynamic light scattering (DLS), while zeta potential verified their positive charged surface. X-ray diffraction (XRD) patterns revealed that BUD was encapsulated in crystalline state in nanoparticles but with a lower degree of crystallinity than the neat drug, which was also proven by differential scanning calorimetry (DSC) and melting peak measurements. This could be attributed to interactions that take place between BUD and CS, which were revealed by FTIR and by an extended computational study. An in vitro release study of budesonide showed a slight enhancement in the BUD dissolution profile, compared to the neat drug. However, drug release was substantially increased by introducing PVA during the nanoencapsulation procedure, which is attributed to the higher amorphization of BUD on these nanoparticles. The release curves were analyzed using a diffusion model that allows estimation of BUD diffusivity in the nanoparticles.

Innovative Skin Product Emulsions with Enhanced Antioxidant, Antimicrobial and UV Protection Properties Containing Nanoparticles of Pure and Modified Chitosan with Encapsulated Fresh Pomegranate Juice

“…Chitosan with molecular weight 18000 g/mol, and a degree of deacetylation > 94% as described in a previous paper of our group [ 31 ], was supplied by Kraeber &Co GmbH (Ellerbek, Germany). Sodium tripolyphosphate (TPP) used as the ionic cross-linker for the preparation of the nanoparticles was supplied from Aldrich chemicals (St. Louis, Missouri, United States) and was of 85% w / w purity.…”

“…Over the last years, nanoparticles have been utilized as potent carriers of various pharmaceutical drugs and cosmetic active ingredients [ 29 ]. More specifically, chitosan has been extensively studied for various applications namely drug nano-encapsulation for ocular release [ 30 ], COPD treatment [ 31 ], patches [ 32 ] and porous dressings [ 33 ] for sustained release, as well as encapsulation of annatto and saffron for the preparation of UV protective cosmetic emulsions [ 34 ].…”

Microencapsulation of Fluticasone Propionate and Salmeterol Xinafoate in Modified Chitosan Microparticles for Release Optimization

“…In detail, the MPs were prepared as a result of the ionic interactions between the negative charged TPP groups and the cationic amino groups of CS. Relative projects studying the aforementioned technique have been reported previously by our research team, including the synthesis of nanoencapsulated budesonide particles for pulmonary delivery [56], deferoxamine mesylate-laden CS nanoparticles for iron chelator release [57], timolol maleate-loaded particles for ocular delivery [31] as well as paliperidone incorporation in polymeric carriers for intranasal delivery [58]. A significant factor affecting the final size of the formulated particles is the ratio between chitosan and TPP.…”

Preparation and Evaluation of Collagen-Based Patches as Curcumin Carriers

“…First, EDC forms an active ester intermediate via reaction with the -COOH groups of Coll and/or Hep, which undergoes nucleophilic substitution in the presence of the primary amine groups of Coll and/or CS [ 70 ]. Many FTIR bands of CS ( Figure 2 ) appear in similar wavenumbers as Coll, including the O-H stretching vibrations at 3400 cm −1 , the amide I at 1656 cm −1 , and the amide II NH 2 bending vibration at 1595 cm −1 [ 71 , 72 ], making it difficult to distinguish these bands between Coll and CS. However, some differences are noticeable between the spectrum of Coll and the spectra of Coll with CS-NPs, mainly in the region 1700–1600 cm −1 .…”