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Preparation and Characterization of Chitosan-Alginate Microspheres Loaded with Quercetin.

ABSTRACT: The aim of this paper was to formulate microspheres based on biodegradable polymers (chitosan and sodium alginate), using the complex coacervation technique. Subsequently, the prepared microspheres were loaded with quercetin (QUE), a pharmacological active ingredient insoluble in water and unstable to light, temperature and air. After preparation, the loaded microspheres underwent several studies for physical chemical characterization (performed by scanning electron microscopy-SEM, laser 3D scanning, and thermal analysis-TA). Furthermore, they were analyzed in order to obtain information regarding swelling index, drug entrapment, and in vitro release capacity. The obtained experimental data demonstrated 86.07% entrapment of QUE into the microspheres, in the case of the one with the highest Ch concentration. Additionally, it was proved that such systems allow the controlled release of the active drug over 24 h at the intestinal level. SEM micrographs proved that the prepared microspheres have a wrinkled surface, with compact structures and a large number of folds. On the basis of the TA analysis, it was concluded that the obtained microspheres were thermally stable, facilitating their usage at normal physiological temperatures as drug delivery systems.

SUBMITTER: Frent OD

PROVIDER: S-EPMC8839549 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature

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Preparation and Characterization of Chitosan-Alginate Microspheres Loaded with Quercetin.

Frenț Olimpia Daniela OD Duteanu Narcis N Teusdea Alin Cristian AC Ciocan Stefania S Vicaș Laura L Jurca Tunde T Muresan Mariana M Pallag Annamaria A Ianasi Paula P Marian Eleonora E

Polymers 20220126 3

The aim of this paper was to formulate microspheres based on biodegradable polymers (chitosan and sodium alginate), using the complex coacervation technique. Subsequently, the prepared microspheres were loaded with quercetin (QUE), a pharmacological active ingredient insoluble in water and unstable to light, temperature and air. After preparation, the loaded microspheres underwent several studies for physical chemical characterization (performed by scanning electron microscopy-SEM, laser 3D scan ...[more]

PMID: 35160478

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Project description:BackgroundOsteoarthritis (OA) is the most prevalent arthritic disease characterized by cartilage degradation and low-grade inflammation, for which there remains a lack of efficacious therapeutic interventions. Notably, mitigating the impact of oxidative stress (OS) and inflammatory factors could help alleviate or hinder the advancement of OA. Given the benefits of both quercetin (Que) and Magnesium ion (Mg2+) in OA treatment, coupled with the structural properties of Que, we have innovatively developed the Que-Mg2+ nanoparticles (NPs), aiming to deliver both Que and Mg2+ simultaneously and achieve enhanced therapeutic outcomes for OA. Moreover, to avoid the adverse reactions linked to frequent injections, sodium alginate (SA) microspheres encapsulating Que-Mg2+ NPs (Que-Mg@SA) were designed to treat the H2O2-induced OA cell model.MethodsQue-Mg@SA microspheres were synthesized using the ionotropic gelation technique, with calcium chloride acting as the cross-linking agent. Comprehensive characterization of the Que-Mg@SA was conducted through transmission electron microscope (TEM), dynamic light scattering (DLS), optical microscope, and scanning electron microscope (SEM), which provided detailed insights into their size, zeta potential, morphology, and micromorphology. Additionally, the microsphere swelling rate and Que release were evaluated. The biocompatibility of Que-Mg@SA microspheres, along with their impact on chondrocyte viability, were detected through CCK-8 assay and live/dead cell staining. Furthermore, the antioxidant and anti-inflammatory properties of Que-Mg@SA were evaluated by examining the ROS scavenging ability and pro-inflammatory factors levels, respectively. Finally, the regulatory influence of Que-Mg@SA microspheres on extracellular matrix (ECM) metabolism in OA was assessed by immunofluorescence staining and Western blot.ResultsCharacterization results revealed that Que-Mg NPs exhibit nanoscale diameter, exceptional stability, and good dispersibility, while Que-Mg@SA possesses high entrapment efficiency (EE%) and loading efficiency (LE%), pronounced hygroscopic properties, and sustained drug-release capabilities. Additionally, in vitro cellular assays revealed that the biocompatible Que-Mg@SA microspheres significantly restored chondrocyte viability, scavenged H2O2-induced excessive ROS, reduced the levels of inflammatory cytokines, upregulated cartilage anabolic gene expression, downregulated cartilage catabolic protease gene expression, and maintained the metabolic balance of cartilage tissue.ConclusionThe functionalized Que-Mg@SA microspheres developed in our study hold great promise as a drug delivery system for OA and potentially other biomedical applications.Clinical trial numberNot applicable.

Dataset Information

Preparation and Characterization of Chitosan-Alginate Microspheres Loaded with Quercetin.

Publications

Preparation and Characterization of Chitosan-Alginate Microspheres Loaded with Quercetin.

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