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High drug loading hydrophobic cross-linked dextran microspheres as novel drug delivery systems for the treatment of osteoarthritis.

ABSTRACT: Drug delivery via intra-articular (IA) injection has proved to be effective in osteoarthritis (OA) therapy, limited by the drug efficiency and short retention time of the drug delivery systems (DDSs). Herein, a series of modified cross-linked dextran (Sephadex, S0) was fabricated by respectively grafting with linear alkyl chains, branched alkyl chains or aromatic chain, and acted as DDSs after ibuprofen (Ibu) loading for OA therapy. This DDSs expressed sustained drug release, excellent anti-inflammatory and chondroprotective effects both in IL-1β induced chondrocytes and OA joints. Specifically, the introduction of a longer hydrophobic chain, particularly an aromatic chain, distinctly improved the hydrophobicity of S0, increased Ibu loading efficiency, and further led to significantly improving OA therapeutic effects. Therefore, hydrophobic microspheres with greatly improved drug loading ratio and prolonged degradation rates show great potential to act as DDSs for OA therapy.

SUBMITTER: Li Z

PROVIDER: S-EPMC10425896 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature

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High drug loading hydrophobic cross-linked dextran microspheres as novel drug delivery systems for the treatment of osteoarthritis.

Li Zhimin Z Feng Xianjing X Luo Shixing S Ding Yanfeng Y Zhang Zhi Z Shang Yifeng Y Lei Doudou D Cai Jinhong J Zhao Jinmin J Zheng Li L Gao Ming M

Asian journal of pharmaceutical sciences 20230725 4

Drug delivery via intra-articular (IA) injection has proved to be effective in osteoarthritis (OA) therapy, limited by the drug efficiency and short retention time of the drug delivery systems (DDSs). Herein, a series of modified cross-linked dextran (Sephadex, S0) was fabricated by respectively grafting with linear alkyl chains, branched alkyl chains or aromatic chain, and acted as DDSs after ibuprofen (Ibu) loading for OA therapy. This DDSs expressed sustained drug release, excellent anti-infl ...[more]

PMID: 37588991

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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

High drug loading hydrophobic cross-linked dextran microspheres as novel drug delivery systems for the treatment of osteoarthritis.

Publications

High drug loading hydrophobic cross-linked dextran microspheres as novel drug delivery systems for the treatment of osteoarthritis.

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