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硫酸软骨素用于软骨再生,通过纳米结构制剂局部给药。

Chondroitin Sulfate for Cartilage Regeneration, Administered Topically Using a Nanostructured Formulation.

机构信息

Instituto de Investigaciones Farmacéuticas, Facultad de Farmacia, Universidad de Costa Rica, San José 11501, Costa Rica.

Pharmacy, Pharmaceutical Technology and Physico-Chemical Department, Universitat de Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain.

出版信息

Int J Mol Sci. 2024 Sep 18;25(18):10023. doi: 10.3390/ijms251810023.

Abstract

In the pharmaceutical sector, solid lipid nanoparticles (SLN) are vital for drug delivery incorporating a lipid core. Chondroitin sulfate (CHON) is crucial for cartilage health. It is often used in osteoarthritis (OA) treatment. Due to conflicting results from clinical trials on CHON's efficacy in OA treatment, there has been a shift toward exploring effective topical systems utilizing nanotechnology. This study aimed to optimize a solid lipid nanoparticle formulation aiming to enhance CHON permeation for OA therapy. A 3 × 3 × 2 Design of these experiments determined the ideal parameters: a CHON concentration of 0.4 mg/mL, operating at 20,000 rpm speed, and processing for 10 min for SLN production. Transmission electron microscopy analysis confirmed the nanoparticles' spherical morphology, ensuring crucial uniformity for efficient drug delivery. Cell viability assessments showed no significant cytotoxicity within the tested parameters, indicating a safe profile for potential clinical application. The cell internalization assay indicates successful internalization at 1.5 h and 24 h post-treatment. Biopharmaceutical studies supported SLNs, indicating them to be effective CHON carriers through the skin, showcasing improved skin permeation and CHON retention compared to conventional methods. In summary, this study successfully optimized SLN formulation for efficient CHON transport through pig ear skin with no cellular toxicity, highlighting SLNs' potential as promising carriers to enhance CHON delivery in OA treatment and advance nanotechnology-based therapeutic strategies in pharmaceutical formulations.

摘要

在制药领域,固体脂质纳米粒(SLN)对于包含脂质核心的药物传递至关重要。硫酸软骨素(CHON)对于软骨健康至关重要。它常用于骨关节炎(OA)的治疗。由于临床试验中关于 CHON 在 OA 治疗中的疗效的结果相互矛盾,因此人们开始转向探索利用纳米技术的有效局部系统。本研究旨在优化一种旨在增强 CHON 渗透以用于 OA 治疗的固体脂质纳米粒制剂。这些实验的 3×3×2 设计确定了理想的参数:CHON 浓度为 0.4mg/ml,转速为 20,000rpm,处理时间为 10min 以生产 SLN。透射电子显微镜分析证实了纳米粒的球形形态,确保了高效药物传递所需的关键均匀性。细胞活力评估表明在测试参数内没有明显的细胞毒性,表明对于潜在的临床应用具有安全的特性。细胞内化试验表明在处理后 1.5 小时和 24 小时内成功内化。生物制药研究支持 SLN,表明它们是通过皮肤有效传递 CHON 的载体,与传统方法相比,显示出改善的皮肤渗透和 CHON 保留。总之,本研究成功优化了 SLN 制剂,以实现 CHON 通过猪耳皮肤的有效传递,且没有细胞毒性,突出了 SLN 作为增强 OA 治疗中 CHON 递送的有前途的载体的潜力,并推进了基于纳米技术的药物制剂的治疗策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2876/11432425/579e38ee1107/ijms-25-10023-g001.jpg

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