Gurgul Sebastian J, Moreira Anabela, Xiao Yi, Varma Swastina Nath, Liu Chaozong, Costa Pedro F, Williams Gareth R
UCL School of Pharmacy, University College London, London WC1N 1AX, UK.
Biofabics, 4200-135 Porto, Portugal.
Polymers (Basel). 2023 Mar 2;15(5):1275. doi: 10.3390/polym15051275.
The restoration of cartilage damage is a slow and not always successful process. Kartogenin (KGN) has significant potential in this space-it is able to induce the chondrogenic differentiation of stem cells and protect articular chondrocytes. In this work, a series of poly(lactic-co-glycolic acid) (PLGA)-based particles loaded with KGN were successfully electrosprayed. In this family of materials, PLGA was blended with a hydrophilic polymer (either polyethyleneglycol (PEG) or polyvinylpyrrolidone (PVP)) to control the release rate. Spherical particles with sizes in the range of 2.4-4.1 µm were fabricated. They were found to comprise amorphous solid dispersions, with high entrapment efficiencies of >93%. The various blends of polymers had a range of release profiles. The PLGA-KGN particles displayed the slowest release rate, and blending with PVP or PEG led to faster release profiles, with most systems giving a high burst release in the first 24 h. The range of release profiles observed offers the potential to provide a precisely tailored profile via preparing physical mixtures of the materials. The formulations are highly cytocompatible with primary human osteoblasts.
软骨损伤的修复是一个缓慢且并非总能成功的过程。卡托金（KGN）在这方面具有巨大潜力——它能够诱导干细胞的软骨形成分化并保护关节软骨细胞。在这项研究中，成功地通过电喷雾法制备了一系列负载KGN的聚乳酸 - 乙醇酸共聚物（PLGA）基颗粒。在这个材料家族中，PLGA与亲水性聚合物（聚乙二醇（PEG）或聚乙烯吡咯烷酮（PVP））混合以控制释放速率。制备出了尺寸在2.4 - 4.1微米范围内的球形颗粒。发现它们由无定形固体分散体组成，包封率高于93%。聚合物的各种共混物具有一系列的释放曲线。PLGA - KGN颗粒显示出最慢的释放速率，与PVP或PEG混合导致更快的释放曲线，大多数体系在前24小时有较高的突释。观察到的释放曲线范围提供了通过制备材料的物理混合物来提供精确定制曲线的潜力。这些制剂与原代人成骨细胞具有高度的细胞相容性。
