a Department of Pharmaceutics , Indian Institute of Technology, Banaras Hindu University , Varanasi , India.
b Moti Lal Nehru Medical College , Allahabad , India.
Artif Cells Nanomed Biotechnol. 2018 Sep;46(6):1180-1193. doi: 10.1080/21691401.2017.1366331. Epub 2017 Aug 23.
Periodontal disease is chronic, highly prevalent infectious disease that requires prolonged and controlled delivery of antimicrobial agents into pockets. To achieve this objective, dual antimicrobials encapsulated chitosan fortified calcium alginate (CS-Ca-SA) microspheres were formulated by application of Plackett-Burman factorial design. The microspheres were optimized for particle size (PS), entrapment efficiency (EE) and drug release. The optimized microspheres presented average PS of 74-461 µm and EE of 62.45-86.20% with controlled drug delivery for 120 hours. FTIR disclosed successful complexation between SA and CS. DSC and XRD studies showed changes in the crystallinity of drugs in microspheres. Shape factor and SEM demonstrated spherical to pear-shaped microspheres. Release exponent >0.43 and high diffusion coefficients revealed non-Fickian-based diffusion-limited drug release. CS-Ca-SA microspheres exhibited surface pH of 6.5 ± 0.5, moderate swelling, less erosion and improved mucoadhesion over Ca-SA microspheres. Also, significant antimicrobial activity against Escherichia coli and Staphylococcus aureus and cytocompatibility with L929 cell lines were observed. Further, microspheres exhibited long-term stability on refrigeration. The outcomes of study supported the potential of dual polymer and dual drug-based biodegradable, stable, non-toxic, mucoadhesive, controlled and prolonged drug release microspheres as more patient compliant by administration into periodontal pockets for the management of periodontal disease.
牙周病是一种慢性、高发性传染病，需要将抗菌剂长时间、受控地输送到牙周袋中。为了实现这一目标，采用 Plackett-Burman 因子设计法，制备了载双抗菌剂壳聚糖强化海藻酸钠（CS-Ca-SA）微球。对微球的粒径（PS）、包封率（EE）和药物释放进行了优化。优化后的微球平均 PS 为 74-461μm，EE 为 62.45-86.20%，可控制药物释放 120 小时。FTIR 表明 SA 与 CS 成功络合。DSC 和 XRD 研究表明药物在微球中的结晶度发生了变化。形状因子和 SEM 表明微球呈球形到梨形。释放指数>0.43 和高扩散系数表明药物释放是基于非 Fickian 的扩散限制。CS-Ca-SA 微球的表面 pH 值为 6.5±0.5，具有适度的溶胀、较少的侵蚀和改善的粘弹性，优于 Ca-SA 微球。此外，还观察到对大肠杆菌和金黄色葡萄球菌的显著抗菌活性以及与 L929 细胞系的细胞相容性。此外，微球在冷藏条件下具有长期稳定性。研究结果表明，双聚合物和双药物为基础的可生物降解、稳定、无毒、粘弹性、可控和长效药物释放微球具有潜力，可通过向牙周袋内给药来治疗牙周病，从而提高患者的顺应性。
