Jiang Jun, Xiao Jianpeng, Wang Dongqing, Cai Huazhong
School of Pharmacy, Jiangsu University, 301# Xuefu Road, Zhenjiang 212013, Jiangsu Province, China.
Affiliated Hospital of Jiangsu University, Department of Medical Imaging, Zhenjiang 212001, Jiangsu Province, China.
Evid Based Complement Alternat Med. 2021 Jul 27;2021:5580785. doi: 10.1155/2021/5580785. eCollection 2021.
Alveolar bone defects (ABDs) were a perennial problem, especially in the aged. Bisphosphonates, especially etidronate sodium (ET), were frequently used in clinical treatment of ABD. However, the oral administration of ET had poor absorption (<1%). Therefore, optimization of a suitable dosage form substituted with ET to locally repair the ABD was a straightforward approach. Polylactide-co-glycolide (PLGA) is a biodegradable material and had been used in locally implanted medical devices. Therefore, an ET-PLGA microcapsule may help local delivery and prolong the activity of healing ABD. In this paper, a preparation method of ET-PLGA microcapsule was optimized by the single-factor investigation and response surface method. Subsequently, the rat ABD model was used to evaluate the enhancement effect of these microcapsules. Finally, the optimum parameters were determined as follows: 40% dichloromethane, 160 mg/mL PLGA, 10% internal aqua/oil phase, 4% PVA, and emulsifying for 10 min. These microcapsules were spherical in shape and fairly monodisperse in a particle size of 27,51 m (PDI = 0.3), encapsulation rate 96.6%, and drug loading 4.58%. Compared with the ET groups, the total healing volume of ABD in ET-PLGA groups was significantly increased ( < 0.05). ET-PLGA microcapsules significantly enhanced the effect of ET on ABD. This study provided important technical support for the treatment of ABD with bisphosphonates by local administration. This paper has an exploratory significance for the development of water-soluble bioactive components with low bioavailability for ABD.
牙槽骨缺损(ABDs)一直是个难题,尤其是在老年人中。双膦酸盐,特别是依替膦酸钠(ET),常用于ABDs的临床治疗。然而,ET口服吸收较差(<1%)。因此,优化一种用ET替代的合适剂型以局部修复ABDs是一种直接的方法。聚乳酸-羟基乙酸共聚物(PLGA)是一种可生物降解材料,已用于局部植入式医疗器械。因此,ET-PLGA微胶囊可能有助于局部给药并延长ABDs愈合活性。本文通过单因素考察和响应面法优化了ET-PLGA微胶囊的制备方法。随后,采用大鼠ABDs模型评估这些微胶囊的增强效果。最后,确定最佳参数如下:二氯甲烷40%、PLGA 160mg/mL、内水/油相10%、聚乙烯醇4%,乳化10分钟。这些微胶囊呈球形,粒径为27.51μm时相当单分散(多分散指数PDI = 0.3),包封率96.6%,载药量4.58%。与ET组相比,ET-PLGA组ABDs的总愈合体积显著增加(P<0.05)。ET-PLGA微胶囊显著增强了ET对ABDs的治疗效果。本研究为双膦酸盐局部给药治疗ABDs提供了重要的技术支持。本文对开发ABDs生物利用度低的水溶性生物活性成分具有探索意义。