Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.
Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.
Int J Pharm. 2017 Mar 30;520(1-2):39-48. doi: 10.1016/j.ijpharm.2017.01.039. Epub 2017 Jan 31.
A pseudo-bone thermo-gel was synthesized and evaluated for its physicochemical, mechanical and rheological properties, with its application to treat small bone fractures. The pseudo-bone thermo-gel was proven to have thermo-responsive properties, behaving as a solution in temperatures below 25°C, and forming a gelling technology when maintained at physiological conditions. Poly propylene fumerate (PPF), Pluronic F127 and PEG-PCL-PEG were strategically blended, obtaining a thermo-responsive delivery system, to mimic the mechanical properties of bone with sufficient matrix hardness and resilience. A Biopharmaceutics Classification System (BCS) class II drug, simvastatin, was loaded in the pseudo-bone thermo-gel, selected for its bone healing properties. In vitro release analysis was undertaken on a series of experimental formulations, with the ideal formulations obtaining its maximum controlled drug release profile up to 14days. Ex vivo studies were undertaken on an induced 4mm diameter butterfly-fractured osteoporotic human clavicle bone samples. X-ray, ultrasound as well as textural analysis, undertaken on the fractured bones before and after treatment displayed significant bone filling, matrix hardening and matrix resilience properties. These characteristics of the pseudo-bone thermo-gel thus proved significant potential for application in small bone fractures.
一种假骨温敏凝胶被合成并评估其物理化学、机械和流变学性能，以应用于治疗小骨骨折。假骨温敏凝胶被证明具有温敏特性，在 25°C 以下表现为溶液状态，在生理条件下形成凝胶状态。聚丙交酯富马酸酯（PPF）、泊洛沙姆 F127 和聚乙二醇-聚己内酯-聚乙二醇被策略性地混合，获得一种温敏递药系统，以模拟具有足够基质硬度和弹性的骨骼机械性能。辛伐他汀是一种生物药剂学分类系统（BCS）II 类药物，被加载到假骨温敏凝胶中，因其具有骨愈合特性而被选中。对一系列实验配方进行了体外释放分析，理想的配方在 14 天内获得了最大的控制药物释放曲线。对诱导的 4mm 直径蝶形骨质疏松性人锁骨骨折样本进行了离体研究。在治疗前后对骨折骨进行了 X 射线、超声以及质地分析，显示出显著的骨填充、基质硬化和基质弹性特性。因此，这种假骨温敏凝胶的特性证明了其在小骨骨折治疗中的潜在应用价值。
