Schnieders Julia, Gbureck Uwe, Thull Roger, Kissel Thomas
Department of Pharmaceutics and Biopharmacy, Philipps-University Marburg, Ketzerbach 63, 35032 Marburg, Germany.
Biomaterials. 2006 Aug;27(23):4239-49. doi: 10.1016/j.biomaterials.2006.03.032. Epub 2006 Apr 18.
Modification of a self setting bone cement with biodegradable microspheres to achieve controlled local release of antibiotics without compromising mechanical properties was investigated. Different biodegradable microsphere batches were prepared from poly(lactic-co-glycolic acid) (PLGA) using a spray-drying technique to encapsulate gentamicin crobefate varying PLGA composition and drug loading. Microsphere properties such as surface morphology, particle size and antibiotic drug release profiles were characterized. Microspheres were mixed with an apatitic calcium phosphate bone cement to generate an antibiotic drug delivery system for treatment of bone defects. All batches of cement/microsphere composites showed an unchanged compressive strength of 60 MPa and no increase in setting time. Antibiotic release increased with increasing drug loading of the microspheres up to 30% (w/w). Drug burst of gentamicin crobefate in the microspheres was abolished in cement/microsphere composites yielding nearly zero order release profiles. Modification of calcium phosphate cements using biodegradable microspheres proved to be an efficient drug delivery system allowing a broad range of 10-30% drug loading with uncompromised mechanical properties.
研究了用可生物降解微球对自固化骨水泥进行改性，以实现抗生素的可控局部释放，同时不影响其机械性能。使用喷雾干燥技术，由聚（乳酸 - 乙醇酸）（PLGA）制备不同批次的可生物降解微球，以包封不同PLGA组成和载药量的克倍宁庆大霉素。对微球的表面形态、粒径和抗生素药物释放曲线等性质进行了表征。将微球与磷灰石磷酸钙骨水泥混合，以生成用于治疗骨缺损的抗生素药物递送系统。所有批次的水泥/微球复合材料的抗压强度均保持在60 MPa不变，凝固时间也未增加。随着微球载药量增加至30%（w/w），抗生素释放量增加。在水泥/微球复合材料中，微球中克倍宁庆大霉素的药物突释现象被消除，呈现出近乎零级的释放曲线。事实证明，使用可生物降解微球对磷酸钙骨水泥进行改性是一种有效的药物递送系统，其载药量范围为10% - 30%，且机械性能不受影响。
