Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Department of Microbiology of Supplementary General Science, Faculty of Oral and Dental Medicine, Future University in Egypt, Cairo, Egypt.
AAPS PharmSciTech. 2019 Feb 8;20(3):104. doi: 10.1208/s12249-019-1292-4.
The application of minimally invasive surgical techniques in the field of orthopedic surgery has created a growing need for new injectable synthetic materials that can be used for bone grafting. In this work, novel injectable thermosensitive foam was developed by mixing nHAP powder with a thermosensitive polymer with foaming power (Pluronic F-127) and loaded with a water-soluble bisphosphonate drug (risedronate) to promote osteogenesis. The foam was able to retain the porous structure after injection and set through temperature change of PF-127 solution to form gel inside the body. The effect of different formulation parameters on the gelation time, porosity, foamability, injectability, and in vitro degradation in addition to drug release from the prepared foams were analyzed using a full factorial design. The addition of a co-polymer like methylcellulose or sodium alginate into the foam was also studied. Results showed that the prepared optimized thermosensitive foam was able to gel within 1 min at 37°C, and sustain the release of drug for 72 h. The optimized formulation was further tested for any interactions using DSC and IR, and revealed no interactions between the drug and the used excipients in the prepared foam. Furthermore, the ability of the pre-set foam to support osteoblastic-like Saos-2-cell proliferation and differentiation was assessed, and revealed superior function on promoting cellular proliferation as confirmed by fluorescence microscope compared to the plain drug solution. The activity of the foam treated cells was also assessed by measuring the alkaline phosphatase activity and calcium deposition, and confirmed that the cellular activity was greatly enhanced in foam treated cells compared to those treated with the plain drug solution only. The obtained results show that the prepared risedronate-loaded thermosensitive foam would represent a step forward in the design of new materials for minimally invasive bone regeneration.
微创外科技术在骨科领域的应用,产生了对新型可注射合成材料的日益增长的需求,这些材料可用于骨移植。在这项工作中,通过将 nHAP 粉末与具有成孔能力的温敏聚合物(泊洛沙姆 F-127)混合,并负载水溶性双膦酸盐药物(利塞膦酸钠)来促进成骨,开发了新型可注射温敏泡沫。泡沫在注射后能够保留多孔结构,并通过 PF-127 溶液的温度变化而凝固,在体内形成凝胶。使用完全析因设计分析了不同配方参数对凝胶时间、孔隙率、成孔性、可注射性以及制备泡沫体外降解和药物释放的影响。还研究了在泡沫中添加共聚物如甲基纤维素或海藻酸钠的效果。结果表明,制备的优化温敏泡沫在 37°C 下 1 分钟内能够凝胶,并能持续释放药物 72 小时。进一步对优化配方进行了 DSC 和 IR 分析,结果表明药物与所用辅料之间没有相互作用。此外,还评估了预成型泡沫支持成骨样 Saos-2 细胞增殖和分化的能力,与单纯药物溶液相比,荧光显微镜证实预成型泡沫在促进细胞增殖方面具有更好的功能。还通过测量碱性磷酸酶活性和钙沉积来评估泡沫处理细胞的活性,并证实与仅用单纯药物溶液处理的细胞相比,泡沫处理细胞的细胞活性大大增强。研究结果表明,制备的载利塞膦酸钠温敏泡沫将代表微创骨再生新型材料设计的一个进步。