Alendronate functionalized PLGA based nanoparticles for the effective treatment of osteoporosis-Formulation to in-vitro release kinetic studies

S. Pathak, S. Shukla, Bharat Patel, S. Tripathi, A. Pandey
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Abstract

Osteoporosis is a bone disease caused due to the reducing bone mineral density. Porous and more fragile bones increase the risk of fractures. Hip, spine, shoulder, and wrist bones are commonly affected by osteoporosis. Low bone density is a leading cause of osteoporosis. The most efficient prescribed drugs for the treatment of osteoporosis are bisphosphonates drugs. Alendronate was the first FDA approved bisphosphonate drug for the treatment of osteoporosis. Osteoclast cells are the primary targeting site for alendronate, responsible for bone resorption. A biopharmaceutical classification system class III bisphosphonate acts as a potent, efficient, and bone resorption inhibitor drug. In the present study, alendronate functionalized PLGA based nanoparticles were developed by a solvent diffusion method and optimized for different process variables. The formulated nanoparticles were characterized for surface morphology, particle size distribution, surface charge and drug-polymer compatibility. The scanning electron microscopy and transmission electron microscopy results showed nanoparticle size in the range below 200 nm. The average particle size and zeta potential of the formulated nanoparticles were found to be 175.3 nm and -13.98 mV, respectively. The highest encapsulation efficiency was 65.23%. The release profile was dissolution medium dependent and followed by the Higuchi model of release kinetics.
阿仑膦酸盐功能化PLGA基纳米颗粒有效治疗骨质疏松症制剂的体外释放动力学研究
骨质疏松症是一种由于骨密度降低而引起的骨病。多孔和更脆弱的骨骼会增加骨折的风险。髋部、脊椎、肩部和腕部骨骼通常受到骨质疏松症的影响。低骨密度是骨质疏松症的主要原因。治疗骨质疏松症最有效的处方药是双磷酸盐类药物。阿仑膦酸盐是美国食品药品监督管理局批准的第一种治疗骨质疏松症的双磷酸盐药物。破骨细胞是阿仑膦酸盐的主要靶向位点,负责骨吸收。生物药物分类系统III类双磷酸盐是一种有效的骨吸收抑制剂。在本研究中,通过溶剂扩散法开发了阿仑膦酸盐功能化的PLGA基纳米颗粒,并针对不同的工艺变量进行了优化。对所配制的纳米颗粒的表面形态、粒度分布、表面电荷和药物-聚合物相容性进行了表征。扫描电子显微镜和透射电子显微镜结果显示纳米颗粒尺寸在200nm以下的范围内。发现配制的纳米颗粒的平均粒径和ζ电位分别为175.3nm和-13.98mV。最高包封率为65.23%。释放曲线依赖于溶解介质,其次是Higuchi释放动力学模型。
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