CONTEXT: Osteoporosis (OP) is the most common metabolic bone disease predominantly found in elderly people. It is associated with reduced bone mineral density, results in a higher probability of fractures, especially of the hip, vertebrae, and distal radius. Worldwide prevalence of OP is considered a serious public health concern. OBJECTIVE: The purpose of the present work was to develop and evaluate polymeric nanoparticles (NPs) of risedronate sodium (RIS) for the treatment of OP using intranasal (IN) route in order to reduce peripheral toxic effects. MATERIALS AND METHODS: Polymeric NPs of RIS were prepared by nanoprecipitation methods. Formulations were developed and evaluated in context to in vitro drug release, ex vivo permeation, in vivo study, and biochemical studies. RESULTS AND DISCUSSIONS: The particles size, entrapment efficiency (EE) (%), and loading capacity (LC) (%) of optimized formulations were found to be 127.84 ± 6.33 nm, 52.65 ± 5.21, and 10.57 ± 1.48, respectively. Release kinetics showed diffusion-controlled, Fickian release pattern. Ex vivo permeation study showed RIS from PLGA-NPs permeated significantly (p < 0.05) through nasal mucosa. In vivo study showed a marked difference in micro-structure (trabeculae) in bone internal environment. Biochemical estimation of treated group and RIS PLGA indicated a significant recovery (p < 0.01) as compared with the toxic group. CONCLUSION: Polymeric NPs of RIS were prepared successfully using biodegradable polymer (PLGA). Intranasal delivery showed a good result in in vivo study. Thus PLGA-NPs have great potential for delivering the RIS for the treatment and prevention of OP after clinical evaluation in near future.
CONTEXT: Osteoporosis (OP) is the most common metabolic bone disease predominantly found in elderly people. It is associated with reduced bone mineral density, results in a higher probability of fractures, especially of the hip, vertebrae, and distal radius. Worldwide prevalence of OP is considered a serious public health concern. OBJECTIVE: The purpose of the present work was to develop and evaluate polymeric nanoparticles (NPs) of risedronate sodium (RIS) for the treatment of OP using intranasal (IN) route in order to reduce peripheral toxic effects. MATERIALS AND METHODS: Polymeric NPs of RIS were prepared by nanoprecipitation methods. Formulations were developed and evaluated in context to in vitro drug release, ex vivo permeation, in vivo study, and biochemical studies. RESULTS AND DISCUSSIONS: The particles size, entrapment efficiency (EE) (%), and loading capacity (LC) (%) of optimized formulations were found to be 127.84 ± 6.33 nm, 52.65 ± 5.21, and 10.57 ± 1.48, respectively. Release kinetics showed diffusion-controlled, Fickian release pattern. Ex vivo permeation study showed RIS from PLGA-NPs permeated significantly (p < 0.05) through nasal mucosa. In vivo study showed a marked difference in micro-structure (trabeculae) in bone internal environment. Biochemical estimation of treated group and RIS PLGA indicated a significant recovery (p < 0.01) as compared with the toxic group. CONCLUSION: Polymeric NPs of RIS were prepared successfully using biodegradable polymer (PLGA). Intranasal delivery showed a good result in in vivo study. Thus PLGA-NPs have great potential for delivering the RIS for the treatment and prevention of OP after clinical evaluation in near future.
Authors: Wei Wang; Kun Fang; Miao-Chen Li; Di Chang; Khawar Ali Shahzad; Tao Xu; Lei Zhang; Ning Gu; Chuan-Lai Shen Journal: Oncotarget Date: 2016-03-15