title: Design and Development of Bioceramic Based Functionalized PLGA Nanoparticles of Risedronate for Bone Targeting: In-vitro Characterization and Pharmacodynamic Evaluation.
abstract: OBJECTIVE
  Bioceramic(Hydroxyapatite) based Poly(D,L-lactide-co-glycolide) (PLGA) and polyethylene glycol (PEG) nanoparticles of Risedronate was prepared by dialysis method for bone-targeting.
  
  
  METHODS
  Risedronate, a targeting moiety that has a strong affinity for bone, was conjugated to PLGA via carbodiimide chemistry. Mono-methoxy PEG(mPEG)-PLGA block polymers were synthesized and used to impart surface hydrophilicity to nanoparticles to avoid its uptake by reticuloendothelial system (RES). The structure of prepared di block copolymers were characterized by FT-IR and NMR spectrometry. Risedronate was adsorbed on the surface of hydroxyapatite (RIS-HA) and it was conjugated with different ratios of mPEG-PLGA. The formation of surface-modified PLGA nanoparticle prepared with various ratios of risedronate as well as hydroxyapatite and mPEG was confirmed by (1)H NMR and FT-IR spectrometry.
  
  
  RESULTS
  Size and % entrapment of the prepared nanoparticle was found to be 79.3 ± 2.3 nm and 93 ± 3.1%. Transmission electron microscopy (TEM) revealed that mPEG-PLGA-RIS-HA nanoparticles possess smooth and uniform surface. Pharmacodynamic study was performed on Dexamethasone (DEX) induced osteoporotic model. The effect of various formulations (mPEG-PLGA-RIS, mPEG-PLGA-RIS-HA and RISOFOS tablet) on bone was studied by Volume bone density (VBD) and by histopathological evaluation. Interestingly mPEG-PLGA-RIS-HA, showed a significant enhancement in bone micro-architecture when compared with other formulations.
  
  
  CONCLUSIONS
  The results strongly implicated that mPEG-PLGA-RIS-HA has a therapeutic benefits over risedronate sodium monotherapy for the treatment of osteoporosis in a rat model.
authors.affiliation: Nanomedicine Research Lab, Department of Pharmaceutics Faculty of Pharmacy, Jamia Hamdard, New Delhi, 110062, India.
authors.forename: Purnima
authors.initials: P
authors.lastname: Rawat
authors.affiliation: Molecular Sciences Lab, National Institute of Immunology, New Delhi, New Delhi, 110067, India.
authors.forename: Kapil
authors.initials: K
authors.lastname: Manglani
authors.affiliation: Molecular Sciences Lab, National Institute of Immunology, New Delhi, New Delhi, 110067, India.
authors.forename: Sarika
authors.initials: S
authors.lastname: Gupta
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Jamia Hamdard, New Delhi, 110062, India.
authors.forename: Abul
authors.initials: A
authors.lastname: Kalam
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Jamia Hamdard, New Delhi, 110062, India.
authors.forename: Divya
authors.initials: D
authors.lastname: Vohora
authors.affiliation: Nanomedicine Research Lab, Department of Pharmaceutics Faculty of Pharmacy, Jamia Hamdard, New Delhi, 110062, India.
authors.forename: Farhan Jalees
authors.initials: FJ
authors.lastname: Ahmad
authors.affiliation: Nanomedicine Research Lab, Department of Pharmaceutics Faculty of Pharmacy, Jamia Hamdard, New Delhi, 110062, India. stalegaonkar@gmail.com.
authors.forename: Sushama
authors.initials: S
authors.lastname: Talegaonkar
mesh_terms: D000818:Animals; D001842:Bone and Bones / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003907:Dexamethasone / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D017886:Durapatite / Q000737:chemistry* / Q000494:pharmacology*; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D000068296:Risedronic Acid / Q000737:chemistry* / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013607:Tablets / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004337:Drug Carriers; D011091:Polyesters; D011108:Polymers; D013607:Tablets; C558447:methoxypolyethyleneglycol-poly(lactic-co-glycolic acid); D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D003907:Dexamethasone; C028210:monomethoxypolyethylene glycol; D017886:Durapatite; D000068296:Risedronic Acid
keywords: bioceramic; bone density; nanoparticle; osteoporosis; risedronate
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