title: Targeting of diacerein loaded lipid nanoparticles to intra-articular cartilage using chondroitin sulfate as homing carrier for treatment of osteoarthritis in rats.
abstract: Targeted delivery of antiosteoarthritic drug diacerein to articular tissue could be a major achievement and soluble polysaccharide chondroitin sulfate (ChS) may be a suitable agent for this. Therefore, diacerein loaded solid lipid nanoparticles modified with ChS (ChS-DC-SLN) were prepared for synergistic effect of these agents to combat multidimensional pathology of osteoarthritis (OA). Prepared formulation were of size range 396±2.7nm, showed extended release up to 16h and increased bioavailability of diacerein by 2.8 times. ChS-DC-SLN were evaluated for their effect on histopathology of femoro-tibial joint of rat knee and amount of ChS and rhein (an active metabolite of diacerein) at targeted site. Concentration of rhein was significantly higher in case of ChS-DC-SLN (7.8±1.23μg/ml) than that of drug dispersion (2.9±0.45μg/ml). It can be stated that ChS served as homing to articular cartilage for targeting of drug. Thus, ChS-DC-SLN have great potential to enhance the overall efficacy of treatment for OA.
  
  
  BACKGROUND
  This study demonstrates the feasibility of targeted delivery of diacerein to articular tissue using soluble polysaccharide chondroitin sulfate as the targeting vector. This approach has the potential to significantly increase anti-arthritic drug concentration in joints without leading to systemic toxicity.
authors: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India; National Institute of Pharmaceutical Education and Research (NIPER), Raebareli, India.
authors: Achint
authors: A
authors: Jain
authors: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India.
authors: Sandeep Kumar
authors: SK
authors: Mishra
authors: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India.
authors: Parameswara Rao
authors: PR
authors: Vuddanda
authors: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India.
authors: Sanjay Kumar
authors: SK
authors: Singh
authors: Department of Anatomy, Institute of Medical Sciences, Banaras Hindu University, Varanasi, India.
authors: Royana
authors: R
authors: Singh
authors: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi, India. Electronic address: ssingh.phe@iitbhu.ac.in.
authors: Sanjay
authors: S
authors: Singh
mesh_terms: D000818:Animals; D000880:Anthraquinones / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use; D002358:Cartilage, Articular / Q000187:drug effects*; D002809:Chondroitin Sulfates / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010003:Osteoarthritis / Q000188:drug therapy*; D051381:Rats
chemical_list: D000880:Anthraquinones; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D008055:Lipids; C025292:diacerein; D002809:Chondroitin Sulfates
keywords: Articular cartilage; Chondroitin sulfate; Diacerein; Histopathology; Nanoparticles