Drug targeting to arthritic region via folic acid appended surface-engineered multi-walled carbon nanotubes.
This study was aimed at developing and investigating folate anchored carbon nanotubes for targeting an anti-arthritic drug, Methotrexate (MTX) to inflammatory arthritic region. The folic acid (FA) was conjugated to amidated multi-walled carbon nanotubes (MWCNTs) and confirmed by Fourier transform infrared (FTIR), (1)H NMR spectroscopy and X-ray diffraction analysis. The MTX was loaded into the pristine and functionalized-MWCNTs and extensively characterized in vitro and in vivo studies. The drug entrapment efficiency was found high in folate conjugated MWCNTs. In vitro drug release in PBS (pH 7.4) from pristine MWCNTs and folate conjugated MWCNTs formulation was found to be 66.35 ± 2.3 and 56.88 ± 1.9% in 24 h, respectively. Folate conjugated MWCNTs significantly increased (p < 0.005) the percentage inhibition of arthritis, biological half-life and volume of distribution of MTX as compared to MTX-loaded naked MWCNTs as well as free MTX. In in vivo biodistribution studies, MTX was found to be significantly higher (p < 0.005) in arthritic joints from folate functionalized MWCNTs as compared to free drug as well as drug-loaded naked MWCNTs. The present outcomes highlights the propensity of drug-loaded functionalized MWCNTs to alter the pharmacokinetics as well as sustained and targeted drug delivery system as well.
a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India .
Jitendra
J
Kayat
a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India .|b Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics , ISF College of Pharmacy , Moga , Punjab , India , and.
Neelesh Kumar
NK
Mehra
c Center for Nanobioscience, Agharkar Research Institute , Pune , Maharashtra , India.
Virendra
V
Gajbhiye
a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India .|b Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics , ISF College of Pharmacy , Moga , Punjab , India , and.
Narendra Kumar
NK
Jain
D000818:Animals; D018501:Antirheumatic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001169:Arthritis, Experimental / Q000188:drug therapy / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005492:Folic Acid / Q000737:chemistry*; D006614:Hindlimb / Q000187:drug effects / Q000378:metabolism; D007596:Joints / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008727:Methotrexate / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D036103:Nanotechnology; D037742:Nanotubes, Carbon / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013499:Surface Properties; D014018:Tissue Distribution
D018501:Antirheumatic Agents; D004337:Drug Carriers; D037742:Nanotubes, Carbon; D005492:Folic Acid; D008727:Methotrexate
Arthritic region; folate; methotrexate; multi-walled carbon nanotube; targeting