Polymeric microspheres for radionuclide synovectomy containing neutron-activated holmium-166.
Poly-L-lactic acid (PLA) microspheres containing neutron-activated 166Ho were investigated as potential agents for radionuclide synovectomy. Stable 165Ho, complexed to acetylacetone (AcAc), was incorporated into PLA spheres by the solvent evaporation technique. Spheres prepared with the optimal mean particle size of 7.2 microns (range 2-13 microns) containing 25.4% 165Ho-AcAc (9.1% 165Ho) were irradiated in a high neutron flux to produce 31.1-36.0 mCi 166Ho. In vitro human plasma studies showed that the irradiated spheres retained 99.0 +/- 0.01% of the 166Ho at 314 hr. In-vivo retention studies were conducted by administering irradiated PLA spheres with 257-591 microCi 166Ho into the joint space of normal rabbits (n = 6). Biodistribution analysis and gamma camera analysis showed 166Ho retention in the joint space after 120 hr of 97.7% +/- 0.8% and 98.2% +/- 2.4%, respectively, with no uptake by the lymph nodes. The ease with which the PLA spheres can be made in the optimal size range for later irradiation and their ability to retain the 166Ho make them attractive agents for radionuclide synovectomy.
Mumper
R J
RJ
Division of Medicinal Chemistry and Pharmaceutics, University of Kentucky, Lexington 40536-0082.
Mills
B J
BJ
Ryo
U Y
UY
Jay
M
M
D000818:Animals; D006695:Holmium / Q000493:pharmacokinetics / Q000627:therapeutic use*; D007719:Knee Joint / Q000378:metabolism*; D008863:Microspheres; D011817:Rabbits; D011868:Radioisotopes / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013585:Synovitis / Q000378:metabolism / Q000532:radiotherapy*; D014018:Tissue Distribution
D011868:Radioisotopes; D006695:Holmium