Synthesis and preliminary evaluation of 99mTc-Hynic-fragments [F(ab′)2 and F(ab′)] of Rituximab as radioimmunoscintigraphic agents for patients with Non-Hodgkin's lymphoma

This study was to evaluate the potential of Tc-99m-Hynic-fragments of Rituximab as radioimmunoscintigraphic agents for diagnosis of patients with Non-Hodgkin's Lymphoma (NHL). Rituximab was digested with immobilized pepsin and papain to yield F(ab')(2) -Rituximab and F(ab')-Rituximab fragments respectively. Purified fragments were characterized by SE-HPLC and SDS-PAGE and subsequently radiolabeled with technetium-99m using Hynic as bifunctional chelator. The Tc-99m-Hynic-F(ab')(2)-Rituximab and Tc-99m-Hynic-F(ab')-Rituximab exhibited good in-vitro stability and specificity to Raji cells. Biodistribution studies demonstrated rapid pharmacokinetics and clearance predominantly through renal route.