Methotrexate-Loaded Surface-Modified Solid Lipid Nanoparticles Targeting Cancer Expressing COX-2 Enzyme.

Cancer is a major public health problem worldwide, and it is the second leading cause of death of humans in the world. The present study has been directed toward the preparation of methotrexate-loaded surface-modified solid lipid nanoparticles (SLNs) for potential use as a chemotherapeutic formulation for cancer therapy. A lipid (C-AAP) derived from myristic acid (CHO) and acetaminophen (AAP) was employed as a targeting ligand for human breast and lung cancer cells that overexpress the cyclooxygenases-2 (COX-2) enzyme.

Intricacies in the Preparation of Patient Doses of [Lu]Lu-Rituximab and [Lu]Lu-Trastuzumab Using Low Specific Activity [Lu]LuCl: Methodological Aspects.

The development of humanized monoclonal antibodies (MAbs) with Lutetium-177 ([Lu]Lu) has brought a paradigm shift in the arena of targeted therapy of various cancers. [Lu]Lu-DOTA-Rituximab and [Lu]Lu-DOTA-Trastuzumab have gained prominence due to their improved therapeutic efficacy in the treatment of lymphoma and breast cancer. The clinical dose formulation of these radiolabeled MAbs, using low specific activity [Lu]LuCl, requires extensive optimization of the radiolabeling protocol.

Ga-Labeled Trastuzumab Fragments for ImmunoPET Imaging of Human Epidermal Growth Factor Receptor 2 Expression in Solid Cancers.

Trastuzumab, the first humanized antibody approved for therapeutic use has shown promising results for the treatment of patients with human epidermal growth factor receptor 2 (HER2) positive cancers. The aim of this study was to formulate immunoPET agents based on trastuzumab fragments and demonstrate their potential for early diagnosis of HER2-positive tumors. F(ab') and F(ab') fragments of trastuzumab were prepared by enzymatic digestion and conjugated with chelator NOTA for labeling with Ga.

Clinical Dose Preparation of [Lu]Lu-DOTA-Pertuzumab Using Medium Specific Activity [Lu]LuCl for Radioimmunotherapy of Breast and Epithelial Ovarian Cancers, with HER2 Receptor Overexpression.

The overexpression of human epidermal growth factor receptor 2 (HER2) is commonly associated with metastatic breast cancer and epithelial ovarian cancer. The U.S.

Automated radiochemical synthesis of pharmaceutical grade [ F]FLT using 3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine precursor and its Sep-Pak® purification employing selective elution from reversed phase.

Pharmaceutical grade 3'-deoxy-3'-[ F]fluorothymidine [ F]FLT was synthesized using 3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine (BOC-Nosyl) precursor, in the general purpose TRACERlab FX modules. Purification of [ F]FLT, via solid phase extraction (SPE) after radiosynthesis, using a combination of different SPE cartridges, yielded satisfactory results, with radiochemical and chemical purity >99%. While the non-decay corrected radiochemical yield (RCY) with 20 mg (24 μmole) of BOC-Nosyl precursor was found to be 6.

Therapeutic Multidose Preparation of a Ready-to-Use Lu-PSMA-617 Using Carrier Added Lutetium-177 in a Hospital Radiopharmacy and Its Clinical Efficacy.

[Lu]Lu-prostate-specific membrane antigen (PSMA)-617 has emerged as a promising radiopharmaceutical for targeting PSMA in metastatic castrate-resistant prostate carcinoma (mCRPC). We have optimized the radiolabeling protocol for a multidose formulation (27-28.8 GBq equivalent to 6-7 patient-doses) of [Lu]Lu-PSMA-617 using [Lu]Lu produced via Lu(n,γ)Lu route with moderate specific activity (0.

On the Separation of Yttrium-90 from High-Level Liquid Waste: Purification to Clinical-Grade Radiochemical Precursor, Clinical Translation in Formulation of Y-DOTATATE Patient Dose.

The quality control parameters of in-house-produced Y-Acetate from high-level liquid waste (HLLW) using supported liquid membrane (SLM) technology were validated and compared with the pharmacopeia standard. The radiolabeling of DOTATATE yielding Y-DOTATATE in acceptable radiochemical purity (RCP), with expected pharmacological behavior in models, establish the quality of Y-Acetate. Clinical translation of Y-Acetate in formulation of Y-DOTATATE adds support toward its use as clinical-grade radiochemical.