Facile functionalization of Teriflunomide-loaded nanoliposomes with Chondroitin sulphate for the treatment of Rheumatoid arthritis.

This research aims to coat Teriflunomide (TEF) loaded conventional nanoliposomes (CON-TEF-LIPO) with Chondroitin sulphate (CS) to produce CS-TEF-LIPO for the effective treatment of Rheumatoid arthritis (RA). Both CON-TEF-LIPO and CS-TEF-LIPO were produced, characterized and evaluated for their active targeting potential towards CD44 receptors. Cell cytotoxicity, cell viability and intracellular uptake study on differentiated U937 and MG-63 cells demonstrated the active targeting of CS-TEF-LIPO towards CD44 receptors. Furthermore, in vivo pharmacodynamic, biochemical, radiological and histopathological studies performed in adjuvant induced arthritic (AIA) rat model showed a significant (P < 0.05) reduction in inflammation in arthritic rat paw in CS-TEF-LIPO group compared to TEF and CON-TEF-LIPO groups. Moreover, liver toxicity study revealed that CS-TEF-LIPO showed no signs of toxicity and biodistribution study revealed the accumulation of CS-TEF-LIPO in synovial region of arthritic rat. Taken together, results suggest that CS-TEF-LIPO could provide a new insight for an effective treatment of RA.

Role of 99mTc-Tetrofosmin delayed scintigraphy and color Doppler sonography in characterization of solitary thyroid nodules.

OBJECTIVES: A study was undertaken to evaluate the diagnostic efficiency of Tc-Tetrofosmin scan and color Doppler in the characterization of benign and malignant solitary thyroid nodules. METHODS: Fifty-two patients found to have a cold solitary thyroid nodule on Tc-pertechnetate scintigraphy were included in this study. All patients underwent a single-injection dual-phase (30 min and 120 min) Tc-Tetrofosmin scan. The intranodular vascularity was measured using color Doppler sonography. Fine-needle aspiration cytology was performed on all the patients. In the following days and weeks all patients underwent surgery. RESULTS: Thirteen out of 15 patients with thyroid cancer showed delayed retention of radiotracer (on 120 min images as compared to the initial 30 min image). Thirty-six out of 37 patients harboring benign solitary nodules showed significant washout of tracer on delayed images. Sensitivity, specificity, positive predictive value and negative predictive value of delayed Tc-Tetrofosmin scintigraphy were found to be 86.6, 97.2, 92.8 and 94.7%, respectively. The Doppler study was able to demonstrate increased vascularity in the center of 8 of the 15 malignant nodules. Thirty-two patients harboring a benign solitary nodule showed normal or increased peripheral vascularity on Doppler study. Sensitivity, specificity, positive predictive value and negative predictive value of color Doppler were found to be 53.5, 86.4, 61.5 and 82%, respectively. CONCLUSION: Delayed Tc-Tetrofosmin scintigraphy is a highly sensitive and specific method for characterizing solitary thyroid nodules, while color Doppler has a low sensitivity but relatively high specificity in differentiating benign from malignant thyroid lesions.

Synthesis, characterization, and in vivo skeletal localization of a new (99m)Tc-based multidentate phosphonate chelate: 5-Amino-1,3-bis(ethylamine-(N,N dimethyl diphosphonic acid) acetamido) benzene.

The tetraphosphonate ligand, 5-amino-1,3-bis(ethylamine-(N,N-dimethyl diphosphonic acid) acetamido) benzene (IPTMP) used in the present study was prepared from 5-nitroisophthalate dimethylester to label with radionuclide for targeted diagnosis and therapy. The synthesized multidentate phosphonate ligand was characterized on the basis of spectroscopic techniques, which exhibited good metal ion control properties when complexed to (99m)Tc with high in vitro and in vivo stability. Excellent quality bone images of rabbit were imaged showing rapid clearance of background activity and visualization of skeleton at 1h.