Brain penetration and neurological effects of gadobenate dimeglumine in the rat

1997 ◽  
Vol 38 (2) ◽  
pp. 268-272 ◽  
Author(s):  
F. Luzzani ◽  
P. Cipolla ◽  
M. L. Pelaprat ◽  
F. Robert ◽  
C. Gotti ◽  
...  
1997 ◽  
Vol 38 (2) ◽  
pp. 268-272 ◽  
Author(s):  
F. Luzzani ◽  
P. Cipolla ◽  
M. L. Pélaprat ◽  
F. Robert ◽  
C. Gotti ◽  
...  

Purpose: the study aimed at measuring the amount of the gadobenate ion that crosses an experimentally disrupted blood-brain barrier (BBB) in rats following i.v. administration of gadobenate dimeglumine (GD). the intention was also to compare this amount with the minimally effective intrathecal dose that alters the cerebral function. Methods: Sprague Dawley rats with an osmotically disrupted BBB received 0.3 mmol/kg of (153Gd)GD, i.v. Radioactivity was measured in plasma and brain parenchyma. the effect on the cerebral function was evaluated by means of a standard motor coordination test (Rota-rod test). Results: Brain levels of the gadobenate ion were approximately 60 nmol/g tissue after i.v. injection of GD. in rats with an intact BBB, the lowest dose of GD able to slightly impair motor coordination was 0.01 mmol/kg following intracisternal injection. Conclusion: I.v. administration of GD to rats with a disrupted BBB results in brain levels of the gadobenate ion that are more than 20 times lower than those reached following intrathecal administration of the minimal effective dose, as determined by the Rota-rod test.


Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.


2014 ◽  
Author(s):  
Stephen McGuire ◽  
Paul Sherman ◽  
Patrick Grogan ◽  
John Sladky ◽  
Gerald York ◽  
...  
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