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Some Facts About Liposomal Clodronate

By Roxanne Cruz


Liposomal clodronate therapy is a very useful drug formulation for treating autoimmune hemolytic anemia. This particular autoimmune disease destroys red blood cells. Usual therapies include the use of corticosteroids and splenectomy, but this one gives very fast and promising results by destroying macrophages.

Clodronate is a member of the family of bisphosphonates. It was first used as a treatment for osteolytic bone diseases. Thanks to its characteristics, now it is effectively used in liposome mediated macrophage suicide technique, for depleting macrophages from different organs and tissues. This targeted therapy is very successful in all previous medical research.

Although clodronate itself wouldn't be able to successfully pass through all cell membranes, using liposomes as the vehicles efficiently solves this problem. Macrophages eagerly eat those liposomes, filling their cells with encapsulated clodronate, until the critical concentration is reached. At this point, they simply destroy themselves.

This drug itself is not toxic, and when it is finally released from those dead macrophage cells, it has very short half-life in the circulation. This means that it will soon be completely removed from the organism by the renal system. Specificity of this method is that these ingredients give very quick results. This is especially important in cases where it is necessary to get a quick response to therapy.

Liposomes cannot get through capillary walls. This means that intravenous therapy can be useful for depleting macrophages in spleen, lung, joints, peritoneal cavity and other organs, including testis. Targeted therapy is also possible, using intraperitoneal injection. Macrophages won't be completely removed, but they are needed for different processes in the organism, anyway.

This method is developed for in vivo use. After destroying targeted macrophages, the drug gets released and enters the circulation. Thanks to the fact it has quite short half life once it reaches the circulation, it will be soon removed from the organism, and it won't be accumulated in surrounding cells. That's why this suspension cannot be so efficient in in vitro research.

The required temperature for storing and keeping this suspension is 4 degrees of Celsius. It is very important to take a good care about this temperature, and to use the product within a few days. Before using the product, it should reach a room temperature slowly. It means you have to leave it there for some time, and to shake it well before injecting it. Other things to remember are not to freeze the product ever, and not to expose it to temperatures above 30 degrees of Celsius.

Intravenous injection should not be more than 0.1 ml per 10 grams of body weight. For intraperitoneal injection, this volume may be increased considerably. However, the concentration the drug in the aqueous compartments within the liposomes is limited by the solubility of clodronate.

Liposomal clodronate therapy will effectively destroy macrophages. The absence of macrophages may cause an increase in e. G., virus titers, bacteria or yeasts. Test animals should always be perfectly clean where injected, to avoid possible microbial contamination. You should always shake the syringe, to get a homogeneous suspension, especially if you use the same one on all your test animals, which is not recommended.




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