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Promising Immunosuppressive Results Through Liposomal Clodronate

| Wednesday, 12 June 2013
By Teri Farley


Liposomal clodronate is a new form of treatment for autoimmune diseases as well as prevention of transplant rejection. It is used to deplete macrophages, thus suppressing immune activity which at present may be heightened for people having an autoimmune disease or those who just came out from transplant surgery.

The results concerning clodronate liposome therapy has been quite fascinating. It showed a strong performance in suppressing the immune system which gave a new hope for rejected transplant patients as well as those that have been suffering on the worst stage of their autoimmune disease. Additionally, such therapy also showed positive results in conjunction with cancer drugs.

Originally clodronic acid is biphosphonate, anti-osteoporotic drug. It was approved for the treatment and prevention of osteoporosis particularly to women and hyperparathyroidism, hypercalcemia and vertebral fracture to men. It was noticed that clodronic acid has a potent analgesic and anti inflammatory effects as it significantly reduced important inflammatory markers.

Inflammatory marker as the name implies is a sign that inflammation is currently going on. Famous inflammatory markers includes interleukin 6,8 and 1 as well as TNF-alfa. However, these markers are only a tiny part of the immune system. Indeed, the immune system consists of thousands of cells all of which has its own tiny role.

Macrophages can be a good thing or bad thing. For an instance, in simple virus infection the macrophages will be the one to fight with the virus thus preventing further infection. But in certain autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis and so on, macrophages are fighting against your healthy cells which caused such diseases.

Clodronic acid is administered through the trachea, directly into the lungs and absorbed by the blood stream. Using liposomes as vehicle, the liposome will be ingested by the macrophages through endocytosis. Certain chemicals inside the cells will disrupt the layer of the liposome releasing the clodronate. There will be an accumulation of clodronic acid inside the macrophage and after exceeding threshold, will cause the macrophage to die through apoptosis.

The mechanism of action on such therapy by far remains to be the most promising form treatment. Immune system suppression is not a new patient management or treatment for certain medical diseases, there have been several oral, parenteral or intravenous drugs were already made to achieve similar results. But some patients remain unresponsive.

With the discovery of clodronic acid therapy, these possibilities may be the least of your concerns. Through the use of liposomes as the drug vehicle the main drug, clodronic acid will be delivered inside the macrophages and after exceeding its threshold, dies by apoptosis. Liposomes are easily engulfed by macrophages which makes it a great choice as a drug vehicle. As the drug is delivered directly into the phagocytic cells, there's a greater chance of suppressing the immune system.

The liposomal clodronate is no doubt a wonder drug as far as autoimmune diseases and transplantation is concerned. Medical studies and experiments are still going on for the therapeutic effect of such therapy in anti neoplastic drugs or Cancer in particular.




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