All trans retinoic acid

Apr 3
08:21

2012

David Yvon

David Yvon

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All-trans formic acid’s antitumor effect was regarded as one of three discoveries of the anti-cancer drugs in the 1990s. It has a strong induction of differentiation of tumor cells and aroused the concern of the international pharmaceutical industry.

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It is the first choice clinical drug in acute promyelocytic leukemia,All trans retinoic acid Articles bone marrow dysplasia and especially the promyelocytic leukemia. Clinical evidence shows it can be used in the treatment of acne, lichen planus, vitiligo, multiple common warts and keratotic skin diseases. It has a significant effect.

All-trans tretinoin induced tumor cell differentiation and apoptosis in the tumor. It increases the sensitivity of cancer cells to chemotherapeutic drugs promotes the proliferation of immune cells. Retinoic acid enhanced the immune cells to kill tumor cells. All-trans retinoic acid for the treatment of acute promyelocytic leukemia, ATRA reduced cytotoxic chemotherapy cell damage and disseminated intravascular coagulation, which reduces the early mortality of newly diagnosed APL, make the most of the patients to achieve complete remission. In addition, ATRA can also be used for the treatment of digestive system tumors of the colon, esophageal, pancreatic, solid tumors, especially for the treatment of liver cancer has good prospects. The oral bioavailability of the drug use is low, and long-term use is easy to produce drug resistance, because of the sharp decline in drug concentration in the blood. And because of its fat-soluble strong, conventional means is difficult to prepare minoxidil injectable formulations. Will be the ATRA prepared liposomes can significantly increase the therapeutic index and lower toxicity.

All-trans retinoic acid has following advantages: improve the stability of the drug can significantly reduce the oxygen of the light and heat damage to the retinoic acid; targeting liposomes to carry drugs, primarily blankets nuclear macrophage system of phagocytes uptake rich in reticuloendothelial cells of the liver, spleen and bone marrow organ distribution more effective role in the target area; increase the sustained-release liposome significantly increased the retention time of the drug in the blood and play a long-lasting effect; encapsulated in liposomes of lipophilic drugs, retinoic acid injection as possible.

Liposomes as anticancer drug carriers can increase the affinity of cancer cells to overcome the resistance and increase the cancer cells to drug intake. It reduces dose, improve efficacy and reduce toxicity characteristics. Experimental results show that the liposome doxorubicin toxicity than free drug reduced by 50% to 70% in the tumor suppressor activity of liposome formulations are much higher than the free drug, repeated treatment prolong the survival time of tumor-bearing animals. Targeted, long-lasting effect and reduce glutathione drug toxicity is the three characteristics of the liposome, which targeted the most prominent advantage of liposomes as drug carriers

Combination of oral all-trans retinoic acid and chemotherapy can acute promyelocytic leukemia in complete molecular biology alleviates. But oral ATRA alone can not achieve these results. The exclusive use of liposomes coated all-trans retinoic acid can be effective in newly diagnosed APL patients achieving complete molecular biology alleviate The researchers believe that the lipoATRA and oral ATRA have higher serum concentration and duration. They can be used as the induction of remission drugs in newly diagnosed APL patients. It also has mitigation effect in hematology and molecular biology.Source:http://www.cosprm.com