Solubilization artemisinin

Dihydroartemisinin ethers. A water-soluble derivative of artemisinin, the sodium salt of artesunic acid (the succinic half-ester derivative of dihydroartemisinin Fig. 35.2), can be administered by intravenous injection, a property that makes it especially useful in the treatment of advanced and potentially lethal cases of Plasmodium falciparum. Sodium artesunate is capable of rapidly reversing parasitaemia and causing the restoration to consciousness of the comatose cerebral malaria patient. The utility of sodium artesunate, however, is impaired by its poor stability due to the facile hydrolysis of the ester linkage. To overcome the ease of hydrolysis of the ester function in sodium artesunate, Lin et aO prepared a series of analogues in which the solubilizing moiety is joined to dihydroartemisinin by an... 

The amphiphilic molecules constituting the micelles can be surfactants, like sodium dodecyl sulfate (SDS) for the solubilization of artemisinin and curcumin or for the delivery of polyphe-nolic fractions from Hamamelis virginianaP The micelles can also be formed of synthetic block copolymers. For example, copolymers of caprolactone 2-(methacryloyloxy)ethyl ester units with poly(meth)acrylic acid side chains have been self-assembled in micelles of quercetin associated with indomethacin for the treatment of inflammatory diseases (Figure 36.10). Resveratrol has been loaded into PCL-PEG micelles for its protective effect against oxidative stress. An aqueous formulation of luteolin has been developed with the same PCL-PEG micelles, with potential anticancer effect. ... 

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