Drug property improvement solubilization

The different chemical solutions to solubilizing problems discussed in this chapter reveal that in many cases the chemical transformation used also improves the activity profile of the parent molecule. This can be due to purely pharmacokinetic factors such as a better resorption from the organism and faster transport and diffusion. These factors explain also why solubilized drugs are generally faster eliminated and therefore show fewer symptoms of toxicity. But the pharmacological profile also can be affected. Chlorpromazine, for example (Figure 38.26), has neuroleptic properties, whereas the parent phenothi-azine possesses anthelminthic properties. In this example, the attachment of the basic moiety has totally modified the pharmacological profile. However, the replacement of the basic moiety by its carboxylic counterpart yielded a compound totally inactive as neuroleptic (C. G. Wermuth, unpublished result). 

Definition Complex mixture formed from the transesterification of olive oil and PEG-6 Properties Oil nonionic Uses Emollient, solubilizer, emulsifier for cosmetics, pharmaceuticals amphiphilic agent improving drug delivery Features Hydrophilic... 

Putting these properties together, one possible mode of use of dendrimers is as nanoscale containers hosting drugs or other payload in their center—providing solubilization, improved pharmacokinetics (slow release/clearing), membrane permeability, and so on. They also allow the possibility of targeting and/or responsive behavior by surface modification. 

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