Poly(amidoamine) dendrimers as a pharmaceutical excipient. Are we there yet?
Abstract
Drug solubility could affect the therapeutic use of a drug because the biological activity of a drug is only
possible if some fraction of a dissolved drug can permeate and overcome biological membranes to reach
its site of action. The solubility-permeation interplay is therefore, probably the most important factor in
determining a successful therapeutic outcome of any drug because more than 40% of marketed drugs and
more than 70% of pipeline drugs show poor water solubility. Several solubilization techniques are used
and include, balancing of pH-pKa properties, employment of cosolvents, and the solubilization by hostguest
carriers. A relatively new addition to the polymer plethora of solubilizers are the poly(amidoamine)
dendrimers. These highly branched, “tree-like” nanocarriers have a significant solubilization capacity for
drugs in their cavities and also potentially via their terminals. Despite their successful solubilization
capability, they are still plagued by some undesired properties such as cytotoxicity. Poly(amidoamine)
however, seems to be a very lucrative target to develop into a pharmaceutical excipient, which will
ultimately be confirmed by an official pharmacopeial monograph
URI
http://hdl.handle.net/10394/26435https://www.sciencedirect.com/science/article/pii/S0022354917307037
https://doi.org/10.1016/j.xphs.2017.10.011
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- Faculty of Health Sciences [2404]