Drug solubilization by complexation

Loftsson T

Drugs must possess some solubility in water to be therapeutically effective after oral or topical administration to the eye, and drugs must be soluble to be formulated as aqueous solutions for, for example, parenteral delivery. A variety of methods can be applied to enhance aqueous solubility of poorly soluble drugs one of which is the usage of solubilizing complexing agents. There are numerous types of complexes and some are more water-soluble than others. Coordination complexes consist of drugs that act as complexing agents (i.e. ligands) and metal ions (i.e. substrates). Examples of coordination complexes are some water-soluble tetracycline-metal ion complexes. Organic molecular complexes can consist of a small substrate (i.e. the drug) and a small (e.g., caffeine) or a large (e.g., polyvinylpyrrolidone) ligand. In inclusion complexes the substrate is partly or completely enveloped by the complexing agent (e.g., cyclodextrin). Finally, pharmacosomes are drug-phospholipid complexes that can not only enhance aqueous solubility of poorly soluble drugs but also their solubility ...