Research Article published MDPI
Clinical applications of many small molecules are limited due to poor solubility and lack
of controlled release besides lack of other desirable properties. Experimental and computational
studies have reported on the therapeutic potential of polyamidoamine (PAMAM) dendrimers as
solubility enhancers in pre-clinical and clinical settings. Besides formulation strategies, factors such
as pH, PAMAM dendrimer generation, PAMAM dendrimer concentration, nature of the PAMAM
core, special ligand and surface modifications of PAMAM dendrimer have an influence on drug
solubility and other recommendable pharmacological properties. This review, therefore, compiles the
recently reported applications of PAMAM dendrimers in pre-clinical and clinical uses as enhancers
of solubility and other desirable properties such as sustained and controlled release, bioavailability,
bio-distribution, toxicity reduction or enhancement, and targeted delivery of small molecules with
emphasis on cancer treatment.