The use of biomaterials as drug carriers is being extensively investigated as a drug delivery strategy in pharmaceutical research. However, the selection of materials for such systems is rather complicated. Lately, the advent of biomaterials brought the use of polymers as drug vehicles into the spotlight. Chitosan and albumin are two of the most promising biomaterials for the development of drug delivery systems. These are widely available in nature and can be used as scaffolds of unprecedented novel structure, presenting high biocompatibility and biodegradability and reduced toxicity. Moreover, these molecules promote optimized pharmacokinetics for targeted drug delivery and controlled release, and avoid accumulation or undesired side effects in healthy tissues Chitosan is a linear polysaccharide obtained from chitin and, when used as drug carrier, demonstrates to improve drugs pharmacokinetic profiles when comparing with the drug alone. Albumin is the most abundant protein in blood plasma, which has been receiving renewed interest in the development of drug delivery systems. Importantly, albumin is already an “off-the-shelf” product. Advances in the study of engineered biomaterials represent a step forward in the exploitation, development and commercialization of new therapies for old, poorly served medical needs.