It is clear that biology has much to offer nanotechnology in demonstrating how to organize, functionalize, and assemble new molecular and submolecular materials and tools to design nanosize carriers for bioactive substances. From the chemical point of view, it is important to synthesize newer polymers and surfactants to match the hydrophilic and hydrophobic properties of the bioactive substances. Implementation of cavitands for the formation of inclusion complexes can dramatically increase the loading capacity of carriers in combination with polymer nanoparticles and liposomes. Their new amphiphilic derivatives are capable of forming nanospheres and nanocapsules, presenting a high loading capacity toward both hydrophobic and hydrophilic drugs without any polymerization process. In order to provide the targeted delivery and controlled release of the bioactive substance, designing the carriers with tailored surface characteristics based on specific peptide, protein, polynucleotide, or polysaccharide motifs with preordained functions becomes the regular strategy.