Polymer-dendrimer Hybrids as Carriers of Anticancer Agents.

In recent years, polymeric materials with the ability to self-assemble into micelles have been increasingly investigated for application in various fields, mainly in biomedicine. Micellar morphology is important and interesting in the field of drug transport and delivery since micelles can encapsulate hydrophobic molecules in their nucleus, improve the solubility of drugs, have active molecules in their outer layer, and, due to their nanometric size, they can take advantage of the EPR effect, prolong circulation time and avoid renal clearance. Furthermore, bioactive molecules (could be joined covalently or by host-host interaction), such as drugs, bioimaging molecules, proteins, targeting ligands, "cross-linkable" molecules, or linkages sensitive to internal or external stimuli, can be incorporated into them. The confined multivalent cooperativity and the ability to modify the dendritic structure provide versatility to create and improve the amphiphiles used in the micellar supramolecular field. As discussed in this review, the most studied structures are hybrid copolymers, which are formed by the combination of linear polymers and dendrons. Amphiphilic dendrimer micelles have achieved efficient and promising results in both in vitro and in vivo tests, and this encourages research for their future application in nanotherapies.

Nanomedical Applications of Amphiphilic Dendrimeric Micelles.

In recent years, polymeric materials with the ability to self-assemble into micelles have been increasingly investigated for application in various fields, mainly in biomedicine. Micellar morphology is interesting in the field of drug transport and delivery since micelles can encapsulate hydrophobic molecules in their nucleus, have active molecules in their outer layer, and due to their nanometric size, can take advantage of the enhanced permeability and retention (EPR) effect, prolong the time in circulation and avoid renal clearance. In addition, nanobioactive molecules (joined in covalent form or by host-host interaction), such as drugs, bioimaging molecules, targeting ligands, "crosslinkable" molecules or bonds, sensitive to internal or external stimuli, can be incorporated into them and showed better activity as anticancer agents, siRNA delivery agents as well as antiviral and antiparasitic compounds. The present work is a review of the information published, which is the most important about the synthesis and biological importance of the confined multivalent cooperation and the ability to modify the dendritic structure, provide the versatility to create and improve the amphiphiles used in the micellar supramolecular field. The most studied structures are the hybrid copolymers formed by the combination of linear polymers and dendrons. However, small dendritic molecules that do not involve linear polymers have also been developed, such as Janus dendrimers, facial dendrons, and dendritic amphiphiles with only one dendron. Amphiphilic dendrimer micelles have achieved efficient and promising results, both in in vitro and in vivo tests, which encourage their research for future application in nanotherapies.

Synthesis and anticancer activity of open-resorcinarene conjugates.

The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells. The conjugates with naproxen and indomethacin showed high selectivity towards U-251 tumor cells.