e-journal
Dendrimers in Oncology: An Expanding Horizon
Drug delivery is a critical aspect in formulation because proper selection of the delivery system can control the bioavailability, the concentration profile, and undesirable side effects. Dendrimers pose an exciting opportunity for chemists to fabricate macromolecular structures with a specifically tailored function. They are the same size as serum protein and hence are capable of directly entering into the tumor microvasculature. Dendrimers can be efficiently used to achieve pH-dependent release with a slower release of their payload under normal physiological conditions and a burst release at the acidic tumor site. In addition, the irritating behavior of polycationic dendrimers toward biomembranes creates transient nanoholes, which further helps in the exchange of payload across the biomembrane.
However, in reality, drug-loaded dendrimeric formulations release a considerable portion of the loaded bioactives at extra-tumorous sites after administration. To avoid such peripheral drug release, drug conjugation was explored. The abundance of free amine groups on the dendrimers’ surface allowed easy covalent conjugation of drugs. But the open conformation of dendrimers still continued to exhibit higher hemolytic toxicity and low biocompatibility. PEGylation of the dendrimers produced biocompatible and long circulating
nanocarriers with a sustained release effect. The liposomal “locked in” dendrimers were also reported to reduce dendrimer related toxicity as well as to make the system long circulating.
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