Dendrimers are nanosized, treelike, branched polymeric molecules that have numerous functional surface groups and an interior core. The word dendrimer comes from the Greek word 'dendri' meaning tree. Dendrimers are highly branched macromolecules having three distinct morphological regions - a central core, internal cavities or branching units and external functional surface groups. Dendrimers are generally synthesized in a step-by-step repetitive process which builds up spherical, three-dimensional highly branched structures from the center outwards. Dendrimers possess a certain degree of uniformity and monodispersity, which make them suitable for technological applications.
Key advantages of dendrimers for drug delivery
Some key advantages of dendrimers for drug delivery applications include:
- Nanoscale size: Dendrimers typically range between 1–10 nanometers in size which enable passive diffusion into tissues from the bloodstream. Their nanoscale size also allows accumulation in solid tumors through the enhanced permeability and retention effect.
- Multivalency: Dendrimers And Polymer Drugs Conjugate can carry multiple functional groups and drug molecules on their surface which enables enhanced drug loading capacity and multivalent binding to biological targets.
- Modifiability: Drug molecules, targeting ligands and other functional groups can be easily conjugated or encapsulated inside dendrimer scaffold both during and after synthesis, allowing for versatile surface functionalization and multimodal applications.
- Controlled release: The properties of dendrimers can be tuned to enable controlled or triggered release of encapsulated drug molecules in response to physiological stimuli like pH, temperature or enzymes.
- Biocompatibility: Some classes of dendrimers like PAMAM (polyamidoamine) dendrimers have been proven to be biocompatible and non-immunogenic. However, cytotoxic effects may occur depending on the dendrimer generation, charge and concentration used.
How polymer-drug conjugation improves drug delivery
Conjugating drugs to synthetic polymers is an effective drug delivery strategy that improves the solubility, stability and pharmacokinetics of many drugs. Some key ways how polymer-drug conjugation benefits drug delivery include:
- Enhanced solubility: Attaching hydrophobic drug molecules to hydrophilic polymer carriers improves their water solubility and bioavailability significantly without using organic solvents.
- Prolonged circulation: Polymer-drug conjugates exhibit increased hydrodynamic size which prevents renal clearance and favors prolonged blood circulation through enhanced permeability and retention effect.
- Passive tumor targeting: The increased size of polymer-drug conjugates allows preferential accumulation in tumor tissues via leakier vasculature compared to normal tissues.
- Controlled release: Drugs are released from the polymer carrier gradually via biodegradation or cleavage oflinker bonds inside tumors over an extended period for better efficacy.
- Reduced toxicity: Direct conjugation to polymers masks the charges and functional groups of drugs to minimize non-specific toxicity to normal tissues.
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