by Dendrimers are spherical, nanoscale macromolecules having a well-defined, branched architecture and numerous functional surface groups. The precise control over their size, shape, surface functionality and internal cavities/voids makes them promising candidates for targeted drug delivery and imaging applications. Conjugation of drugs to dendrimers allows improvement of their solubility, stability, bioavailability and targeted delivery. Various types of polymer-drug conjugates are also being explored as an approach for enhancing efficacy of therapies.
Dendrimers For Drug Delivery
Dendrimers offer several advantages over other nano carriers for drug delivery. Their highly branched, repetitively branched structure provides a large surface area for conjugating targeting ligands and drugs. Multiple functionalities on the surface enable attachment of tissue/organ-specific targeting moieties like peptides, antibodies etc. Drugs can be encapsulated inside the core or covalently attached to the surface functional groups.
The number of functional groups that can be modified also makes it possible to conjugate groups that improve dendrimer bioavailability like PEG chains. Due to controlled synthesis process, properties like size, functionality and drug loading capacity can be precisely tuned. Studies have shown conjugated drugs have improved aqueous solubility, stability and bioavailability compared to free drugs. Targeted delivery is also feasible due to reactive surface groups available for ligands. Overall, dendrimers have emerged as a promising nanocarrier for delivery of anticancer, anti-inflammatory and antimicrobial drugs.
Polymer-Drug Dendrimers And Polymer Drugs Conjugate
Dendrimers And Polymer Drugs Conjugate to synthetic polymers like PEG, PLA, PLGA etc. is another active area of research. Like dendrimers, it allows drugs to circulate for longer time in body while releasing the drug at the target site gradually via biodegradation of linker. Common techniques used are formulation into polymer nanoparticles or covalent attachment to backbone via hydrolyzable bonds.
The flexibility and hydrophilicity conferred by polymers helps address issues like poor solubility and stability of many drugs. For instance, PEG chains attached to drug molecules increase their hydrodynamic size and shield them from renal filtration or uptake by the reticuloendothelial system (RES). This enhances permeability and retention (EPR) effect at tumors. Polymer-drug conjugates having biodegradable linkers are also promising for controlled intracellular drug release.
Applications In Cancer Therapy
Both dendrimers and polymer drug conjugates shows potential for improving cancer chemotherapy. They offer ability to selectively target tumor tissues via passive or active targeting. This enhances drug concentrations at tumors while reducing toxicity to normal cells.
For example, poly(lactic-co-glycolic acid) (PLGA) nanoparticle encapsulating doxorubicin showed efficient tumor accumulation in vivo. Conjugation of camptothecin, an anticancer topoisomerase I inhibitor to poly(l-glutamic acid) also improved its solubility, pharmacokinetic properties and efficacy in cancer models.
Dendrimers functionalized with folic acid as a targeting ligand showed potential for folate receptor positive cancer cells. They were found to selectively internalize into cancer cells and inhibit their growth compared to free drug. Antibody conjugated dendrimers are actively explored for delivery of variety of chemotherapeutics as well for targeted therapy of cancers like glioma.
Other Applications
Beyond oncology, polymer-drug and dendrimer constructs also holds promise for managing chronic conditions as well as local diseases and infections. For example, conjugation of anti-HIV drugs azidothymidine and dideoxyadenosine to generation 5 polyamidoamine dendrimers was found to alter their biodistribution in favor of lymphatic tissues. This could aid treatment of viral reservoirs.
In ophthalmology, some constructs like dendrimer-fluocinolone acetonide showed potential for sustained drug delivery to posterior segment of eye for treating retinal diseases. Polymers have also been explored as carriers for antibiotic, antifungal and antimicrobial agents to treat infections locally as drug conjugates. Their ability to facilitate intracellular delivery and sustained release makes them attractive carriers for gene and oligonucleotide therapeutics delivery as well.
Dendrimers and synthetic polymer based drug delivery systems have demonstrated ability to improve pharmacokinetics, biodistribution and therapeutic efficacy of variety of drugs. Their tunable properties enable targeted and controlled delivery. While further optimizations are required, they represent a promising platform technology for next-generation therapies. With advances in material design and formulations, these carrier systems could help address current limitations and facilitate management of both acute and chronic diseases more effectively.
*Note:
1. Source: Coherent Market Insights, Public sources, Desk research
2. We have leveraged AI tools to mine information and compile it
About Author - Alice Mutum
Alice Mutum is a seasoned senior content editor at Coherent Market Insights, leveraging extensive expertise gained from her previous role as a content writer. With seven years in content development, Alice masterfully employs SEO best practices and cutting-edge digital marketing strategies to craft high-ranking, impactful content. As an editor, she meticulously ensures flawless grammar and punctuation, precise data accuracy, and perfect alignment with audience needs in every research report. Alice's dedication to excellence and her strategic approach to content make her an invaluable asset in the world of market insights. LinkedIn
