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Updated: Jun 20, 2025
Synthesis, Cellular Delivery and In vivo Application of Dendrimer-based pH Sensors
Published on: September 10, 2013
Core-Tunable Dendritic Polymer: A Folate-Guided Theranostic Nanoplatform for Drug Delivery Applications
Neelima Koti1, Trishna Timalsena1, Kajal Kajal2
1Department of Chemistry and Biochemistry, Missouri State University, 901 S. National Avenue, Springfield, Missouri 65897, United States.
Abstract:
Clinical application of anticancer drugs is mostly limited due to their hydrophobic nature, which often results in lower bioavailability and lesser retention in systemic circulation. Despite extensive research on the development of targeted drug delivery systems for cancer treatment, delivery of hydrophobic therapeutic drugs to tumor cells remains a major challenge in the field. To address these concerns, we have precisely engineered a new hyperbranched polymer for the targeted delivery of hydrophobic drugs by using a malonic acid-based A2B monomer and 1,6-hexanediol. The choice of monomer systems in our design allows for the formation of higher molecular weight polymers with hydrophobic cavities for the efficient encapsulation of therapeutic drugs that exhibit poor water solubility. Using several experimental techniques such as NMR, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform-infrared (FT-IR), and gel permeation chromatography (GPC), the synthesized polymer was characterized, which indicated its dendritic structure, thermal stability, and amorphous nature, making it suitable as a drug delivery system. Following characterizations, theranostic nanoplatforms were formulated using a one-pot solvent diffusion method to coencapsulate hydrophobic drugs, BQU57 and doxorubicin. To achieve targeted delivery of loaded therapeutic drugs in A549 cancer cells, the surface of the polymeric nanoparticle was conjugated with folic acid. The therapeutic efficacy of the delivery system was determined by various cell-based in vitro experiments, including cytotoxicity, cell internalizations, reactive oxygen species (ROS), apoptosis, migration, and comet assays. Overall, findings from this study indicate that the synthesized dendritic polymer is a promising carrier for hydrophobic anticancer drugs with higher biocompatibility, stability, and therapeutic efficacy for applications in cancer therapy.
Insights
This study developed a novel dendritic polymer for targeted delivery of hydrophobic anticancer drugs. The engineered nanocarrier demonstrated enhanced biocompatibility, stability, and therapeutic efficacy in cancer cells.
Area of Science:
- Polymer Chemistry
- Nanotechnology
- Cancer Therapeutics
Background:
- Hydrophobic anticancer drugs face challenges in clinical application due to poor bioavailability and limited systemic circulation.
- Targeted drug delivery systems are crucial for overcoming these limitations and improving cancer treatment efficacy.
Purpose of the Study:
- To engineer a novel hyperbranched polymer for efficient encapsulation and targeted delivery of hydrophobic anticancer drugs.
- To formulate and characterize theranostic nanoplatforms for enhanced cancer therapy.
Main Methods:
- Synthesis and characterization of a hyperbranched polymer using malonic acid-based A2B monomer and 1,6-hexanediol.
- Formulation of polymeric nanoparticles via a one-pot solvent diffusion method, coencapsulating hydrophobic drugs (BQU57, doxorubicin).
- Surface functionalization with folic acid for targeted delivery to A549 cancer cells, followed by in vitro efficacy assessments.
Main Results:
- Characterization confirmed a dendritic structure, thermal stability, and amorphous nature suitable for drug delivery.
- Folic acid conjugation enabled targeted delivery and enhanced cellular uptake in cancer cells.
- In vitro assays demonstrated significant improvements in cytotoxicity, apoptosis induction, and reduced migration.
Conclusions:
- The synthesized dendritic polymer serves as a promising carrier for hydrophobic anticancer agents.
- The developed nanoplatform exhibits enhanced biocompatibility, stability, and therapeutic potential for cancer treatment.
