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Hyperbranched polyphosphates for drug delivery application: design, synthesis, and in vitro evaluation
Jinyao Liu1, Wei Huang, Yan Pang
1School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, PR China.
Biomacromolecules
|April 7, 2010
Summary
A novel water-soluble hyperbranched polyphosphate (HPHEEP) shows excellent biocompatibility and biodegradability. This polymer is a promising candidate for developing effective drug delivery systems, particularly for anticancer therapies.
Area of Science:
- Polymer Chemistry
- Biomaterials Science
- Nanotechnology
Background:
- Developing biocompatible and biodegradable drug carriers is crucial for effective drug delivery.
- Hyperbranched polymers offer unique properties for drug encapsulation and release.
- Polyphosphates represent an emerging class of biomaterials with potential therapeutic applications.
Purpose of the Study:
- To synthesize a water-soluble hyperbranched polyphosphate (HPHEEP) using self-condensation ring-opening polymerization (SCROP).
- To evaluate the in vitro biocompatibility, biodegradability, and cellular uptake of HPHEEP.
- To assess the efficacy of HPHEEP as a drug carrier for an anticancer drug, chlorambucil.
Main Methods:
- Synthesis of HPHEEP via SCROP of 2-(2-hydroxyethoxy)ethoxy-2-oxo-1,3,2-dioxaphospholane (HEEP).
- In vitro biocompatibility assessed using MTT and live/dead staining assays on COS-7 cells.
- Biodegradability evaluated by NMR; degradation products tested for toxicity.
- Cellular internalization and localization studied via flow cytometry and confocal microscopy.
- HPHEEP-chlorambucil conjugate efficacy tested against MCF-7 cells using MTT assay.
Main Results:
- HPHEEP demonstrated excellent biocompatibility and non-toxic degradation products.
- HPHEEP was readily internalized by cells and localized in the perinuclear region.
- The HPHEEP-chlorambucil conjugate showed potent anticancer activity against MCF-7 cells.
- The conjugate required a higher dose for 50% growth inhibition compared to free chlorambucil, suggesting efficient intracellular drug release.
Conclusions:
- HPHEEP is a biocompatible and biodegradable polymer suitable for drug delivery.
- HPHEEP facilitates cellular uptake and perinuclear accumulation.
- The polymer's properties enable effective delivery of hydrophobic anticancer drugs.
- HPHEEP presents a promising platform for designing advanced drug delivery systems for therapeutic applications.
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