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Biocompatible polymeric micelles with polysorbate 80 for use in brain targeting
E F Craparo1, M C Ognibene, M P Casaletto
1Dipartimento di Chimica e Tecnologie Farmaceutiche, Università degli Studi di Palermo, Via Archirafi, 32, 90123 Palermo, Italy.
Nanotechnology
|August 13, 2011
Summary
Novel amphiphilic graft copolymers were synthesized and formed into polymeric micelles. These biocompatible micelles show promise for cellular delivery and avoiding phagocytosis, offering new avenues in biomaterial applications.
Area of Science:
- Biomaterials Science
- Polymer Chemistry
- Nanotechnology
Background:
- Amphiphilic graft copolymers are crucial for developing advanced drug delivery systems.
- Poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA) and polylactic acid (PLA) offer tunable properties for biomaterial applications.
- Designing novel copolymers with specific functionalities is essential for targeted therapeutic interventions.
Purpose of the Study:
- To synthesize and characterize novel amphiphilic graft copolymers based on a PHEA backbone with PLA side chains.
- To form and analyze polymeric micelles from these copolymers for potential biomedical applications.
- To evaluate the biocompatibility, cellular uptake, and immune evasion capabilities of the developed micellar systems.
Main Methods:
- Synthesis of PHEA-ethylenediamine (PHEA-EDA) functionalized with polysorbate 80 (PS(80)) and/or PLA.
- Characterization using 1H-NMR and Size Exclusion Chromatography (SEC) to determine derivatization and molecular weight.
- Formation of polymeric micelles via dialysis and characterization of size, zeta potential, CAC, and surface composition (XPS).
- In vitro cytotoxicity assays on multiple cell lines and hemolysis tests.
- Cellular penetration and phagocytosis escape studies using Neuro2a and J774 A1 cell lines.
Main Results:
- Successfully synthesized PHEA-EDA-PS(80)-PLA and PHEA-EDA-PLA copolymers with confirmed derivatization degrees.
- Polymeric micelles formed exhibited controlled size, surface properties, and critical aggregation concentrations.
- XPS analysis confirmed the presence of PS(80) on the surface of PHEA-EDA-PS(80)-PLA micelles.
- In vitro studies showed no cytotoxic or hemolytic effects.
- Micelles demonstrated efficient cellular uptake in Neuro2a cells and evasion of phagocytosis by J774 A1 macrophages, particularly PS(80) decorated micelles.
Conclusions:
- Novel amphiphilic graft copolymers and their derived polymeric micelles possess excellent biocompatibility.
- The developed micellar systems are capable of cellular internalization and exhibit potential for evading immune responses.
- These findings highlight the potential of PHEA-PLA based copolymers for advanced biomedical and drug delivery applications.
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