Abstract
Two series of amphiphilic block copolymers with a hybrid linear-dendritic structure are presented. The compounds consisted of a hydrophilic poly (ethylene glycol) (PEG) block and a 2,2′-bis(hydroxymethyl)propionic acid (bis-MPA) dendron functionalized with stearic acid chains that impart a hydrophobic nature to the block. Different self-assembled nanostructures with a hydrophobic interior and a hydrophilic external part were obtained depending on the length of the PEG chain (Mn = 2000 and Mn = 5000) and the generation of the bis-MPA dendron. The materials were characterized by transmission electron microscopy (TEM). The shapes of the aggregates ranged from spherical or cylindrical micelles to flexible bilayers. The hydrophobic core enabled these nanostructures to encapsulate the water-insoluble drug plitidepsin. The efficacy of these new plitidepsin-containing carriers was evaluated in four cancer cell-lines and they showed similar anticancer activity to the current standard drug formulation.
Highlights
Polymer-based carriers for anticancer drugs bring significant benefits to cancer therapy and these include responsiveness to external stimuli, increased drug efficacy, localized drug delivery, and decreased side effects [1,2,3]
The aggregates proved to be useful as host systems to encapsulate a hydrophobic drug, namely plitidepsin, and the best amphiphilic compound in this respect was poly(ethylene glycol). PSN1 cells (PEG) 5000-G3(C17)8
The results demonstrated the importance of the size of the lipophilic fraction and the influence of the balance between the lipophilic and the hydrophilic content in order to stabilize in water the highest quantity of the drug
Summary
Polymer-based carriers for anticancer drugs bring significant benefits to cancer therapy and these include responsiveness to external stimuli, increased drug efficacy, localized drug delivery, and decreased side effects [1,2,3]. Among the different polymeric architectures, hybrid linear-dendritic block copolymers are perfectly suited for several applications in the biomedical field, including the encapsulation of guest molecules, the delivery of genetic material, and the ability to mimic the cell membrane [4,5,6,7,8]. Hybrid linear-dendritic block copolymers (HLDBCs) are macromolecules composed of a linear polymeric chain linked at one end with a dendrimeric wedge. These materials contain segments of different molecular architectures and combine the characteristics of the rigid, globular, multi-branched dendritic wedge with the high mobility of the linear polymeric chain [9,10].
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