Polymer nano-particles have been widely investigated in the last decade due to a variety of potential applications. In particular, polymers which can self assemble into micellar nano-particles can be effectively used as vehicles for drug delivery. Considerable efforts are underway to develop better drug delivery nano carriers for high drug loading capacity for a wide variety of bioactive compounds. In this study, several new polymers were synthesized in bulk (solventless condition) by a chemo-enzymatic methodology using Candidaantarctica lipase B (Novozyme 435) and molecular sieves (MS). The synthesized polymers demonstrated high drug loading capacity and the potential to encapsulate drugs which are poorly soluble in aqueous solvents. 相似文献
In two ABA type amphiphilic block copolymers (P1, P2), the hydrophobic B block consists of a bioreducible segmented poly(disulfide) (PDS), while poly‐N‐isopropylacrylamide (PNIPAM) or poly(triethyleneglycol)methylether‐methacrylate (PTEGMA) serve as the hydrophilic A blocks in P1 and P2, respectively, leading to the formation of polymersome and micelle, owing to the difference in the packing parameters. Both exhibit comparable doxorubicin (Dox) encapsulation efficiency, but glutathione (GSH) triggered release appears much faster from the polymersome than micelle owing to the complete degradation of the PDS segment in polymersome morphology unlike in micelle. Dox‐loaded polymers (P1‐Dox and P2‐Dox) exhibit minimum toxicity to normal cells like C2C12. By contrast, P1‐Dox shows excellent killing efficiency to the HeLa cells (cancer cell) (in which the GSH concentration is significantly higher). However, P2‐Dox reveals a rather poor activity even to HeLa cells. Fluorescence microscopy studies show comparable cellular uptake of P1‐Dox and P2‐Dox. But the polymersome entrapped dye escapes fast from the cargo and reach the nucleus, while the drug‐loaded micelle remains trapped in the perinuclear zone explaining the significant difference in the drug delivery performance of polymersome and micelle. 相似文献
Amphiphilic polymers can self assemble into micellar nano-particles and can be effectively used as nano carriers for drug delivery. A number of macromolecular delivery systems are under investigation to improve the efficacy of prospective drugs. In this study, seven new co-polymers were synthesized under mild reaction conditions in bulk (without solvent) by chemoenzymatic approach using Candidaantarctica lipase (Novozyme 435) and molecular sieves, subsequently these polymers were treated with different long chain bromoalkanes and acid chlorides for attachment of the lipophilic moieties to the backbone polymer via an ether or an ester linkage, respectively in order to make them amphiphilic. These synthesized nano-particles demonstrated high drug loading capacity and have the potential to encapsulate hydrophobic drugs. 相似文献
A novel type of biodegradable/biocompatible amphiphilic hyperbranched copolymer (H40‐PLA‐b‐MPEG) was synthesized. Its micellar properties were studied by DLS, fluorescence spectroscopy and TEM. The drug release profile showed that the H40‐PLA‐b‐MPEG micelles provide an initial burst release, followed by a sustained release of the entrapped hydrophobic model drug over a period of 4 to 58 h. The copolymer degraded hydrolytically within 6 weeks under physiological conditions. The MTT assay showed no obvious cytotoxicity against a human endothelial cell line at a concentration range of 0–400 µg · mL−1. These results indicate that the H40‐PLA‐b‐MPEG micelles have great potential as hydrophobic drug delivery carriers.
Graphene oxide (GO)-grafted nanosupramolecules have recently emerged as neoteric nano drug carriers in the therapy of refractory diseases. Herein, a multicomponent nanosupramolecular drug carrier based on a targeted peptide and magnetic GO is reported, the drug-release behavior of which can be regulated by an alternating magnetic field (AMF). This multicomponent nanosupramolecular carrier is composed of β-cyclodextrin (β-CD)/nickel nanoparticle-modified graphene oxide (GONiCD) and mitochondrial ion-targeting peptide (MitP)-grafted hyaluronic acid (HAMitP). Owing to the host–guest interaction between β-cyclodextrin and the cyclohexyl groups on MitP, GONiCD and HAMitP could form supramolecular assemblies during the doxorubicin (Dox) loading process, which not only remarkably enhances the drug-loading capacity, but also improves the drug-release efficiency under AMF stimulus. During co-incubation with tumor cells, the Dox-loaded assemblies could strongly target the tumor mitochondria and damage both the mitochondria and the nuclei, owing to Dox release from the assemblies induced by AMF. This study sheds light on the exploration of peptide caps for controlled drug loading/release of supramolecular nanocarriers for efficient drug delivery and anticancer therapy. 相似文献