Enzyme/pH-triggered anticancer drug delivery of chondroitin sulfate modified doxorubicin nanocrystal.

In this paper, we developed a novel strategy of preparing doxorubicin (DOX) nanocrystal (NC) exerting spherical particles with a diameter of 102 nm, which experienced following coating of chondroitin sulphate derivative (CSOA) shell electrostatic and hydrophobic interactions. Such multifunctional outerwear resulted in drug nanocapsules with high drug loading content up to 70% and high colloidal stability under physiological conditions. It exhibited accelerated drug release behaviour when dispersing in hyaluronidase (HAase) containing medium or incubated with cancer cells.

The effect of π-Conjugation on the self-assembly of micelles and controlled cargo release.

Here we presented a novel micelle self-assembled from amphiphiles with π-conjugated moieties (OEG-DPH). The π-conjugated structural integrity of the micelles enabled stable encapsulation of Nile Red (NR, model drug). The self-assembly behaviour of the amphiphiles and the release profile of NR loaded micelles were investigated.

Oral delivery of camptothecin using cyclodextrin/poly(anhydride) nanoparticles.

Camptothecin (CPT), a molecule that shows powerful anticancer activity, is still not used in clinic due to its high hydrophobicity and poor active form's stability. In order to solve these drawbacks, the combination between poly(anhydride) nanoparticles and cyclodextrins was evaluated. CPT-loaded nanoparticles, prepared in the presence of 2-hydroxypropyl-β-cyclodextrin, (HPCD-NP) displayed a mean size close to 170nm and a payload of 50μg per mg (25 times higher than the one of the control nanoparticles).

Capsid-like supramolecular dendritic systems as pH-responsive nanocarriers for drug penetration and site-specific delivery.

Unlabelled: Supramolecular dendritic systems emerge as a promising new-generation bioinspired nanoplatform for nanomedicine. Herein, we report capsid-like mimics self-assembled from peptide dendrimers and functionalized peptides to enhance drug penetration and site-specific delivery for tumor therapy. These drug-loaded supramolecular dendritic systems are endowed with capsid-like component and nanostructure by a facile supramolecular approach.

Polymeric micelles with π-π conjugated moiety on glycerol dendrimer as lipophilic segments for anticancer drug delivery.

Polymeric micelles are important nanovehicles for anticancer drug delivery. The lipophilic segment in polymeric micelles is an important factor to affect the drug loading properties. In our previous work, we found that small molecules with π-π conjugated structures could be used to replace hydrophobic polymeric chains as lipophilic segments for anticancer drug delivery.

Nanoparticles generated by PEG-Chrysin conjugates for efficient anticancer drug delivery.

Nanoparticle-based drug delivery systems promise the safety and efficacy of anticancer drugs. Herein, we presented a facile approach to fabricate novel nanoparticles generated by PEG-Chrysin conjugates for the delivery of anticancer drug doxorubicin. Chrysin was immobilized on the terminal group of methoxy poly(ethylene glycol) (mPEG) to form mPEG-Chrysin conjugate.

Polymeric micelles with small lipophilic moieties for drug delivery.

The aim of this study was to develop a new polymeric micelle delivery system for antitumor drugs. An amphiphile of methoxypoly(ethylene glycol)-histidine-di(cinnamic acid) (PEGHC) with a small lipophilic moiety instead of a hydrophobic biodegradable polymer chain was synthesized and characterized. The PEGHC self-assembled into micelles.

Novel pH-sensitive micelles generated by star-shape copolymers containing zwitterionic sulfobetaine for efficient cellular internalization.

pH-sensitive micelles are considered promising carriers for tumor targeted drug delivery. In this study, novel pH-sensitive star-shape copolymers of amphiphilic poly(epsilon-caprolactone)-b-poly(N, N-diethylaminoethyl methacrylate)-r-poly(N-(3-sulfopropyl)-N-methacryloxyethy-N, N-diethylammoniumbetaine) (4sPCLDEAS) are designed and synthesized with the combination of ring opening polymerization (ROP) and atom radical transferpolymerization (ATRP). The structure of the copolymers is characterized by proton nuclear magnetic resonance spectra (1HNMR).

Polymeric micelles with π-π conjugated cinnamic acid as lipophilic moieties for doxorubicin delivery.

In this paper, π-π conjugated cinnamic acid (CIN) was used as a lipophilic moiety to fabricate polymeric micelles. The amphiphiles with one or two cinnamic acid molecules as lipophilic architectures (mPEG-CIN and mPEG-Lys-DCIN) were synthesized. We expressly investigated the effect of the lipophilic parts on size, morphology and stability of the self-assembly micelles.

Novel nanoparticles generated by polymeric amphiphiles with pi-pi conjugated small molecules for anti-tumor drug delivery.

In recent years, the self-assembly polymeric nanoparticles are widely used for anti-tumor drug delivery. Multiple interactions such as hydrogen bonding, host-guest interaction, hydrophobic interaction and electrostatic interaction have been utilized to generate the nanoparticles. Herein, a new polymeric amphiphile with methoxy poly(ethylene glycol) (mPEG) as hydrophilic block and pi-pi conjugated small molecule N-(9-Fluorenylmethoxycarbonyl)-L-phenylalanines (Fmoc-Phe-OH) instead of hydrophobic polymer chain as lipophilic segment was synthesized.

Ultrasound accelerated gelation of novel L-lysine based hydrogelators.

We reported a novel hydrogelator with L-lysine as a linker to connect 7-carboxyl methoxycoumarin and hydrazine as lipophilic and water-soluble moieties. Ultrasound accelerated the gelation and induced homogenous self-assembly of fibrils into entangled 3D networks. The hydrogel exhibits great potential for future biomedical applications.

Anticancer drug delivery of PEG based micelles with small lipophilic moieties.

Herein, we reported a new type of self-assembly micelles based on amphiphilic polymers of cinnamate and coumarin derivatives modified PEG for drug delivery applications. Lipophilic cinnamic acid (CIN) and 7-carboxyl methoxycoumarin (COU) were immobilized on the terminal groups of poly(ethylene glycol) (PEG) to prepare amphiphiles. The amphiphiles self-assembled into micelles.

Supramolecular nanoparticles generated by the self-assembly of polyrotaxanes for antitumor drug delivery.

A new approach of fabricating supramolecular nanoparticles generated by self-assembly polyrotaxanes for antitumor drug delivery has been reported. Cinnamic-acid-modified poly(ethylene glycol) chains were threaded in α-cyclodextrins to form polyrotaxanes. The polyrotaxanes self-assembled supramolecular nanoparticles.

Cationic lipid-coated PEI/DNA polyplexes with improved efficiency and reduced cytotoxicity for gene delivery into mesenchymal stem cells.

Background: Effective gene transfection without serum deprivation is a prerequisite for successful stem cell-based gene therapy. Polyethylenimine (PEI) is an efficient nonviral gene vector, but its application has been hindered by serum sensitivity and severe cytotoxicity.

Methods: To solve this problem, a new family of lipopolyplexes was developed by coating PEI/DNA polyplexes with three serum-resistant cationic lipids, namely, lysinylated, histidylated, and arginylated cholesterol.

Effects of pH-sensitive chain length on release of doxorubicin from mPEG-b-PH-b-PLLA nanoparticles.

Background: Two methoxyl poly(ethylene glycol)-poly(L-histidine)-poly(L-lactide) (mPEG-PH-PLLA) triblock copolymers with different poly(L-histidine) chain lengths were synthesized. The morphology and biocompatibility of these self-assembled nanoparticles was investigated.

Methods: Doxorubicin, an antitumor drug, was trapped in the nanoparticles to explore their drug-release behavior.

Stabilization of pH-sensitive mPEG-PH-PLA nanoparticles by stereocomplexation between enantiomeric polylactides.

Methoxy poly(ethylene glycol)-poly(L-histidine)-poly(lactide) (mPEG(45)-PH(30)-PLA(82)) triblock copolymers self-assemble into nanoparticles by sterocomplexation. The properties of the stereocomplex nanoparticles including morphology, stability, and biocompatibility are investigated. The results reveal that the stereocomplexation between PLLA and PDLA segments could prevent the aggregation of the nanoparticles when the pH value is around 6.

A novel micelle of coumarin derivative monoend-functionalized PEG for anti-tumor drug delivery: in vitro and in vivo study.

In this paper, a novel micelle for anti-tumor drug delivery was reported. Two 7-carboxymethoxy coumarin molecules were immobilized on the terminal group of a methoxy poly(ethylene glycol) chain via l-lysine as linker. The amphiphilic 7-carboxymethoxy coumarin monoend-functionalized methoxy poly(ethylene glycol) (mPEG-Lys-DCOU) chains were self-assembled micelles.

Supramolecular self-assembly of monoend-functionalized methoxy poly(ethylene glycol) and α-cyclodextrin: from micelles to hydrogel.

An effective strategy was developed to fabricate a supramolecular hydrogel with the complexation of α-cyclodextrins (α-CDs) and monoend-functionalized low molecular weight methoxy poly(ethylene glycol) (mPEG, Mn=2000) micelles. Hydrophobic cinnamic acid was immobilized on methoxy poly(ethylene glycol) via L-lysine as linker to prepare amphiphilic mPEG. The monoend-functionalized mPEG self-assembled micelles in aqueous solution.

Anti-tumor drug delivery of pH-sensitive poly(ethylene glycol)-poly(L-histidine-)-poly(L-lactide) nanoparticles.

pH-sensitive poly(ethylene glycol)-poly(L-histidine)-poly(L-lactide) (PEG-PH-PLLA) nanoparticles were prepared and used as carriers for anti-tumor drug delivery. The morphology and properties of the nanoparticles such as pH sensitivity, zeta potential and mean diameters were investigated. The cytotoxicity of PEG-PH-PLLA nanoparticles was evaluated.

A novel poly(l-glutamic acid) dendrimer based drug delivery system with both pH-sensitive and targeting functions.

The functionalization of pH-sensitiveness and cellular targeting is a promising strategy to fabricate drug delivery systems with high efficiency, high selectivity and low toxicity. In this paper, a poly(l-glutamic acid) dendrimer based drug delivery system with both pH-sensitive and targeting functions is reported. Poly(l-glutamic acid) dendrimers with a polyhedral oligomeric silsesquioxane (POSS) nanocubic core were synthesized.