Camptothecin prodrug block copolymer micelles with high drug loading and target specificity

2014 ◽  
Vol 5 (18) ◽  
pp. 5320-5329 ◽  
Author(s):  
Adnan R. Khan ◽  
Johannes Pall Magnusson ◽  
Sue Watson ◽  
Anna M. Grabowska ◽  
Robert W. Wilkinson ◽  
...  
Keyword(s):  
Block Copolymer ◽  
Luteinizing Hormone ◽  
Tumour Cell ◽  
Drug Loading ◽  
Luteinizing Hormone Releasing Hormone ◽  
High Drug ◽  
Block Copolymer Micelles ◽  
Tumour Cell Lines ◽  
Copolymer Micelles ◽  
High Drug Loading

The effects of a novel functional reducible camptothecin (CPT) block copolymer conjugate, targeting luteinizing hormone releasing hormone receptor (LHRHR) were evaluated against differing LHRHR expressing tumour cell lines and immune populations.

Supramolecular micellar drug delivery system based on multi-arm block copolymer for highly effective encapsulation and sustained-release chemotherapy

2019 ◽  
Vol 7 (37) ◽  
pp. 5677-5687 ◽  
Author(s):  
Li Zhang ◽  
Dongjian Shi ◽  
Chunling Shi ◽  
Tatsuo Kaneko ◽  
Mingqing Chen
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
High Drug ◽  
Release Drug ◽  
Drug Loading Efficiency ◽  
High Drug Loading

A novel multi-arm polyphosphoester-based nanomaterial provides high drug loading efficiency and sustained-release drug delivery for effective chemotherapy.

Thermoresponsive block copolymer micelles with tunable pyrrolidone-based polymer cores: structure/property correlations and application as drug carriers

2015 ◽  
Vol 3 (5) ◽  
pp. 814-823 ◽  
Author(s):  
X.-L. Sun ◽  
P.-C. Tsai ◽  
R. Bhat ◽  
E. M. Bonder ◽  
B. Michniak-Kohn ◽  
...  
Keyword(s):  
Block Copolymer ◽  
Drug Release ◽  
Physicochemical Properties ◽  
Drug Loading ◽  
Drug Carriers ◽  
Structure Property ◽  
Loading Efficiency ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles ◽  
Drug Loading Efficiency

Residue structure affects the physicochemical properties, drug loading efficiency, and thermoresponsive drug release profiles of block copolymer micelles with pyrrolidone-based polymer cores.

Novel pH Sensitive Block Copolymer Micelles for Solvent Free Drug Loading

2006 ◽  
Vol 6 (2) ◽  
pp. 179-186 ◽  
Author(s):  
Woo Sun Shim ◽  
Sung Wan Kim ◽  
Eun-Kyung Choi ◽  
Heon-Joo Park ◽  
Jin-Seok Kim ◽  
...  
Keyword(s):  
Block Copolymer ◽  
Drug Loading ◽  
Ph Sensitive ◽  
Free Drug ◽  
Solvent Free ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles

scholarly journals Preparation and In Vivo Evaluation of Dichloro(1,2-Diaminocyclohexane)platinum(II)-Loaded Core Cross-Linked Polymer Micelles

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Hardeep S. Oberoi ◽  
Natalia V. Nukolova ◽  
Yi Zhao ◽  
Samuel M. Cohen ◽  
Alexander V. Kabanov ◽  
...  
Keyword(s):  
Drug Loading ◽  
Xenograft Model ◽  
Tumor Xenograft ◽  
Ovarian Cancer Cells ◽  
In Vivo Evaluation ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles ◽  
High Drug Loading

The therapeutic performance of oxaliplatin can be improved by incorporating the central cis-dichloro(1,2-diaminocyclohexane)platinum(II) (DACHPt) motif into the core cross-linked block copolymer micelles. We describe here the preparation, cellular uptake, and in vivo evaluation of core cross-linked micelles loaded with DACHPt. Stable drug-loaded micelles were prepared at high drug loading (~25 w/w%) and displayed a considerably increased in vitro cytotoxicity compared to free oxaliplatin against A2780 ovarian cancer cells. The DACHPt-loaded micelle formulation was well tolerated in mice and exhibited improved antitumor activity than oxaliplatin alone in an ovarian tumor xenograft model.

Investigating the influence of aromatic moieties on the formulation of hydrophobic natural products and drugs in poly(2-oxazoline) based amphiphiles

2018 ◽  
Author(s):  
Robert Luxenhofer ◽  
Michael M Lübtow ◽  
Lukas Hahn ◽  
Thomas Lorson ◽  
Rainer Schobert
Keyword(s):  
Natural Products ◽  
Small Molecules ◽  
Water Solubility ◽  
Drug Loading ◽  
High Drug ◽  
Long Term Stability ◽  
Aromatic Content ◽  
Important Interaction ◽  
Amorphous Structures ◽  
High Drug Loading

Many natural compounds with interesting biomedical properties share one physicochemical property, namely a low water solubility. Polymer micelles are, among others, a popular means to solubilize hydrophobic compounds. The specific molecular interactions between the polymers and the hydrophobic drugs are diverse and recently it has been discussed that macromolecular engineering can be used to optimize drug loaded micelles. Specifically, π-π stacking between small molecules and polymers has been discussed as an important interaction that can be employed to increase drug loading and formulation stability. Here, we test this hypothesis using four different polymer amphiphiles with varying aromatic content and various natural products that also contain different relative amounts of aromatic moieties. While in the case of paclitaxel, having the lowest relative content of aromatic moieties, the drug loading decreases with increasing relative aromatic amount in the polymer, the drug loading of curcumin, having a much higher relative aromatic content, is increased. Interestingly, the loading using schizandrin A, a dibenzo[a,c]cyclooctadiene lignan with intermediate relative aromatic content is not influenced significantly by the aromatic content of the polymers employed. The very high drug loading, long term stability, the ability to form stable highly loaded binary coformulations in different drug combinations, small sized formulations and amorphous structures in all cases, corroborate earlier reports that poly(2-oxazoline) based micelles exhibit an extraordinarily high drug loading and are promising candidates for further biomedical applications. The presented results underline that the interaction between the polymers and the incorporated small molecules are complex and must be investigated in every specific case.<br>

β-lactam Functionalized Poly(isoprene-b-ethylene oxide) Amphiphilic Block Copolymer Micelles as a New Nanocarrier System for Curcumin

2010 ◽  
Vol 6 (3) ◽  
pp. 277-284 ◽  
Author(s):  
Konstantinos Gardikis ◽  
Konstantinos Dimas ◽  
Aristidis Georgopoulos ◽  
Eleni Kaditi ◽  
Stergios Pispas ◽  
...  
Keyword(s):  
Block Copolymer ◽  
Ethylene Oxide ◽  
Amphiphilic Block Copolymer ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles

Donnan Equilibria in Polymeric Micellar Systems with Weak Polyelectrolyte Shells: The Lowering of the pH Value

1997 ◽  
Vol 62 (11) ◽  
pp. 1730-1736 ◽  
Author(s):  
Petr Munk ◽  
Zdeněk Tuzar ◽  
Karel Procházka
Keyword(s):  
Ionic Strength ◽  
Block Copolymer ◽  
Ph Value ◽  
Electrolyte Solutions ◽  
Hydrogen Ions ◽  
Micellar Systems ◽  
Weak Electrolytes ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles ◽  
Polyelectrolyte Solutions

When two electrolyte solutions are separated and only some of the ions can cross the boundary, the concentrations of these ions are different on both sides of the boundary. This is the well-known Donnan effect. When weak electrolytes are involved, the imbalance includes also hydrogen ions: there is a difference of pH across the boundary and the dissociation of nondiffusible weak electrolytes is suppressed. The effect is very pronounced when the concentration of the weak electrolyte is high and ionic strength is low. The significance of this phenomenon is discussed for polyelectrolyte solutions, and particularly for block copolymer micelles with weak polyelectrolyte shells. The effect is quite dramatic in the latter case.

A Monte Carlo Study of Flexible Polymer Chain Conformations in Restricted Volumes. I. A Model for Insoluble Blocks Conformations in Swollen Cores of Multimolecular Spherical Block Copolymer Micelles

1993 ◽  
Vol 58 (10) ◽  
pp. 2290-2304 ◽  
Author(s):  
Zuzana Limpouchová ◽  
Karel Procházka
Keyword(s):  
Monte Carlo ◽  
Block Copolymer ◽  
Monte Carlo Study ◽  
Volume Effect ◽  
Micellar Systems ◽  
Flexible Polymer ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles ◽  
Chain Conformations ◽  
Chain Lengths

Monte Carlo simulations of chain conformations in a restricted spherical volume at relatively high densities of segments were performed for various numbers of chains, N, and chain lengths (number of segments), L, on a tetrahedral lattice. All chains are randomly end-tethered to the surface of the sphere. A relatively uniform surface density of the tethered ends is guaranteed in our simulations. A simultaneous self-avoiding walk of all chains creates starting conformations for a subsequent equilibration. A modified algorithm similar to that of Siepmann and Frenkel is used for the equilibration of the chain conformations. In this paper, only a geometrical excluded volume effect of segments is considered. Various structural and conformational characteristics, e.g. segment densities gS(r), free end densities gF(r) as functions of the position in the sphere (a distance from the center), distributions of the tethered-to-free end distances, ρTF(rTF), etc. are calculated and their physical meaning is discussed. The model is suitable for studies of chain conformations is swollen cores of multimolecular block copolymer micelles and for interpretation of non-radiative excitation energy migration in polymeric micellar systems.

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