Polymeric worm micelles as nano-carriers for drug delivery.
TL;DR: W worm micelles as blends of degradable polylactic acid and inert block copolymer amphiphiles were prepared for controlled release and initial study of carrier transport through nano-porous media, suggesting a new class of hydrophobic drug nano-carriers that are capable of tissue permeation as well as controlled release.
Abstract: Nanoscale carriers of active compounds, especially drugs, need not be spherical in shape. Worm micelles as blends of degradable polylactic acid (PLA) and inert block copolymer amphiphiles were prepared for controlled release and initial study of carrier transport through nano-porous media. The loading capacity of a typical hydrophobic drug, Triamterene, and the release of hydrophobic dyes were evaluated together with morphological changes of the micelles. Degradation of PLA by hydrolysis led to the self-shortening of worms and a clear transition towards spherical micelles, correlating with the release of hydrophobic dyes. Perhaps equally important for application is the flexibility of worm micelles, which we show allows them to penetrate nanoporous gels where 100 nm sized vesicles cannot enter. Such gels have served as tissue models, and so the results here collectively suggest a new class of hydrophobic drug nano-carriers that are capable of tissue permeation as well as controlled release.
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TL;DR: The antimicrobial and wound healing studies quite interestingly reveal that hydrophobic pluronic P123 remains more effective than F127 as carrier for antimicrobial agent, whereas pluronic F127 based liquid crystalline hydrogel stands superior as topical drug delivery matrix than its P123 counterpart because of its better wound healing abilities.
15 citations
TL;DR: The feasibility of both chemical and physical incorporation of block co-polymer micelles within pHEMA hydrogels as a means to achieve sustained release of drugs for potential application in ophthalmic therapies is demonstrated.
Abstract: Poly(2-hydroxyethyl methacrylate) (pHEMA) hydrogels loaded with core cross-linked PEG-b-PCL micelles with different morphologies (spherical and rod-like) were prepared and evaluated for use as drugeluting soft contact lenses. The relationship between the composition of micelle-loaded pHEMA hydrogels and properties such as transparency and swelling were determined. The incorporation of core crosslinked micelles into pHEMA hydrogels led to the formation of different internal nanostructures which were dependent on the amount and morphology of the micelles added. 7-Hydroxy-9H-(1,3-dichloro-9,9′-dimethylacridin-2-one) (DDAO), a hydrophobic fluorescent dye, was loaded into the micelles prior to their incorporation within the hydrogel matrix. The in vitro release of DDAO demonstrated the potential of the micelles/pHEMA hydrogels to provide controlled drug delivery for at least 14 days. This study demonstrates the feasibility of both chemical and physical incorporation of block co-polymer micelles within pHEMA hy...
14 citations
TL;DR: Folate-targeted cyclodextrin/retinoic acid (CD/RA) conjugate was synthesized using carbonyldiimidazole (CDI) and dimethylaminopyridine (DMAP) and the developed macromolecule could self-aggregate to form micelles.
Abstract: Folate-targeted cyclodextrin/retinoic acid (CD/RA) conjugate was synthesized using carbonyldiimidazole (CDI) and dimethylaminopyridine (DMAP). The structure of the produced macromolecule was studied by FTIR and 1HNMR. The developed macromolecule could self-aggregate to form micelles. Critical micelle concentration (CMC) of the macromolecule was determined by pyrene as a fluorescent probe. Doxorubicin (DOX)-loaded micelles were prepared by direct dissolution method. To optimize the effect of cyclodextrin type (α or β), the molar ratio of RA to CD and the drug content, a full factorial design was used and their effects on particle size, polydispersity index, zeta potential, loading efficiency (LE%), and release efficiency (RE24%) in 24 h were studied. Orientation of folate ligand on the surface of the micelles was studied by X-ray photoelectron spectroscopy (XPS) technique. The cytotoxicity of DOX-loaded micelles was studied on KG-1 cells which overexpressed folate receptor (FR) and FR-negative HepG2 cells using MTT assay. FTIR and 1HNMR spectra confirmed successful production of the micelles and XPS spectra showed surface orientation of folate. The best results obtained from β-cyclodextrin with molar ratio of 4 to RA and 15 % drug content. The optimized micelles showed the particle size of 103 ± 4 nm, zeta potential of −36 mV, polydispersity index of 0.28 ± 0.05, LE% of 100 %, and RE24% of 69.88 ± 1.6 %. The IC50 of targeted micelles was half of non-targeted micelles and free DOX.
14 citations
TL;DR: This work tends to provide a comprehensive description of the connection between structure-changing thermodynamics, kinetics, and influencing factors, thus to enlighten more pathways for future developments in the field of drug delivery.
Abstract: Amphiphilic block copolymers are able to self-assemble into rich morphologies with high controllability for drug delivery. Great efforts have been made for decades to construct efficient drug deliv...
14 citations
01 Jan 2017
TL;DR: This chapter provides an overview of the Quantitative Structure-Activity Relationships (QSAR) studies performed so far towards predicting nanoparticles’ environmental toxicity, and focuses on the setup of a QSAR perturbation-based model for the assessment of ecotoxic effects of nanoparticles in diverse conditions.
Abstract: Nanotechnology is a newly emerging field, posing substantial impacts on society, economy, and the environment. In recent years, the development of nanotechnology has led to the design and large-scale production of many new materials and devices with a vast range of applications. However, along with the benefits, the use of nanomaterials raises many questions and generates concerns due to the possible health-risks and environmental impacts. This chapter provides an overview of the Quantitative Structure-Activity Relationships (QSAR) studies performed so far towards predicting nanoparticles’ environmental toxicity. Recent progresses on the application of these modeling studies are additionally pointed out. Special emphasis is given to the setup of a QSAR perturbation-based model for the assessment of ecotoxic effects of nanoparticles in diverse conditions. Finally, ongoing challenges that may lead to new and exciting directions for QSAR modeling are discussed.
13 citations
Cites background from "Polymeric worm micelles as nano-car..."
...Many of these modalities include polymeric NPs (Stupp et al., 2005), micelles (Kim et al., 2005), liposomes and dendrimers (Popat et al., 2007; Portney & Ozkan, 2006), hydrogels (Vinogradov et al., 2002), nanoshells (Zahr et al., 2005), and smart surfaces....
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References
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TL;DR: The utility of polymeric micelles formed through the multimolecular assembly of block copolymers as novel core-shell typed colloidal carriers for drug and gene targeting and their feasibility as non-viral gene vectors is highlighted.
3,457 citations
TL;DR: This review examines the chemical nature of polymeric micelles as well as the methods used to characterize them with regard to drug delivery and potential medical applications, especially in cancer chemotherapy, are described and discussed.
1,200 citations
TL;DR: Experiments with poly(1,2-butadiene-b-ethylene oxide) diblock copolymers are described, which form Y-junctions and three-dimensional networks in water at weight fractions of PEO intermediate to those associated with vesicle and wormlike micelle morphologies.
Abstract: Amphiphilic compounds such as lipids and surfactants are fundamental building blocks of soft matter. We describe experiments with poly(1,2-butadiene-b-ethylene oxide) (PB-PEO) diblock copolymers, which form Y-junctions and three-dimensional networks in water at weight fractions of PEOintermediate to those associated with vesicle and wormlike micelle morphologies. Fragmentation of the network produces a nonergodic array of complex reticulated particles that have been imaged by cryogenic transmission electron microscopy. Data obtained with two sets of PB-PEOcompounds indicate that this type of self-assembly appears above a critical molecular weight. These block copolymers represent versatile amphiphiles, mimicking certain low molecular weight three-component (surfactant/water/oil) microemulsions, without addition of a separate hydrophobe.
1,126 citations
TL;DR: With all compositions, in both 100 nm and giant vesicles, the average release time reflects a highly quantized process in which any given vesicle is either intact and retains its encapsulant, or is porated and slowly disintegrates.
638 citations
TL;DR: A low molecular weight poly(ethyleneoxide)-poly(butadiene) (PEO-PB) diblock copolymer containing 50 weight percent PEO forms gigantic wormlike micelles at low concentrations (<5 percent by weight) in water.
Abstract: A low molecular weight poly(ethyleneoxide)-poly(butadiene) (PEO-PB) diblock copolymer containing 50 weight percent PEO forms gigantic wormlike micelles at low concentrations (<5 percent by weight) in water. Subsequent generation of free radicals with a conventional water-based redox reaction leads to chemical cross-linking of the PB cores without disruption of the cylindrical morphology, as evidenced by cryotransmission electron microscopy and small-angle neutron scattering experiments. These wormlike rubber micelles exhibit unusual viscoelastic properties in water.
626 citations