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https://www.readbyqxmd.com/read/28110039/heat-induced-solubilization-of-curcumin-in-kinetically-stable-pluronic-p123-micelles-and-vesicles-an-exploit-of-slow-dynamics-of-the-micellar-restructuring-processes-in-the-aqueous-pluronic-system
#1
R Ganguly, A Kunwar, B Dutta, S Kumar, K C Barick, A Ballal, V K Aswal, P A Hassan
Wide therapeutic potential combined with low cost and negligible toxicity makes curcumin one of the most sought after drugs in recent times. Its poor aqueous solubility and low bioavailability are often overcome by using micelles and vesicles as its carriers. The substances that are commonly used for this purpose are a class of nonionic surfactants called pluronics. Solubilization of curcumin in aqueous systems of these surfactants is carried out by thin film hydration method presumably because slow dynamics of micellar restructuring processes in them creates hindrance for direct solubilization...
January 17, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28097871/redox-responsive-self-assembly-micelles-from-poly-n-acryloylmorpholine-block-2-acryloyloxyethyl-ferrocene-carboxylate-amphiphilic-block-copolymers-as-drug-release-carriers
#2
Feng Xu, He Li, Yan-Ling Luo, Wei Tang
Novel well-defined redox-responsive ferrocene-containing amphiphilic block copolymers (PACMO-b-PAEFC) were synthesized by ATRP, with poly(N-acryloylmorpholine) (PACMO) as hydrophilic blocks and poly(2-acryloyloxyethyl ferrocenecarboxylate) (PAEFC) as hydrophobic blocks. The copolymers were characterized by FTIR, 1H NMR, and gel permeation chromatography, and the crystalline behavior was determined by X-ray diffraction and small-angle X-ray scattering. The results showed that the size of the lamellar crystals and crystallinity vary with the systematic compositions while the periodic structure of the lamellar stacks has no obvious change...
January 18, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28094989/-bitter-sweet-polymeric-micelles-formed-by-block-copolymers-from-glucosamine-and-cholic-acid
#3
Kun Zhang, Yongguang Jia, I-Huang Tsai, Satu Strandman, Li Ren, Liangzhi Hong, Guangzhao Zhang, Ying Guan, Yongjun Zhang, Julian X X Zhu
Natural compounds glucosamine and cholic acid have been used to make acrylic monomers which are subsequently used to prepare amphiphilic block copolymers by reversible addition-fragmentation chain transfer (RAFT) polymerization. Despite the striking difference in polarity and solubility, three diblock copolymers consisting of glucosamine and cholic acid pendants with different hydrophilic and hydrophobic chain lengths have been synthesized without the use of protecting groups. They are shown to self-assemble into polymeric micelles with a "bitter" bile acid core and "sweet" sugar shell in aqueous solutions as evidenced by dynamic light scattering and transmission electron microscopy...
January 17, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28094978/phase-behavior-and-self-assembly-of-perfectly-sequence-defined-and-monodisperse-multi-block-copolypeptides
#4
Sarah R MacEwan, Isaac Weitzhandler, Ingo Hoffmann, Jan Genzer, Michael Gradzielski, Ashutosh Chilkoti
This paper investigates how the properties of multi-block copolypeptides can be tuned by their block architecture, defined by the size and distribution of blocks along the polymer chain. These parameters were explored by the precise - genetically encoded - synthesis of recombinant elastin-like polypeptides (ELPs). A family of ELPs was synthesized in which the composition and length were conserved while the block length and distribution were varied, thus creating eleven ELPs with unique block architectures. To our knowledge, these polymers are unprecedented in their intricately and precisely varied architectures...
January 17, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28089916/stable-curcumin-loaded-polymeric-micellar-formulation-for-enhancing-cellular-uptake-and-cytotoxicity-to-flt3-overexpressing-eol-1-leukemic-cells
#5
Singkome Tima, Songyot Anuchapreeda, Chadarat Ampasavate, Cory Berkland, Siriporn Okonogi
The present study aims to develop a stable polymeric micellar formulation of curcumin (CM) with improved solubility and stability, and that is suitable for clinical applications in leukemia patients. CM-loaded polymeric micelles (CM-micelles) were prepared using poloxamers. The chemical structure of the polymers influenced micellar properties. The best formulation of CM-micelles, namely CM-P407, was obtained from poloxamer 407 at drug to polymer ratio of 1:30 and rehydrated with phosphate buffer solution pH 7...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088632/nanosized-complexation-assemblies-housed-inside-reverse-micelles-churn-out-monocytic-delivery-cores-for-bendamustine-hydrochloride
#6
Yuvraj Singh, Anumandla Chandrashekhar, Jaya Gopal Meher, K K Durga Rao Viswanadham, Vivek K Pawar, Kavit Raval, Komal Sharma, Pankaj K Singh, Animesh Kumar, Manish K Chourasia
OBJECTIVE: We explore a plausible method of targeting bendamustine hydrochloride (BM) to circulatory monocytes by exploiting their intrinsic endocytic/phagocytic capability. METHODS: We do so by complexation of sodium alginate and chitosan inside dioctyl sulfo succinate sodium (AOT) reverse micelles to form bendamustine hydrochloride loaded nanoparticles (CANPs). Dynamic light scattering, electrophoretic mobility and UV spectroscopy were used to detail intra-micellar complexation dynamics and to prove that drug was co-captured during interaction of carbohydrate polymers...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087380/polymeric-mixed-micelles-as-nanomedicines-achievements-and-perspectives
#7
REVIEW
Maximiliano Cagel, Fiorella C Tesan, Ezequiel Bernabeu, Maria J Salgueiro, Marcela B Zubillaga, Marcela A Moretton, Diego A Chiappetta
During the past few decades, polymeric micelles have raised special attention as novel nano-sized drug delivery systems for optimizing the treatment and diagnosis of numerous diseases. These nanocarriers exhibit several in vitro and in vivo advantages as well as increased stability and solubility to hydrophobic drugs. An interesting approach for optimizing these properties and overcoming some of their disadvantages is the combination of two or more polymers in order to assemble polymeric mixed micelles. This review article gives an overview on the current state of the art of several mixed micellar formulations as nanocarriers for drugs and imaging probes, evaluating their ongoing status (preclinical or clinical stage), with special emphasis on type of copolymers, physicochemical properties, in vivo progress achieved so far and toxicity profiles...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28080053/lipid-drug-conjugate-for-enhancing-drug-delivery
#8
Danielle Irby, Chengan Du, Feng Li
Lipid-drug conjugates (LDCs) are drug molecules that have been covalently modified with lipids. The conjugation of lipids to drug molecules increases lipophilicity and also changes other properties of drugs. The conjugates demonstrate several advantages including improved oral bioavailability, improved targeting to the lymphatic system, enhanced tumor targeting, and reduced toxicity. Based on the chemical nature of drugs and lipids, various conjugation strategies and chemical linkers can be utilized to synthesize LDCs...
January 12, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28079955/solubilization-of-membrane-proteins-into-functional-lipid-bilayer-nanodiscs-using-a-diisobutylene-maleic-acid-copolymer
#9
Abraham Olusegun Oluwole, Bartholomäus Danielczak, Annette Meister, Jonathan Oyebamiji Babalola, Carolyn Vargas, Sandro Keller
Once removed from their natural environment, membrane proteins depend on membrane-mimetic systems to retain their native structures and functions. To this end, lipid-bilayer nanodiscs that are bounded by scaffold proteins or amphiphilic polymers such as styrene/maleic acid (SMA) copolymers have been introduced as alternatives to detergent micelles and liposomes for in vitro membrane-protein research. Herein, we show that an alternating diisobutylene/maleic acid (DIBMA) copolymer shows equal performance to SMA in solubilizing phospholipids, stabilizes an integral membrane enzyme in functional bilayer nanodiscs, and extracts proteins of various sizes directly from cellular membranes...
January 12, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28068593/visible-light-induced-crosslinking-and-physiological-stabilization-of-diselenide-rich-nanoparticles-for-redox-responsive-drug-release-and-combination-chemotherapy
#10
Shaodong Zhai, Xianglong Hu, Yongjun Hu, Baoyan Wu, Da Xing
Undesired physiological instability of nanocarriers and premature drug leakage during blood circulation result in compromised therapeutic efficacy and severe side effects, which have significantly impeded the development of nanomedicine. Facile crosslinking of drug-loaded nanocarriers while keeping the potency of site-specific degradation and drug release has emerged as a viable strategy to overcome these drawbacks. Additionally, combination therapy has already shown advantages in inhibiting advanced tumors and life extension than single drug therapy...
March 2017: Biomaterials
https://www.readbyqxmd.com/read/28068545/design-preparation-and-characterization-of-ph-responsive-prodrug-micelles-with-hydrolyzable-anhydride-linkages-for-controlled-drug-delivery
#11
Girija Seetharaman, Adarsh R Kallar, Vineeth M Vijayan, Jayabalan Muthu, Shivaram Selvam
We report a new prodrug micelle-based approach in which a model hydrophobic non-steroidal anti-inflammatory drug (NSAID), ibuprofen (Ibu), is tethered to amphiphilic methoxy polyethylene glycol-polypropylene fumarate (mPEG-PPF) diblock copolymer via hydrolytic anhydride linkages for potential controlled release applications of NSAIDs. Synthesized mPEG-PPF-Ibu polymer drug conjugates (PDCs) demonstrated high drug conjugation efficiency (∼90%) and self-assembled to form micellar nanostructures in aqueous medium with critical micelle concentrations ranging between 16 and 30μg/mL...
December 31, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28068313/two-dimensional-assemblies-from-crystallizable-homopolymers-with-charged-termini
#12
Xiaoming He, Ming-Siao Hsiao, Charlotte E Boott, Robert L Harniman, Ali Nazemi, Xiaoyu Li, Mitchell A Winnik, Ian Manners
The creation of shaped, uniform and colloidally stable two-dimensional (2D) assemblies by bottom-up methods represents a challenge of widespread current interest for a variety of applications. Herein, we describe the utilization of surface charge to stabilize self-assembled planar structures that are formed from crystallizable polymer precursors by a seeded growth approach. Addition of crystallizable homopolymers with charged end-groups to seeds generated by the sonication of block copolymer micelles with crystalline cores yields uniform platelet micelles with controlled dimensions...
January 9, 2017: Nature Materials
https://www.readbyqxmd.com/read/28064499/poly-glycerol-used-for-constructing-mixed-polymeric-micelles-as-t1-mri-contrast-agent-for-tumor-targeted-imaging
#13
Yi Cao, Min Liu, Kunchi Zhang, Guangyue Zu, Ye Kuang, Xiaoyan Tong, Dangsheng Xiong, Renjun Pei
There was much interest in the development of nanoscale delivery vehicles based on polymeric micelles to realize the diagnostic and therapeutic applications in biomedicine. Here, with the purpose of constructing a micellar magnetic resonance imaging (MRI) contrast agent (CA) with well biocompatibility and targeting specificity, two types of amphiphilic diblock polymers, mPEG-PG(DOTA(Gd))-b-PCL and FA-PEG-b-PCL, were synthesized to form mixed micelles by coassembly. The nanostructure of the resulting micellar system consisted of poly(caprolactone) (PCL) as core and poly(glycerol) (PG) and poly(ethylene glycol) (PEG) as shell, simultaneously modified with DOTA(Gd) chelates and folic acid (FA), which afforded functions of MRI contrast enhancement and tumor targeting...
January 9, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28054329/a-first-in-human-phase-1-study-of-epirubicin-conjugated-polymer-micelles-k-912-nc-6300-in-patients-with-advanced-or-recurrent-solid-tumors
#14
Hirofumi Mukai, Takahiro Kogawa, Nobuaki Matsubara, Yoichi Naito, Masaoki Sasaki, Ako Hosono
Background K-912 also known as NC-6300 is a novel epirubicin pro-drug conjugate developed using micellar nanoparticle technology. We conducted a first-in-human, Phase 1, open-label, non-randomized dose escalation study to evaluate the safety, tolerability, efficacy, and pharmacokinetics of K-912 administered as monotherapy in patients with advanced or recurrent solid tumors. Methods Patients aged 41 to 72 years with histologically or cytologically confirmed advanced or recurrent malignant solid tumors either refractory to standard therapy or had no other viable treatment options were enrolled...
January 4, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28052447/a-multiresponsive-amphiphilic-supramolecular-diblock-copolymer-based-on-pillar-10-arene-paraquat-complexation-for-rate-tunable-controlled-release
#15
Xiaodong Chi, Xiaofan Ji, Li Shao, Feihe Huang
Herein, for rate-tunable controlled release, the authors report a new facile method to prepare multiresponsive amphiphilic supramolecular diblock copolymers via the cooperative complexation between a water-soluble pillar[10]arene and paraquat-containing polymers in water. This supramolecular diblock copolymer can self-assemble into multiresponsive polymeric micelles at room temperature in water. The resultant micelles can be further used in the controlled release of small molecules with tunable release rates depending on the type of single stimulus and the combination of various stimuli...
January 3, 2017: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/28051292/truxene-based-hyperbranched-conjugated-polymers-fluorescent-micelles-detect-explosives-in-water
#16
Wei Huang, Emanuel Smarsly, Jinsong Han, Markus Bender, Kai Seehafer, Irene Wacker, Rasmus R Schroeder, Uwe H F Bunz
We report two hyperbranched conjugated polymers (HCP) with truxene units as core and 1,4-didodecyl-2,5-diethynylbenzene as well as 1,4-bis(dodecyloxy)-2,5-diethynyl¬benzene as co-monomers. Two analogous poly(para-phenylene¬ethynylene)s (PPE) are also prepared as comparison to demonstrate the difference between the truxene and the phenyl moieties in their optical properties and their sensing performance. The four polymers are tested for nitroaromatic analytes and display different fluorescence quenching responses...
January 4, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28048748/su-f-t-159-monte-carlo-simulation-studies-of-three-dimensional-dose-distribution-for-polymer-gel-dosimeter-and-radiochromic-gel-dosimeter-in-a-proton-beam
#17
M Park, G Kim, H Jung, S Park, S Park, Y Ji, J Yun
PURPOSE: The purpose of this simulation study is to evaluate the proton detectability of gel dosimeters, and estimate the three-dimensional dose distribution of protons in the radiochromic gel and polymer gel dosimeter compared with the dose distribution in water. METHODS: The commercial composition ratios of normoxic polymer gel and LCV micelle radiochromic gel were included in this simulation study. The densities of polymer and radiochromic gel were 1.024 and 1...
June 2016: Medical Physics
https://www.readbyqxmd.com/read/28035817/nanoscale-proteinosomes-fabricated-by-self-assembly-of-a-supra-molecular-protein-polymer-conjugate
#18
Guangda Han, Jin-Tao Wang, Xiaotian Ji, Li Liu, Hanying Zhao
Proteinosomes are a type of protein-based spherical capsules, which have potential applications in drug delivery, cell imaging, gene expression and biocatalysis. In this research, a novel approach to the fabrication of proteinosomes entirely composed of protein molecules based on self-assembly of a supramolecular protein-polymer conjugate, is proposed. A supramolecular protein-polymer conjugate was prepared by mixing βCD-modified bovine serum albumin (BSA) and adamantane-terminated poly(N-isopropylamide) (Ad-PNIPAM) in aqueous solution...
December 30, 2016: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28029254/pegylated-and-functionalized-aliphatic-polycarbonate-polyplex-nanoparticles-for-intravenous-administration-of-hdac5-sirna-in-cancer-therapy
#19
Antoine Frère, Alexandra Baroni, Elodie Hendrick, Anne-Sophie Delvigne, François Orange, Olivier Peulen, George R Dakwar, Jérôme Diricq, Philippe Dubois, Brigitte Evrard, Katrien Remaut, Kevin Braeckmans, Stefaan C De Smedt, Julie Laloy, Jean-Michel Dogné, Georges Feller, Laetitia Mespouille, Denis Mottet, Geraldine Piel
Guanidine and morpholine functionalized aliphatic polycarbonate polymers able to efficiently deliver histone deacetylase 5 (HDAC5) siRNA into the cytoplasm of cancer cells in vitro leading to a decrease of cell proliferation were previously developed. To allow these biodegradable and biocompatible polyplex nanoparticles to overcome the extracellular barriers and be effective in vivo after an intravenous injection, polyethylene glycol chains (PEG750 or PEG2000) were grafted on the polymer structure. These nanoparticles, showed an average size of about 150 nm and a slightly positive zeta potential with complete siRNA complexation...
December 28, 2016: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28029204/translating-thermal-response-of-triblock-copolymer-assemblies-in-dilute-solution-to-macroscopic-gelation-and-phase-separation
#20
Zhe Sun, Ye Tian, Wendy L Hom, Oleg Gang, Surita R Bhatia, Robert B Grubbs
The thermal response of semi-dilute solutions (5 w/w%) of two amphiphilic thermoresponsive poly(ethylene oxide)-b-poly(N,N-diethylacrylamide)-b-poly(N,N-dibutylacrylamide) (PEO45 -PDEAmx -PDBAm12 ) triblock copolymers, which differ only in the size of the central responsive block, in water was examined. Aqueous PEO45 -PDEAm41 -PDBAm12 solutions, which undergo a thermally induced sphere-to-worm transition in dilute solution, were found to reversibly form soft (G'≈10 Pa) free-standing physical gels after 10 min at 55 °C...
December 28, 2016: Angewandte Chemie
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