ACS Applied Materials & Interfaces
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2017
·
IF 7.504
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 FT-IR and 1H NMR spectroscopies 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. These block copolymers could self-assemble and form globular nanoscaled core–shell micellar aggregates in aqueous solution. The reductive ferrocene groups could be changed into hydrophilic ferrocenium via mild oxidation, whereas the polymer micelles at the oxidation state could reversibly recover from their original states upon reduction by vitamin C. The tunable redox response was investigated and verified by transmission electron microscopy, ultraviolet–visible spectroscopy, cyclic voltammetry, and dynamic light scattering measurements. The copolymer micelles were used to entrap anticancer drug paclitaxel (PTX), with high drug encapsulation efficiency of 61.4%, while the PTX-loaded drug formulation exhibited oxidation-controlled drug release, and the release rate could be mediated by the kinds and concentrations of oxidants. MTT assay was performed to disclose the biocompatibility and security of the copolymer micelles and to assess anticancer efficiency of the PTX-loaded nanomicelles. The developed copolymer nanomicelles with reversible redox response are anticipated to have potential in targeted drug delivery systems for cancer therapy.
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高影响因子
RSC Advances
·
2016
·Vol. 6
·期 76
·72439-72446
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IF 3.289
Jinyang Shen,Ye Jin,Hongli Tian,Yuan Wang,Xiaolin Yang,Zhonglin Yang,Changrun Guo,Fei Li
Akebia saponin D (ASD), a triterpenoid saponin with numerous pharmacological activities, is isolated from the rhizome of Dipsacus asper Wall. However, the poor oral bioavailability of ASD restricts its development and clinical use. The purpose of this research is to develop a solid dispersion (ASD-SD) to improve the oral bioavailability of ASD. Poloxamer 407 was employed to prevent ASD from aggregation and Cremophor® RH 40 was used to inhibit multidrug resistance associated protein (MRP) mediated efflux in several new formulations. The particle size was remarkably reduced from 380 nm (ASD) to 230 nm (ASD-SD1 [composition: ASD : Poloxamer 407 : Cremophor® RH 40; ratio: 5 : 9 : 1, w/w/w]). The cumulative release percentage of molecular ASD from dialysis bags was improved from 63.78% (ASD) to 97.12% (ASD-SD1). Single-pass intestinal perfusion studies showed that the absorption of ASD in ASD-SD2 (composition: ASD : Poloxamer 407; ratio: 5 : 9, w/w) was increased approximately 1.8-fold compared to ASD which was mainly due to the particle size reduction, and further promoted by ASD-SD1 about 2.1-fold compared to ASD-SD2 which might be through the MRP inhibition of Cremophor® RH 40. Furthermore, the oral bioavailability in rats was enhanced significantly to 156.9% and 233.1% by ASD-SD2 and ASD-SD1, respectively. Therefore, ASD-SD1 could be a promising drug delivery system to improve the oral absorption of ASD which might be by destroying self-micelles and inhibiting MRP-mediated efflux.
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RSC Advances
·
2016
·Vol. 6
·期 68
·63597-63606
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IF 3.289
Shasha Zhao,Xiaoshan Fan,Xiaoyan Li,Xianglin Lv,Weiwei Zhang,Zhiguo Hu
Y-Shaped amphiphilic copolymers (zwitterionic-(PLLA2.5K)2 and MPEG-(PDLA2.5K)2) were simply synthesized through click reaction of alkyne-(PLA2.5K)2 and zwittterionic-N3 or MPEG-N3. Gel permeation chromatography (GPC) and 1H nuclear magnetic resonance (1H NMR) were employed to characterize the composition and structure of these copolymers. The stereocomplexes were prepared from pairs zwitterionic-(PLLA2.5K)2/MPEG-(PDLA2.5K)2 (molar ratio = 1 : 1), and confirmed by differential scanning calorimeter (DSC). Furthermore the aggregation behaviors for these synthesized polymers and their stereocomplexes had been proved by fluorescence spectroscopy (PL), transmission electron microscopy (TEM), dynamic light scattering (DLS) and static light scattering (SLS), and zeta potential. Their critical micelle concentration (CMC) obtained by PL was 0.0213 mg mL−1 for zwitterionic-(PLLA2.5K)2/MPEG1.9K-(PDLA2.5K)2 and 0.1265 mg mL−1 for zwitterionic-(PLLA2.5K)2/MPEG5K-(PDLA2.5K)2. The stereocomplexes could self-assemble into spherical micelles with diameters of 76 nm (zwitterionic-(PLLA2.5K)2/MPEG1.9K-(PDLA2.5K)2) and 89 nm (zwitterionic-(PLLA2.5K)2/MPEG5K-(PDLA2.5K)2) respectively. The biocompatibility of these copolymers and their stereocomplexes was evaluated with relatively low cytotoxicity. The DOX-loaded micelles of the stereocomplexes had a higher drug loading content and encapsulation efficiency, and could release DOX in a controlled manner. Therefore, the new stereocomplex zwitterionic-(PLLA)2/MPEG-(PDLA)2 has great potential as a hydrophobic drug nanocarrier.
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POLYCYCLIC AROMATIC COMPOUNDS
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2016
·
IF 0.959
Jian Long,Senlin Tian,Yanhua Niu,Yueming Jin,Lin Li
Reduplicate utilization of surfactants is a key factor for Surfactant-Enhanced Remediation (SER) technology to reduce its high operation costs. In order to achieve the reuse of surfactants, this study attempted to construct a novel reversible solubilization system for SER. Three typical polycyclic aromatic hydrocarbons (PAHs) pyrene, phenanthrene, and acenaphthene were controllably solubilized and released by the mixed micelles composed of redox-active cationic surfactant (11-Ferrocenylundecyl) trimethylammoniunm bromide (FTMA) and conventional nonionic surfactant Tween80. Solubilization of PAHs is assumed to be controlled by changing the redox states of FTMA. Cyclic voltammograms tests of FTMA showed the oxidation and reduction potential were 0.4570 and 0.4068 V, respectively, and the peak currents ratio of FTMA and FTMA+ was 1.26, verified that FTMA possesses electrochemically reversible property. In FTMA-Tween80 mixed solutions, CMC values demonstrated the nonideal interaction between the two surfactants and the interaction parameters (β) was -5.5296 when the mass ratio was FTMA:Tween80 = 2:8. Due to the synergistic solubilization effect, the apparent water solubilities of PAHs were significantly enhanced by the mixed surfactant, and they were much higher than those in single surfactant. After oxidation, more than 50% of the PAHs in mixed micelles could be released, the cumulative release efficiency of selected PAHs followed the order of pyrene > pherantherene > acenaphthene. Briefly, such results in this article provide a facile method to meliorate the SER technology.
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MOLECULAR PHARMACEUTICS
·
2017
·
IF 4.44
Xiaoxiao Shi,Meili Hou,Shuang Bai,Xiaoqian Ma,Yong-E Gao,Bo Xiao,Peng Xue,Yuejun Kang,Zhigang Xu,Chang Ming Li
Stimuli-responsive nanomedicine with theranostic functionalities with reduced side-effects has attracted growing attention, although there are some major obstacles to overcome before clinical applications. Herein, we present an acid-activatable theranostic unimolecular micelles based on amphiphilic star-like polymeric prodrug to systematically address typical existing issues. This smart polymeric prodrug has a preferable size of about 35 nm and strong micellar stability in aqueous solution, which is beneficial to long-term blood circulation and efficient extravasation from tumoral vessels. Remarkably, the polymeric prodrug has a high drug loading rate up to 53.1 wt%, which induces considerably higher cytotoxicity against tumor cells (HeLa cells and MCF-7 cells) than normal cells (HUVEC cells) suggesting a spontaneous tumor-specific targeting capability. Moreover, the polymeric prodrug can serve as a fluorescent nanoprobe activated by the acidic microenvironment in tumor cells, which can be used as a promising platform for tumor diagnosis. The superior antitumor effect in this in vitro study demonstrates the potential of this prodrug as a promising platform for drug delivery and cancer therapy.
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RSC Advances
·
2014
·Vol. 4
·期 91
·49866-49872
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IF 3.708
Zhihui Fang,Duanguang Yang,Yong Gao,Huaming Li
In this study, we reported a novel, facile, Pickering emulsion-templating method to prepare massage ball-like, hollow-structured Au/SiO2 microspheres. Firstly, oil-in-water Pickering emulsions stabilized by Au@poly(ethylene oxide)-b-poly(4-vinylpyridine) (Au@PEO-b-P4VP) hybrid emulsifier micelles, which were formed by a P4VP/Au complex induced self-assembly process, were generated. Then hollow Au/SiO2 hybrid microspheres with nano-/submicro-sized protrusions on their shells, termed as massage ball-like microspheres, were successfully synthesized using the generated Pickering emulsion as template, in which the P4VP catalyzed hydrolysis and condensation of tetraethoxysilane (TEOS) in the TEOS/n-decanol mixed oil phase occurred at the oil/water interface. As a result, a continuous SiO2 shell was formed. The uneven adsorption of polydisperse hybrid micelles at the oil/water interface as well as the volume shrinkage of the oil phase during the early hydrolysis and condensation of TEOS facilitated the formation of protrusions on the shell surface. After further removal of the polymer components embedded in the shell by calcination, hollow Au/SiO2 hybrid microspheres with micropore/mesopore bimodal porous shells were produced. The as-prepared Au/SiO2 hybrid microspheres were applied as catalysts for the reduction of p-nitrophenol with NaBH4, showing a high catalytic activity with a good recyclability owing to the large specific areas, the easily accessible Au active centres, and the enhanced mass transportation.
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International Journal of Nanomedicine
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2015
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IF 4.383
Tianpeng Zhang,Huan Wang,Yanghuan Ye,Xingwang Zhang,Baojian Wu
Polymeric micelles receive considerable attention as drug delivery vehicles, depending on the versatility in drug solubilization and targeting therapy. However, their use invariably suffers with poor stability both in in vitro and in vivo conditions. Here, we aimed to develop a novel nanocarrier (micellar emulsions, MEs) for a systemic delivery of genistein (Gen), a poorly soluble anticancer agent. Gen-loaded MEs (Gen-MEs) were prepared from methoxy poly(ethylene glycol)-block-(ε-caprolactone) and medium-chain triglycerides (MCT) by solvent-diffusion technique. Nanocarriers were characterized by dynamic light scattering, transmission electron microscopy, and in vitro release. The resulting Gen-MEs were approximately 46 nm in particle size with a narrow distribution. Gen-MEs produced a different in vitro release profile from the counterpart of Gen-ME. The incorporation of MCT significantly enhanced the stability of nanoparticles against dilution with simulated body fluid. Pharmacokinetic study revealed that MEs could notably extend the mean retention time of Gen, 1.57- and 7.38-fold as long as that of micelles and solution formulation, respectively, following intravenous injection. Furthermore, MEs markedly increased the elimination half-life (t1/2β) of Gen, which was 2.63-fold larger than that of Gen solution. Interestingly, Gen distribution in the liver and kidney for MEs group was significantly low relative to the micelle group in the first 2 hours, indicating less perfusion in such two tissues, which well accorded with the elongated mean retention time. Our findings suggested that MEs may be promising carriers as an alternative of micelles to systemically deliver poorly soluble drugs.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
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IF 7.7
Yuanyuan Zhang,Yongbin Meng,Siying Wang,Yuangang Zu,Xiuhua Zhao
The oral route of administration is considered the optimal choice for treating chronic diseases due to its convenience and non-invasiveness, which can help prevent physical and mental harm to patients undergoing long-term treatment. However, challenges such as safety, gastrointestinal stability, and bioavailability of oral drugs often limit their effectiveness. Natural biomacromolecule micelles, known for their safety, stability, biocompatibility, and diverse functions, have emerged as promising carriers for oral treatment of chronic diseases like systemic lupus erythematosus (SLE) with fat-soluble drugs. This study introduces an innovative approach by developing an oral delivery system using chemically synthesized natural biomacromolecules to load artesunate for treating SLE. By synthesizing amphiphilic polymer micelles from pectin and casein through a carbodiimide reaction, a more stable structure is achieved. The hydrophobic core of these micelles encapsulates artesunate, resulting in the formation of an oral delivery system (PC-AS) with several advantages, including high drug loading and encapsulation efficiency, small particle size, negative potential, strong stability in the gastrointestinal tract, low toxicity and side effects, strong adhesion in the small intestine, and high bioavailability. These advantages facilitate efficient absorption of artesunate in the gastrointestinal tract, leading to improved bioavailability and effective alleviation of SLE-like symptoms in MRL/ lpr mice. By utilizing chemically synthesized natural macromolecular micelles for delivering artesunate in the treatment of SLE, this study overcomes the oral barriers associated with the original drug and presents a novel solution for the long-term oral treatment of chronic diseases.
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CARBOHYDRATE POLYMERS
·
2024
·
IF 10.7
Yufan Guo,Xiuru Yang,Yihong Zhang,Fazhen Luo,Juan Yang,Xupeng Zhang,Jinxia Mi,Yan Xie
Cancer multidrug resistance (MDR) dramatically hindered the efficiency of standard chemotherapy. Mitochondria are highly involved in the occurrence and development of MDR; thus, inducing its malfunction will be an appealing strategy to treat MDR tumors. In this paper, a natural polysaccharides-based nanoplatform (TDTD@UA/HA micelles) with cell and mitochondria dual-targeting ability was facilely fabricated to co-deliver ursolic acid (UA) and doxorubicin (DOX) for combinatorial MDR therapy. TDTD@UA/HA micelles featured a spherical morphology, narrow size distribution (∼140 nm), as well as favorable drug co-loading capacity (DOX: 8.41 %, UA : 9.06 %). After hyaluronic acid (HA)-mediated endocytosis , the lysosomal hyaluronidase promoted the degradation of HA layer and then the positive triphenylphosphine groups were exposed, which significantly enhanced the mitochondria-accumulation of nano micelles . Subsequently, DOX and UA were specifically released into mitochondria under the trigger of endogenous reactive oxygen species (ROS), followed by severe mitochondrial destruction through generating ROS, exhausting mitochondrial membrane potential, and blocking energy supply, etc. ; ultimately contributing to the susceptibility restoration of MCF-7/ADR cells to chemotherapeutic agents. Importantly, TDTD@UA/HA micelles performed potent anticancer efficacy without distinct toxicity on the MDR tumor-bearing nude mice model. Overall, the versatile nanomedicine represented a new therapeutic paradigm and held great promise in overcoming MDR-related cancer.
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DYES AND PIGMENTS
·
2011
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IF 2.635
Shenguang Ge,Juanjuan Lu,Mei Yan,Feng Yu,Jinghua Yu,Xiujin Sun
Bovine serum albumin in micelles was effectively detected by a fluorescence resonance energy transfer -based molecular sensor using CdTe quantum dots as energy donors and neutral red as energy acceptors. The fluorescence resonance energy transfer efficiency was enhanced by the construction of cetyltrimethylammonium bromide micelles, which significantly reduced the distance between the donor and the acceptor. The results indicated that the addition of the albumin easily leads to the fluorescence quenching of CdTe-neutral red fluorescence resonance energy transfer due to the formation of CdTe-albumin complexes which have weak affinity to CdTe and repels the dyes from CdTe surface. The fluorescence intensity of the CdTe-neutral red sensor quenched with the increasing concentration of albumin. The linear range of albumin was from 0.4 × 10 −3 to 11.00 × 10 −3 g L −1 . The detection limit was 0.13 g L −1 .
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MACROMOLECULAR CHEMISTRY AND PHYSICS
·
2011
·Vol. 212
·期 23
·2511-2521
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IF 2.437
Dong Chen,Huimin Liang,Yuehui Yang,Zhenting Yuan,Pingtian Ding,Yihui Deng
A new type of drug delivery system consisting of an amphiphilic polymer micelle with pH-sensitive groups is reported. The polymer comprises mPEG [poly(ethylene glycol) monomethyl ether], PCL [poly(ϵ-caprolactone)], and either PAA [poly(acrylic acid)] or PMAA [poly(methacrylic acid)]. Both mPEG -b- PCL and mPEG -b- PCL -b- PAA/PMAA are characterized by 1 H NMR, FTIR, and gel permeation chromatography (GPC). The diameters of the mPEG -b- PCL -b- PAA/PMAA micelles are found to increase with increases in pH and studies show that in vitro release of nifedipine from mPEG -b- PCL -b- PAA/PMAA micelles becomes faster as the pH value of phosphate-buffered saline (PBS) increases. This new type of pH-sensitive polymeric micelle can potentially be used as a drug carrier for oral administration of water-insoluble drugs.
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BIOMATERIALS
·
2015
·
IF 8.557
Tingjie Yin,Lei Wang,Lifang Yin,Jianping Zhou,Meirong Huo
In this study, a novel redox-sensitive micellar system constructed from a hyaluronic acid-based amphiphilic conjugate (HA-ss-(OA-g-bPEI), HSOP) was successfully developed for tumor-targeted co-delivery of paclitaxel (PTX) and AURKA specific siRNA (si-AURKA). HSOP exhibited excellent loading capacities for both PTX and siRNA with adjustable dosing ratios and desirable redox-sensitivity independently verified by morphological changes of micelles alongside in vitro release of both drugs in different reducing environments. Moreover, flow cytometry and confocal microscopy analysis confirmed that HSOP micelles were capable of simultaneously delivering PTX and siRNA into MDA-MB-231 breast cancer cells via HA-receptor mediated endocytosis followed by rapid transport of cargoes into the cytosol. Successful delivery and transport amplified the synergistic effects between the drugs while leading to substantially greater antitumor efficacy when compared with single drug-loaded micelles and non-sensitive co-loaded micelles. In vivo investigation demonstrated that HSOP micelles could effectively accumulate in tumor sites and possessed the greatest antitumor efficacy over non-sensitive co-delivery control and redox-sensitive single-drug controls. These findings indicated that redox-sensitive HSOP co-delivery system holds great promise for combined drug/gene treatment for targeted cancer therapy.
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