Co-reporter:Zhengfei Wu;Na Hao;Hai Zhang;Zhaoyuan Guo;Rong Liu;Bin He
Biomaterials Science (2013-Present) 2017 vol. 5(Issue 5) pp:1032-1040
Publication Date(Web):2017/05/02
DOI:10.1039/C7BM00028F
Metal–organic frameworks as a powerful platform for drug delivery have attracted significant attention in recent years. In this study, mesoporous iron-metal–organic framework nanoparticles (mesoMOFs) were synthesized via the double-template method. Cetyltrimethylammonium bromide (CTAB) and citric acid (CA) were chosen as the double-template agent. The mesoMOFs were characterized by EDX, elemental analysis, TG, BET, SEM, TEM, and DLS. The anticancer drug doxorubicin hydrochloride (DOX) was encapsulated in the mesoMOFs, and the DOX loading content was up to 55 wt%. The mesoMOFs are non-toxic to both 4T1 breast cancer cells and 3T3 fibroblasts. The DOX-loaded mesoMOFs exhibit a better anti-tumor effect than free doxorubicin in vitro. The in vivo anticancer activities of the DOX-loaded mesoMOFs were investigated in 4T1 breast cancer-bearing mice. The intratumoral injection of DOX-loaded mesoMOFs revealed that the mesoMOFs could significantly reduce the systemic toxicity of DOX, sustainably release DOX, and maintain an effective DOX concentration for chemotherapy. The DOX-loaded mesoMOFs exhibit excellent therapeutic efficacy and low side effects in local chemotherapy.
Co-reporter:Y. Chen, Y. X. Zhang, Z. F. Wu, X. Y. Peng, T. Su, J. Cao, B. He and S. Li
RSC Advances 2016 vol. 6(Issue 63) pp:58160-58172
Publication Date(Web):13 Jun 2016
DOI:10.1039/C6RA06040D
Three poly(ethylene glycol)–poly(ε-carprolactone) (PEG–PCL) copolymers with different topologies but identical molar ratio between PEG to PCL were designed. These copolymers, namely, diblock (L-PEG–PCL), triblock (B-PEG–PCL), and star shaped (S-PEG–PCL) copolymers, were extensively characterized by 1H Nuclear Magnetic Resonance (1H NMR), Fourier Transform Infrared Spectroscopy (FTIR), and Gel Permeation Chromatography (GPC) analyses. The effect of topology on crystallization was investigated by X-Ray Diffraction (XRD), Differential Scanning Calorimetry (DSC). Results showed that the diblock copolymer possessed the highest crystallinity, followed by triblock and star shaped copolymers. Although the topology did not affect the self-assembly behavior of copolymers, the effects on size, size distribution, drug loading content, and drug release rate of the polymeric micelles were observed. The micelles self-assembled from linear diblock copolymer achieved higher cellular uptake and lower half maximal inhibitory concentration (IC50). These findings are favorable to establish the foundation to further design proper structure of amphiphilic copolymers as nanocarrier systems for efficient anticancer therapy.
Co-reporter:Song Luo, Yixin Zhang, Jun Cao, Bin He, Sai Li
Colloids and Surfaces B: Biointerfaces 2016 Volume 148() pp:181-192
Publication Date(Web):1 December 2016
DOI:10.1016/j.colsurfb.2016.07.023
•Arginine modified poly(ethylene glycol)-b-poly(ε-caprolactone) diblock copolymer was synthesized.•The effect of arginine on the cellular internalization of drug loaded micelles was investigated.•The arginine enhanced endolysosome escape of drug loaded polymeric micelles to improve the anticancer activity.A new drug delivery system with improved endocytosis efficiency based on arginine modified poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-PCL) diblock copolymers was developed successfully. The structures of amphiphilic copolymers were verified by proton Nuclear Magnetic Resonance (1H NMR), Fourier Transform Infrared (FTIR) and Gel Permeation Chromatography (GPC). The amphiphilic copolymers could self-assemble into spherical micelles with critical micelle concentration (CMC) at approximately 0.03 mg/mL. Biocompatibility, cellular internalization efficiency and in vitro antitumor effect of the polymeric micelles were studied. Results showed that drug-free micelles were nontoxic to cells. The Confocal Laser Microscopy (CLSM) and the flow cytometry as well as the antitumor activity tests all revealed that drug-loaded micelles modified by arginine groups (guanidino) exhibited higher endocytosis efficiency than those without modification, resulting in a lower IC50 value to kill tumor cells and meanwhile averting the “competitive binding” problem. Also, in vivo results demonstrated that arginine modified polymeric micelles could deliver the drug to tumor site more efficiently than ones without any modification, thus indicating guanidino in polymeric micelles could benefit the internalization of micelles to fully exert the function of killing tumors. In general, guanidinylation strategy in this splendid novel micelle system has a great potential to improve the therapeutic effect of nanoparticle-based drug delivery system for cancer therapy in the future.
Co-reporter:Yuanlin Li, Ting Su, Sai Li, Yusi Lai, Bin He and Zhongwei Gu
Biomaterials Science 2014 vol. 2(Issue 5) pp:775-783
Publication Date(Web):03 Mar 2014
DOI:10.1039/C3BM60267B
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. Herein, we report a novel polymeric micelle with π–π conjugated cinnamate moiety on glycerol dendrimer as lipophilic segment, the modified dendritic segment was connected to poly(ethylene glycol) (PEG) via click chemistry. The received amphiphiles self-assembled into micelles in aqueous medium. The properties of the polymeric micelles such as critical micelle concentration (CMC), mean size and morphology were investigated. Anticancer drug doxorubicin (DOX) was loaded in the polymeric micelles. The π–π interaction, drug release profile and in vitro anticancer efficiency of the DOX loaded micelles were studied. The results showed that the micelles with more cinnamate moieties exhibited a lower CMC. The drug loading content and release rate of the micelles increased with increasing generation of glycerol dendrimer. Strong π–π stacking interaction was detected between DOX and carriers. The DOX loaded polymeric micelles exhibited efficient anticancer activity in vitro.
Co-reporter:Shangfeng Pan, Song Luo, Sai Li, Yusi Lai, Yanyan Geng, Bin He and Zhongwei Gu
Chemical Communications 2013 vol. 49(Issue 73) pp:8045-8047
Publication Date(Web):12 Jul 2013
DOI:10.1039/C3CC44767G
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.
Co-reporter:Jun Cao, Aijing Lu, Chenglong Li, Mengtan Cai, Yuanwei Chen, Sai Li, Xianglin Luo
Colloids and Surfaces B: Biointerfaces 2013 Volume 112() pp:35-41
Publication Date(Web):1 December 2013
DOI:10.1016/j.colsurfb.2013.07.038
•Various architectures of polymers contained sulfobetaines were successfully synthesized.•The copolymers can self-assemble into micelles with small size and narrow size distribution.•The number of arm had a great effect on the micellar properties.•The core of micelles can efficiently solubilize the hydrophobic drug.Linear and star-shape poly(ɛ-caprolactone)-b-poly(N-(3-sulfopropyl)-N-methacryloxyethyl-N,N-diethylammoniumbetaine) (L/sPCL-b-PDEAS) with 4 and 6 arms were synthesized with the combination of Ring Opening Polymerization (ROP) and Atom Transfer Radical Polymerization (ATRP). These copolymers self-assembled into micelles via solvent evaporation method. The critical micelle concentration (CMC), determined by fluorescence spectroscopy using pyrene as a probe, was lower than 10−3 mg/mL and decreased with increasing arm numbers. Atom force microscopy (AFM) images showed that the micelles were spherical in shape with narrow size distribution. The hydrophobic drug model carotene was efficiently loaded in the polymeric micelles. The sizes and drug loading content (DLC) of the carotene-loaded micelles increased with increasing drug content in feed. In vitro drug release experiment demonstrated that the release rate of carotene from the micelles was closely related to the arm numbers and drug loading content. Linear copolymer micelles showed the fastest release rate, 4-arm star shape copolymer micelles exhibited the lowest release rate. The micelles with higher drug loading content showed lower release rate. The release kinetics of carotene from micelles fitted the Ritger–Peppas equation.
Co-reporter:Danna Yang;Lin Wang;Xiaoxian Zhang;Dongwei Wang;Zhiqiang Shen
Nano-Micro Letters 2011 Volume 3( Issue 3) pp:146-152
Publication Date(Web):2011 September
DOI:10.1007/BF03353665
Depositing single-walled carbon nanotubes (SWNTs) with controllable density, pattern and orientation on electrodes presents a challenge in today’s research. Here, we report a novel solvent evaporation method to align SWNTs in patterns havingnanoscale width and micronscale length. SWNTs suspension has been introduced dropwise onto photoresist resin microchannels; and the capillary force can stretch and align SWNTs into strands with nanoscale width in the microchannels. Then these narrow and long aligned SWNTs patterns were successfully transferred to a pair of gold electrodes with different gaps to fabricate carbon nanotube field-effect transistor (CNTFET). Moreover, the electrical performance of the CNTFET show that the SWNTs strands can bridge different gaps and fabricate good electrical performance CNTFET with ON/OFF ratio around 106. This result suggests a promising and simple strategy for assembling well-aligned SWNTs into CNTFET device with good electrical performance.
Co-reporter:Shangfeng Pan, Song Luo, Sai Li, Yusi Lai, Yanyan Geng, Bin He and Zhongwei Gu
Chemical Communications 2013 - vol. 49(Issue 73) pp:NaN8047-8047
Publication Date(Web):2013/07/12
DOI:10.1039/C3CC44767G
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.
Co-reporter:Yuanlin Li, Ting Su, Sai Li, Yusi Lai, Bin He and Zhongwei Gu
Biomaterials Science (2013-Present) 2014 - vol. 2(Issue 5) pp:NaN783-783
Publication Date(Web):2014/03/03
DOI:10.1039/C3BM60267B
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. Herein, we report a novel polymeric micelle with π–π conjugated cinnamate moiety on glycerol dendrimer as lipophilic segment, the modified dendritic segment was connected to poly(ethylene glycol) (PEG) via click chemistry. The received amphiphiles self-assembled into micelles in aqueous medium. The properties of the polymeric micelles such as critical micelle concentration (CMC), mean size and morphology were investigated. Anticancer drug doxorubicin (DOX) was loaded in the polymeric micelles. The π–π interaction, drug release profile and in vitro anticancer efficiency of the DOX loaded micelles were studied. The results showed that the micelles with more cinnamate moieties exhibited a lower CMC. The drug loading content and release rate of the micelles increased with increasing generation of glycerol dendrimer. Strong π–π stacking interaction was detected between DOX and carriers. The DOX loaded polymeric micelles exhibited efficient anticancer activity in vitro.
Co-reporter:Zhengfei Wu, Na Hao, Hai Zhang, Zhaoyuan Guo, Rong Liu, Bin He and Sai Li
Biomaterials Science (2013-Present) 2017 - vol. 5(Issue 5) pp:NaN1040-1040
Publication Date(Web):2017/03/30
DOI:10.1039/C7BM00028F
Metal–organic frameworks as a powerful platform for drug delivery have attracted significant attention in recent years. In this study, mesoporous iron-metal–organic framework nanoparticles (mesoMOFs) were synthesized via the double-template method. Cetyltrimethylammonium bromide (CTAB) and citric acid (CA) were chosen as the double-template agent. The mesoMOFs were characterized by EDX, elemental analysis, TG, BET, SEM, TEM, and DLS. The anticancer drug doxorubicin hydrochloride (DOX) was encapsulated in the mesoMOFs, and the DOX loading content was up to 55 wt%. The mesoMOFs are non-toxic to both 4T1 breast cancer cells and 3T3 fibroblasts. The DOX-loaded mesoMOFs exhibit a better anti-tumor effect than free doxorubicin in vitro. The in vivo anticancer activities of the DOX-loaded mesoMOFs were investigated in 4T1 breast cancer-bearing mice. The intratumoral injection of DOX-loaded mesoMOFs revealed that the mesoMOFs could significantly reduce the systemic toxicity of DOX, sustainably release DOX, and maintain an effective DOX concentration for chemotherapy. The DOX-loaded mesoMOFs exhibit excellent therapeutic efficacy and low side effects in local chemotherapy.