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Superparticles Formed by Amphiphilic Tadpole-like Single Chain Polymeric Nanoparticles and Their Application as an Ultrasonic Responsive drug carrier

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Chinese Journal of Chemical Physics 2017年第2期30卷 211-218,I0002页

作者：江力李会亚陈道勇复旦大学高分子科学系聚合物分子工程国家重点实验室上海200433

Herein, we report self-assembly of tadpole-like single chain polymeric nanoparticles （TPPs） and the ultrasonic response of the resultant superparticles. The TPPs are with an intramolecularly crosslinked poly（2-（methacryloyloxy）ethyl pent-4-ynoate）-rpoly（hydroxyethyl methacrylate）（PMAEP-r-PHEMA） chain as the ＂head＂ and a poly（2- （dimethylamino）ethyl methacrylate （PDMAEMA） linear chain as the ＂tail＂, and are pre- pared simply and emciently by Glaser-coupling of the pendant alkynes in the PMAEP-r- PHEMA block in the common solvent methanol. The formation of the TPPs was confirmed by gel permeation chromatograph, nuclear magnetic resonance spectroscopy, dynamic light scattering, static dynamic scattering, and transmission electron microscopy. In aqueous solution, the amphiphilic TPPs could self-assemble into regular superparticles, driven by aggregation of the hydrophobic ＂heads＂. Since in the structure there is no chain entanglement and the embedding of PDMAEMA chains disturb close-packing of the ＂heads＂, the superpartieles are responsive to a low-energy ultrasonic vibration, as evidenced by greatly enhanced release of the functional molecules from the superparticles by treatment of a low-energy ultrasound. Therefore, the superparticles should be very promising in the use as the drug carriers that can be manipulated from a long distance, considering that ultrasonic energy can be focused at a small area in a relatively long distance from the ultrasound-radiating source.

关键词： Single chain polymer nanoparticles Superparticles Ultrasonic response drug carrier

Preparation and Stability Evaluation of Size-Controllable PDHCA-β-CD Nanoparticles as drug carrier

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Chinese Journal of Chemistry 2017年第7期35卷 1125-1132页

作者： Hong Chu Xue Zhao Shirong Liu Zhongbin Ni Dongjian Shi Mingqing Chen School of Chemical and Material Engineering Jiangnan University Wuxi Jiangsu 214122 China The Key Laboratory of Food Colloids andBiotechnology Ministry of Education Jiangnan University Wuxi Jiangsu 214122 China

A novel biocompatible polymer was prepared by grafting the derivate of β-cyclodextrin （6-SH-β-CD） onto poly（3,4-dihydroxycinnamic acid）（PDHCA） via Michael addition. PDHCA-β-CD nanoparticles were prepared by the self-assembly of amphiphilic PDHCA-β-CD polymer with N,N-dimethylformamide （DMF） as good solvent and water as poor solvent. The PDHCA-β-CD nanoparticles were monodispersed with spherical morphology as shown in the scanning electron microscopic （SEM） images in accord with the result of dynamic light scattering （DLS） measurement. The size of the nanoparticles could be controlled from 60 to 180 nm by tuning the grafting degree （GD） of PDHCA-β-CD polymer and also significantly influenced by the amount of water used during the process. These as-prepared nanoparticles were stable without any significant change in the particle size after six-months＇ storage and even after being irradiated by UV at 2〉280 nm for hours. The formation mechanism of PDHCA-β-CD nanoparticles was explored. The content of doxombicin （DOX） loaded onto the nanoparticles was up to 39% with relatively high loading efficiency （approximately 78.8% of initial DOX introduced was loaded）. In vitro release studies suggested that DOX released slowly from PDHCA-β-CD nanoparticles. These features strongly support the potential of developing PDHCA-β-CD nanoparticles as carriers for the controlled delivery of drug.

关键词： PDHCA-β-CD nanoparticles controllable and desirable size high stability drug carrier

Preparation and drug-release Behavior of β-TCP Ceramics drug carrier in vitro

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Journal of Wuhan University of Technology(Materials Science) 2012年第6期27卷 1058-1060页

作者：张启焕 YAN Xin YAN Yuhua DAI Honglian JIANG Xin LI Shipu College of Chemical and Biological Engineering Yancheng Institute of Technology Biomedical Materials and Engineering Center Wuhan University of TechnologyWuhan 430070China

β-TCP ceramics drug carrier was first prepared and characterized. SEM showed that β-TCP carrier was in porous amorphous structure with diameters around 10 μm. The physical properties including apparent porosity, volume-weight, tensile strength and the permeability were measured and the results indicated those properties fit the clinical usage of β-TCP drug carrier. Furthermore, drug release experiment in vitro showed that the carrier could prolong drug release in simulated body fluid which provides basis for the clinical use of β-TCP ceramics as drug carrier.

关键词： β-TCP ceramics drug carrier physicochemical properties drug release clinical use

Research progress on pharmacological action and effective drug carrier of berberine

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Journal of Hainan Medical University 2020年第17期26卷 61-65页

作者： Yue Liu Bai-Jie Ren Xin-Ying Zou Jing-Yi Lu Lei Wang Dong-Hui Gao Department of Periodontics Hospital of StomatologyJilin UniversityChangchun 130021JilinChina

Berberine(BBR)is an isoquinoline alkaloid that can be extracted from the traditional Chinese medicine Huang *** has anti-inflammatory,anti-cancer,protection of nerves,hypoglycemic,blood lipid,anti-oxidation,antibacterial and other *** can be used clinically to treat chronic colitis,bacterial vaginitis,rheumatoid arthritis,breast cancer,liver cancer,Alzheimer's disease,diabetes,obesity and other common *** paper reviews the pharmacological effects of berberine and the research progress of effective drug carriers in order to provide new ideas for the clinical application of berberine.

关键词： Berberine Pharmacological effects drug carrier

A new potential pH-sensitive drug carrier based on PEG-ketal polymer

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A new potential pH-sensitive drug carrier based on PEG-ketal...

Research progress in nanoparticles as anticancer drug carrier

2013年中国药学大会暨第十三届中国药师周

作者： Daquan Chen Kaoxiang Sun Wanhui Liu Youxin Li School of Pharmacy Yantai University Yantai State Key Laboratory of Long-acting and Targeting drug Delivery System

In this article, we report a novel pH-sensitive ketal polymer as drug carrier, mPEG-IS （PI）. PI designed to deliver drugs to the acidic environments of tumors, inflammatory tissues, and phagosomes. PI carrying pH-sensitive ketal group as hydrophobic moieties and PEG group as hydrophilic moieties was synthesized. The PI micelles encapsulated curcumin was formed and improved the solubility of curcumin （Cur） with size around 100–200 nm. The PI micelles could release encapsulated curcumin with accelerated rate under lower pH condition. The encapsulated curcumin PI micelles （Cur-PM） were stable and have less toxicity compared to curcumin suspension. The anti-tumor efficacy in vivo suggested that Cur-PM suppressed tumor growth most efficiently. These findings have shed some light on the PI polymer as potential drug carrier for curcumin.

关键词： pH-sensitive ketal polymer mPEG-IS (PI) curcumin drug carrier

来源： cnki会议评论

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The Chinese-German Journal of Clinical Oncology 2014年第10期13卷 489-493页

作者： Yingying Sun Huaqing Lin Chuqin Yu Suna Lin Department of Guangdong Pharmacy College Guangdong Key Laboratory for New Pharmaceutical Dosage Forms

Nanoparticles drug delivery system has sustained and controlled release features as well as targeted drug delivery, which can change the characteristics of drug distribution in vivo. It can increase the stability of the drug and enhance drug bioavailability. The selective targeting of nanoparticles can be achieved through enhanced permeability and retention effect and a conjugated specific ligand or through the effects of physiological conditions, such as pH and temperature. Nanoparticles can be prepared by using a wide range of materials and can be used to encapsulate chemotherapeutic agents to reduce toxicity, which can be used for imaging, therapy, and diagnosis. In this research, recent progress on nanoparticles as a targeted drug delivery system will be reviewed, including positive-targeting, negative-targeting, and physicochemical-targeting used as anticancer drug carriers.

关键词： nanoparticles anticancer drugs drug carrier

Size,shape,charge and“stealthy”surface:carrier properties affect the drug circulation time in vivo

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Asian Journal of Pharmaceutical Sciences 2021年第4期16卷 444-458页

作者： Jinwei Di Xiang Gao Yimeng Du Hui Zhang Jing Gao Aiping Zheng State Key Laboratory of Toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyBeijing 100850China

The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation *** most drugs,sufficient in vivo circulation time is the basis of high *** carrier plays an irreplaceable role in helping drug avoid being quickly recognized and cleared by mononuclear phagocyte system,to give drug enough time to arrive at targeted organ and tissue to play its therapeutic *** physical and chemical properties of drug carriers,such as size,shape,surface charge and surface modification,would affect their in vivo circulation time,metabolic behavior and *** final circulation time of carriers is determined by the balance between macrophage recognitions,blood vessel penetration and urine ***,when designing the drug delivery system,we should pay much attention to the properties of drug carriers to get enough in vivo circulation time to arrive at target site *** article mainly reviews the effect of carrier size,size,surface charge and surface properties on its circulation time in vivo,and discusses the mechanism of these properties affecting circulation *** review has reference significance for the research of long-circulation drug delivery system.

关键词： drug carrier Circulation time Physical and chemical properties Macrophages Phagocytosis

Dendritic macromolecules as nano-scale drug carriers:Phase solubility,in vitro drug release,hemolysis and cytotoxicity study

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Asian Journal of Pharmaceutical Sciences 2015年第4期10卷 306-313页

作者： Pravinkumar M.Patel Rinkesh Patel Devang Wadia Rajni M.Patel Industrial Chemistry Department V.P.&R.P.T.P.Science CollegeAffiliated to Sardar Patel UniversityVallabh VidhyanagarGujaratIndia Nirlife Healthcare Division Nirma LimitedAhmedabadGujaratIndia P.D.Patel Institute of Pure and Applied Sciences Charusat UniversityChangaGujaratIndia

Potential of nanoscale triazine based dendritic macromolecules G1,G2 and G3 as solubility enhancers of drug was *** of pH,concentration and generation of synthesized dendritic macromolecules on solubility of ketoprofen was studied.G3 dendrimer was further exploited as carrier for sustained *** was encapsulated by inclusion complex method and also characterized by Flourier Transform Infrared *** release study of ketoprofen from ketoprofen loaded dendrimer was carried out and compared with free *** potential and Cytotoxicity assay using A-549 lung cancer cell lines revealed that synthesized triazine based dendritic macromolecules having more potential that commercially available PAMAM dendrimer.

关键词： Triazine based dendrimer Ketoprofen drug carrier Cytotoxicity Hemolysis

Preparation and Characterization of Polymeric Micelles from Poly (D, L-lactide) and Methoxypolyethylene Glycol Block Copolymers as Potential drug carriers

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Tsinghua Science and Technology 2007年第4期12卷 493-496页

作者：张建峥姜维赵秀文王运东 State Key Laboratory of Chemical Engineering Department of Chemical Engineering Tsinghua University

Amphiphilic diblock copolymers composed of methoxy polyethylene glycol （MePEG） and poly（D,L-lactide）（PDLLA） were prepared for the preparation of polymeric micelles, The use of MePEG-PDLLA as drug carriers has been reported in the open literature, but there are only few data on the application of a series of MePEG-PDLLA copolymers with different lengths in the medical field, The shape of the polymeric micelles is also important in drug delivery, Studies on in vitro drug release profiles require a good sink condition. The critical micelle concentration of a series of MePEG-PDLLA has a significant role in drug release. To estimate their feasibility as a drug carrier, polymeric micelles made of MePEG-PDLLA block copolymer were prepared by the oil in water （O/VV） emulsion method. From dynamic light scattering （DLS） measurements, the size of the micelle formed was less than 200 nm, The critical micelle concentration of polymeric micelles with various compositions was determined using pyrene as a fluorescence probe. The critical micelle concentration decreased with increasing number of hydrophobic segments. MePEG-PDLLA micelles have a considerably low critical micelle concentration （0.4～0.5 μg/mL）, which is apparently an advantage in utilizing these micelles as drug carriers. The morphology of the polymeric micelles was observed using scanning electron microscopy （SEM） and transmission electron microscopy （TEM）, The micelles were found to be nearly spherical. The yield of the polymeric micelles obtained from the O/W method is as high as 85%.

关键词： poly(D,L-lactide) methoxy polyethylene glycol polymeric micelle drug carrier