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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2015 · IF 2.101

Preparation and in vitro characterization of pluronic-attached polyamidoamine dendrimers for drug delivery

Zhuojun Gu,Meng Wang,Qiongyan Fang,Huaiyu Zheng,Feiyue Wu,Dai Lin,Ying Xu,Yi Jin

Context: Polyamidoamine (PAMAM) dendrimers have attracted lots of interest as drug carriers. And little study about whether pluronic-attached PAMAM dendrimers could be potential drug delivery systems has been carried on.Objective: Pluronic F127 (PF127) attached PAMAM dendrimers were designed as novel drug carriers.Methods: Two conjugation ratios of PF127-attached PAMAM dendrimers were synthesized. 1H nuclear magnetic resonance (1H-NMR), Fourier transform infrared spectrum (FTIR), element analysis and ninhydrin assay were used to characterize the conjugates. Size, zeta potential and critical micelle concentrations (CMC) were also detected. And DOX was incorporated into the hydrophobic interior of the conjugates. Studies on their drug loading and drug release were carried on. Furthermore, hemolysis and cytotoxicity assay were used to evaluate the toxicity of the conjugates.Results and discussion: PF127 was successfully conjugated to the fifth generation PAMAM dendrimer at two molar ratios of 19% and 57% (PF127 to surface amine per PAMAM dendrimer molecular). The conjugates showed an increased size and a reduced zeta potential. And higher CMC values were obtained than pure PF127. Compared with unconjugated PAMAM dendrimer, PF127 conjugation significantly reduced the hemolytic toxicity and cytotoxicity of PAMAM dendrimer in vitro. The encapsulation results showed that the ability to encapsulate DOX by the conjugate of 19% conjugation ratio was better than that of 57% conjugation ratio. And the maximum is ∼12.87 DOX molecules per conjugate molecule. Moreover, the complexes showed a sustained release behavior compared to pure DOX.Conclusion: Findings from the in vitro study show that the PF127-attached PAMAM dendrimers may be potential carriers for drug delivery.

CAS / MDL: 7789-20-0
研究领域: 药学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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POLYMER COMPOSITES · 2013 ·Vol. 35 ·期 4 ·627-635 · IF 1.482

Effect of dendrimer-like PAMAM grafted attapulgite on the microstructure and morphology of Nylon-6

Lei Xia,Baoqing Shentu,Zhixue Weng

The effect of dendrimer-like polyamidoamine grafted attapulgite (ATP-PAMAM) on the microstructure and morphology of Nylon-6 (PA6) was investigated. The ATP-PAMAM nanoparticles were prepared by treating attapulgite (ATP) with heat and acid followed by grafting with polyamidoamine (PAMAM) molecules, which was confirmed by Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), and dispersion state in formic acid. The X-ray diffraction (XRD) analysis result indicated that the grafting modification was occurred on the surface of fibrous crystals and did not shift the crystal structure of ATP. PA6/ATP-PAMAM (G 2.0 ) nanocomposites with different modified ATP content were prepared by melt compounding in a twin screw extruder. XRD measurements suggested that the intensity of diffraction peak of α crystalline form of PA6 decreased gradually as the inclusion of ATP-PAMAM(G 2.0 ) into the PA6 matrix, while that of γ crystalline form increased gradually. The results of molau experiment and scanning electron microscopy (SEM) observation showed not only a uniform dispersion of ATP-PAMAM(G 2.0 ) in the PA6 matrix but also a strong interfacial adhesion between them. Mechanical investigation (by tensile test) showed an obvious improvement in the presence of surface modified ATP. POLYM. COMPOS., 35:627–635, 2014. © 2013 Society of Plastics Engineers

CAS / MDL: 919-30-2
研究领域: 材料科学 · 高分子化学
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2015 · IF 3.35

Dendrimeric anticancer prodrugs for targeted delivery of ursolic acid to folate receptor-expressing cancer cells: Synthesis and biological evaluation

Yu Gao,Zhihong Li,Xiaodong Xie,Chaoqun Wang,Jiali You,Fan Mo,Biyu Jin,Jianzhong Chen,Jingwei Shao,Haijun Chen,Lee Jia

The anticancer efficacy of ursolic acid (UA) was limited by poor water solubility, non-specific tumor distribution, and low bioavailability. To overcome this problem, polyamidoamine (PAMAM) conjugated with UA and folic acid (FA) as novel dendrimeric prodrugs were designed and successfully synthesized by a concise one-pot synthetic approach. Both FA and UA were covalently conjugated to the surface of PAMAM through acid-labile ester bonds and the covalently linked UA could be hydrolysed either in acidic (pH 5.4) or in neutral (pH 7.4) PBS solution. The cellular uptake study indicated that the presence of FA enhanced uptake of the dendrimeric prodrugs in folate receptor (FR) over-expressing Hela cells. The enhanced cellular uptake could be due to the electrostatic absorptive endocytosis and FR-mediated endocytosis. In contrast, for HepG2 cells, a FR-negative cell line, FA conjugation on the surface of the dendrimer showed no effect on the cellular uptake. In MTT assay and cell cycle analysis, FA-modified dendrimeric prodrugs showed significantly enhanced toxicity than non-FA-modified ones in Hela cells. These results suggested that FA-modified dendrimeric UA prodrugs have the potential for targeted delivery of UA into cancer cells to improve its anti-tumor efficacy.

CAS / MDL: 69-93-2
研究领域: 药理学 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MICROCHEMICAL JOURNAL · 2021 · IF 4.821

Poly amidoamine functionalized poly (styrene-divinylbenzene-glycidylmethacrylate) composites for the rapid enrichment and determination of N-phosphoryl peptides

Dandan Guo,Shuxin Yu,Nadeem Muhammad,Shaohua Huang,Yan Zhu

In this work, poly amidoamine grafted composites were proposed as enrichment adsorption materials. The composites were synthesized by grafting poly amidoamine dendrimers onto the surface of poly (styrene–divinylbenzene-glycidylmethacrylate) beads. The number of surface functional groups and adsorption capacities of the composites were controllable by varying the generations of poly amidoamine dendrimers. Afterward, adsorption parameters and desorption eluents were optimized by using N-phosphoryl dipeptide as a target molecular. Under the optimized condition, N-phosphoryl dipeptides in aqueous could be rapidly adsorbed within 30 s, and comparatively high selectivity, enrichment efficiency and recovery efficiency were obtained at pH 3 to 7. The used adsorbents show good reproducibility after being washed by methanol solvent. Reliability of the adsorbents was demonstrated by the determination of N-phosphoryl dipeptide in drinking water samples with the efficient dispersive solid phase extraction-high performance liquid chromatography method. According to the obtained result, the adsorbent showed satisfactory repeatability (RSD ≤ 5.51) and good recoveries (90.52–102.84%).

研究领域: 分析化学 · 生物化学
✓ 已验证 DOI 高影响因子
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Polymer Chemistry · 2013 ·Vol. 4 ·期 6 ·2164-2167 · IF 5.231

Poly(amidoamine) modified graphene oxide as an efficient adsorbent for heavy metal ions

Yang Yuan,Guanghui Zhang,Yang Li,Guoliang Zhang,Fengbao Zhang,Xiaobin Fan

Poly(amidoamine) modified graphene oxide was prepared via a grafting-from method and characterized by Fourier transform infrared spectroscopy (FT-IR), X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM) and atomic force microscopy (AFM). Evaluation of its adsorption capacity for heavy metal ions demonstrated that the poly(amidoamine) modified graphene oxide had superior adsorption ability towards heavy metal ions such as Cu2+, Zn2+, Fe3+, Pb2+ and Cr3+.

CAS / MDL: 107-15-3 96-33-3
研究领域: 材料科学 · 环境科学
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JOURNAL OF PHYSICAL CHEMISTRY B · 2014 · IF 3.377

Poly(amidoamine) and Poly(propyleneimine) Dendrimers Show Distinct Binding Behaviors with Sodium Dodecyl Sulfate: Insights from SAXS and NMR Analysis

Tianfu Li,Naimin Shao,Yuntao Liu,Jingjing Hu,Yu Wang,Li Zhang,Hongli Wang,Dongfeng Chen,Yiyun Cheng

We investigate the interactions of generation 3 (G3) poly(amidoamine) (PAMAM) and G3 poly(propylenimine) (PPI) dendrimers with sodium dodecyl sulfate (SDS) in aqueous solution. Size and structure of the dendrimer–SDS aggregates as a function of SDS/dendrimer molar ratio were revealed by SAXS and NMR. G3 PAMAM has a relatively open and dense-core structure, while G3 PPI with the same number of surface amine groups possesses a compact and uniform structure. Upon addition of SDS, much more SDS monomers were encapsulated in the interior of PPI rather than in PAMAM. More significant size increase in PAMAM–SDS aggregate is observed at low SDS concentrations, due to the binding of SDS on PAMAM surface and further assembly into larger supramolecular structures. Both noncooperative and cooperative binding of SDS on G3 PPI surface are observed, while only noncooperative binding is proposed on G3 PAMAM, due to its open surface and large surface group distance. The size of the PPI–SDS complex is larger than that of PAMAM–SDS at higher SDS concentrations. Within the investigated SDS concentrations, SDS exhibits much stronger interactions with G3 PPI than with G3 PAMAM. These results provide new insights into dendrimer–surfactant interactions and explain why PPI is much more cytotoxic than PAMAM.

CAS / MDL: 151-21-3
研究领域: 生物化学 · 材料科学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2019 · IF 5.399

A polyamidoamine-mediated competitive colorimetric assay based on gold nanoparticles for determining acid values in edible sunflower seed, corn and extra virgin olive oils

Yujun Guo,Xiao Liang,Junmin Bi,Rui Ling,Yuhao Jiang,Zhoufan Mou,Feng Huang,Weidong Qin

We synthesized polyamidoamine (PAMAM) dendrimers and citrate-capped gold nanoparticles (AuNPs), and explored the applicability of the PAMAM/AuNP assay in determining total free fatty acid (FFA) contents in edible oils based on a competitive colorimetry, in which the PAMAM-triggered AuNP aggregation was suppressed by FFAs. The generation and concentration of PAMAMs, the chain lengths of FFAs as well as the concentration and pH of the background electrolytes of the assay were optimized. The average acid values of the sunflower seed, corn and extra virgin olive oils determined by PAMAM/AuNP assay were 1.31 ± 0.07, 0.33 ± 0.02 and 1.49 ± 0.07, respectively, which were not significantly different from the corresponding 1.27 ± 0.08, 0.32 ± 0.01 and 1.61 ± 0.06 by the standard nonaqueous titration. Our results suggest that the method is promising in detecting FFAs in edible oils, and implementation of the method expands the technological scope for FFA analysis.

研究领域: 食品科学 · 分析化学
✓ 已验证 DOI 高影响因子
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DRUG DELIVERY · 2014 · IF 2.202

Development of biodegradable polymeric implants of RGD-modified PEG-PAMAM-DOX conjugates for long-term intratumoral release

Ke Wang,Xiaofeng Zhang,Lihong Zhang,Lili Qian,Chang Liu,Jiajun Zheng,Yanyan Jiang

Context: The sustained release implants can be directly implanted in tumor site by surgery and are promising for cancer treatment.Objective: RGD-modified PEGylated polyamidoamine (PAMAM) dendrimer with doxorubicin (DOX) conjugated by acid-sensitive linkage (RGD-PPCD) was a potential conjugate for tumor-targeted therapy. In order to enhance tumor retention ability and long-term effect of drug, we developed the DOX and its conjugate implants using poly(dl-lactic-co-glycolic acid) (PLGA), poly(dl-lactic acid) (PLA) and polyethylene glycol (PEG) as carrier materials.Methods: The implants were prepared by a simple solvent evaporation method. Different formulations with varying ratios of three polymers were designed, prepared and evaluated on the basis of viscosity, in vitro release and drying time. Furthermore, in vivo biodistribution and antitumor activity of the implants were studied in mice with subcutaneous C6 xenografts.Results: The optimized formulation was obtained with the 3:1 ratio of PLGA/PLA (w/w) and 1% PEG (wt.%). The drug release behavior of DOX, PPCD and RGD-PPCD implants prepared by the optimized formulation was similar according to the assessment of similarity factor f2, and the release curves were fell into three phases, including a lag-period, then the second phase which was consistent with zero-order model followed by a plateau. Data of total DOX remained in implants indicated the release were faster in vivo than in vitro. Moreover, intratumoral drug amount of RGD-PPCD implants was the highest 45 days after implantation. Correspondingly, the RGD-PPCD implants exhibited the strongest antitumor activity compared with PPCD and free DOX implants.Discussion and conclusion: This paper presents an exploratory research on macromolecule-drug conjugates, including RGD-PPCD and PPCD, which have the potential to be developed into long-term effect implants for tumor therapy with high efficiency and low systematic toxicity.

研究领域: 肿瘤学 · 药剂学
✓ 已验证 DOI 高影响因子
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Silicon · 2017 ·Vol. 10 ·期 2 ·483-493 · IF 0.829

Preparation and Characterization of a Cyclophosphamide-Core PAMAM Dendritic Montmorillonite

Wen Zhao,Jincheng Wang

Polyamidoamine modified organo-montmorillonites (OMMT) bearing flame-retardant elements were prepared through montmorillonite (MMT) and polyamidoamines with different generations. These materials turned out to be a possible use for the flame-retardency of polymers. Different generations of dendrimers, G1.0, G2.0, and G3.0, were synthesized from a cyclotriphosphazene core. Characteristics of these dendrimers were studied by Fourier transform infrared (FTIR) spectroscopy, hydrogen nuclear magnetic resonance ( 1 H-NMR), ultraviolet (UV-Vis) spectroscopy, and intrinsic viscosity (IV). It was demonstrated that different generations of dendrimers had been well synthesized. These dendrimers were used as an organic intercalation agent to modify natural clay, Na + -MMT. Different generations of flame-retardant dendrimer modified OMMT, G1.0-OMMT, G2.0-OMMT, and G3.0-OMMT, were prepared. The interlayer spacing, thermal stability, and surface morphology of these dendritic MMTs were investigated by FTIR, thermogravimetric analysis (TGA), X-ray diffraction (XRD), and scanning electron microscopy (SEM) as well as energy dispersing spectrometry (EDS). It was seen that the thermal stability of G1.0-OMMT, G2.0-OMMT, and G3.0-OMMT was obviously improved with the increase of generations compared with that of MMT. In addition, an exfoliated structure existed in these dendrimer modified silicate layers.

研究领域: 材料科学 · 化学工程
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CHINESE JOURNAL OF POLYMER SCIENCE · 2021 ·Vol. 39 ·期 10 ·1319-1327 · IF 3.603

Strong, Removable, and Photoluminescent Hyperbranched Polyamide-amine Hot Melt Adhesive

Zhang Si-Jia,Chen Xing-Xing,Cui Chen-Hui,Ma Li,Zhong Qian-Yun,Shen Kai-Xiang,Yu Jing,Li Zhen,Wu You-Shen,Zhang Qiang,Cheng Yi-Long,He Ling,Zhang Yan-Feng

The development of adhesive technology is gaining increasing attention in machinery, electronics, aviation, and other fields. However, traditional adhesives are difficult to be peeled and removed after cross-linking and curing due to the limited solubility in common solvents, which causes pollution and damage to the surface of the adherend. In this work, we synthesized random hyperbranched polyamide-amine hot melt adhesives through Michael addition of 1,8-octanediamine and N,N ’-methylene diacrylamide (ODA-RHP HMA). Owing to the presence of various polar groups, ODA-RHP HMA exhibited robust lap shear strength to different substrates, including glass (6.6 MPa), ceramics (10.3 MPa), steel (11.5 MPa), and aluminum (11.8 MPa). Due to the hydrogen bonds in ODA-RHP, the HMA demonstrated intrinsic self-healing ability, which can be used repeatedly when being subjected to cyclic heating and cooling. Since ODA-RHP HMA can be swollen or dissolved in ethanol, the adhesives can be easily removed through erasing. In addition, ODA-RHP exhibited aggregation-induced luminescence due to the tertiary amine structure in the molecular structure of ODA-RHP, which can be used in the field of cultural relics restoration.

研究领域: 材料科学 · 化学工程 · 文物保护
✓ 已验证 DOI 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2013 · IF 3.554

Reduction-degradable PEG-b–PAA-b–PEG triblock copolymer micelles incorporated with MTX for cancer chemotherapy

Yong Sun,Yihang Huang,Shaoquan Bian,Jie Liang,Yujiang Fan,Xingdong Zhang

Reduction-breakable core–shell type polymeric micelles from reduction-degradable amphiphilic polyethylene glycol- b –polyamide amine- b –polyethylene glycol triblock copolymers (PEG- b –PAA- b –PEG) were prepared as new drug carriers of methotrexate (MTX) for cancer chemotherapy. The PEG- b –PAA- b –PEG copolymers were synthesized in a simple one-step process under mild condition through Michael addition. Spherical micelles with diameters ranging from 65 to 123   nm were successfully fabricated from the copolymers. These micelles could effectively encapsulate the anti-cancer drug MTX in the core with drug loading content around 13%. The incorporation of MTX resulted in a little size increase but did not influence the morphology of micelles. The drug was hardly released from the micelles in normal condition without DDT as the reductant, but fast released up to 100% within 24   h when the structure of micelle core was broken in the presence of DTT, thus provided a potential tool for tumor targeting delivery of MTX using the higher concentration of reductant in tumor tissues. The proliferation inhibition experiments demonstrate that MTX-encapsulated micelles show significant cytotoxicity to KB, HepG2 and 4T1 tumor cells, especiallythe 4T1 cells.

CAS / MDL: 133073-73-1
研究领域: 药剂学 · 肿瘤学 · 生物材料学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2012 · IF 2.236

Thermosensitivity of low generation poly(amidoamine) dendrimers with enriching peripheral functional groups

Yanjun Zhao,Li Shen,Ying Wan,Xiaoxia Zhu,Zheng Wang

Low generation poly(amidoamine) (PAMAM) dendrimers are less cytotoxic, but it is generally difficult to render them with thermosensitive properties due to the lack of surface terminal groups. Hydroxymethyl aminomethane was employed to modify PAMAM so as to increase the density of hydroxyl groups on PAMAM surface. Two types of thermosensitive units with different hydrophobicity were covalently linked to the hydroxyl groups of PAMAM surface to obtain thermosensitive PAMAM derivatives. The thermosensitivity of the surface-modified PAMAM can be precisely controlled by manipulating the hydrophobicity of the dendrimer periphery and regulating the ionization of the dendrimer interior.

CAS / MDL: 24650-42-8 107-06-2
研究领域: 生物化学 · 纳米医学 · 药物递送
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