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药剂学
POLYMER TESTING · 2022 · IF 4.931

Preparation and properties of a fast curing carboxymethyl chitosan hydrogel for skin care

Yang-he Mo,Hui Wang,Shao-hua Jin,Ke-lin Peng,Zi-ming Yang,Pu-wang Li,Yu Chen

Fast curing hydrogels are highly valuable in the skin care industry. Multi-arm polyethylene glycol (PEG) is a commonly used crosslinking agent for the preparation of fast curing hydrogels. However, the hydrogel preparation using multi-arm PEG crosslinking agents usually requires the end group modifications of reactants, which makes the preparation process complicated and produces hydrogels with low curing rates. In the present study, a fast in situ curing hydrogel, 4-arm-PEG-succinimidyl carbonate/carboxymethyl chitosan (PEG-SC/CMCS), was prepared using 4-arm-PEG-SC as the crosslinking agent and carboxymethyl chitosan (CMCS), a derivative of natural polysaccharide with excellent comprehensive properties, as the framework without any end groups modified. The structure and properties of the prepared hydrogel were characterized by FTIR, XRD, SEM, rheology and swelling kinetics. The effects of reaction conditions on the structure and properties of hydrogel were investigated. The PEG-SC/CMCS hydrogel exhibited pH-sensitive swelling behaviors. Its application potential in skin care products is demonstrated with its excellent sustained-release performance of Vitamin C, a model drug for skin treatment, and high adsorption capacity of heavy metal ions that are easily deposited on skin surface. Our work has provided a new strategy for building multifunctional gel materials for skin care and offered a PEG-SC/CMCS hydrogel with great application potentials.

研究领域: 生物材料 · 高分子化学 · 药剂学 · 皮肤科学 · 组织工程 · 药物递送系统 · 环境毒理学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2012 · IF 3.35

Temperature- and pH-responsive nanoparticles of biocompatible polyurethanes for doxorubicin delivery

Anning Wang,Hui Gao,Yanfang Sun,Yu-long Sun,Ying-Wei Yang,Guolin Wu,Yinong Wang,Yunge Fan,Jianbiao Ma

A series of temperature- and pH-responsive polyurethanes based on hexamethylene diisocyanate (HDI) and 4,4′-diphenylmethane diisocyanate (MDI) were synthesized by a coupling reaction with bis-1,4-(hydroxyethyl) piperazine (HEP), N -methyldiethanolamine (MDEA) and N -butyldiethanolamine (BDEA), respectively. The chemical structure , molecular weight, thermal property and crystallization properties were characterized by Fourier transform infrared (FT-IR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, gel permeation chromatography (GPC), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) spectroscopy. The resulting polyurethanes were then used to prepare nanoparticles either by direct dispersion method or dialysis method. Their pH and temperature responsibilities were evaluated by optical transmittance and size measurement in aqueous media. Interestingly, HDI-based and MDI-based polyurethanes exhibited different pH and temperature responsive properties. Nanoparticles based on HDI-HEP and HDI-MDEA were temperature-responsive, while MDI-based biomaterials were not. All of them showed pH-sensitive behavior. The possible responsive mechanism was investigated by 1 H NMR spectroscopy. The cytotoxicity of the polyurethanes was evaluated using methylthiazoletetrazolium (MTT) assay in vitro . It was shown that the HDI-based polyurethanes were non-toxic, and could be applied to doxorubicin (DOX) encapsulation. The experimental results indicated that DOX could be efficiently encapsulated into polyurethane nanoparticles and uptaken by Huh-7 cells. The loaded DOX molecules could be released from the drug-loaded polyurethane nanoparticles upon pH and temperature changes, responsively.

研究领域: 生物材料学 · 药剂学 · 肿瘤学 · 高分子科学 · 纳米医学
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JOURNAL OF APPLIED POLYMER SCIENCE · 2019 ·Vol. 136 ·期 36 ·47922 · IF 2.188

Long time release of water soluble drug from hydrophilic nanofibrous material

Nan Pan,Juanrong Qin,Yuwei Fan,Zeke Li,Botao Song

In this study, mesoporous silica nanoparticles (MSNs) were embedded into the hydrophilic poly(vinyl alcohol) (PVA) nanofibrous mats to achieve sustained release of water soluble drug from hydrophilic nanofibrous mats. MSNs were successfully prepared based on a sol–gel method. Water soluble drug naproxen sodium was then loaded into the mesopores of the MSNs, and different amounts of the drug-loaded MSNs were further incorporated into the fibers by the electrospinning process. Morphology of the nanofibrous mats was investigated, and it was found that all the fibers exhibited fibrous structure. Interestingly, lots of protrusions could be observed from the scanning electron microscopy images with high magnification, and numbers of the protrusions increased with the increasing of loading ratios of the MSNs from 5 to 15%. In addition, the wetting behaviors of the nanofibrous mats were also measured, and the water contact angles of all the mats were measured to be 0°. Finally, the drug release results indicated that all the PVA/MSNs composite nanofibrous mats showed an obviously prolonged drug release. The optimal loading ratio of the MSNs in the nanofibers was 10% due to the slowest drug release rate. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136 , 47922.

研究领域: 药剂学 · 生物材料 · 纳米医学 · 药物递送系统 · 高分子科学
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Materials Science & Engineering C-Materials for Biological Applications · 2016 · IF 3.42

Bioactive apatite incorporated alginate microspheres with sustained drug-delivery for bone regeneration application

Haibin Li,Fei Jiang,Song Ye,Yingying Wu,Kaiping Zhu,Deping Wang

The strontium-substituted hydroxyapatite microspheres (SrHA) incorporated alginate composite microspheres (SrHA/Alginate) were prepared via adding SrHA/alginate suspension dropwise into calcium chloride solution, in which the gel beads were formed by means of crosslinking reaction. The structure, morphology and in vitro bioactivity of the composite microspheres were studied by using XRD, SEM and EDS methods. The biological behaviors were characterized and analyzed through inductively coupled plasma optical emission spectroscopy (ICP-OES), CCK-8, confocal laser microscope and ALP activity evaluations. The experimental results indicated that the synthetic SrHA/Alginate showed similar morphology to the well-known alginate microspheres (Alginate) and both of them possessed a great in vitro bioactivity. Compared with the control Alginate, the SrHA/Alginate enhanced MC3T3-E1 cell proliferation and ALP activity by releasing osteoinductive and osteogenic Sr ions. Furthermore, vancomycin was used as a model drug to investigate the drug release behaviors of the SrHA/Alginate, Alginate and SrHA. The results suggested that the SrHA/Alginate had a highest drug-loading efficiency and best controlled drug release properties. Additionally, the SrHA/Alginate was demonstrated to be pH-sensitive as well. The increase of the pH value in phosphate buffer solution (PBS) accelerated the vancomycin release. Accordingly, the multifunctional SrHA/Alginate can be applied in the field of bioactive drug carriers and bone filling materials.

研究领域: 生物材料学 · 骨组织工程 · 药物递送系统 · 生物医学工程 · 再生医学 · 生物无机化学 · 药剂学
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JOURNAL OF MATERIALS CHEMISTRY · 2011 ·Vol. 21 ·期 40 ·16028-16034 · IF 5.101

Biomimetic fabrication of alginate/CaCO3 hybrid beads for dual-responsive drug delivery under compressed CO2

Jun Shi,Zhengzheng Zhang,Gefei Li,Shaokui Cao

Alginate/CaCO3 hybrid beads with pH- and thermal-responsive drug release properties were prepared under compressed CO2 using aliphatic poly(urethane-amine)s (PU) as the thermal-responsive component. Polyacrylic acid (PAA) was used as a crystal growth additive to control the structure of the hybrid beads. The hybrid beads were characterized by using scanning electron microscopy, X-ray powder diffraction and thermogravimetric analysis. The interaction between PAA and aliphatic PU contributed to the formation of alginate beads with a compact CaCO3 shell. Indomethacin release behaviour was found to be pH- and thermal-responsive. The release profiles were sustained with CaCO3 microparticles, indicating that the compact CaCO3 shell could hinder the permeability of the encapsulated drug and reduce the drug release effectively. The results suggest that the hybrid alginate beads can be used as “smart” polysaccharide materials for sustained dual-responsive drug delivery.

研究领域: 生物材料 · 药物递送系统 · 高分子科学 · 纳米医学 · 药剂学 · 生物化学 · 组织工程
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MATERIALS LETTERS · 2013 · IF 2.224

Synthesis of fibrous monodisperse core–shell Fe3O4/SiO2/KCC-1

Kejie Yu,Xuebin Zhang,Hongwu Tong,Xiangyan Yan,Shaomin Liu

Fibrous monodisperse core–shell structured Fe 3 O 4 /SiO 2 /KCC-1 nanoparticles were synthesised successfully through a surfactant-templated microemulsion formation process. The structure and morphology of the synthesised nanoparticles were investigated by scanning electron microscopy , transmission electron microscopy , superconducting quantum interference device susceptometer, X-ray diffraction, thermogravimetric analysis and N 2 adsorption/desorption. These nanoparticles showed monodisperse spherical morphology, high magnetism , good thermal stability , large surface area , direct channels, easily accessible large pores and narrow size distribution. A mechanism for the synthesis of these nanoparticles was proposed and explained. Adsorption experiments indicated that the as-prepared materials had good adsorption capacity for dye and could perform a fast transfer of molecules, indicating its promising application in purification of industrial wastewater, drug delivery and so on.

研究领域: 纳米医学 · 材料科学 · 环境工程 · 生物材料 · 药剂学 · 胶体与界面化学
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RSC Advances · 2016 ·Vol. 6 ·期 112 ·111217-111225 · IF 3.289

pH-sensitive drug release of star-shaped micelles with OEG brush corona

Sijie Zhao,Huiru Yang,Cai Zuo,Lu Sun,Liwei Ma,Hua Wei

Star-shaped polymers are attractive as drug carriers due to the integration of relatively easy synthesis compared to the preparation of hyper-branched dendrimers and their potential ability to form unimolecular nanoparticles with enhanced stability to survive the high dilution-associated deformation and subsequently premature drug release in the body fluids and blood during circulation. Clearly, the star structure exerts a significant effect on their bioproperties and potential applications. In this study, three star-shaped amphiphilic copolymers with the same polymer compositions but different star structures were synthesized to investigate the effect of star architecture on their properties as well as potential applications as drug carriers. Three different branched alcohols, 2-(hydroxymethyl) propane-1,3-diol, pentaerythritol and dipentaerythritol with 3, 4, and 6 respective hydroxyl groups were chosen as the starting core to generate the target star-shaped amphiphilic block copolymers composed of hydrophobic poly(ε-caprolactone) (PCL) and hydrophilic poly(oligoethyleneglycol methacrylate) (POEGMA) with 3, 4, and 6 corresponding star arms by a combination of ring-opening polymerization (ROP) and atom transfer radical polymerization (ATRP). Dynamic light scattering (DLS) measurements and pyrene fluorescence probe technique confirmed the capability of the resultant star-shaped amphiphilic copolymers to form unimolecular micelles with average diameters smaller than 50 nm in an aqueous phase. A comparison of the drug loading capacity revealed that the micelles of 4-star-PCL–POEGMA (4s-PCL–POEGMA) exhibited the highest drug loading content (DLC) of all the three formulations. More importantly, in vitro doxorubicin (DOX) release study showed unique pH-mediated drug release behaviors, i.e., dramatically accelerated release at pH 6.0 but a much slower profile at pH 7.4, from these generally recognized “pH-insensitive” 4-arm star-shaped micelles. An acid-triggered degradation and an acid–base titration were performed to further reveal that such interesting pH-responsive drug release behaviors were attributed primarily to the hydrophilic corona of OEG brushes. This study is believed to provide a new insight into the structure–bioproperties relationship of star-shaped polymers, thus should be useful for the future design and development of novel star-shaped polymers for controlled drug delivery.

研究领域: 高分子药剂学 · 纳米医学 · 药物控释 · 生物材料 · 药剂学 · 肿瘤治疗 · 纳米载体
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MONATSHEFTE FUR CHEMIE · 2014 ·Vol. 146 ·期 3 ·441-447 · IF 1.347

Preparation and characterization of 5-fluorouracil surface-imprinted thermosensitive magnetic microspheres

Li Longfei,Chen Lin,Liu Weifeng,Yang Yongzhen,Liu Xuguang,Chen Yongkang

5-Fluorouracil surface-imprinted thermosensitive magnetic microspheres were prepared by using Fe 3 O 4 -encapsulating carbon microspheres as cores, N -isopropylacrylamide as thermosentitive monomer, ammonium persulfate as initiator, N , N ′-methylenebisacrylamide as crosslinker, and 5-fluorouracil as template molecule. The formation of these hybrid microspheres was verified by field emission scanning electron microscopy, transmission electron microscopy, Fourier transformation infrared spectroscopy, thermogravimetry, and dynamic light scattering. The results of the latter measurements show that the as-synthesized microspheres have a hydrodynamic diameter of 326 nm with the lower critical solution temperature of around 43 °C. The obtained microspheres are magnetic and show good potential for controlled loading and release of 5-fluorouracil. Graphical abstract

研究领域: 药剂学 · 纳米医学 · 肿瘤治疗 · 高分子材料科学 · 靶向给药系统
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PHYSICA STATUS SOLIDI A-APPLICATIONS AND MATERIALS SCIENCE · 2020 ·Vol. 217 ·期 6 ·1900536 · IF 1.759

Synthesis of Nanobentonite–Poly(vinyl alcohol)–Bacterial Cellulose Nanocomposite by Electrospinning for Wound Healing Applications

Parisa Zeaiean Firouzabadi,Hajar Ghanbari,Nafiseh Mahmoudi,Seyed Mohammad Amin Haramshahi,Jafar Javadpour

Polymer-based composites are used for wound healing applications. This work aims to prepare an inorganic-polymer nanocomposite based on bentonite, poly(vinyl alcohol), and bacterial cellulose by electrospinning for wound healing. The nanocomposite is synthesized using a solution intercalation technique, with 1–2 wt% nanobentonite concentration variation. The effects of commercial and laboratory-synthesized nanobentonite as well as the extract of the green walnut shell (EGWS) are examined and characterized by different techniques. The addition of nanobentonite increases the average size of fibers and tensile strength up to 200 nm and more than 15 MPa, respectively, due to the presence of hydrogen bonding formed between the nanobentonite sheets and polymer matrix. By the addition of synthetic nanoclay and EGWS, moderate elongation and strength are achieved. The hydrophilicity shows a decreasing trend up to 2 wt% of commercial nanobentonite; however, the laboratory-synthesized nanobentonite is not significantly effective. Effects of extracts on the viability of cultured human adipose tissue–derived mesenchymal stem cells (ADSCs) are quantitated, where the samples containing 1–2 wt% of commercial nanobentonite have less toxicity than others. Antibacterial activity is tested against both Escherichia coli and Staphylococcus aureus bacteria according to the agar diffusion test for 72 h, in which EGWS-based mats exhibit strong antimicrobial activity.

研究领域: 生物材料学 · 组织工程 · 纳米医学 · 再生医学 · 药剂学 · 微生物学 · 高分子科学
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JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE · 2017 ·Vol. 28 ·期 5 ·67 · IF 2.325

Self-assembled polyelectrolyte complexes films as efficient compression coating layers for controlled-releasing tablets

Li Wenyan,Huo Mengmeng,Sen Chaudhuri Arka,Yang Chen,Cao Dazhong,Wu Zhenghong,Qi Xiaole

Currently, polysaccharide-based hydrogels are widely studied macromolecular networks to modify drug dissolution from controlled-releasing matrix tablets. Among them, polyelectrolyte complexes (PEC) films consisted of chitosan (CS) and sodium alginate (SA) could be obtained via spontaneously assembling under physiological gastrointestinal environment. Here, we utilized these self-assembled PEC films as an efficient coating materials to develop controlled-released matrix tablets through compression coating process, with paracetamol (APAP) as model drug. The constitutive and morphology characteristic studies on these PEC films illustrated that the mixture of CS and SA with the weight ratio of 1:1 would be an promising outer layer for compression-coating tablets. In addition, the in vitro drug releasing behavior experiments demonstrated that the optimized compression coating tablets displayed satisfied zero-order drug releasing profits. Furthermore, the in vivo pharmacokinetic studies of these APAP loaded compression-coated tablets in New Zealand rabbits gave that the T max (12.32 ± 1.05 h) was significantly prolonged ( p  < 0.01), compared to that (0.89 ± 0.26 h) of common APAP tablets (Jinfuning ® ) after oral administration. These studies suggest that the compression-coated tablets with self-assembled PEC film as coating outer layer may be a promising strategy for peroral controlled release delivery system of water soluble drugs. Graphical

研究领域: 药剂学 · 生物材料 · 药物递送系统 · 药代动力学 · 胃肠药理学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2020 · IF 4.845

Multifunctional composite nanoparticles based on hyaluronic acid-paclitaxel conjugates for enhanced cancer therapy

Kaipei Luo,Shaoping Yin,Ruixia Zhang,Hua Yu,Guangji Wang,Juan Li

The efficient delivery of chemotherapeutic drugs to the tumor tissues unavoidably encounters numerous obstacles, such as poor tumor targeting capability, slow intracellular drug release and massive accumulation in the liver. In this study, by self-assembling methoxy poly (ethylene glycol)-poly (lactide) block copolymer (mPEG-PLA) and hyaluronic acid-paclitaxel conjugate (HA-PTX), the composite nanoparticles (mPPHP NPs) were fabricated for efficient therapy of cancer. mPPHP NPs formed self-assembled nanoparticles (116 nm in diameter) with a narrow size distribution; and showed a rapid release of PTX in the presence of hyaluronidase and esterase . mPPHP NPs exhibited enhanced internalization by cells via CD44 receptors and selected cytotoxicity against A549 cells in vitro . More importantly, compared with other PTX formulations, mPPHP NPs were demonstrated to present the reduced liver accumulation, excellent tumor-targeting ability and superior antitumor efficacy in vivo , with a TIR of 75.9%. The multifunctional composite nanoparticles could be developed as a promising nano-carrier for improved therapeutic efficacy.

研究领域: 肿瘤学 · 纳米医学 · 药剂学 · 分子靶向治疗 · 药物递送系统 · 转化医学
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2017 · IF 3.756

Phenazopyridine-phthalimide nano-cocrystal: Release rate and oral bioavailability enhancement

Yu Huang,Jin-Mei Li,Zhi-Hui Lai,Jun Wu,Tong-Bu Lu,Jia-Mei Chen

Both cocrystal and nanocrystal technologies have been widely used in the pharmaceutical development for poorly soluble drugs. However, the synergistic effects due to the integration of these two technologies have not been well investigated. The aim of this study is to develop a nano-sized cocrystal of phenazopyridine (PAP) with phthalimide (PI) to enhance the release rate and oral bioavailability of PAP. A PAP–PI nano-cocrystal with particle diameter of 21.4   ±   0.1   nm was successfully prepared via a sonochemical approach and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and dynamic light scattering (DLS) analysis. An in vitro release study revealed a significant release rate enhancement for PAP–PI nano-cocrystal as compared to PAP–PI cocrystal and PAP hydrochloride salt. Further, a comparative oral bioavailability study in rats indicated significant improvement in C max and oral bioavailability (AUC 0   −   ∞ ) by 1.39- and 2.44-fold, respectively. This study demonstrated that this novel nano-cocrystal technology can be a new promising option to improve release rate and absorption of poorly soluble compounds in the pharmaceutical industry.

研究领域: 药剂学 · 药物递送 · 纳米医学 · 药物代谢 · 晶体工程
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