COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2016
·
IF 2.76
Shanshan Zhang,Xuerui Chen,Shiping Ding,Qunfang Lei,Wenjun Fang
The interactions of human serum albumin (HSA) with four cationic gemini surfactants and four single-chain surfactants have been investigated from the measurements of fluorescence spectroscopy, dynamic lights scattering (DLS), zeta potential, and circular dichroism (CD). The fluorescence results show the binding strength of surfactants to HSA, along with the blue shift under the maximum emission wavelength ( λ max ) which is sensitive to the protein conformations. It has been found that the hydrodynamic diameters of the protein aggregates are enlarged and the electrokinetic potentials of them get positive with increasing the concentration of the surfactants. The conformational transformation of the secondary structures of surfactant–HSA aggregates has been confirmed through the quantitative analysis of the CD spectra. The isothermal titration microcalorimetry (ITC) has been employed to further analyze the binding process of single-chain surfactants to HSA. The comprehensive results obtained from various approaches have shown that both hydrophobic and electrostatic interactions are present in the cationic surfactant–HSA systems. Compared with the corresponding single-chain surfactants, the gemini ones have much stronger binding ability to induce the unfolding of HSA. These investigations on the interactions between HSA and surfactants with the altered chain architecture in different concentration regimes can facilitate the application of surfactant-protein systems in pharmaceutical, biotechnology and related fields.
研究领域:
生物物理化学
·
分子生物学
·
药剂学
·
蛋白质科学
·
药物代谢
·
胶体与界面科学
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DOI
高影响因子
JOURNAL OF FOOD BIOCHEMISTRY
·
2021
·Vol. 46
·期 1
·e14007
·
IF 2.72
Jing Liu,Zhongan Zhu,Yuhang Yang,Michael Adu-Frimpong,Lin Chen,Hao Ji,Elmurat Toreniyazov,Qilong Wang,Jiangnan Yu,Ximing Xu
A liposome of Licochalcone A (LCA-Liposomes) was purposively prepared to ameliorate the low in vivo availability and efficacy of LCA. Physical characterization of LCA-Liposomes was carried out mainly by determining particle size, morphology, zeta potential (Z-potential), and efficiency of LCA encapsulation (EE) via appropriate techniques. Also, the rate of LCA release in vitro and distribution in vivo (plasma and tissues) was evaluated. Evaluation of the antirenal activity of LCA-liposomes was carried out by establishing chronic renal failure (CRF) model in mice through intragastric administration of adenine (200 mg/kg) and subsequent determination of biochemical parameters and examination of tissue sections. Respectively, the mean size of liposomal particles, Z-potential and EE of LCA-Liposomes were 71.78 ± 0.99 nm, −38.49 ± 0.06 mV, and 97.67 ± 1.72%. Pharmacokinetic and tissue distribution studies showed that LCA-Liposomes could improve the availability of LCA in the blood and tissues, whereas during pharmacodynamics studies, the liposome effectively improved the therapeutic effect of LCA on CRF mice by potentially protecting the renal tissues while exhibiting antioxidant activity. In conclusion, LCA-Liposomes could effectively improve the bioavailability of LCA and provide platform for the development of LCA-related functional products. Practical applications As a traditional Chinese medicine, licorice is widely used in food and pharmaceutical industries. LCA is a small molecule flavonoid extracted from the root of licorice. In this study, LCA was loaded on liposome carriers, which significantly improved the water solubility and oral bioavailability, and proved that LCA-Liposomes have certain therapeutic effects on chronic renal failure, thereby providing a basis for the development of LCA into drugs or functional food in the future.
研究领域:
药剂学
·
药理学
·
分子药理学
·
药物代谢
·
纳米医学
·
中药药理学
✓ 已验证
DOI
高影响因子
MACROMOLECULAR MATERIALS AND ENGINEERING
·
2018
·Vol. 303
·期 9
·1800060
·
IF 2.69
Titao Jing,Tuanwei Li,Zheng Ruan,Quan Cheng,Lifeng Yan
A negatively charged polypeptide nanogel, near-infrared (NIR) cyanine dye (Cy5.5) conjugated and 2,3-dimethylmaleic anhydride (DMA) modified poly- l -lysine-co- l -cystine (CDPLC), is synthesized and is used as an imaging-guided sequential drug delivery system. The CDPLC nanogel can respond to two general stimulations in sequence: extracellular tumor acidic microenvironment pHe (6.8–6.5) and intracellular high concentration glutathione (GSH). Under pHe, the DMA shell of the nanogel is removed and a charge reversal takes place, resulting in positively charged nanogel which can be internalized by cancer cells easily. Once internalized into tumor cells, the increased intracellular GSH concentration further promotes DOX release from the nanogel and DOX is enriched to the nucleus. Cy5.5 is conjugated to the nanogel as an NIR fluorescent probe, making it possible for imaging-guided drug delivery, which is confirmed by the MTT and confocal laser scanning microscopy via in vitro experiments. The as-prepared nanogel is a potential theranostic for cancer therapy.
研究领域:
肿瘤学
·
药剂学
·
分子影像学
·
生物材料
·
纳米医学
·
药物递送系统
✓ 已验证
DOI
高影响因子
Evidence-based Complementary and Alternative Medicine
·
2015
·Vol. 2015
·期 1
·239749
·
IF 1.88
Zhiping Wang,Junbiao Wu,Qun Zhou,Yifei Wang,Tongsheng Chen
Berberine (Ber), an isoquinoline derivative alkaloid and active ingredient of Coptis, has been demonstrated to possess antidiabetic activities. However its low oral bioavailability restricts its clinical application. In this report, Ber nanosuspension (Ber-NS) composed of Ber and D- α -tocopheryl polyethylene glycol 1000 succinate (TPGS) was prepared by high pressure homogenization technique. Antidiabetic effects of Ber-NS relative to efficacy of bulk Ber were evaluated in streptozotocin (STZ) induced diabetic C57BL/6 mice. The particle size and zeta potential of Ber-NS were 73.1 ± 3.7 nm and 6.99 ± 0.17 mV, respectively. Ber-NS (50 mg/kg) treatment via oral gavage for 8 weeks resulted in a superior hypoglycemic and total cholesterol (TC) and body weight reduction effects compared to an equivalent dose of bulk Ber and metformin (Met, 300 mg/kg). These data indicate that a low dosage Ber-NS decreases blood glucose and improves lipid metabolism in type 2 diabetic C57BL/6 mice. These results suggest that the delivery of Ber as a nanosuspension is a promising approach for treating type 2 diabetes.
研究领域:
药剂学
·
药理学
·
分子药理学
·
药物递送系统
·
糖尿病研究
·
药物代谢
·
纳米医学
✓ 已验证
DOI
高影响因子
CARBOHYDRATE POLYMERS
·
2018
·
IF 5.158
Lei Du,Amin GhavamiNejad,Zhi-Chao Yan,Chandra Sekhar Biswas,Florian J. Stadler
Here, we report on the effect of functional copolymer poly(N-isopropylacrylamide-co-4-vinyl-phenylboronic acid) (NIBA) on the rheology and network structure formed by sodium alginate (SA) through linear and nonlinear viscoelasticity measurements. The hydrogel moduli at pH 3 increased with increasing NIBA addition, while the yield point decreased. Furthermore, these hydrogels showed strain-softening behavior, weak G″-overshoot marking the onset of nonlinearity, and good self-healing properties after large deformation. The zero-strain nonlinearity parameter (Q 0 ) was found to be more sensitive to NIBA-addition than the linear viscoelastic properties. The blends showed a clear peak in the startup test except for SA alone and the peak intensity increased with increasing NIBA-concentration. Finally, based on all data, gelation mechanism and interaction of SA and NIBA will be clarified.
研究领域:
高分子材料科学
·
生物医学工程
·
软物质物理
·
药剂学
·
组织工程
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DOI
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2016
·
IF 3.42
Jing Li,Sanming Li,Zhonggui He
In the present work, molecular imprinting silica xerogel (MISX) with selective recognition function aiming to regulate drug therapy was synthesized using biomimetic method with poly(ethyleneimine)s (PEIs) as the polymer template and levorotatory ofloxacin (LOFL) as recognition template. Ultraviolet spectroscopy wavelength scanning was used to test the removal process of LOFL, and characteristics of selective loading ofloxacin (OFL) into MISX were investigated using Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Molecular recognition functionality of MISX was intensively studied, including OFL loading and release. The results suggested that MISX possessed ability to recognize and selectively adsorb LOFL into MISX in OFL aqueous solution. Amorphous phase of adsorbed molecules contributed to molecular recognition because amorphous state increased the stability of LOFL that were selectively adsorbed into MISX, which induced stronger hydrogen bonding formed between LOFL and MISX so as to improve LOFL recognition ability. In vitro release revealed that OFL-MISX tablet initially released LOFL and later gradually OFL into dissolution medium. Thus conversion of drug release with different pharmacological activity had special value in delivering systems.
研究领域:
药剂学
·
药物化学
·
纳米医学
·
生物材料
·
分子识别
·
药物递送系统
✓ 已验证
DOI
高影响因子
FLAVOUR AND FRAGRANCE JOURNAL
·
2012
·Vol. 27
·期 5
·378-385
·
IF 1.424
Zhangfu Zeng,Yanxiong Fang,Hongbing Ji
The reason for low encapsulation efficiency of vanillin compared to p -hydroxybenzaldehyde within β -cyclodextrin was investigated. Fourier transform infrared spectra proved intermolecular interaction between guest and β -cyclodextrin. UV–visible studies indicated that vanillin and p -hydroxybenzaldehyde form 1:1 inclusion complexes with β -cyclodextrin. Nuclear magnetic resonance and quantum computational methods gave the most favourable orientation in which the guest molecule (vanillin or p -hydroxybenzaldehyde) is totally sequestered in the hydrophobic cavity of the cyclodextrin with the phenolic end located near the primary hydroxyls of the β -cyclodextrin and the aldehyde group near the secondary hydroxyls with hydrogen bonding formation. Encapsulation efficiency of the β -cyclodextrin inclusion with vanillin is about 29% lower than that with p -hydroxybenzaldehyde. This result could be attributable to the effect that the side chain methoxy group weakened the guest/host non-covalent intermolecular interaction, specifically, hydrogen bond interaction. Copyright © 2012 John Wiley & Sons, Ltd.
研究领域:
药物化学
·
超分子化学
·
分析化学
·
药剂学
·
分子识别
·
计算化学
✓ 已验证
DOI
高影响因子
RSC Advances
·
2014
·Vol. 4
·期 39
·20208-20215
·
IF 3.708
Lei Sun,Xinge Zhang,Jinxia An,Cui Su,Qianqain Guo,Chaoxing Li
Currently, the major challenge for cancer treatment is to develop simple and smart nanocarriers that can efficiently retain the encapsulated drug during blood circulation, recognize tumor cells and quickly release the drug under stimulation. In this paper, such a pH-sensitive core–shell composite nanoparticles is prepared based on a 3-aminophenylboronic acid modified mesoporous silica nanoparticles (MSN–APBA) core coated with a lactobionic acid grafted chitosan (CS–LA) shell via boronate ester bonds. The MSN core increases drug loading capacity and stability, and lactobionic acid offers abundant diols which can form pH sensitive boronate ester bonds with APBA on MSN. Meanwhile, the lactobionic acid-conjugated shell could also efficiently target the asialoglycoprotein receptor over expressing hepatoma cells. The successful synthesis of CS–LA and MSN–APBA is confirmed by the results of TGA, TEM, DLS, FT-IR, 1H-NMR and N2 adsorption–desorption. Doxorubicin hydrochloride (DOX) is applied as a model drug and the behaviors of drug loading/release are investigated. The drug loading behavior is pH-dependent, and its drug encapsulation efficiency is near 80% and loading capacity is 13.05%. The results of cumulative in vitro release indicate that at neutral pH, the pores of the MSN are effectively capped with a polymer shell and the drug release is strongly inhibited, almost zero release. While at acidic pH, the hydrolysis of the boroester bond takes place and thus results in a rapid release of the entrapped drug. The cytotoxicity assay indicates high cell biocompatibility of this material and it is suitable as a drug carrier. When loaded with DOX, it presents distinctly cytotoxic behavior to HepG2 cells, due to the sustained release of drug. These results imply that the core–shell nanoparticles are promising platforms to construct simple and effective pH-responsive controlled drug delivery systems for cancer therapy.
研究领域:
肿瘤学
·
药剂学
·
纳米医学
·
生物材料
·
分子药理学
·
靶向治疗
✓ 已验证
DOI
高影响因子
Materials Today Communications
·
2020
·
IF 2.678
Fang Lu,Yurong Ma,Huibo Wang,Mengling Zhang,Bo Wang,Yue Zhang,Hui Huang,Fan Liao,Yang Liu,Zhenhui Kang
Multidrug-resistant bacterial infections are one of the most serious public health threats in the world, which bring an urgent need to discover novel antibiotics with enhanced broad-spectrum antibacterial activity . Curcumin , as a widely used natural product , has good anti-inflammatory and antioxidant properties; while, the bioavailability, bioactivity and antibacterial activity design are limited by its poor water-solubility. Here, to improve the bioactivity of curcumin, we show the fabrication of highly water-solvable carbon dots (CDs) by hydrothermal method from citric acid and curcumin. The CDs possess excellent broad-spectrum antibacterial activity and antibiofilm activity because they can do damage to the bacterial walls when they get into the bacteria. The bactericidal efficiency of CDs (375 μg/mL) achieves up to 100 % for Gram-negative bacteria ( Escherichia coli and Pseudomonas aeruginosa ). Additionally, for Gram-positive bacteria ( Staphylococcus aureus and Bacillus subtilis ), the bactericidal efficiency reaches 80 %. In addition, these CDs also can completely inhibit the formation of biofilm for the Gram-negative bacteria and the Gram-positive bacteria. This work has a significant meaning in studying new antibacterial nanomaterials derived from natural product and the treatment of infections.
研究领域:
纳米医学
·
微生物学
·
药剂学
·
天然产物化学
·
感染性疾病
·
生物材料
✓ 已验证
DOI
高影响因子
Asian Journal of Pharmaceutical Sciences
·
2017
·Vol. 12
·期 6
·580-585
·
IF 0
Shijie Wei,Jingbo Ren,Ning Li,Wuzhen Huo,Chongkai Gao
An LCC delivery system for Fenofibrate (Fen) was developed to improve its poorly oral bioavailability. Fen-LCC preparation methods were screened, and the prepared Fen-LCC was then characterized by a polarizing microscope and transmission electron microscopy (TEM). The spray drying technique was selected to dry and solidify particles into powder. The in vitro release of Fen-LCC was measured and in vivo pharmacokinetic experiments were carried out on rats after oral administration. Particles prepared through the high-temperature input method exhibited structural characteristics of LCC, and re-dissolved particles maintained the same features. The LCC delivery system can significantly improve in vitro release outcomes. After oral administration, AUCs of the suspension and LCC systems were measured at 131.6853 µg⋅h/ml and 1435.72893 µg⋅h/ml, respectively. The spray drying process presented here better maintains cubic structures, and the LCC system significantly improves bioavailability levels.
研究领域:
药剂学
·
药物递送系统
·
纳米医学
·
药代动力学
·
药物代谢
✓ 已验证
DOI
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2019
·
IF 4.213
Qian Du,Jianqiu Chen,Guojun Yan,Fannan Lyu,Jie Huang,Jin Ren,Liuqing Di
This study compared the in vitro and in vivo effects of different aliphatic acid grafted N -trimethyl chitosan (TMC) surface-modified nanostructured lipid carriers (NLC) by oral delivery. Medium-chain fatty acids, decylic acids (DA), and long-chain fatty acids, palmitic acids (PA) were selected as contrasting objects. TMC, DA grafted TMC (DA-TMC), and PA grafted TMC (PA-TMC) were successively synthesized. Kaempferol loaded NLC (KNLC), KNLC coated with DA-TMC (DA-TMC-KNLC) and PA-TMC (PA-TMC-KNLC) were fabricated, respectively. KNLC were subspherical in shape at nano-size limits. The particle size increased from 93.6 to 125.5 nm and the zeta potential changed from negative to positive due to surface-modification. The KNLC surface-modified with different aliphatic acid grafted TMC displayed a diverse release profiles at the simulative physiological environment, which contrasted that of KNLC. Pharmacokinetic studies demonstrated that the nanoparticles all could improve the AUC values and prolong blood retention times compared to that of kaempferol suspensions. Cell uptake and in situ intestinal perfusion experiments revealed that DA-TMC-KNLC and PA-TMC-KNLC could remarkably enhance cellular uptake of kaempferol into Caco-2 cells and drug absorption in each intestinal segment in comparison with KNLC, repectively. Wherein, DA-TMC-KNLC exhibits the greatest uptake and absorption efficiency as compared to kaempferol suspensions, KNLC and PA-TMC-KNLC. Collectively, DA-TMC surface-modified NLC might serve as a potential drug carrier for oral delivery of water-insoluble flavonoid ingredients.
研究领域:
药剂学
·
药物递送
·
纳米技术
·
药代动力学
·
胶体与界面科学
✓ 已验证
DOI
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2016
·
IF 3.782
Hui Zhang,Jiangkang Xu,Liang Xing,Jianbo Ji,Aihua Yu,Guangxi Zhai
Doxorubicin (DOX) is one of the most common chemotherapeutic agents for the treatment of various cancers, but its clinical usage is limited by dose-dependent cardiotoxicity. We have recently synthesized a series of Chondroitin sulfate/poly ( d , l -lactideco-glycolide) block copolymers (Chs- b -PLGA) with different length of hydrophobic block by an end-to-end coupling strategy. The structure of the amphiphilic block copolymers with low critical micelle concentration (∼28 mg/L) were confirmed by 1 H NMR. The copolymers could self-assemble into stable micelles in aqueous environment with homogeneous size distribution and negative zeta potential . The hemolytic study indicated their excellent blood compatibility and potential application for intravenous administration. DOX can be efficiently encapsulated by the Chs- b -PLGA micelles. The DOX-loaded micelles showed a sustained and pH dependent drug release behavior. The cytotoxicity assay showed no associated toxicity with blank micelles while concentration-related cell inhibition with DOX-loaded micelles. Moreover, fast cellular uptake of DOX-loaded micelles was observed by fluorescent microscope. In vivo pharmacokinetics study showed that the Chs- b -PLGA micelles could significantly prolong the blood circulation time of DOX. The maximum tolerated dose (MTD) of DOX-loaded micelles in Kunming mice was about 2-fold higher of the MTD of free DOX, indicating a high tolerance of the DOX-loaded micelles. In conclusion, the Chs- b -PLGA micelles would be a potentially useful drug delivery system for cancer therapy.
研究领域:
药剂学
·
药物递送
·
纳米医学
·
高分子科学
·
癌症治疗
·
生物医学工程
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）