Biomolecules
·
2021
·Vol. 11
·期 5
·635
·
IF 4.879
Ding Li,Menglong Wang,Wen-Liang Song,Deng-Guang Yu,Sim Wan Annie Bligh
A side-by-side electrospinning process characterized by a home-made eccentric spinneret was established to produce the Janus beads-on-a-string products. In this study, ketoprofen (KET) and methylene blue (MB) were used as model drugs, which loaded in Janus beads-on-a-string products, in which polyvinylpyrrolidone K90 (PVP K90) and ethyl cellulose (EC) were exploited as the polymer matrices. From SEM images, distinct nanofibers and microparticles in the Janus beads-on-a-string structures could be observed clearly. X-ray diffraction demonstrated that all crystalline drugs loaded in Janus beads-on-a-string products were transferred into the amorphous state. ATR-FTIR revealed that the components of prepared Janus nanostructures were compatibility. In vitro dissolution tests showed that Janus beads-on-a-string products could provide typical double drugs controlled-release profiles, which provided a faster immediate release of MB and a slower sustained release of KET than the electrospun Janus nanofibers. Drug releases from the Janus beads-on-a-string products were controlled through a combination of erosion mechanism (linear MB-PVP sides) and a typical Fickian diffusion mechanism (bead KET-EC sides). This work developed a brand-new approach for the preparation of the Janus beads-on-a-string nanostructures using side-by-side electrospinning, and also provided a fresh idea for double drugs controlled release and the potential combined therapy.Keywords:side-by-side electrospinning;Janus structure;beads-on-a-string;immediate release;sustained release
研究领域:
药剂学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2022
·
IF 16.744
Rui Wang,Song Liu,Feng-shou Sun,Xin Yu,Xiao Liu,Bei-xing Li,Wei Mu,Da-xia Zhang,Feng Liu
The development of microencapsulation is currently blocked by the mismatch between the release rate and pest-control demand in terms of improving the photostability of pesticides. Achieving both long-term stability and quick release of pesticides through the use of microcapsules (MCs) is an effective way to increase pesticide efficiency. Sodium lignosulfonate and four types of polyalkyl quaternary ammonium salts (PQAS) were used as shell materials in the fabrication of four types of microcapsules by electrostatic self-assembly. The effects of the PQAS alkyl chain length on the morphology, zeta potential, molecular electrostatic potential, particle size distribution , encapsulation efficiency, release behaviour, anti-photolysis performance, and field application effects of the MCs were investigated. The four types of MCs were spherical and 0.5–3 μm in size, and they had an encapsulation efficiency of more than 75 %. The X-ray diffraction results showed that the longer the alkyl chain of PQAS was, the looser the material formed by electrostatic attraction was. With the increase of the alkyl chain length of PQAS, the MCs shell was looser and easier to deform, leading to rapid nuclear release. Therefore, the MCs shells were looser and more prone to deformation with increasing PQAS alkyl chain length, resulting in the quick release of the core. This quick release of the core to the bottom of the microcapsules and the loose shell formed a double-layer structure, which effectively prevented ultraviolet degradation. Therefore, abamectin MCs with quick-release and favourable anti-photolysis performances showed advantages in controlling Plutella. xylostella and Pieris. rapae insect pests . Octadecyl dimethyl benzyl ammonium chloride can be used to fabricate loose MCs by electrostatic self-assembly, which achieves both rapid and long-term pest control.
研究领域:
农业科学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
LANGMUIR
·
2021
·
IF 3.882
Ashish Trital,Weili Xue,Longgang Wang,Shengfu Chen
Chemotherapeutic nanodrugs have to penetrate through many biological barriers before reaching the tumor cells. Thus, high stability of the nanocarrier before reaching tumor cells and fast release of the carried drugs in targeted tumor cells are required. In this work, inspired by the intrinsic zwitterionic surface property, mainly formed by glutamic acid and lysine residues, of the plasma protein surface, the zwitterionic poly(glutamyl lysine-co-aspartic acid-co-cysteine) peptide (P(EK-D-C)) was synthesized for conjugating n-mercaptoalkanoic acid (MA) with different chain lengths on cysteine residues through a disulfide linkage to load hydrophobic doxorubicin (DOX). The results showed that the slightly negative-biased zwitterionic nanodrugs were very stable in both resistance to nonspecific plasma protein adsorption and prevention of premature DOX release at physiological pH 7.4 due to the zwitterionic polypeptide shell and the sharp contrast in polarity between the shell and DOX-loaded core, while they can quickly release the loaded DOX through responding to both low pH values in the endosome/lysosome and high glutathione concentrations in the tumor cell cytoplasm. Furthermore, the enhanced internalization of these nanodrugs led to about 60% higher in vitro cytotoxicity against MCF-7 cells at pH 6.7 than at pH 7.4, whereas the in vitro cytotoxicity of DOX·HCl at pH 6.7 was only 75% of the value at pH 7.4. In vivo results revealed that the stable nanodrugs conjugated with the long hydrophobic 12-mercaptododecanoic acid had higher tumor inhibition rate and lower systematic toxicity on MCF-7 tumor-bearing mice than the less stable nanodrugs conjugated with the short 8-mercaptooctaoic acid and were significantly superior to DOX·HCl. These results indicate that the combination of high stability in circulation and fast release in tumor cells of nanodrugs can enhance high efficacy targeted chemotherapy. This pH/redox-sensitive zwitterionic polypeptide nanocarrier might provide an excellent vehicle for solid tumor treatment.
研究领域:
生物材料学
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肿瘤学
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药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
·
IF 4.9
Lele Wang,Tijie Duan,Yawen Gao,Heqing Liu,Rui Sun,Tong Wu,Jihui Tang
Subject The release rate of hydrophilic gel tablets varies depending on their surface area. In this study, we aimed to develop a sustained-release tablet that maintains a constant release area during drug release. Methods Initially, commercially accessible gliclazide, sinomenine hydrochloride, and trimetazidine hydrochloride tablets were side coated with ethylcellulose to ensure a constant release area. Next, sustained-release gliclazide tablets were prepared by altering their size and thickness to assess the impact of specific surface area on drug release. Then, two types of sustained-release gliclazide tablets were developed and evaluated in vitro. One involved side-coating the tablets with an ethylcellulose solution. The second was a novel three-layer donut-shaped tablet. Finally, these novel sustained-release tablets were evaluated for in vivo drug release and pharmacokinetics in rabbits. Results After lateral coating, commercial tablets altered drug release from first-order to zero-order kinetics. Tablets with the same specific surface area, but different diameters and thicknesses, can have similar release profiles. If the drug release area is unchanged, the tablet typically exhibits zero-order release behavior. Thus, we developed two types of gliclazide sustained-release tablets with a constant release area that achieved zero-order drug release. In vivo, they showed smoother plasma concentration profiles with lower C max , extended T max , and reduced fluctuation, and were bioequivalent to commercial tablets in pharmacokinetic studies. Conclusions Stable drug release can be achieved by maintaining a constant release area. In this study, the novel tablet preparations exhibited consistent drug release both in vivo and in vitro.
研究领域:
药剂学
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药物研发
✓ 已验证
产品关联
DOI
高影响因子
Materials
·
2018
·Vol. 11
·期 10
·2041
·
IF 2.467
Jingjing Wang,Yajing Jiao,Yiran Shao
Low-energy ultrasound (LEUS), exhibiting obvious advantages as a safe therapeutic strategy, would be promising for cancer therapy. We had synthesized a LEUS-responsive targeted drug delivery system based on functional mesoporous silica nanoparticle for cancer therapy. Paclitaxel (PTX) was loaded in mesoporous silica nanoparticles with a hydrophobic internal channel, and folic acid (FA) functionalized β-Cyclodextrin (β-CD) was capped on the surface of the nanoparticles (DESN), which acted as a cancer-targeting moiety and solubilizer. The existence of a hydrophobic internal channel in the DESN was beneficial to the storage of hydrophobic PTX, along with the enhancement of the cavitation effect produced by mild low-energy ultrasound (LEUS, ≤1.0 W/cm2, 1 MHz). The DESN showed significantly enhanced cavitation effect, selective targeting, and achieved a rapid drug release under mild LEUS. To investigate the in vivo antitumor efficacy of the DESN upon LEUS irradiation, we established a 4T1 mammary tumor model. The DESN were confirmed to be of great biodegradability/biocompatibility. The tumor growth was significantly inhibited when the mice were treated with DESN (10 mg/kg) + LEUS with the relative tumor volume reduced to 4.72 ± 0.70 compared with the control group (V/V0= 17.12 ± 2.75). The DESN with LEUS represented excellent inhibiting effect on tumor cell in vivo. This work demonstrated that DESN mediating dual mode chemo-sonodynamic therapy could be triggered by extracorporeal remote control, may suggest a promising clinical application in cancer therapy.Keywords:low-energy ultrasound;mesoporous silica;folic acid;rapid release;chemo-sonodynamic therapy
研究领域:
生物医学工程
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
Polymers
·
2022
·Vol. 14
·期 9
·1816
·
IF 4.967
Chengjia Xie,Qun Zhang,Zhao Li,Shaohua Ge,Baojin Ma
During wound healing, bacterial infection is one of the main limiting factors for the desired efficiency. Wound dressing-mediated antibiotics therapies could overcome this problem to a great extent due to sustained drug release and controllable dose. Here, we designed a kind of alginate injectable hydrogel loaded with minocycline ([email protected]) as a dressing for staphylococcus aureus-infected wound healing.[email protected]hydrogel possessed good injectability and can be injected by syringes. MC participated in the gel formation, causing the microstructure change based on the morphology characterization. The element mapping and FT-IR spectra further confirmed the successful loading of MC in SA hydrogel. Interestingly, MC was released more efficiently in a weakly alkaline condition (pH 7–8) than in a weakly acidic condition (pH 4–6) from[email protected]injectable hydrogel, which means that there is an accelerated release to respond to the weakly alkaline wound microenvironment. Meanwhile,[email protected]injectable hydrogel had high biocompatibility and excellent antibacterial activity due to the sustained release of MC. Further, in vivo experiment results demonstrated that[email protected]injectable hydrogel promoted staphylococcus aureus-infected wound healing efficiently. In summary, the injectable composite hydrogel can serve as an ideal dressing to prevent bacterial infection and promote wound healing.Keywords:injectable hydrogel;alginate;microenvironment-accelerated release;antibacterial activity;wound healing
研究领域:
药学
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材料科学
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生物医学工程
·
伤口护理
✓ 已验证
产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2025
·
IF 6.5
Jing Yuan,Wenhao Su,Jingyang Gao,Xiaoqing Ma,Ronghuan Yin,Tong Jia
Purpose Praziquantel (PZQ) is currently the preferred medication for treating various parasites. However, its use is hindered by several issues, such as poor solubility, first-pass effect, and individual variability. A novel immediate release system was developed by loading PZQ onto Pluronic P123/L64 mixed micelles (PMMs). This approach aims to improve its bioavailability following oral administration.Methods PZQ-PMMs were prepared by thin film dispersion method. The encapsulation efficiency (EE), particle size, and polydispersity index (PDI) were utilized to identify the optimal formulation. Characterization techniques, including electron microscopy, infrared spectroscopy, thermal analysis, and X-ray diffraction were utilized to get an understanding of the molecular interactions between PZQ and micelles. This system was compared with commercially available preparations both in vitro and in vivo.Results The particle size of the prepared PZQ-PMMs (P123:L64 1:1, w/w) was 19.33 ± 0.22 nm, with a PDI value of 0.106 ± 0.044, an EE of 86.88 ± 4.60%, and a drug loading of 4.16 ± 0.21%. Structural characterization results indicated that the spherical micelles were uniformly dispersed, with the drug existing in an amorphous form within PMMs. In vitro, PZQ-PMMs exhibited a faster immediate release in both pH 1.2 and pH 6.8 buffers. In vivo, at the same dosage, the micelles rapidly produced higher blood drug concentrations. The relative bioavailability of PZQ-PMMs was comparable to that of the PZQ 30% ethanol solution and was 1.7 times greater than that of commercially available preparations, with the increase in bioavailability being highly significant (P < 0.01).Conclusion The findings of this study confirm that Pluronic P123/L64 PMMs represent a novel and promising approach for enhancing solubility and bioavailability of PZQ, both in vitro and in vivo. The development of immediate release formulations is anticipated to be an effective option for drugs exhibiting a notable first-pass effect.
研究领域:
药剂学
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药物递送系统
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药代动力学
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纳米医学
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生物药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Pharmaceutics
·
2022
·Vol. 14
·期 7
·1518
·
IF 6.525
Mengchen An,Mengxiao Shi,Jingjing Su,Yueru Wei,Rongrong Luo,Pengchao Sun,Yongxing Zhao
Although the inhibitors of the interleukin-6 receptor (IL-6R) and tumor necrosis factor-α (TNF-α) have achieved a certain success in the clinical treatment of rheumatoid arthritis (RA), great effort should be made to overcome side effects and to improve patient compliance. The present research aimed to address these problems by the co-delivery of tocilizumab (TCZ)—an inhibitor of IL-6R—and an aptamer Apt1-67, which specifically inhibits TNF receptor 1 via separable microneedles (MN). MN were featured with a sustained release of TCZ from needle tips and a rapid release of Apt1-67 from needle bodies by using methacrylate groups grafted hyaluronic acid as the fillings of needle tips and polyvinyl alcohol/polyvinyl pyrrolidone as the fillings of needle bodies. Our results demonstrated that TCZ and Apt1-67 were distributed in MN as expected, and they could be released to the surroundings in the skin. In vivo studies revealed that combined medication via MN (TCZ/[email protected]) was superior to MN loaded with a single drug. Compared with subcutaneous injection, TCZ/[email protected]was of great advantage in inhibiting bone erosion and alleviating symptoms of CIA mice. This study not only provides a novel approach for combined medication with different release properties but also supplies a strategy for improving drug efficacy.Keywords:separable microneedles;tocilizumab;aptamer Apt1-67;rheumatoid arthritis
研究领域:
药学
·
生物医学工程
·
风湿病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）