查找使用阿拉丁产品的科研文献

Portable wireless electrochemical sensing of breviscapine using core–shell ZIFs-derived Co nanoparticles embedded in N-doped carbon nanotube polyhedra-modified electrode

Zhang Zejun,Shi Fan,Ai Yijing,Li Xiaoqing,Zhang Dan,Wang Lisi,Sun Wei

A core–shell ZIF-67@ZIF-8-derived Co nanoparticles embedded in N-doped carbon nanotube polyhedra (Co/C-NCNP) hybrid nanostructure was prepared by a pyrolysis method. The synthesized Co/C-NCNP was modified on the screen-printed carbon electrode and used for the portable wireless sensitive determination of breviscapine (BVC) by differential pulse voltammetry. The Co/C-NCNP had a large surface area and excellent catalytic activity with increasing Co sites to combine with BVC for selective determination, which led to the improvement of the sensitivity of the electrochemical sensor. Under optimized conditions, the constructed sensor had linear ranges from 0.15 to 20.0 µmol/L and 20.0 to 100.0 µmol/L with the limit of detection of 0.014 µmol/L (3S 0 /S). The sensor was successfully applied to BVC tablet sample analysis with satisfactory results. This work provided the potential applications of zeolitic imidazolate framework-derived nanomaterials in the fabrication of electrochemical sensors for the sensitive detection of drug samples. Graphical abstract

Preparation, Characterization, and Evaluation of Breviscapine Nanosuspension and Its Freeze-Dried Powder

Ting Zhang,Xixi Li,Juewen Xu,Jingbao Shao,Meihong Ding,Senlin Shi

As a biopharmaceutics classification system (BCS) class IV drug, breviscapine (Bre) has low solubility in water, poor chemical stability, a short biological half-life and rapid removal from plasma. This paper prepared a Bre nanosuspension (Bre-NS) by an ultrasound-assisted anti-solvent precipitation method. Characterization of Bre-NS was studied using a Box–Behnken design concerning drug concentration in DMSO, an anti-solvent-to-solvent ratio, and sonication time. Under the optimized conditions of 170 mg/mL for the drug concentration, a 1:60 solvent-to-anti-solvent ratio, and a 9 min sonication time, the particle size of Bre-NS was 303.7 ± 7.3 nm, the polydispersity index was 0.178 ± 0.015, and the zeta potential was −31.10 ± 0.26 mV. Combined with the results from differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform-infrared spectroscopy (FT-IR), the findings indicated that the crystal form and chemical structure of Bre-NS did not change during the entire process. The optimized formulation displayed good stability, increased solubility, and better in vitro release. Therefore, the results of this study can be a reference for the delivery system design of insoluble active components and effective parts in traditional Chinese medicine.Keywords:breviscapine;nanosuspension;Box–Behnken design

Preparation and characterization of coamorphous breviscapine-huperzine a system: A computational-experimental study

Jiao Wang,Tong Zhang,Zibin Zou,Yuxia Mo,Qiuru Tan,Lili Cui,Yanni Ma,Wenping Wang

Carrier-free co-amorphous breviscapine-huperzine A via solvent evaporation. • DFT and multi-spectra show H-bonding and π–π stacking stabilize amorphization. • Aqueous solubility of both compounds is significantly enhanced. • Synergistic antioxidant and AChE inhibition suggest multi-target Alzheimer’s potential. Both breviscapine and huperzine A have antioxidant effects, and huperzine A has excellent anticholinesterase effect. Poor aqueous solubility and limited bioavailability of natural products remain major obstacles in drug development. We report the first systematic investigation of a co-amorphous system composed of breviscapine and huperzine A fabricated by solvent evaporation without polymeric carriers. Polarized-light microscopy, thermal and crystallographic analysis confirmed complete amorphization. Density functional theory (DFT) calculations demonstrated strong non-covalent stabilization of the BRE–HupA dimer, and multi-spectral characterization further confirmed supramolecular interactions of hydrogen bonding and π–π stacking. Apparent solubility in water and artificial nasal fluid rose 41- and 65-fold for BRE, respectively, and 2-fold for HupA. The system exhibited reduced hygroscopicity and excellent stability under accelerated storage (40 °C/75% RH, 12 weeks). Biological evaluation revealed superior antioxidant performance in DPPH, superoxide, and hydroxyl radical assays, alongside stronger acetylcholinesterase inhibition compared to raw drugs and their physical mixture. These findings highlight the critical role of non-covalent interactions in stabilizing the co-amorphous state and demonstrate the dual benefit of solubility enhancement and pharmacological synergy. The BRE–HupA co-amorphous system provides a promising carrier-free strategy for developing multi-target formulations against Alzheimer’s disease and related neurodegenerative disorders. Download: Download high-res image (278KB) Download: Download full-size image

Breviscapine alleviates podocyte injury by inhibiting NF-κB/NLRP3-mediated pyroptosis in diabetic nephropathy

Linlin Sun,Miao Ding,Fuhua Chen,Dingyu Zhu,Xinmiao Xie

Podocyte injury is a critical factor in the pathogenesis of diabeticnephropathy (DN). Emerging evidence has demonstrated that breviscapine (Bre) exerts a renoprotective effect on diabetic rats. However, the effects of Bre on regulating podocyte injury under high glucose (HG) conditions remain unclear. In this study, an experimental mouse model of DN was induced by intraperitoneal injections of streptozotocin (STZ) in vivo . The effects of Bre on podocyte injury were assessed using cell counting kit-8 (CCK-8) assay, TdT-mediated dUTPnick-endlabelling (TUNEL) staining, quantitative real-time PCR (qRT‒PCR) and western blot analysis. We found that renal function was significantly decreased in diabetic mice, and this effect was blocked by Bre treatment. Bre effectively increased podocyte viability and inhibited HG-induced cell apoptosis. Furthermore, Bre ameliorated HG-induced podocyte injury, as evidenced by decreased α-smooth muscle actin (α-SMA) expression and increased podocin and synaptopodin expression. Mechanistically, Bre inhibited HG-induced nuclear factorkappaB (NF-κB) signalling activation and subsequently decreased NLR family pyrin domain containing 3 (NLRP3) inflammasome activation, resulting in a decrease in pyroptosis. Pharmacological inhibition of NLRP3 decreased HG-induced podocyte injury, whereas the NLRP3 agonist abrogated the effects of Bre on inhibiting podocyte injury. In summary, these results demonstrate that Bre alleviates HG-induced podocyte injury and improves renal function in diabetic mice, at least in part by inhibiting NF-κB/NLRP3-mediated pyroptosis.

Oral fast dissolving films for co-administration of breviscapine and matrine: Formulation optimization and in vitro characterization

Huiyun Yin,Wenbin Jin,Jiao Wang,Jin Ke,Wenping Zhang,Chen Liu,Wenping Wang

Oral fast dissolving films (OFDFs) are popular dosage forms for enhanced oral absorption of active ingredients without experiencing gastrointestinal interference or first-pass metabolism. The primary challenge in OFDF design is balancing drug loading capacity with film properties, particularly for poorly soluble drugs. In the present work, an OFDF formulation containing co-amorphous mixture was successfully designed for co-administration of two natural products at a drug content of 14%. Breviscapine and matrine are commonly used for cardiovascular and cerebrovascular related diseases, but their clinical application was limited by low bioavailability, short biological half-life, and instability problems. Their co-administration as a compound remedy requires a novel product too enhance drug dissolution and patient compliance. A 3 3 Box-Behnken design was used to generate OFDF preparations by solvent casting method. The optimized blank film formulation, comprising 57.40% HPMC E50, 14.01% PEG 400 and 5.35% L-HPC, demonstrated a rapid disintegration in 18 seconds. XRD and FTIR analysis on drug-loaded films revealed good compatibility of drugs and polymers, and amorphous state of films with co-precipitates. The films were evaluated for morphology, folding endurance, disintegration time and in vitro BRE dissolution. Drugs incorporation extended the disintegration time of blank films, yet remained under 30 seconds. The co-amorphous mixture of BRE and MAT in films exhibited a faster BRE dissolution rate compared to the physical mixture. In conclusion, a compound OFDF formulation featuring a co-amorphous mixture of BRE and MAT offers an efficient strategy for hydrophobic drug delivery at high dose.

Enhanced encapsulation and bioavailability of breviscapine in PLGA microparticles by nanocrystal and water-soluble polymer template techniques

Hong Wang,Guangxing Zhang,Xueqin Ma,Yanhua Liu,Jun Feng,Kinam Park,Wenping Wang

Poly (lactide-co-glycolide) (PLGA) microparticles are widely used for controlled drug delivery. Emulsion methods have been commonly used for preparation of PLGA microparticles, but they usually result in low loading capacity, especially for drugs with poor solubility in organic solvents . In the present study, the nanocrystal technology and a water-soluble polymer template method were used to fabricate nanocrystal-loaded microparticles with improved drug loading and encapsulation efficiency for prolonged delivery of breviscapine . Breviscapine nanocrystals were prepared using a precipitation-ultrasonication method and further loaded into PLGA microparticles by casting in a mold from a water-soluble polymer. The obtained disc-like particles were then characterized and compared with the spherical particles prepared by an emulsion-solvent evaporation method. X-ray powder diffraction (XRPD) and confocal laser scanning microscopy (CLSM) analysis confirmed a highly-dispersed state of breviscapine inside the microparticles. The drug form, loading percentage and fabrication techniques significantly affected the loading capacity and efficiency of breviscapine in PLGA microparticles, and their release performance as well. Drug loading was increased from 2.4% up to 15.3% when both nanocrystal and template methods were applied, and encapsulation efficiency increased from 48.5% to 91.9%. But loading efficiency was reduced as the drug loading was increased. All microparticles showed an initial burst release, and then a slow release period of 28   days followed by an erosion-accelerated release phase, which provides a sustained delivery of breviscapine over a month. A relatively stable serum drug level for more than 30   days was observed after intramuscular injection of microparticles in rats. Therefore, PLGA microparticles loaded with nanocrystals of poorly soluble drugs provided a promising approach for long-term therapeutic products characterized with preferable in vitro and in vivo performance.

Cross-and-Capture: A Dual-Ligand PAMAM Nanocarrier for Sequential BBB Penetration and Ischemic Lesion Retention of Breviscapine

The clinical management of ischemic stroke is severely constrained by the blood–brain barrier (BBB), which restricts therapeutic drug access to the brain parenchyma, and the rapid systemic clearance of neuroprotective agents such as breviscapine (Bre). To overcome this dual challenge, we engineered a dual-targeting nanocarrier, L57&PGP-PEG-PAMAM, designed to sequentially traverse the BBB and anchor within the ischemic inflammatory microenvironment. This construct employs a PEGylated fifth-generation polyamidoamine (PAMAM) dendrimer scaffold functionalized with two distinct peptides: L57, which mediates transcytosis via LRP1 receptors on the BBB, and PGP, which targets CXCR2 receptors overexpressed on infiltrating neutrophils at the lesion. The resulting nano particles exhibited a hydrodynamic diameter of 140.2 ± 0.6 nm (zeta potential: 9.32 mV) and encapsulated Bre with a loading capacity of 20.12% and encapsulation efficiency of 71.78%, displaying sustained release (54.6% over 72 h). Crucially, in vivo fluorescence imaging confirmed markedly superior brain accumulation relative to non-targeted and PEGylated-only controls, while in a rat MCAO model, the formulation reduced infarct volume to 21.7 ± 6.4%, improved neurological scores to 1.52 ± 0.28, and suppressed pro-inflammatory IL-15/IL-27 levels—collectively outperforming free Bre. This work establishes a robust “cross-and-capture” strategy that effectively decouples BBB penetration from lesion-specific retention for ischemic stroke therapy.