Preparation and In Vivo Evaluation of Huperzine A-Loaded PLGA Microspheres

XU-DONG FU,YONG-LIANG GAO,QI-NENG PING,Tang Ren 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.9

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/W emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with 10% released per day. Thereafter drug release rate became slow gradually and about 90% drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4 mg/kg and microspheres were intramuscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration (Cmax ) after i.m. microspheres was only 32% of that after i.m. solution. Drug in plasma could be detectd until day 14 and about 8% of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was 94.7%. Inhibition of acyecholinesterase activity (AchE) in rat’s cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

Preparation and In Vivo Evaluation of Huperzine A-Loaded PLGA Microspheres

FU XU-DONG,GAO YONG-LIANG,PING QI-LENG,Ren Tang The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.9

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

Presentation of a Novel E-Core Transverse-Flux Permanent Magnet Linear Motor and Its Magnetic Field Analysis Based on Schwarz-Christoffel Mapping Method

Dong-Shan Fu,Yan-Liang Xu 대한전기학회 2017 Journal of Electrical Engineering & Technology Vol.12 No.5

In order to overcome the manufacturing difficulty of the transverse-flux permanent magnet linear motor (TFPMLM) and enhance its performance much better, a novel TFPMLM with Ecore and 3 dimension (3D) magnetic structures is proposed in this paper. Firstly, its basic structure and operating principle are presented. Then the equivalent 2D configuration of the TFPMLM is transformed, so that the Schwarz-Christoffel (SC) mapping method can be used to analyze the motor. Furthermore, the air gap flux density distribution is solved by SC mapping method, based on which, the EMF waveform, no-load cogging force waveform and load force waveform are obtained. Finally, the prototyped TLPMLM is manufactured and the results are obtained from the experiment and 3D FEM, respectively, which are used to compare with those from SC mapping method.

Presentation of a Novel E-Core Transverse-Flux Permanent Magnet Linear Motor and Its Magnetic Field Analysis Based on Schwarz-Christoffel Mapping Method

Fu, Dong-Shan,Xu, Yan-Liang The Korean Institute of Electrical Engineers 2017 Journal of Electrical Engineering & Technology Vol.12 No.5

In order to overcome the manufacturing difficulty of the transverse-flux permanent magnet linear motor (TFPMLM) and enhance its performance much better, a novel TFPMLM with E-core and 3 dimension (3D) magnetic structures is proposed in this paper. Firstly, its basic structure and operating principle are presented. Then the equivalent 2D configuration of the TFPMLM is transformed, so that the Schwarz-Christoffel (SC) mapping method can be used to analyze the motor. Furthermore, the air gap flux density distribution is solved by SC mapping method, based on which, the EMF waveform, no-load cogging force waveform and load force waveform are obtained. Finally, the prototyped TLPMLM is manufactured and the results are obtained from the experiment and 3D FEM, respectively, which are used to compare with those from SC mapping method.

Pose Measuring and Aligning of a Micro Glass Tube and a Hole on the Micro Sphere

Fu-Dong Li,De Xu,Zheng-Tao Zhang,Ya-Li Shi,Fei Shen 한국정밀공학회 2014 International Journal of Precision Engineering and Vol. No.

To ensure high uniformity of the inner space of the hollow sphere after assembly, the glass tube must be inserted into the hole on thesphere towards the center of the sphere. This paper deals with the pose measuring of the hole on the sphere and the glass tube andpose aligning of the two objects. The sphere is 500 mm in diameter with a 20 mm hole on it, and the glass tube is 17 mm in diameter. Novel pose measuring method for the hole on the sphere and the glass tube is developed, using two microscopic cameras, each oneacquires a projection vector of the object to be measured. A plane containing the optical axis of the microscopic camera and the posevector of the object is determined, with the microscopic camera calibrated in advance. Pose vector of the object to be measured canbe calculated by the intersection of the two planes acquired by the two microscopic cameras. Error analysis of the pose measuringmethod is conducted and experimental results were consistent with analytical results. Less than 0.7o pose aligning error is achievedusing the proposed pose measuring method and pose aligning method.

Lack of Association of Glutathione S-transferase M3 Gene Polymorphism with the Susceptibility of Lung Cancer

Feng, Xu,Dong, Chun-Qiang,Shi, Jun-Jie,Zhou, Hua-Fu,He, Wei,Zheng, Bao-Shi Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.9

Objective: The conclusions of published reports on the relationship between the glutathione S-transferase M3 (GSTM3) A/B gene polymorphism and the risk of lung cancer are still debated. This meta-analysis was performed to evaluate the association between GSTM3 and the risk of lung cancer. Methods: Association investigations were identified from PubMed, Embase, and Cochrane Library, and eligible studies were included and synthesized using a meta-analysis method. Results: Eight reports were included into this meta-analysis for the association of GSTM3 A/B gene polymorphism and lung cancer susceptibility, covering 1,854 patients with lung cancer and 1,926 controls. No association between the GSTM3 A/B gene polymorphism and lung cancer was found in this meta-analysis (B allele: OR = 1.25, 95% CI: 0.89-1.76, P = 0.20; BB genotype: OR = 1.53, 95% CI: 0.71-3.32, P = 0.28; AA genotype: OR = 0.85, 95% CI: 0.59-1.23, P = 0.39). Conclusions: The GSTM3 A/B gene polymorphism is not associated with lung cancer susceptibility. However, more studies on the relationship between GSTM3 A/B gene polymorphism and the risk of lung cancer should be performed in the future.

Bionic natural small molecule co-assemblies towards targeted and synergistic Chemo/PDT/CDT

Shiyao Fu,Mingao Wang,Bin Li,Xu Li,Jianjun Cheng,Haitian Zhao,Hua Zhang,Aijun Dong,Weihong Lu,Xin Yang 한국생체재료학회 2023 생체재료학회지 Vol.27 No.00

Background Multi-component nano-delivery systems based on chemotherapy (chemo)- photodynamic therapy (PDT)- chemodynamic therapy (CDT) have gained increased attention as a promising strategy to improve clinical outcomes in cancer treatment. However, there remains a challenge in developing biodegradable, biocompatible, less toxic, yet highly efficient multicomponent nanobased drug delivery systems (DDS). Here, our study presents the screening and development of a novel DDS based on co-assemblies natural small molecule (NSMs). These molecules (oleanolic acid, and betulinic acid) are combined with photosensitizers Chlorine6 (Ce6) and Cu2+ that are encapsulated by tumor cell membranes. This nanocarrier encapsulated in tumor cell membranes achieved good tumor targeting and a significant improvement in tumor accumulation. Methods A reprecipitation method was used to prepare the co-assembled nanocarrier, followed by the introduction of Cu2 + into the DDS (OABACe6 NPs). Then, by wrapping the surface of NPs with the cell membranes of 4T1 which is a kind of mouse breast cancer cells (CM@OABACe6/Cu NPs). and analysis of its structure and size distribution with UV– Vis, XPS, FT-IR, SEM, TEM, and DLS. The synergistic effects of in vitro chemotherapy, CDT and PDT and targeting were also validated by cellular and animal studies. Results It was shown that CM@OABACe6/Cu NPs achieved good tumor targeting and a significant improvement in tumor accumulation. In the composite nano-assembly, the NSMs work together with the Ce6 to provide effective and safe chemo and PDT. Moreover, the effect of reduced PDT due to the depletion of reactive oxygen species (ROS) by excess glutathione (GSH) in the tumor can be counteracted when Cu2 + is introduced. More importantly, it also confers CDT through a Fenton-like catalytic reaction with H2O overexpressed at the tumor site. Conclusions By constructing CM@OABACe6/Cu NPs with homologous targeting, we create a triple synergistic platform for cancer therapy using PDT, chemo, and CDT. We propose here a novel combinatorial strategy for designing more naturally co-assembled small molecules, especially for the development of multifunctional synergistic therapies that utilize NSMs.

Structural Evolution of Sub-10 nm Octahedral Platinum–Nickel Bimetallic Nanocrystals

Chang, Qiaowan,Xu, Yuan,Duan, Zhiyuan,Xiao, Fei,Fu, Fang,Hong, Youngmin,Kim, Jeonghyeon,Choi, Sang-Il,Su, Dong,Shao, Minhua American Chemical Society 2017 NANO LETTERS Vol.17 No.6

<P>Octahedral Pt alloy nanocrystals (NCs) have shown excellent activities as electrocatalysts toward oxygen reduction reaction (ORR). As the activity and stability of NCs are highly dependent on their structure and the elemental distribution, it is of great importance to understand the formation mechanism of octahedral NCs and to rationally synthesize shape-controlled alloy catalysts with optimized ORR activity and stability. However, the factors controlling the structural and compositional evolution during the synthesis have not been well understood yet. Here, we systematically investigated the structure and composition evolution pathways of Pt-Ni octahedra synthesized with the assistance of W(CO)(6) and revealed a unique core-shell structure, consisting of a Pt core and a Pt-Ni alloy shell. Below 140 degrees C, sphere-like pure Pt NCs with the diameter of 3-4 nm first nucleated, followed by the isotropic growth of Pt-Ni alloy on the seeds at temperatures between 170 and 230 degrees C forming Pt@Pt-Ni core-shell octahedra with {111} facets. Owing to its unique structure, the Pt@Pt-Ni octahedra show an unparalleled stability during potential cycling, that is, no activity drop after 10 000 cycles between 0.6 and 1.0 V. This work proposes the Pt@Pt-Ni octahedra as a high profile electrocatalyst for ORR and reveals the structural and composition evolution pathways of Pt-based bimetallic NCs.</P>

VSV-G Viral Envelope Glycoprotein Prepared from Pichia pastoris Enhances Transfection of DNA into Animal Cells

( Xin Liu ),( Ying Dong ),( Jingquan Wang ),( Long Li ),( Zhenmin-zhong ),( Yun-pan Li ),( Shao-jun Chen ),( Yu-cai Fu ),( Wen-can Xu ),( Chi-ju Wei ) 한국미생물생명공학회(구 한국산업미생물학회) 2017 Journal of microbiology and biotechnology Vol.27 No.6

Vesicular stomatitis virus G glycoprotein (VSV-G) has been widely used for pseudotyping retroviral, lentiviral, and artificial viral vectors. The objective of this study was to establish a potential approach for large-scale production of VSV-G. To this end, VSV-G was cloned with an N-terminal His-tag into Pichia pastoris expression vector pPIC3.5K. Three clones (Mut^s) containing the VSV-G expression cassette were identified by PCR. All clones proliferated normally in expansion medium, whereas the proliferation was reduced significantly under induction conditions. VSV-G protein was detected in cell lysates by western blot analysis, and the highest expression level was observed at 96 h post induction. VSV-G could also be obtained from the condition medium of yeast protoplasts. Furthermore, VSV-G could be incorporated into Ad293 cells and was able to induce cell fusion, leading to the transfer of cytoplasmic protein. Finally, VSV-G-mediated DNA transfection was assayed by flow cytometry and luciferase measurement. Incubation of VSV-G lysate with the pGL3-control DNA complex increased the luciferase activity in Ad293 and HeLa cells by about 3-fold. Likewise, incubation of VSV-G lysate with the pCMV-DsRed DNA complex improved the transfection efficiency into Ad293 by 10% and into HeLa cells by about 1-fold. In conclusion, these results demonstrate that VSV-G could be produced from P. pastoris with biofunctionalities, demonstrating that large-scale production of the viral glycoprotein is feasible.

Role of Blood Pressure Management in Stroke Prevention: A Systematic Review and Network Meta-Analysis of 93 Randomized Controlled Trials

Xiao-Ling Zhong,Yi Dong,Wei Xu,Yu-Yuan Huang,Hui-Fu Wang,Tian-Song Zhang,Li Sun,Lan Tan,Qiang Dong,Jin-Tai Yu 대한뇌졸중학회 2021 Journal of stroke Vol.23 No.1

Background and Purpose: The present study aimed to compare the efficacy and tolerability of different blood pressure (BP)-lowering strategies. Methods: Randomized controlled trials that compared various antihypertensive treatments and stroke outcomes were included. Eligible trials were categorized into three scenarios: single or combination antihypertensive agents against placebos; single or combination agents against other agents; and different BP-lowering targets. The primary efficacy outcome was the risk reduction pertaining to strokes. The tolerability outcome was the withdrawal of drugs, owing to drug-related side effects (PROSPERO registration number CRD42018118454 [20/12/2018]). Results: The present study included 93 trials (average follow-up duration, 3.3 years). In the pairwise analysis, angiotensin-converting enzyme inhibitors (ACEis) and beta-blockers (BBs) were inferior to calcium channel blockers (CCBs) (odds ratio [OR], 1.123; 95% confidence interval [CI], 1.008 to 1.252) (OR, 1.261; 95% CI, 1.116 to 1.425) for stroke prevention, BB was inferior to angiotensin II receptor blockers (ARB) (OR, 1.361; 95% CI, 1.142 to 1.622), and diuretics were superior to ACEi (OR, 0.871; 95% CI, 0.771 to 0.984). The combination of ACEi+CCB was superior to ACEi+diuretic (OR, 0.892; 95% CI, 0.823 to 0.966). The network meta-analysis confirmed that diuretics were superior to BB (OR, 1.34; 95% CI, 1.11 to 1.58), ACEi+diuretic (OR, 1.47; 95% CI, 1.02 to 2.08), BB+CCB (OR, 2.05; 95% CI, 1.05 to 3.79), and renin inhibitors (OR, 1.87; 95% CI, 1.25 to 2.75) for stroke prevention. Regarding the tolerability profile, the pairwise analysis revealed that ACEi was inferior to CCB and less tolerable, compared to the other treatments. Conclusions: Monotherapy using diuretics, CCB, or ARB, and their combinations could be employed as first-line treatments for stroke prevention in terms of efficacy and tolerability.