1.Advances in oral distant targeted nanodelivery systems
Min SUN ; Chuan-sheng HUANG ; Li-ping WANG ; Xu-li RUAN ; Yun-li ZHAO ; Xin-chun WANG
Acta Pharmaceutica Sinica 2025;60(1):72-81
Due to patient compliance and convenience, oral medication is likely the most common and acceptable method of drug administration. However, traditional dosage forms such as tablets or capsules may lead to low drug bioavailability and poor therapeutic efficiency. Therefore, with advancements in material science and micro/nano manufacturing technology, various carriers have been developed to enhance drug absorption in the gastrointestinal tract. In this context, we initially discuss the key biological factors that hinder drug transport and absorption (including anatomical, physical, and biological factors). Building on this foundation, recent progress in both conventional and innovative oral drug delivery routes aimed at improving drug bioavailability and targeting is reviewed. Finally, we explore future prospects for oral drug delivery systems as well as potential challenges in clinical translation.
2.Effect of different expression levels of GRIM-19 on the resistance of prostate cancer cells to docetaxel chemotherapy
Hai-Li LIN ; Yong-Xin HE ; Tian-Qi LIN ; Zai-Xiong SHEN ; Liu-Tao LUO ; Si-Xing HUANG ; Yi HUANG ; Yu ZHOU ; Min-Yi RUAN
National Journal of Andrology 2024;30(10):884-888
Objective:To investigate the effect of GRIM-19 on the resistance of carcinoma cells to the chemotherapeutic agent docetaxel in the treatment of PCa.Methods:Using siRNA technology to interfere with the gene expression in PCa cells,we estab-lished a model of GRIM-19 overexpression/knockdown in PCa cells.We investigated the effect of different expression levels of GRIM-19 on docetaxel-induced death of the PCa cells by qPCR,Western blot and flow cytometry,and assessed the value of GRIM-19 in re-ducing the chemotherapy-resistance of PCa cells.Results:GRIM-19 was down-regulated in PCa tissues and cells.Knockout of GRIM-19 significantly decreased the expression of siGRIM19 in the PC-3 and LNCaP cells,and reduced their death rate when treated with docetaxel compared with the control group.The expressions of GRIM-19 mRNA and protein were remarkably upregulated after transfection with GRIM-19,and the overexpressed GRIM-19 promoted the death of the PC-3 and LNCaP cells treated with docetaxel in a dose-dependent manner.Flow cytometry analysis showed a lower apoptosis rate of PC-3-R cells than that of PC-3 cells at different time points of docetaxel-induction at different doses.Conclusion:GRIM-19 is a PCa suppressor gene with a significant facilitating effect on the apoptosis of PCa cells,and the overexpression of GRIM-19 promotes docetaxel-induced PCa cell death and improves the sensitivity of chemotherapy.
3.A new alkaloid from Huperzia serrata and its biological activity
Xiao-ting QIAO ; Xin-xin CHENG ; Dan WANG ; Mei-han LAI ; Jia-qi WANG ; Xiao-min WANG ; Cai-lian RUAN ; Duo CAO
Acta Pharmaceutica Sinica 2024;59(12):3342-3346
The methanol extract of
4.Clinical trial of western medicine treatment combined with Xuefu Zhuyu decoction in the treatment elderly patients with refractory hypertension
Guan-Jun WANG ; Lie-Min RUAN ; Ni DAI ; Yun-Xin JI ; Ying CHAI
The Chinese Journal of Clinical Pharmacology 2017;33(12):1158-1160
Objective To evaluate the clinical effect of Xuefu Zhuyu decoction combined with western medicine on elderly patients with refractory hypertension.Methods A total of 120 elderly patients with refractory hypertension were randomly divided into treatment group (n =60) and control group (n =60).Control group was given propranolol 5-10 mg orally,tid or qid;captopril 12.5 mg orally bid or tid;indapamide 2.5 mg orally qd.Treatment group was given Xuefu Zhuyu decoction 100 mL · d-1,bid on the basis of control group.All patients were treated for 90 d.The clinical symptoms and blood pressure were compared before and after treatment.Results The clinical efficacy was 95.00% (57/60 cases) and 78.33% (47/60 cases,P <0.05).After treatment,the systolic blood pressure (SBP) were (130.09 ±9.95),(113.08 ±15.24) mmHg in control group and treatment group,and diastolic blood pressure (DBP) were (84.40 ±9.05),(81.02 ±6.56) mmHg (P <0.05).There was 1 case of dizziness in control group,and no adverse drag reaction occurred in treatment group,with no significant difference (P > 0.05).Conclusion Xuefu Zhuyu decoction combined with western medicine maybe an effective treatment on elderly patients with refractory hypertension.
5.Effect of Huxin Formula on reverse cholesterol transport in ApoE-gene knockout mice.
Wei JIANG ; Song LI ; Wei MAO ; Guang YANG ; Xin-mei LI ; Guang-juan ZHENG ; Huan-lin WU ; Xin-min RUAN ; Ke-ji CHEN
Chinese journal of integrative medicine 2012;18(6):451-456
OBJECTIVETo observe the effect of Huxin Formula on expressions of the chief reverse cholesterol transport (RCT) associated genes, caveolin-1 and scavenger receptor-BI (SR-BI) in ApoE-gene knockout [ApoE (-/-)] mice.
METHODSThirty ApoE (-/-) mice of 4-6 weeks old were randomly divided into three groups (A-C). After being fed with high-fat diet for 16 weeks, they were treated with HXF (1 mL/100 g), pravachol (0.3 mg/100 g), and saline in equal volume respectively for 16 weeks successively; in addition, a blank group was set up with 10 C57BL/6J mice of 6-week old received 16-week high-fat feeding and saline treatment. Animals were sacrificed at the termination of the experiment, their paraffin sections of aortic tissue were used to measure the size of plaque, expressions of cavolin-1 and SR-BI were detected by immunological histochemical method.
RESULTSAs compared with the blank group, levels of caveolin-1 and SR-BI were increased in Groups A and B (P<0.01); but the increase in Group A was more significant than that in Group B (P<0.05). The plaque/aorta area ratio decreased significantly in Groups A and B, but showed insignificant difference between the two groups.
CONCLUSIONHXF could obviously increase the expressions of RCT associated genes, caveolin-1 and SR-BI, promote the RCT process, so as to reduce the formation of aorta atherosclerotic plaque in ApoE (-/-) mice.
Animals ; Aorta ; drug effects ; pathology ; Apolipoproteins E ; deficiency ; genetics ; Atherosclerosis ; pathology ; Biological Transport ; drug effects ; Caveolin 1 ; metabolism ; Cholesterol ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; Female ; Immunohistochemistry ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Plaque, Atherosclerotic ; pathology ; Receptors, Scavenger ; metabolism
6.Biological limit value for occupational exposure to N, N-dimethylacetamide.
Ya-lin QIAN ; Cheng-min XU ; Yan-yan LU ; Hong-fan TANG ; Zheng RUAN ; Han WANG ; Hai-bao ZHU ; Dan-hua LIU ; Xin ZHANG
Chinese Journal of Industrial Hygiene and Occupational Diseases 2012;30(9):709-711
OBJECTIVETo establish Biological Limit Value (BLV) for N, N-dimethylacetamide (DMAC).
METHOD201 workers in 3 spandex factories exposed to DMAC were recruited. Air samples were collected using personal air samplers, and urine samples from each works were collected at the end of shift at end of workweek. The urinary metabolite NMAC and air samples of DMAC were determined by gas chromatography (GC). Percentile and relative internal exposure (RIE) were analyzed and proposed a BLV for DMAC.
RESULTSThe number of workers who exposure to DMAC below OELs were 133 (66.2%) among 201 workers monitored. Geometric mean (range) concentration of DMAC in air was 19.4 (0.40 ∼ 300.12) mg/m(3), and that of NMAC in urine was 23.7 (1.30 ∼ 189.42) mg/g Cr. A linear correlation was found between the personal air DMAC and creatinine-adjusted NMAC levels in urine collected at the end of shift at end of workweek (F = 188.872, R(2) = 0.487,P < 0.001). The relationship can be described by the equation Log (NMAC mg/g Cr) = 0.685 + 0.455 log (DMAC mg/m(3)). According to the equation the current China OELs value of 20 mg/m(3) would lead to a mean NMAC concentration of 18.92 mg/g Cr. The 90th percentile biomonitoring result below 20 mg/m(3) 8-hour TWA is 23.9 mg MMAC mg/g Cr, and that of NMAC in urine calculated by relative internal exposure (RIE) was 19.0 mg/g Cr.
CONCLUSIONA BLV of 20 mg/g Cr NMAC in urine at the end of shift at end of workweek for DMAC was recommend by reference to official values from other countries.
Acetamides ; analysis ; urine ; Adult ; Air Pollutants, Occupational ; analysis ; Chromatography, Gas ; Female ; Humans ; Male ; Occupational Exposure ; analysis ; Threshold Limit Values
7.The novel surface-anchored protein SasX promotes aggregation and colonization of Staphylococcus aureus
Jian CHEN ; Xin DU ; Yan SONG ; Feiyi RUAN ; Yuan Lü ; Min LI
Chinese Journal of Microbiology and Immunology 2012;32(6):519-524
Objective To determine whether the novel surface-anchored protein SasX promotes aggregation of S.aureus and adherence of S.aureus to human nasal epithelial cells.Methods MRSA ST-239 HS770 sasX gene mutant ( HS770 △sasX) and complement [ HS770 △sasX (pRBsasX) ] were gotten by gene knock-out and complement methods.The aggregation ability of S.aureus was observed through microscope.By adherence assay which was used for detection of the adherence ability of wild type and mutant to human nasal epithelial cells and blocking experiments which detected the ability of the purified recombinant SasX protein in blocking the adherence of S.aureus to human nasal epithelial cells,we investigated the influence SasX on colonization of S.aureus.Results Compared to wild type,HS770△sasX showed a reduction in cell aggregation,while the complement had no difference with wild type in aggregation. HS770 △sasX showed a significant reduction of adherence to human nasal epithelial cells compared to wild type ( P<0.01 ),and the complement showed a very clear increasement of adherence to human nasal epithelial cells compared to wild type(P<0.01 ).Preincubation of nasal epithelial cells with the purified recombinant SasX protein inhibited S.aureus binding significantly.Conclusion SasX had an influence in aggregation of S.aureus and its adherence to human nasal epithelial cells.By acquiring sasX,S.aureus colonized more easily to the susceptible sites of the host,and thus caused infection.
8.Design of ABC damage variable and positioning system for acetabular fractures and 1122 cases multi-center statistic analysis.
Chun-cai ZHANG ; Shuo-gui XU ; Bao-qing YU ; Fang JI ; Qing-ge FU ; Xin-wei LIU ; Yun-tong ZHANG ; Yun-fei NIU ; Pan-feng WANG ; Jia-can SU ; Lie-hu CAO ; Yong-qing XU ; Mo RUAN ; Zhuang-hong CHEN ; Ji-feng HUANG ; Xian-hua CAI ; Hui-liang SHEN ; Li-min LIU ; Ji-fang WANG ; Yan WANG ; Pei-fu TANG ; Yu-tian LIANG ; Jia-rang WANG ; Yu-ri WANG ; Zhen-hao WANG ; Wen-di LIU ; Wen-rui LI ; Wen-hu LI ; Xu-quan WANG ; Dong-sheng ZHOU ; Peng ZHANG ; Ren WANG ; Gang WANG ; Yu-yue CHEN ; Yong-jian CONG
China Journal of Orthopaedics and Traumatology 2011;24(2):102-108
OBJECTIVETo design ABC damage variable and positioning system for acetabular fracture and explore the feasibility and clinical practical value of the system through the multi-center analysis of 1122 acetabular fractures.
METHODSAccording to acetabular three-column conception, and pelvic ring lesions damage direction caused by acetabular fracture domino effect and injury degree of proximal femur joint, it defined class A as any column acetabular fracture; class B as any two-column acetabular fracture; class C as front, dome and posterior mixture acetabular fracture. Lower case English letters a, m, p represented front, dome, posterior fracture, respectively. Acetabular damage variables: 1 was simple displaced fractures; 2 was comminuted fractures; 3 was compression fractures. Pelvic ring lesions damage variables: alpha was sacroiliac joints or sacroiliac fracture horizontal separation deflection; beta was sacroiliac joints or sacroiliac fracture vertical separation deflection; gamma was pubic symphysis separation/superior and inferior ramus of pubis fracture deflection; alpha beta gamma delta was compound floating damage. Proximal humerus joint damage variables: I was femoral head fracture; II was femoral neck fracture; II was intertrochanteric fractures of femur; IV was I to III compound fracture. The ABC damage variable positioning system for acetabular fracture was made up by the above-mentioned variables. The statistics from March 1997 to February 2010 showed 1122 cases acetabular fractures with 18 cases of double side acetabular fracture and 1140 cases of acetabular fractures. The pelvics anterior-posterior view, ilium and obturator oblique view, and 2/3D-CT materials were analyzed and researched.
RESULTSEach damage variables distribution situation in 1140 cases of acetabular fracture involved A in 237 cases (20.8%), B in 605 cases (53.1%), C in 298 cases (26.1%);front column fracture in 808 cases(70.9%), dome fracture in 507 cases (44.5%), posterior fracture in 1026 cases (90%). Acetabular variables: variabe 1 in 203 cases of simple displaced fracture (17.8%); variabe 2 in 516 cases of comminuted fracture(45.3%); variabe 3 in 421 cases of compression fracture (36.9%); 249 cases of pelvic ring lesions damage (21.8%), 75 cases femoral head fracture (6.6%); 18 cases of double side acetabular fracture and relative pelvic ring and proximal humerus joint variables (1.58%). Key part and curative effect elements of 1140 cases acetabular fracture: 507 cases of dome or posterior acetabular fracture (44.5%); 421 cases of compression fracture (36.9%); 249 cases of pelvic ring variables (21.8%); 75 cases of proximal humerus joint variables (6.6%); 486 cases of simple Aa/pl/2,Bapl/2 acetabular fracture (42.6% ).
CONCLUSIONCompression fracture, especially defected compression fracture, takes important part in acetabular damage variables, and also presents that acetabular fracture with pelvic ring and proximal femoral damage variables are not rare at all. The relationship of the acetabular fracture damage variables, and its percentage shows the key points and elements in clinical treatment: weight-bearing to dome accounts for 44.5%; compression to defects account for 36.9%, pelvic ring to float accounts for 21.8%; dome fracture to double side fracture account for 6.6%. The system has significant guiding effects on clinic in terms of evaluation of injury severity, anatomic localization, difficulty index, alternative strategy, operative approach, effect of treatment,and prognosis. And the most important thing is that the system creates the comparison of damage variables in same type of fracture and the communication of homo-language and explores a new method.
Acetabulum ; injuries ; Adolescent ; Adult ; Aged ; Child ; Female ; Fractures, Bone ; classification ; diagnostic imaging ; Humans ; Male ; Medical Informatics ; methods ; Middle Aged ; Tomography, X-Ray Computed ; Young Adult
9.The non-replicating recombinant vaccinia virus expressing six genes of HIV-1 can be passaged stably in CEF.
Xiang-rong QI ; Xiang-min ZHANG ; Yao DENG ; Ying-ying GAO ; Rou-jian LU ; Xin MENG ; Wen-jie TAN ; Li RUAN
Chinese Journal of Virology 2011;27(2):135-143
To investigate the genetic stability (including the vector of vaccinia virus and six foreign genes: gp160, gag, pol, rev, tat and nef) of the HIV-1 non-replicating recombinant vaccinia virus (rNTV-C). rNTV-C was serially passaged to passage 25 (P25) in primary chicken embryo fibroblast (CEF). P9, P12, P15 and P25 were selected to study the genetic stability in four aspects, including the genetic stability of viral vector, the genetic stability of six foreign genes, the expressing stability of foreign genes and the genetic loss of foreign genes. The results showed that the viral vector was non-replicated vaccinia virus of Tiantan strain and was passaged stably; foreign gene sequences matched with designed sequences, the insert sites were right, and the nucleotide mutation rate was less than one over ten thousands within different passages of rNTV-C; the target proteins could be expressed effectively, and the expression level was stable within different passages of rNTV-C; the genetic loss of gag and nef was less than 5% within different passages of rNTV-C. The above results provided important data for the vaccine production.
Animals
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DNA, Recombinant
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genetics
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Fibroblasts
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metabolism
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virology
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Gene Expression
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Genes, Viral
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genetics
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Genetic Engineering
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methods
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Genetic Vectors
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genetics
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HIV-1
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genetics
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Sequence Analysis, DNA
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Vaccinia virus
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genetics

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