1.Development of oral preparations of poorly soluble drugs based on polymer supersaturated self-nanoemulsifying drug delivery technology.
Xu-Long CHEN ; Jiang-Wen SHEN ; Wei-Wei ZHA ; Jian-Yun YI ; Lin LI ; Zhang-Ting LAI ; Zheng-Gen LIAO ; Ye ZHU ; Yue-Er CHENG ; Cheng LI
China Journal of Chinese Materia Medica 2025;50(16):4471-4482
Poor water solubility is the primary obstacle preventing the development of many pharmacologically active compounds into oral preparations. Self-nanoemulsifying drug delivery systems(SNEDDS) have become a widely used strategy to enhance the oral bioavailability of poorly soluble drugs by inducing a supersaturated state, thereby improving their apparent solubility and dissolution rate. However, the supersaturated solutions formed in SNEDDS are thermodynamically unstable systems with solubility levels exceeding the crystalline equilibrium solubility, making them prone to drug precipitation in the gastrointestinal tract and ultimately hindering drug absorption. Therefore, maintaining a stable supersaturated state is crucial for the effective delivery of poorly soluble drugs. Incorporating polymers as precipitation inhibitors(PPIs) into the formulation of supersaturated self-nanoemulsifying drug delivery systems(S-SNEDDS) can inhibit drug aggregation and crystallization, thus maintaining a stable supersaturated state. This has emerged as a novel preparation strategy and a key focus in SNEDDS research. This review explores the preparation design of SNEDDS and the technical challenges involved, with a particular focus on polymer-based S-SNEDDS for enhancing the solubility and oral bioavailability of poorly soluble drugs. It further elucidates the mechanisms by which polymers participate in transmembrane transport, summarizes the principles by which polymers sustain a supersaturated state, and discusses strategies for enhancing drug absorption. Altogether, this review provides a structured framework for the development of S-SNEDDS preparations with stable quality and reduced development risk, and offers a theoretical reference for the application of S-SNEDDS technology in improving the oral bioavailability of poorly soluble drugs.
Solubility
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Administration, Oral
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Polymers/chemistry*
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Drug Delivery Systems/methods*
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Humans
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Emulsions/chemistry*
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Biological Availability
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Animals
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Pharmaceutical Preparations/administration & dosage*
2.Research of miR-508-3p involvement in ovarian cancer progression by regulating ZEB1
Yu-hong XU ; Shuai-ying ZHU ; Jiang-jing SHAN ; Wei-ping ZHENG ; Hui-ya ZHANG ; Yun-gen WANG
The Chinese Journal of Clinical Pharmacology 2025;41(2):193-197
Objective To investigate the expression of microRNA-508-3p(miR-508-3p)in epithelial ovarian cancer(EOC)tissue,its impact on the migration and invasion of ovarian cancer cells,and its regulatory relationship with zinc-finger E-box-binding homeobox 1(ZEB1).Methods The surgical resection of EOC cancer tissues and paired adjacent normal tissues were collected.SKOV3 cells were divided into the NC mimic group(transfected with NC mimic),miR-508-3p mimic group(transfected with miR-508-3p mimic),si-NC group(transfected with si-NC),si-ZEB1 group(transfected with si-ZEB1)and co-transfection group(co-transfected with si-ZEB1 and miR-508-3p mimic).The mRNA expression levels of miR-508-3p and ZEB1 in EOC cancer tissues,adjacent normal tissues and five groups of cells were measured by real-time quantitative polymerase chain reaction.The Transwell assay was used to detect the cell migration and invasion abilities.Results The relative expression levels of miR-508-3p in EOC tissues and adjacent normal tissues were 0.77±0.36 and 1.07±0.40,the relative expression levels of ZEB1 mRNA in EOC tissues and adjacent normal tissues were 2.10±1.21 and 1.29±0.95,and the differences were statistically significant(all P<0.01).The migration cell number of the NC mimic,miR-508-3p mimic,si-NC,si-ZEB1 and co-transfection groups was 633.00±32.49,319.20±19.89,650.40±25.85,375.00±17.25 and 129.40±17.10;the invasion cell number was 527.20±25.01,288.60±16.68,520.00±25.83,293.40±18.37 and 76.60±8.76;the relative expression levels of miR-508-3p were 1.05±0.37,3.94±1.21,1.01±0.21,1.26±0.34 and 3.40±0.41;the relative expression levels of ZEB1 mRNA were 1.00±0.04,0.58±0.05,1.00±0.08,0.54±0.07 and 0.29±0.03,respectively.The above indicators showed statistically significant differences between the miR-508-3p mimic group and the NC mimic group,between the si-NC group and the co-transfection group(P<0.01,P<0.05).Conclusion MiR-508-3p is lowly expressed in EOC cancer tissue,and it may inhibit the migration and invasion of ovarian cancer cells by targeting ZEB1 expression.
3.Research of miR-508-3p involvement in ovarian cancer progression by regulating ZEB1
Yu-hong XU ; Shuai-ying ZHU ; Jiang-jing SHAN ; Wei-ping ZHENG ; Hui-ya ZHANG ; Yun-gen WANG
The Chinese Journal of Clinical Pharmacology 2025;41(2):193-197
Objective To investigate the expression of microRNA-508-3p(miR-508-3p)in epithelial ovarian cancer(EOC)tissue,its impact on the migration and invasion of ovarian cancer cells,and its regulatory relationship with zinc-finger E-box-binding homeobox 1(ZEB1).Methods The surgical resection of EOC cancer tissues and paired adjacent normal tissues were collected.SKOV3 cells were divided into the NC mimic group(transfected with NC mimic),miR-508-3p mimic group(transfected with miR-508-3p mimic),si-NC group(transfected with si-NC),si-ZEB1 group(transfected with si-ZEB1)and co-transfection group(co-transfected with si-ZEB1 and miR-508-3p mimic).The mRNA expression levels of miR-508-3p and ZEB1 in EOC cancer tissues,adjacent normal tissues and five groups of cells were measured by real-time quantitative polymerase chain reaction.The Transwell assay was used to detect the cell migration and invasion abilities.Results The relative expression levels of miR-508-3p in EOC tissues and adjacent normal tissues were 0.77±0.36 and 1.07±0.40,the relative expression levels of ZEB1 mRNA in EOC tissues and adjacent normal tissues were 2.10±1.21 and 1.29±0.95,and the differences were statistically significant(all P<0.01).The migration cell number of the NC mimic,miR-508-3p mimic,si-NC,si-ZEB1 and co-transfection groups was 633.00±32.49,319.20±19.89,650.40±25.85,375.00±17.25 and 129.40±17.10;the invasion cell number was 527.20±25.01,288.60±16.68,520.00±25.83,293.40±18.37 and 76.60±8.76;the relative expression levels of miR-508-3p were 1.05±0.37,3.94±1.21,1.01±0.21,1.26±0.34 and 3.40±0.41;the relative expression levels of ZEB1 mRNA were 1.00±0.04,0.58±0.05,1.00±0.08,0.54±0.07 and 0.29±0.03,respectively.The above indicators showed statistically significant differences between the miR-508-3p mimic group and the NC mimic group,between the si-NC group and the co-transfection group(P<0.01,P<0.05).Conclusion MiR-508-3p is lowly expressed in EOC cancer tissue,and it may inhibit the migration and invasion of ovarian cancer cells by targeting ZEB1 expression.
4.Advances of artificial intelligence technology in the discovery and optimization of lead compounds
Zi-yue LI ; Kai-yuan CONG ; Shi-qi WU ; Qi-hua ZHU ; Yun-gen XU ; Yi ZOU
Acta Pharmaceutica Sinica 2024;59(9):2443-2453
In recent years, artificial intelligence (AI) technology has advanced rapidly and has been widely applied in various fields such as medicine and pharmacy, accelerating the drug development process. Focusing on the application of AI in the discovery and optimization of lead compounds, this review provides a detailed introduction to AI-assisted virtual screening and molecular generation methods for discovering lead compounds, while particularly highlighting the cases of AI-drived drugs into clinical trials. Additionally, we briefly outline the application of AI basic algorithm models in quantitative structure-activity relationship (QSAR) and drug repurposing, offering insights for AI-based drug discovery.
5.A multicenter study on human parainfluenza virus infections among children with community-acquired pneumonia from 2014 to 2020
Shiqi CAI ; Baoping XU ; Changchong LI ; Yun SUN ; Gen LU ; Rong JIN ; Yunxiao SHANG ; Yunlian ZHOU ; Ling CAO ; Aihuan CHEN ; Li DENG ; Yixiao BAO ; Limin NING ; Zhou FU ; Fang GU ; Shuilian YU ; Chunyan LIU ; Ju YIN ; Kunling SHEN ; Yun ZHU ; Zhengde XIE
Chinese Journal of Experimental and Clinical Virology 2023;37(5):472-479
Objective:To investigate the epidemiological and clinical characteristics of human parainfluenza viruses (HPIVs) infection among hospitalized children with community-acquired pneumonia (CAP) in China, and provide basic data for diagnosis, treatment and prevention of HPIVs infection.Methods:From November 2014 to February 2020, 5 448 hospitalized children with CAP were enrolled in 14 hospitals in 11 provinces and municipalities directly under the Central Government in southern China and northern China. Nasopharyngeal aspirates or throat swabs were collected, and the nucleic acids of 18 types respiratory viruses including HPIV1-4 were screened by suspension array technology. Demographic data and clinical information were collected for statistical analysis.Results:The total detection rate of HPIVs in 5 448 children with CAP was 8.83% (481/5 448), and the detection rate in males was higher than that in females (62.79% vs. 37.21%; χ2=0.000, P=0.992). The detection rate of HPIVs in 1~< 3 years age group was higher than that in other age groups, and the difference was statistically significant ( χ2=61.893, P<0.001). The detection rate of HPIVs in the northern region was higher than that in the southern region (9.02% vs 8.65%), but the difference was not statistically significant ( χ2=0.239, P=0.625). The prevalence of HPIV1-4 in northern and southern China was not completely same. HPIV1 was mainly prevalent in autumn in both northern and southern regions. HPIV2 was prevalent in summer in northern China, and the detection rate was low in southern China. HPIV3 reached its peak in both spring and summer in both northern and southern China, but its duration was longer in southern China than in northern China. HPIV4 is mainly popular in autumn in both southern China and northern China. Among 481 children infected with HPIVs, 58.42% (281/481) were infected with HPIV alone, and the main clinical manifestations were cough (90.75%) and fever (68.68%). Out of the HPIV-positive cases, 42.62% (205/481) were co-infected with another type of HPIV or a different virus, while 11.43% (55/481) had co-infections with two or more different viruses. HPIV3 was the most common type of co-infection with other viruses. HPIV3 infection accounted for the largest proportion (76.80%) in 47 HPIVs-positive children with severe pneumonia. Conclusions:HPIVs is one of the most important pathogens causing CAP in children in China, and children under 3 years of age are the main populations of HPIVs infection. The prevalence characteristics of all types of HPIVs in children in the north and south are not completely same. HPIV3 is the dominant type of HPIV infections and causes more severe diseases.
6.Analysis of respiratory syncytial virus infection in hospitalized children with acute lower respiratory tract infection in China from 2017 to 2020.
Yun ZHU ; Gen LU ; Rong JIN ; Yun SUN ; Yun Xiao SHANG ; Jun Hong AI ; Ran WANG ; Xiang Peng CHEN ; Ya Li DUAN ; Meng ZHANG ; Chang Chong LI ; Baoping XU ; Zhengde XIE
Chinese Journal of Preventive Medicine 2022;56(12):1739-1744
Objective: To understand the detection rate, epidemic pattern of respiratory syncytial virus (RSV) in hospitalized children with acute lower respiratory tract infection (ALRTI) in China. Methods: From June 2017 to March 2020, a prospective multi-center study on the viral aetiology among hospitalized children with ALRTI was conducted in six pediatrics hospital of North China, Northeast, Northwest, South China, Southeast, and Southwest China. A total of 2 839 hospitalized children with ALRTI were enrolled, and the respiratory specimens were collected from these cases. A multiplex real-time RT-PCR assay were employed to screen the respiratory viruses, and the molecular epidemiological and clinical characteristics of children infected with RSV were analyzed. Results: The positve rate of RSV was 18.6% (528/2 839), and the positive rate of RSV in different regions ranged from 5.5% to 44.3%. The positive rate of RSV in male was higher than that in female (20.2% vs 16.3%), and there was a significant statistically difference between two groups (χ2=6.74, P=0.009). The positive rate of RSV among children under 5 years old was higher than that among children older than 5 years old (22.3% vs 4.5%), and there was a significant statistically difference between two groups (χ2=97.98,P<0.001). The positive rate of RSV among the <6 months age group was higher than that of other age groups (all P<0.05). During January 2018 and December 2019, RSV was detected in almost all through the year, and showed peaks in winter and spring. RSV-positive cases accounted for 17.0% (46/270) among children with severe pneumonia, including 36 cases infected with RSV alone. Conclusion: RSV is an important viral pathogen in children under 5 years old with ALRTI in China. The virus can be detected almost all through the year and reached the peak in winter and spring. RSV could lead to severe pneumonia in children and caused huge threaten to children's health.
Child
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Humans
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Male
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Female
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Infant
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Child, Preschool
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Respiratory Syncytial Virus Infections/epidemiology*
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Child, Hospitalized
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Prospective Studies
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Respiratory Tract Infections/epidemiology*
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Respiratory Syncytial Virus, Human
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China/epidemiology*
7.Expert consensus on clinical application of pulse oximetry in children
Yuejie ZHENG ; Adong SHEN ; Baoping XU ; Hanmin LIU ; Xing CHEN ; Lili ZHONG ; Guangmin NONG ; Gen LU ; Shenggang DING ; Zhiying HAN ; Yun SUN ; Qiang CHEN ; Yi JIANG ; Xiaoping ZHU ; Suping TANG ; Xiufang WANG ; Yong YIN ; Shuhua AN ; Ju YIN ; Fengxia XUE ; Xiaoli LIU ; Miao LIU ; Yonghong YANG ; Kunling SHEN
Chinese Journal of Applied Clinical Pediatrics 2022;37(23):1761-1772
Hypoxemia is a common complication of pneumonia, asthma, and bronchopulmonary dysplasia in children.Rapid identification of hypoxemia is of great significance for the disposal and management of critical children.Pulse oximetry is recognized by the World Health Organization as the best way to monitor hypoxemia in children, and it can monitor pulse oxygen saturation noninvasively and continuously.Based on the related literature at home and abroad, combined with the clinical needs of pediatrics, the " Expert consensus on clinical application of pulse oximetry in children" is formulated to improve the understanding of pediatricians and nurses on the application in pediatric clinical practice, principle, operation techniques, and limitations of pulse oximetry.
8.Study on knowledge, attitudes and practices of pulse oximetry among pediatric healthcare providers in China and their influencing factors
Fengxia XUE ; Yuejie ZHENG ; Adong SHEN ; Hanmin LIU ; Xing CHEN ; Lili ZHONG ; Guangmin NONG ; Xin SUN ; Gen LU ; Shenggang DING ; Yuanxun FANG ; Jiahua PAN ; Zhiying HAN ; Yun SUN ; Qiang CHEN ; Yi JIANG ; Xiaoping ZHU ; Suping TANG ; Xiufang WANG ; Changshan LIU ; Shaomin REN ; Zhimin CHEN ; Deyu ZHAO ; Yong YIN ; Rongfang ZHANG ; Ming LI ; Yunxiao SHANG ; Yaping MU ; Shuhua AN ; Yangzom YESHE ; Peiru XU ; Yan XING ; Baoping XU ; Jing ZHAO ; Shi CHEN ; Wei XIANG ; Lihong LI ; Enmei LIU ; Yuxin SONG ; Yonghong YANG ; Kunling SHEN
Chinese Journal of Applied Clinical Pediatrics 2022;37(23):1807-1812
Objective:To investigate the knowledge, attitudes, and practices (KAP) of pulse oximetry among pediatric healthcare providers in China and analyze the factor influencing the KAP.Methods:A self-developed questionnaire was used for an online research on the KAP of 11 849 pediatric healthcare providers from 31 provinces, autonomous regions, and municipalities of China from March 11 to 14, 2022.The factors influencing the KAP of pulse oximetry among pediatric healthcare providers were examined by Logistic regression. Results:The scores of KAP, of pulse oximetry were 5.57±0.96, 11.24±1.25 and 11.19±4.54, respectively.The corresponding scoring rates were 69.61%, 74.95%, and 55.99%, respectively. Logistic regression results showed that the gender and working years of pediatric healthcare providers, the region they were located, and whether their medical institution was equipped with pulse oximeters were the main factors affecting the knowledge score (all P<0.05). Main factors influencing the attitude score of pediatric healthcare providers included their knowledge score, gender, educational background, working years, region, medical institution level, and whether the medical institution was equipped with pulse oximeters (all P<0.05). For the practice score, the main influencing factors were the knowledge score, gender, age, and whether the medi-cal institution was equipped with pulse oximeters (all P<0.05). Conclusions:Chinese pediatric healthcare providers need to further improve their knowledge about and attitudes towards pulse oximetry.Pulse oximeters are evidently under-used.It is urgent to formulate policies or guidelines, strengthen education and training, improve knowledge and attitudes, equip more institutions with pulse oximeters, and popularize their application in medical institutions.
9. MicroRNA-128-3p inhibiting epithelial-mesenchymal transition of ovarian cancer cells by regulating zince finger E-bonx binding homeobox 1
Yu-Hong XU ; Hui-Ya ZHANG ; Yun-Gen WANG ; Jun-Xia CHEN
Acta Anatomica Sinica 2022;53(6):762-768
Objective To investigate the effect of mircoRNA-128-3p (miR-128-3p) on epithelial-mesencfrymal transition (EMT) of ovarian cancer cells and its regulatory mechanism on zinc finger E-box binding homobox 1(ZEB1). Methods Real-time PCR technology was used to detect the expression of miR-128-3p in epithelial ovarian cancer tissue (EOC) and adjacent normal tissue (30 cases each), and to observe whether there was a difference. Two human ovarian cancer cell lines, SK0V3 and A2780, were selected and transfected respectively. MiR-128-3p mimic (miR-128-3p mimic group) and negative control mimic (NC mimic group) were used to detect the expression of miR-128-3p in 4 groups by Real-time PCR to verify the interference effect. Transwell assay was used. The migration and invasion abilities of the four groups of cells were observed. The regulatory relationship between miR-128-3p and ZEBl was verified by dual luciferase assay, and the expression level of ZEBl protein after overexpression of miR-128-3p was detected by Western blotting; pcDNA-ZEBl was transfected into SK0V3 and A2780 cell lines to make it overexpression of ZEBl was divided into NC mimic group, miR-128-3p mimic group, and miR-128-3p mimic+pcDNA-ZEBl group. Western blotting was used to detect the EMT-related protein E-cadherin in 6 groups of cells and the expression level of vimentin. Results Real-time PCR result showed that the expression of miR-128-3p in EOC tissues decreased compared with that in adjacent tissues (P < 0. 01); The relative expression of miR-128-3p in the miR-128-3p mimic group was higher than that in the NC mimic group, while the numbers of migrating cells and invasive cells were lower than those in the NC mimic group (P < 0 . 0 1) . The result of dual luciferase experiments showed that miR-128-3p had a negative regulatory effect on ZEBl. In SK0V3 and A2780 cells, the relative expression of ZEBl protein in the miR-128-3p mimic group was lower than that in the NC mimic group, while the relative protein expression of E-cadhein was higher than that in the NC mimic group (P < 0 . 0 1) . The relative protein expression of E-cadhein in the miR-128-3p mimic+pcDNA-ZEBl group was lower than that in the miR-128-3p mimic group (P < 0 . 0 1) . In SKOV3 and A2780 cells, the relative protein expression of vimentin in the miR-128-3p mimic group was lower than that in the NC mimic group, and the relative protein expression of vimentin in the miR-128-3p mimic+pcDNA-ZEBl group was higher than that in the miR-128-3p mimic group (P < 0 . 0 1) . Conclusion The expression of miR-128-3p decreases in epithelial ovarian cancer tissues, which ma)' be due to the regulation of ZEBl to affect the expression of EMT-related proteins and participate in the EMT process of ovarian cancer cells.
10.Study on the clinical epidemiological characteristics of human rhinovirus infection in children with community-acquired pneumonia
Junhong AI ; Gen LU ; Yun SUN ; Changchong LI ; Rong JIN ; Yunxiao SHANG ; Baoping XU ; Zhengde XIE
Chinese Journal of Applied Clinical Pediatrics 2021;36(24):1866-1870
Objective:To analyze the dominant genotypes and epidemic characteristics of human rhinovirus (HRV) in pediatric community-acquired pneumonia (CAP) in China.Methods:Between June 2017 to December 2019, throat swabs or nasopharyngeal aspirates were collected from pediatric CAP patients hospitalized in 6 medical institutions in Southern and Northern China (bounded by Qinling and Huaihe River), respectively.A total of 16 species of common respiratory viruses were screened using respiratory pathogen detection kits.Samples with positive HRV were genotyped for further epidemiological analysis.Results:The total detection rate of HRV in pediatric CAP (2 913 cases) was 12.2%(356 cases) in this study, which was 10.3%(145/1 410 cases) and 14.0%(211/1 503 cases) in Northern and Southern China, respectively.The detection rate of HRV in the Southern region was significantly higher than that in the Northern region, the difference was statistically significant( χ2=9.562, P=0.002). Epidemiological analysis showed that the distribution of HRV-positive cases in the Northern region was similar in all age groups, while 90.5% of positive cases in the Southern region were infants under 3 years.Classified by seasonal distribution, HRV-positive cases in the Northern region were mainly distributed in summer and autumn, while those in the Southern region were mainly distributed in spring and autumn.The coinfection rate of HRV and other pathogens was 40.7%, which was significantly higher in the Southern region than that of Northern region (49.0% vs.28.0%), the difference was statistically significant( χ2=15.801, P<0.001). The most common pathogens mixed with HRV were respiratory syncytial virus (RSV), human boca virus (HBOV) and parainfluenza virus type Ⅲ (PIV3) in the Northern region, with the mixed infection rate of 5.0%, 5.0% and 4.0%, respectively, which were RSV, PIV3 and human metapneumovirus (HMPV) in the Southern region, with the mixed infection rate of 9.0%, 7.0% and 6.0%, respectively.The genotyping results showed that all three HRV genotypes were detected.HRV-A (118/220 cases) was the dominant genotype, followed by HRV-C(82/220 cases). Conclusions:The detection rate of HRV in pediatric CAP cases is 12.2% in this study.There are significant differences in age and seasonal distribution of HRV-positive cases in the Southern and Northern regions.Coinfection of HRV and other pathogens is detected.The coinfection rate is significantly higher in the Southern region than that in the Northern region.HRV-A is the dominant genotype, followed by HRV-C.

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