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Vesicular drug delivery systems for oral absorption enhancement

Chinese Chemical Letters 2024年第7期35卷 73-88页

作者： Linghui Zou Meng Cheng Kaili Hu jianfang feng Liangxing Tu Jiangxi University of Chinese Medicine Nanchang 330006China Guangxi University of Chinese Medicine Nanning 530200China Shanghai University of Traditional Chinese Medicine Shanghai 201203China

Oral administration is the most acceptable route of drug delivery at this stage due to its convenience,safety,and ***,drugs given orally are exposed to a complex gastrointestinal environment,causing a tremendous challenge for their successful absorption into the *** the past decades,researchers have developed various novel pharmaceutical technologies to improve oral absorption,among which the vesicular drug delivery system(like liposomes,niosomes and transfersomes)has received extensive ***,there have been several investigations confirming the improved effect of vesicular drug delivery systems on oral drug ***,the clinical translation of oral vesicular drug delivery systems has been less impressive than implied by the positive results,and few vesicular formulations for oral use have been marketed *** this background,this article provides an overview of the current applications and challenges associated with the vesicular delivery systems available for oral drug delivery,specifically liposomes,niosomes,transfersomes,chitosomes and *** composition,formation mechanism,drug delivery advantages and application cases of these carriers in oral drug delivery are *** possible mechanisms by which vesicular carriers enhance oral drug absorption are analyzed in terms of the in vivo process of oral ***,the challenges that oral vesicular carriers now face,such as safety,undefined in vivo fate,and scale-up production,are summarized,while possible strategies to deal with them are *** reviewing the aforementioned,it can facilitate a more comprehensive knowledge of vesicular systems that can be used for oral drug delivery,providing a theoretical basis and reference for the design of oral formulations.

关键词： Vesicular Oral Mechanism Drug delivery Liposome Niosomes Transfersomes Chitosomes Bilosomes

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紫苏叶HPLC指纹图谱建立及其抗流感病毒活性谱效关系研究

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中草药 2024年第1期55卷 287-296页

作者：刘振杰丘海芯甘金月奉建芳唐红珍谭小青杨海玲广西优势中成药与民族药开发工程技术研究中心广西中医药大学广西南宁530299 广西中药质量标准研究重点实验室广西壮族自治区中医药研究院广西南宁530022 安徽医学高等专科学校安徽合肥230601

目的研究紫苏叶Perillae Folium的化学成分,化学模式识别法建立紫苏叶HPLC指纹图谱,并研究其抗流感病毒活性,为其进一步开发利用提供依据。方法采用超高效液相色谱-三重四级杆飞行时间质谱联用(UPLC-Q-TOF-MS/MS)技术,鉴定紫苏叶的主要... 详细信息

目的研究紫苏叶Perillae Folium的化学成分,化学模式识别法建立紫苏叶HPLC指纹图谱,并研究其抗流感病毒活性,为其进一步开发利用提供依据。方法采用超高效液相色谱-三重四级杆飞行时间质谱联用(UPLC-Q-TOF-MS/MS)技术,鉴定紫苏叶的主要化学成分,建立HPLC指纹图谱,匹配共有峰并进行归属,通过对照品比对指认6种化学成分,使用SPSS 22.0、SIMCA 14.1软件进行聚类分析和主成分分析(principal component analysis,PCA),测定其抗流感病毒生物效价,并通过灰色关联分析(gray correlation analysis,GCA)建立其谱效关系。结果从紫苏叶中鉴定出47个化合物;选取了19个色谱峰作为指纹图谱的共有峰,通过聚类分析可将15批紫苏叶分为2类,PCA与聚类分析结果基本一致;15批不同产地的紫苏叶样品均具有抗流感病毒活性,其生物效价为6.21、5.58、4.19、8.19、6.09、5.82、6.10、5.36、5.54、10.86、4.74、5.78、3.78、7.98、5.65 U/mg。19个共有峰与抗病毒活性存在一定的关联度(0.82~0.97),各共有峰代表的化学成分对其抗病毒活性贡献的大小顺序为峰6(咖啡酸)、19(木犀草素)>2、8、9、12(阿魏酸)>4、5、15(芹菜素-7-O-二葡萄糖醛酸苷)>7、13>11>3、10、17>1、16(野黄芩苷)>14>18(迷迭香酸)。结论构建的紫苏叶抗流感病毒活性生物效价测定方法能关联其临床功效,而UPLC-Q-TOF-MS/MS法能快速鉴定紫苏叶的成分,结合指纹图谱和化学模式识别,发现紫苏叶抗病毒作用为“多成分”共同起效的结果,这将为其质量控制提供科学依据。

关键词：紫苏叶指纹图谱化学模式识别灰色关联分析生物评价抗流感病毒活性灰色关联度分析谱效关系咖啡酸木犀草素阿魏酸芹菜素-7-O-二葡萄糖醛酸苷野黄芩苷迷迭香酸

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降压肽益生菌羊乳发酵工艺优化及冷藏研究

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食品科技 2024年第4期49卷 77-83页

作者：焦孝平刘正鑫雷欢封建芳康红娟马琳舒国伟庆阳市科学技术开发中心甘肃庆阳745099 百跃羊乳(合水)古象有限公司甘肃庆阳745100 陕西科技大学食品科学与工程学院陕西西安710021

高血压是心血管类疾病高死亡率的主要原因之一,开发降压肽乳品预防和缓解高血压很有必要。文章以羊乳为原料,以血管紧张素转换酶(Angiotensin-I converting enzyme,ACE)抑制率为主要指标,采用完全析因设计对唾液链球菌嗜热亚种ST和鼠李... 详细信息

高血压是心血管类疾病高死亡率的主要原因之一,开发降压肽乳品预防和缓解高血压很有必要。文章以羊乳为原料,以血管紧张素转换酶(Angiotensin-I converting enzyme,ACE)抑制率为主要指标,采用完全析因设计对唾液链球菌嗜热亚种ST和鼠李糖乳酪杆菌LR22发酵羊乳产降压肽工艺及其冷藏进行了研究。结果表明,降压肽益生菌羊乳的最佳发酵条件为:菌株比例LR22:ST=1.2:1,42℃培养5 h,其ACE抑制率、吸光度值、酸度和感官评价分别为77.94%、0.282、96°T、7.45。随着冷藏时间的延长,其pH值逐渐减小,酸度逐渐增大,ACE抑制率、硬度、黏稠度、凝聚性与黏度指数均先增大后减小。研究结果可为降压肽益生菌乳制品的开发提供支持。

关键词：高血压羊乳降压肽鼠李糖乳酪杆菌完全析因设计冷藏

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Remodeling the blood–brain barrier microenvironment by natural products for brain tumor therapy

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Acta Pharmaceutica Sinica B 2017年第5期7卷 541-553页

作者： Xiao Zhao Rujing Chen Mei Liu jianfang feng Jun Chen Kaili Hu Murad Research Center for Modernized Chinese Medicine Institute of Interdisciplinary Integrative Medicine ResearchShanghai University of Traditional Chinese Medicine Key Laboratory of Smart Drug Delivery Fudan University Ministry of Education

Brain tumor incidence shows an upward trend in recent years; brain tumors account for 5% of adult tumors, while in children, this figure has increased to 70%. Moreover, 20%–30% of malignant tumors will eventually metastasize into the brain. Both benign and malignant tumors can cause an increase in intracranial pressure and brain tissue compression, leading to central nervous system(CNS) damage which endangers the patients' lives. Despite the many approaches to treating brain tumors and the progress that has been made, only modest gains in survival time of brain tumor patients have been achieved. At present, chemotherapy is the treatment of choice for many cancers, but the special structure of the blood–brain barrier(BBB) limits most chemotherapeutic agents from passing through the BBB and penetrating into tumors in the brain. The BBB microenvironment contains numerous cell types, including endothelial cells, astrocytes, peripheral cells and microglia, and extracellular matrix(ECM). Many chemical components of natural products are reported to regulate the BBB microenvironment near brain tumors and assist in their treatment. This review focuses on the composition and function of the BBB microenvironment under both physiological and pathological conditions, and the current research progress in regulating the BBB microenvironment by natural products to promote the treatment of brain tumors.

关键词： Blood–brain barrier Microenvironment Natural products Brain tumors Glioma Extracellular matrix

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Saline-alkali soil reclamation and utilization in China:progress and prospects

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Frontiers of Agricultural Science and Engineering 2024年第2期11卷 216-228页

作者： Guangzhou WANG Gang NI Gu feng Haley MBURRILL jianfang LI Junling ZHANG Fusuo ZHANG State Key Laboratory of Nutrient Use and Management(SKLNUM) College of Resources and Environmental SciencesNational Academy of Agriculture Green DevelopmentChina Agricultural UniversityBeijing 100193China The Institute of Ecology and Evolution University of OregonEugeneOR97403USA

Soil salinity is a global threat to the productivity of arable land. With the impact of population growth and development of social economy in China, the area of arable land has been shrinking in recent decades and is approaching a critical threshold of 120 Mha, the minimum area for maintaining the national food security. Saline-alkaline land, as important backup reserve, has been receiving increased attention as an opportunity to expand land resources. This review first summarizes the general principles and technologies of saline soil reclamation to support plant growth, including leaching salts or blocking the rise of salts, and soil fertility enhancement to improve the buffering *** the progress in this area in China is described including the customization of technologies and practices used in different saline-alkali regions. Following the soil management strategies, the concept of selecting crops for saline soil is proposed. This encompasses halophyte planting, salt-tolerant crop breeding and the application of saline-adapted functional microorganisms to improve the adaptation of crops. Finally, the current problems and challenges are evaluate, and future research directions and prospects proposed for managing this major soil constraint.

关键词： Food security land reserve reclamation saline-alkali soil utilization

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Pharmacological Theory of Traditional Chinese Medicine and Course Reform of Experimental Teaching under the Background of Courses on the Ideological and Political Dimension

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Asian Agricultural Research 2022年第8期14卷 68-70,76页

作者： Yunli TANG jianfang feng Rumei LU Chenyan LIANG College of Pharmacy Guangxi University of Chinese MedicineNanning 530299China

Pharmacology of traditional Chinese medicine is a bridge course linking traditional medicine and modern *** the past,the teaching often focused on the cultivation of basic theories and skills,but did not integrate into the systematic design of ideological and political *** to the characteristics of the course,this paper combines professional courses with ideological and political education from the aspects of teaching objectives,teaching contents,teaching methods,teaching resources and professional teachers’quality,so as to enhance students’recognition of Chinese excellent culture.

关键词： Courses on the ideological and political dimension Pharmacology of traditional Chinese medicine Teaching course

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Analysis on the Construction Path of Database of Zhuang and Yao Medicine Information Resources

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Medicinal Plant 2022年第6期13卷 31-34,43页

作者： Liang LI Cuiliu PAN Chenyan LIANG Shina QIN Yunli TANG jianfang feng College of Pharmacy Guangxi University of Chinese MedicineNanning 530200China Guangxi Dominant Proprietary Chinese Medicine and Ethnic Medicine Development Engineering and Technology Research Center Nanning 530200China Key Laboratory of Chinese Medicine Pharmacology Nanning 530200China Fangchenggang Hospital of Chinese Medicine Fangchenggang 538021China

In order to realize the sharing,exchange,protection and rational utilization of Zhuang and Yao medicine resources,the problems encountered in the development of Zhuang and Yao medicine industry can be solved by using modern information technology in accordance with the present situation of Zhuang and Yao medicine resources in Guangxi Zhuang Autonomous Region and the actual needs of the development of ethnic *** paper expounds the significance of constructing the database of Zhuang and Yao medicine information resources from three aspects:the inheritance and development of Zhuang and Yao medicine,the sustainable development of Zhuang and Yao medicine industry and the information service *** this basis,the principle and framework of constructing Zhuang and Yao medicine information resource database are put forward.

关键词： Zhuang and Yao medicine Information resources Database

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Effects of Ethyl Acetate Extract of Phyllanthus reticulatus Leaves on Autophagy-related Proteins Beclin-1,ATG5 and LC3 in Nude Mice Xenograft Model of HCC

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Medicinal Plant 2022年第3期13卷 43-47,52页

作者： Zhipeng XU Chenyan LIANG Cuiliu PAN Yunli TANG jianfang feng Tong HE Guangxi University of Chinese Medicine Nanning 530020 China Chengdu University of Traditional Chinese Medicine Chengdu 611137 China Wuxuan County Maternal and Child Health Care Hospital Laibin 545900 China

[Objectives]To explore the effects of ethyl acetate extract of Phyllanthus reticulatus leaves on autophagy-related proteins Beclin-1,ATG5 and LC3 by immunohistochemistry,and to preliminarily explore their effects on autophagy.[Methods]BEL-7404 Hepatocellular Carcinoma(HCC)nude mice model was established,and blank group(same volume of pure water),positive control group(20 mg/kg fluorouracil),high dose drug group(600 mg/kg),and medium dose drug group(300 mg/kg),and low dose drug group(150 mg/kg)were set *** 2 weeks of intragastric administration,the nude mice were sacrificed,and the tumor tissues were taken out,processed by immunohistochemistry,and then made into paraffin *** were taken under an optical microscope(10×40),and evaluation and analysis were performed with the aid of the Image-Pro Plus 6.0 image analysis *** were calculated using SPSS 20.0 *** effects of drugs on autophagy-related proteins LC3,Beclin-1 and ATG5 were observed.[Results]Compared with the blank group,the medium and high dose groups of ethyl acetate extract of *** leaves had the effect of promoting the increase of autophagy-related proteins LC3,Beclin-1 and ATG5(P0.05).[Conclusions]The ethyl acetate extract of *** leaves has a promoting effect on autophagy-related proteins LC3,Beclin-1,and ATG5.

关键词： Ethyl acetate extract of Phyllanthus reticulatus leaves Autophagy Hepatocellular Carcinoma(HCC) Nude mice

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口服水飞蓟素固体脂质纳米粒（SM-SLN）肝靶向性的动物实验研究

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高技术通讯 2005年第9期15卷 71-75页

作者：何军奉建芳蔡本琴侯世祥四川大学华西药学院成都610041 上海医药工业研究院药物制剂部上海200437 广西中医学院药学院

采用冷却-匀质法制备了平均粒径为170nm的水飞蓟素固体脂质纳米粒(SM-SLN),用其给小鼠灌胃后,采用高效液相法(HPLC)测定小鼠血浆和各脏器中的药物浓度,以相对摄取率(re)、靶向效率(te)和峰浓度比(Ce)三个指标定量地评价了SM-SLN的肝靶向... 详细信息

采用冷却-匀质法制备了平均粒径为170nm的水飞蓟素固体脂质纳米粒(SM-SLN),用其给小鼠灌胃后,采用高效液相法(HPLC)测定小鼠血浆和各脏器中的药物浓度,以相对摄取率(re)、靶向效率(te)和峰浓度比(Ce)三个指标定量地评价了SM-SLN的肝靶向性.结果表明,SM-SLN组中的肝脏相对于血浆和其它脏器的te值均大于1,且肝脏中的re值(7.50)、Ce值(8.12)均为最大值,说明SM-SLN具有良好的肝靶向性.SLN可以作为治疗肝脏疾病药物的良好肝靶向载体.

关键词：水飞蓟素,固体脂质纳米粒,肝靶向,水飞蓟素固体脂质纳米粒固体脂质纳米粒肝脏疾病水飞蓟素靶向性动物实验口服药物浓度高效液相法平均粒径

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Studies on the preparation and pharmacokinetics of puerarin microcrystals and nanocrystals for oral administration to rat

Studies on the preparation and pharmacokinetics of puerarin ...

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“好医生杯”中药制剂创新与发展论坛

作者： Liangxing Tu Yueneng Yi Wei Wu Fuqiang Hu Kaili Hu jianfang feng Murad Research Center for Modernized Chinese Medicine Shanghai University of Traditional Chinese Medicine School of Pharmacy Fudan University School of Pharmacy Zhejiang University

由中药葛根中提取而来的葛根素目前在临床上广泛用于心血管疾病的治疗。但由于其水溶性差和注射给药所带来的不良反应,目前迫切需要一种技术来用于葛根素口服给药制剂的开发。现如今,纳米结晶技术已慢慢成为难溶性药物口服制剂开发的首... 详细信息

由中药葛根中提取而来的葛根素目前在临床上广泛用于心血管疾病的治疗。但由于其水溶性差和注射给药所带来的不良反应,目前迫切需要一种技术来用于葛根素口服给药制剂的开发。现如今,纳米结晶技术已慢慢成为难溶性药物口服制剂开发的首选技术。在本研究中,我们分别采用高剪切分散法和高压均质法来制备粒径分别为1875.6 nm、525.8 nm的葛根素微米结晶和纳米结晶,并考察了不同粒径的制剂对于药物药动学的影响。同时我们采用DLS、DSC、XRD和SEM技术来对所制备的制剂进行表征,发现在制备过程中葛根素的晶型发生了变化并显示药物颗粒分散于HPMC中。在药动学的研究中,我们发现随着制剂粒径的减小,最大峰浓度(C)和曲线下面积(AUC)增加,同时消除率(CL/F)下降。纳米结晶的绝对生物利用度为21.44%,为葛根素原料药的7.6倍。以上实验结果显示,纳米结晶技术是一种能够有效提高葛根素口服生物利用度的技术。

关键词： puerarin nanocrystals microcrystals bioavailability particle size.

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