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Semi-solid materials for controlled release drug formulation: current status and future prospects

Michelle TRAN,Chun WANG

《化学科学与工程前沿（英文）》 2014年 第8卷 第2期   页码 225-232 doi: 10.1007/s11705-014-1429-7

摘要： Semi-solid materials represent an important category of inactive ingredients (excipients) of pharmaceutical products. Here we review several common semi-solid polymers currently used in the controlled release formulations of many drugs. These polymers are selected based on their importance and broad scope of application in FDA-approved drug products and include several polysaccharides (cellulose, starch, chitosan, alginate) and carbomers, a group of mucoadhesive synthetic polymers. Glyceride-based polymers used in self-emulsifying drug delivery systems (SEDDS) will also be discussed for its importance in formulating poorly water-soluble drugs. Unique features and advantages of each type of semi-solid materials are discussed and examples of their use in oral delivery of drugs are provided. Finally, future prospects of developing new and better semi-solid excipients are discussed with the objective of facilitating clinical translation.

关键词： controlled release     drug delivery     semi-solids     polymer     excipient    

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Controlled drug release of 5-amino salicylic acid by poly(2-hydroxyethylmethacrylate) grafted agar

G. Usha RANI,Kartick Prasad DEY,Srijita BHARTI,Sumit MISHRA

《化学科学与工程前沿（英文）》 2014年 第8卷 第4期   页码 465-470 doi: 10.1007/s11705-014-1452-8

摘要： The utilization of poly (2-hydroxyethylmethacrylate) grafted agar (Ag-g-P(HEMA)) as a matrix for the controlled release of 5-aminosalicylic acid was investigated. Grafted copolymers of 2-hydroxyethylmethacrylate (HEMA) monomers on agar were synthesized by microwave assisted method. drug release studies were performed at pH values of 2 and 7 in order to investigate the possibility of pH triggered release for colon targeted drug delivery. Further, the percent grafting . (the time taken for release of 50% of the enclosed drug) value was studied and the results indicate that it may be possible to develop a programmable drug release matrix based on grafted polysaccharide. Ag-g-P(HEMA) appears to be a useful matrix for controlled release.

关键词： agar     controlled drug release     5-Amino salicylic acid     poly(2-hydroxyethylmethacrylate) grafted agar    

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Biodegradable polymethacrylic acid grafted psyllium for controlled drug delivery systems

Ranvijay KUMAR, Kaushlendra SHARMA

《化学科学与工程前沿（英文）》 2013年 第7卷 第1期   页码 116-122 doi: 10.1007/s11705-013-1310-0

摘要： Polymethacrylic acid (PMA) was synthesized on the backbone of psyllium (Psy) by a microwave assisted method to prepare polymeric grafted materials designated as (Psy- -PMA). Various grades of Psy- -PMA were prepared by changing the degree of grafting from 35%–58% and the materials were then made into tablets. Swelling and biodegradability studies of the tablets were carried out. Acetyl salicylic acid was incorporated in the various Psy- -PMA samples and tablets were prepared to study the in vitro drug release in acidic (pH= 4), neutral (pH= 7), and basic (pH= 9) media. In the acidic medium, the swelling was more than 1300%. In addition, the biodegradable Psy- -PMA had the highest drug release in the acidic medium. This may be attributed to Fickian diffusion since the drug and the medium in which it was released have the same acidic nature.

关键词： psyllium     acetyl salicylic acid     in-vitro drug release     swelling     biodegradation    

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Nanostructured hollow spheres of hydroxyapatite: preparation and potential application in drug delivery

Xiaojing ZHANG, Weixin ZHANG, Zeheng YANG, Zhao ZHANG

《化学科学与工程前沿（英文）》 2012年 第6卷 第3期   页码 246-252 doi: 10.1007/s11705-012-1299-9

摘要： A solvothermal method has been successfully used to prepare nanostructured hydroxyapatite (HA) hollow spheres with average diameters of about 500 nm and shell thicknesses of about 100 nm in a glycerin/water mixed solvent. Transmission electron microscopy (TEM) and field-emission scanning electron microscopy (FESEM) images show that the shells of the HA hollow spheres are actually composed of nanosheets with thicknesses of about 10 nm. By tuning the glycerin/water volume ratio, two other kinds of HA solid spheres with average diameters of about 6 or 20 μm were assembled from nanoflakes. The properties of the different kinds of spheres as drug delivery carriers were evaluated. Ibuprofen (IBU) was chosen as the model drug to load into the HA samples. The nanostructured HA samples showed a slow and sustained release of IBU. The HA hollow spheres exhibited a higher drug loading capacity and more favorable release properties than the HA solid spheres and thus are very promising for controlled drug release applications.

关键词： hydroxyapatite     hollow spheres     synthesis     drug release    

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Design of nanocarriers for efficient cellular uptake and endosomal release of small molecule and nucleic

Vaibhav Mundra, Ram I. Mahato

《化学科学与工程前沿（英文）》 2014年 第8卷 第4期   页码 387-404 doi: 10.1007/s11705-014-1457-3

摘要： There are many challenges in developing efficient and target specific delivery systems of small molecule and nucleic acid drugs. Cell membrane presents one of the major barriers for the penetration of hydrophilic macromolecules across the plasma membrane. Nanocarriers have been designed to enhance their cellular uptake via endocytosis but following their cellular uptake, endosomal escape is the rate limiting step which restricts the value associated with the enhanced uptake by nanocarriers. Viruses are an excellent model for efficient cytosolic delivery by nanocarriers. Viruses exploit intracellular cues to release the genome to cytosol. In this review, we first discuss different endocytic uptake pathways and endosomal escape mechanisms. We then summarize the existing tools for studying the intracellular trafficking of nanocarriers. Finally, we highlight the important design elements of recent virus-based nanocarriers for efficient cellular uptake and endosomal escape.

关键词： nanocarrier     cellular uptake     endosomal release     nucleic acid drug    

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Synthesis and characterization of biocompatible polyurethanes for controlled release of hydrophobic and

Juichen YANG,Hong CHEN,Yuan YUAN,Debanjan SARKAR,Jie ZHENG

《化学科学与工程前沿（英文）》 2014年 第8卷 第4期   页码 498-510 doi: 10.1007/s11705-014-1451-9

摘要： Design of biocompatible and biodegradable polymer systems for sustained and controlled release of bioactive agents is critical for numerous biomedical applications. Here, we designed, synthesized, and characterized four polyurethane carrier systems for controlled release of model drugs. These polyurethanes are biocompatible and biodegradable because they consist of biocompatible poly(ethylene glycol) or poly(caprolactone diol) as soft segment, linear aliphatic hexamethylene diisocyanate or symmetrical aliphatic cyclic dicyclohexylmethane-4,4′-diisocyanate as hard segment, and biodegradable urethane linkage. They were characterized with Fourier transform infrared spectroscopy, atomic force microscope, and differential scanning calorimetry, whereas their degradation behaviors were investigated in both phosphate buffered saline and enzymatic solutions. By tuning polyurethane segments, different release profiles of hydrophobic and hydrophilic drugs were obtained in the absence and presence of enzymes. Such difference in release profiles was attributed to a complex interplay among structure, hydrophobicity, and degradability of polyurethanes, the size and hydrophobicity of drugs, and drug-polymer interactions. Different drug-polyurethane combinations modulated the distribution and location of the drugs in polymer matrix, thus inducing different drug release mechanisms. Our results highlight an important role of segmental structure of the polyurethane as an engineering tool to control drug release.

关键词： phase structure     degradation     polyurethanes     controlled release     drug delivery    

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A novel cataplasma matrix of traditional Chinese medicine

Jing TIAN, Xiaolei ZHANG, Xueqin ZHOU,

《化学科学与工程前沿（英文）》 2010年 第4卷 第1期   页码 91-95 doi: 10.1007/s11705-009-0304-4

摘要： The aim of this paper was to develop a cataplasma matrix that can be applicable to both watersoluble and liposoluble drugs. The gellan gum and konjaku were employed as the scaffold materials of the matrix. With polyacrylic acid sodium and oligosaccharides as tacktifier, the formula of the cataplasma matrix was optimized in the orthogonal method as: gellan gum 0.4 g, xanthan€gum 0.03 g, konjac glue 0.1 g, glycerin 4 g, Gluco-Adhesive T (GAT) 6 g, Gluco-Adhesive E (GAE) 6 g, polyacrylic acid sodium 0.22 g, and sorbitol 3 g. The 180° peel strength, the tensile strength and the elongation at break was 3.043 N, 0.275 MPa and 91.05%, respectively. Furthermore, the drug-compatibilities of the matrix were investigated with baicalin, berberine and curcumin, which were used as the models of hydrophilic, poor-water-soluble and hydrophobic ingredients. The drug contents could reach 4.12% , 2.42% and 3.75%, while the release rate were measured as, 361.79, 55.85 and 104.41 μg·cm·hfor baicalin, berberine and curcumin, respectively. These results indicated that the obtained matrix had good drug-compatibility and drug-release properties for different ingredients.

关键词： drug-release     applicable     berberine     curcumin     different    

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Taking advantage of drug resistance, a new approach in the war on cancer

null

《医学前沿（英文）》 2018年 第12卷 第4期   页码 490-495 doi: 10.1007/s11684-018-0647-7

摘要：

Identification of the driver mutations in cancer has resulted in the development of a new category of molecularly targeted anti-cancer drugs. However, as was the case with conventional chemotherapies, the effectiveness of these drugs is limited by the emergence of drug-resistant variants. While most cancer therapies are given in combinations that are designed to avoid drug resistance, we discuss here therapeutic approaches that take advantage of the changes in cancer cells that arise upon development of drug resistance. This approach is based on notion that drug resistance comes at a fitness cost to the cancer cell that can be exploited for therapeutic benefit. We discuss the development of sequential drug therapies in which the first therapy is not given with curative intent, but to induce a major new sensitivity that can be targeted with a second drug that selectively targets the acquired vulnerability. This concept of collateral sensitivity has hitherto not been used on a large scale in the clinic and holds great promise for future cancer therapy.

关键词： cancer     drug resistance     genetic screens     senescence     targeted therapy    

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Protein microspheres for pulmonary drug delivery

Yongda SUN,

《化学科学与工程前沿（英文）》 2010年 第4卷 第1期   页码 82-86 doi: 10.1007/s11705-009-0307-1

摘要： A new supercritical fluid (SCF) technique was developed for the preparation of microspheres for pulmonary drug delivery (PDD). This technique, based on the anti-solvent process, has incorporated advanced engineering design features to enable improved control of the particle formation process. Human recombinant insulin (HRI) was used as a model compound to evaluate the efficiency of this SCF process. An aqueous solution of HRI with a co-solvent was sprayed into high pressure carbon dioxide that extracted the solvent and water, leading to a dry fine powder with good particle size distribution and near ideal morphology for pulmonary drug delivery.

关键词： advanced engineering     improved     pressure     aqueous     technique    

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Study on the NOx release rule along the boiler during pulverized coal combustion

JIN Jing, ZHANG Zhongxiao, LI Ruiyang

《能源前沿（英文）》 2007年 第1卷 第1期   页码 91-95 doi: 10.1007/s11708-007-0009-7

摘要： Numerical simulation and experimental study on NO release along the boiler during pulverized coal combustion have been conducted. With the increase of temperature the NO emission increased and the peak value of NO release moved forward. But when the temperature increased to a certain degree, NO emission began to reduce. NO emission increased with the increase of nitrogen content of coal. The peak value of NO release moved backwards with the increase of coal rank. NO emission increased obviously with the increase of stoichiometric ratio. There existed a critical average diameter of the pulverized coal (). If "d, NO emission reduced with the decrease of pulverized coal size. If >, NO emission reduced with the increase of the pulverized coal size. The results showed that the simulation results are in agreement with the experimental results for concentration distribution of NO along the axis of the furnace.
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Capacity estimation and preliminary strategy for reducing the release of dioxins in China

YU Gang, ZHANG Qing, HUANG Jun, CAI Zhenxiao, SUI Qian

《环境科学与工程前沿（英文）》 2007年 第1卷 第1期   页码 13-17 doi: 10.1007/s11783-007-0002-8

摘要： As a party of the Stockholm Convention on Persistent Organic Pollutants, China must submit its national implementation plan (NIP) for this convention. The strategy and action plan for reducing the release of dioxins in China are the most important components of the NIP. Three problems are key points for developing such strategy and action plan what are the key sources for applying the best available technology/best environmental practice (BAT/BEP) to reduce the release of dioxins? How about the capacity for reducing the dioxins release from the key sources? Where are the areas of priority for applying BAT/BEP? This paper shows the efforts towards the solution of these problems. The list of key sources covering about half of the total dioxins release was determined considering four criteria. The capacity of key sources were estimated based on the difference between the emission factor corresponding to the actual situation in 2004 and that corresponding to the scenario that all key sources have been applied BAT/BEP to reduce the dioxins release. The priority analysis using the geographical information system (GIS) tool has revealed that eastern provinces should be of high priority in the future reduction activities of dioxins release in China.

关键词： GIS     difference     capacity     scenario     implementation    

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functional supramolecular nanoparticles based on pillar[5]arene for controlled generation, storage and release

《化学科学与工程前沿（英文）》 2023年 第17卷 第3期   页码 307-313 doi: 10.1007/s11705-022-2216-5

摘要： The storage and controlled release of singlet oxygen (1O2) have attracted increasing attention due to the wide application and microsecond lifetime of 1O2 in water. Herein we provide an integrated nanoplatform consisting of a diphenylanthracene derivative, a water-soluble pillar[5]arene and a photosensitizer tetrakis(4-hydroxyphenyl)porphyrin (TPP), that may provide the controlled generation, storage and release of singlet oxygen. We design a new diphenylanthracene derivative with two trimethylammonium bromide groups on both ends that can be well recognized by the pillar[5]arene. The formed nanocarriers can be used to load TPP through their supramolecular self-assembly. The resulting nanoparticles show good water-solubility and uniform spherical morphology. After laser irradiation (660 nm), the nanoparticles exhibit excellent ability for the generation and storage of 1O2. When the irradiated nanoparticles are heated above 80 °C, 1O2 can be released from the system. Therefore, in this paper we pioneer the use of noncovalent interaction to integrate the diphenylanthracene derivatives and photosensitizers into one functional system, which provides a new strategy for the controlled generation, storage and release of singlet oxygen. We believe this groundbreaking strategy will have a great potential in providing necessary amounts of 1O2 for the photodynamic therapy of tumors in dark.

关键词： storage and controlled release of singlet oxygen     supramolecular nanoparticles     noncovalent interactions     pillararenes     diphenylanthracene     photosensitizers    

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Phosphorus release potential and pollution characteristics of sediment in downstream Nansi Lake, China

Zhijian LI, Qinyan YUE, Baoyu GAO, Yanwen WANG, Qing LIU

《环境科学与工程前沿（英文）》 2012年 第6卷 第2期   页码 162-170 doi: 10.1007/s11783-011-0313-7

摘要： The research aimed to evaluate present and potential phosphorous pollution due to high sedimentary phosphorus load and release from sediment, when external phosphorus was reduced in downstream Nansi Lake. Pollution load of the sediment and overlying water was investigated. Kinetics and isotherms of adsorption/release of sedimentary phosphorus were studied to determine equilibrium phosphate concentration (EPC ) and release potential. Kinetics of phosphorus adsorption on sediment and release from sediment were well described by both the pseudo-first-order rate equation and the pseudo-second-order rate equation, but more appropriate to the pseudo-second-order rate equation with the adsorption/release capacity more close to the measured values, suggesting that the processes were chemically rate controlled and dependent on adsorption capacity. Soluble reactive phosphorus (SRP) sorption isotherms on sediment were best fitted by the modified Langmuir model indicating a monolayer adsorption. By comparing EPC and SRP of water, the status (adsorption, releasing or in equilibrium) of sediment phosphorus could be determined. The sediments at site S1, S3, S4, S5, and S7 where the EPC s were greater than the SRPs, had a potential to release phosphorus into the water column. However, those sediments at S9, S10, and S12, where the EPC s were approximately equal to the SRPs, were in impermanent equilibrium with overlying water in status of phosphorus, the sediments can be likely to release phosphorus to the water column once the equilibrium was broken. Therefore, sedimentary phosphorus can be a secondary pollution source in downstream Nansi Lake.

关键词： Nansi Lake     sediment     phosphorus     release potential     equilibrium phosphate concentration    

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Prevalence of antifolate drug resistance markers in in China

《医学前沿（英文）》 2022年 第16卷 第1期   页码 83-92 doi: 10.1007/s11684-021-0894-x

摘要： The dihydrofolate reductase (dhfr) and dihydropteroate synthetase (dhps) genes of Plasmodium vivax and antifolate resistance-associated genes were used for drug resistance surveillance. A total of 375 P. vivax isolates collected from different geographical locations in China in 2009–2019 were used to sequence Pvdhfr and Pvdhps. The majority of the isolates harbored a mutant type allele for Pvdhfr (94.5%) and Pvdhps (68.2%). The most predominant point mutations were S117T/N (77.7%) in Pvdhfr and A383G (66.8%) in Pvdhps. Amino acid changes were identified at nine residues in Pvdhfr. A quadruple-mutant haplotype at 57, 58, 61, and 117 was the most frequent (57.4%) among 16 distinct Pvdhfr haplotypes. Mutations in Pvdhps were detected at six codons, and the double-mutant A383G/A553G was the most prevalent (39.3%). Pvdhfr exhibited a higher mutation prevalence and greater diversity than Pvdhps in China. Most isolates from Yunnan carried multiple mutant haplotypes, while the majority of samples from temperate regions and Hainan Island harbored the wild type or single mutant type. This study indicated that the antifolate resistance levels of P. vivax parasites were different across China and molecular markers could be used to rapidly monitor drug resistance. Results provided evidence for updating national drug policy and treatment guidelines.

关键词： drug resistance     antifolates     molecular markers     Plasmodium vivax     China    

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Clinical analysis of 275 cases of acute drug-induced liver disease

LI Lei, JIANG Wei, WANG Jiyao

《医学前沿（英文）》 2007年 第1卷 第1期   页码 58-61 doi: 10.1007/s11684-007-0012-8

摘要： In order to analyze the causative drugs, clinical manifestation and pathological characteristics of the patients with acute drug-induced liver disease, from January 2000 to December 2005, 275 cases diagnosed as acute drug-induced liver diseases according to Maria Criterion and hospitalized in Zhongshan Hospital of Fudan University were retrospectively reviewed. Each was determined by drug history, clinical symptoms and signs, laboratory tests and therapeutic effects. In 41 cases, the diagnosis was confirmed by liver biopsy. The proportion of acute drug-induced liver disease among all of the acute liver injuries was annually increased. The most common drugs which induced acute liver injuries were traditional Chinese herb medicine (23.3%, 64/275 cases), antineoplastics (15.3%, 42/275), hormones and other immunosuppressant agents (13.8%, 38/275), antihypertensive drugs and other cardiovascular drugs (10.2%, 28/275), NSAIDs (8.7%, 24/275) respectively. Hepatocellular injury was the predominant type in these cases (132 cases, 48%). The principal clinical manifestation included nausea (54.8%), fatigue (50.2%), jaundice (35.6%). 27.9% patients were asymptomatic. Most patients were cured with good prognosis. The total effective rate was 94.2% after treatment. The clinicians should pay attention to the prevention, diagnosis and therapy of drug-induced liver disease.
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标题 作者 时间 类型 操作

Semi-solid materials for controlled release drug formulation: current status and future prospects

Michelle TRAN,Chun WANG

期刊论文

Controlled drug release of 5-amino salicylic acid by poly(2-hydroxyethylmethacrylate) grafted agar

G. Usha RANI,Kartick Prasad DEY,Srijita BHARTI,Sumit MISHRA

期刊论文

Biodegradable polymethacrylic acid grafted psyllium for controlled drug delivery systems

Ranvijay KUMAR, Kaushlendra SHARMA

期刊论文

Nanostructured hollow spheres of hydroxyapatite: preparation and potential application in drug delivery

Xiaojing ZHANG, Weixin ZHANG, Zeheng YANG, Zhao ZHANG

期刊论文

Design of nanocarriers for efficient cellular uptake and endosomal release of small molecule and nucleic

Vaibhav Mundra, Ram I. Mahato

期刊论文

Synthesis and characterization of biocompatible polyurethanes for controlled release of hydrophobic and

Juichen YANG,Hong CHEN,Yuan YUAN,Debanjan SARKAR,Jie ZHENG

期刊论文

A novel cataplasma matrix of traditional Chinese medicine

Jing TIAN, Xiaolei ZHANG, Xueqin ZHOU,

期刊论文

Taking advantage of drug resistance, a new approach in the war on cancer

null

期刊论文

Protein microspheres for pulmonary drug delivery

Yongda SUN,

期刊论文

Study on the NOx release rule along the boiler during pulverized coal combustion

JIN Jing, ZHANG Zhongxiao, LI Ruiyang

期刊论文

Capacity estimation and preliminary strategy for reducing the release of dioxins in China

YU Gang, ZHANG Qing, HUANG Jun, CAI Zhenxiao, SUI Qian

期刊论文

functional supramolecular nanoparticles based on pillar[5]arene for controlled generation, storage and release

期刊论文

Phosphorus release potential and pollution characteristics of sediment in downstream Nansi Lake, China

Zhijian LI, Qinyan YUE, Baoyu GAO, Yanwen WANG, Qing LIU

期刊论文

Prevalence of antifolate drug resistance markers in in China

期刊论文

Clinical analysis of 275 cases of acute drug-induced liver disease

LI Lei, JIANG Wei, WANG Jiyao

期刊论文