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release of Nestorone from Biodegradable Rods System in vitro

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Journal of Wuhan University of Technology(Materials Science) 2010年第1期25卷 4-7页

作者：曹成波 School of Chemistry and Chemical Engineering Shandong University

To study the controlled effect of poly （lactic acid）（PLA）, poly lactic-coglycolic （PLGA） and ethylenediamine （EDA）-maleic anhydride （MAH） modified PLA （EMPLA） for in vitro release of nestorone, rods were prepared using the solvent evaporation method. Amount of drug release in vitro was determined by UV spectrophotometry. Effects of rods diameter, the molecular weight of PLA, the drug percentage and the hydrophilicity of polymers on the release of biodegradable nestorone rods in vitro were investigated. It is indicated that the controlled effect of the biodegradable rods for the release of nestorone in vitro is good. The amount of drug released every week from rods in different diameter is similar to one another. The amount of drug released every week and the accumulative drug released during 12 week were almost in direct proportion with the drug percentage of the rods. The amount of drug released every week is increased as the decreasing of PLA molecular weight. As the hydrophlicity of polymer is improved, the rate of drug release every week is accelerated. The studies show that the plausibility of controlled release of nestorone from PLA, PLGA and EMPLA rods imply the possibility of their application as a controlled delivery system for nestorone. The results show that the greater the molecular weight of PLA is, the slower its degradation is and the slower the drug released; the greater the percentage of nestorone is, the more quickly the drug release. An increase of the hydrophilicity of the polymers will increase their degradation rate and leads to a fast drug release. Anyhow, these rods systems should be further evaluated in vivo.

关键词： nestorone PLA PLGA EMPLA rods in vitro release

Design and evaluation of chitosan-amino acid thermosensitive hydrogel

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Marine Life Science & Technology 2022年第1期4卷 74-87页

作者： Jianan Tong Huiyun Zhou Jingjing Zhou Yawei Chen Jing Shi Jieke Zhang Xinyu Liang Tianyuan Du Chemical Engineering and Pharmaceutics College Henan University of Science and TechnologyLuoyang471023China College of Pharmacy(Engineering Research Center for Medicine) Harbin University of CommerceHarbin150000China

Chitosan/glycerophosphate thermosensitive hydrogel crosslinked physically was a potential drug delivery carrier;however, long gelation time limits its application. Here, chitosan-amino acid (AA) thermosensitive hydrogels were prepared from chitosan (CS), αβ-glycerophosphate (GP), and L-lysine (Lys) or L-glutamic acid (Glu). The prepared CS-Lys/GP and CS-Glu/GP hydrogel showed good thermosensitivity and could form gels in a short time. The optimal parameters of CS-Lys/GP hydrogel were that the concentration of CS-Lys was 2.5%, the ratio of CS/Lys was 3.5/1.0, the ratio of CS-Lys/GP was 4.5/1.0. The optimal parameters of CS-Glu/GP hydrogel were that the concentration of CS-Glu was 3.0%, the ratio of CS/Glu was 2.0/1.0, and the ratio of CS-Glu/GP was 4.0/1.5. Chitosan-amino acid (CS-AA) thermosensitive hydrogel had a three-dimensional network structure. The addition of model drug tinidazole (TNZ) had no obvious effect on the structure of hydrogel. The results of infrared spectroscopy showed that there were hydrogen bonds between amino acids and chitosan. in vitro release results showed that CS-Lys/GP and CS-Glu/GP thermosensitive hydrogels had sustained release effects. Thus, the chitosan-amino acid thermosensitive hydrogels hold great potential as a sustained release drug delivery system.

关键词： Chitosan L-Lysine L-Glutamic acid αβ-Glycerophosphate Thermosensitive hydrogel in vitro release

A Novel Colon-Specific Osmotic Pump Capsule of Compound Salvia miltiorrhiza: in vitro release Mechanism

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A Novel Colon-Specific Osmotic Pump Capsule of Compound Salv...

Extraction of protein from churpi of yak milk origin:Size reduction,nutraceutical potential and as a wall material for resveratrol

2018年第十二届中国药物制剂大会

作者：孙超杰 Rongfeng Hu Song Gao Anhui University of Chinese Medicine Key Laboratory of Xin'an Medicine Jointly Developed by Ministry of Education Anhui “115” Xin'an Pharmaceutical R&D Innovation Team Key Laboratory of Anhui Provincial Traditional Chinese Medicine Research and Development

OBJECTIVE: The study was performed aiming to illustrate the in vitro release mechanism of colon-specific osmotic pump capsule of compound salvia miltiorrhiza. METHODS: The in vitro release experiments were carried out by simulating the physiological environment and the transit time in the stomach, small intestine, and colon. The influence factors, such as the pore size, the punch position and the osmotic pressure of release medium, were investigated and evaluated by the indicators of cumulative release and similar factors（f2）. RESULTS: With the increase of the osmotic pressure, the rate of drug release decreased. And also the drug release was not affected by the pore size and the punch position, which was accorded with the zero-order kinetic equation. CONCLUSION: Therefore, compound salvia miltiorrhiza was primarily released through the orifice on the capsule cap, driven by the osmotic pressure. Yet the diffusion through micropores on the surface had minor impact on the drug release.

关键词： Compound salvia miltiorrhiza colon-specific osmotic pump capsule in vitro release mechanism of drug release

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Food Bioscience 2022年第2期46卷 900-911页

作者： Asir Gani Nairah Noor Adil Gani Jenno Joseph-Leenose-Helen Asima Shah Zanoor ul Ashraf Laboratory of Functional Food and Nutraceuticals Department of Food Science and TechnologyUniversity of KashmirSrinagar190006India

Resveratrol is a known anti-oxidant and anti-cancer bioactive.The low bioavailability and poor water solubility of resveratrol is a major barrier that restricts its usage in food applications.To overcome these problems,the study presents micro and nano encapsulation of resveratrol in casein micelles extracted from Himalayan cheese(Churpi).Resveratrol loaded casein microparticles(CS-rm)were obtained using emulsion-freeze drying.Whereas,resveratrol loaded casein nanoparticles(CS-rn)were obtained using ultrasonication.Both were characterized using dynamic light scattering(DLS),scanning electron microscopy(SEM)and attenuated total reflectance-fourier transform infrared spectroscopy(ATR-FTIR).DLS revealed hydrodynamic diameter of 71.24μm and 387.023 nm and zeta potential of-22.62 and-28.08 mV for CS-rm and CS-rn.FTIR confirmed the characteristic peaks of resveratrol at 965.4,1380.86,1586.66 and 1607 cm-1 confirmed successful micro and nanoencapsulation.CS-rm displayed high encapsulation efficiency(52.32%)and swelling power(77.90 at pH 3 and 68.65 at pH 7.5)than CS-rn.Both micro and nanoencapsulation protected resveratrol in gastric conditions,however,CS-rn showed high release of resveratrol then CS-rm in simulated intestinal conditions.The anti-oxidant and anti-cancer activity of resveratrol under simulated gastric and intestinal conditions(SGID)was significantly higher(p≤0.05)for CS-rn,showing that nanoencapsulation improved release and nutraceutical profile of resveratrol.Resveratrol loaded nano and micro casein particles can be used a source of fortified protein supplement in growing food and nutraceutical industry.

关键词： Casein Encapsulation efficiency in vitro release Anti-cancer

Promising psyllium-based composite containing TiO2 nanoparticles as aspirin-carrier matrix

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Progress in Natural Science:Materials International 2014年第3期24卷 205-209页

作者： Marcela-Corina Rosu Ioan Bratu National Institute for Research and Development of Isotopic and Molecular Technologies

Composite nanomaterials represent a new trend in the biomedical field. Coupling inorganic/organic constituents with non-toxicity/biocompatibility properties leads to develop the new systems having special characteristics that can be used in various bio-applications. This paper describes the preparation and characterization of psyllium-based composites containing TiO2 nanoparticles in order to develop new therapeutic strategies for aspirin drug delivery. The structural characteristics of obtained materials were investigated by FTIR spectroscopy. The UV–vis spectrophotometric analysis was performed to evaluate the aspirin release behavior under different pH conditions at 37 1C. Combining psyllium(as an excellent source of fiber) with TiO2 inorganic unit(as vehicle of aspirin) it was found that polymeric-TiO2networks have promising potential for controlled aspirin release as therapeutic agent.

关键词： Psyllium Titanium dioxide Aspirin in vitro release

Physicochemical properties,antimicrobial activity and oil release of fish gelatin films incorporated with cinnamon essential oil

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Aquaculture and Fisheries 2017年第4期2卷 185-192页

作者： Jiulin Wu Xinyu Sun Xiaoban Guo Shangying Ge Qiqing Zhang Institute of Biomedical and Pharmaceutical Technology Fuzhou UniversityFuzhou 350002China

Fish skin gelatin films incorporated with various concentrations of cinnamon essential oil(CEO)were prepared and characterized.The results showed that tensile strength(TS),elongation at break(EAB),and water content(WC)of the gelatin based film decreased with the increasing concentrations of CEO,but water vapor permeability(WVP)increased.Addition of CEO improved light barrier property of the film.The Scanning electron microscope(SEM)showed that the heterogeneous surface and porous formation appeared in gelatin-CEO films.Fourier transform infrared spectroscopy analyses(FTIR-ATR)spectra indicated the interactions existed between gelatin and CEO.The gelatin-CEO films exhibited good inhibitory effects against the tested microorganisms(Escherichia coli,Staphylococcus aureus,Aspergillus niger,Rhizopus oryzae,and Paecilomyces varioti)and their antifungal activity seemed to be more effective than the resistance to bacterial growth.in vitro release studies showed an initial burst effect of CEO release and that subsequently slowed down at 40℃,but the initial burst release was not obvious at 4℃.The obtained results suggested that incorporation of CEO as a natural antimicrobial agent into gelatin film has potential for developing as active food packaging.

关键词： Gelatin film Cinnamon essential oil Physical property Antimicrobial activity in vitro release

Comparison Study of Chitosan/β-Cyclodextrin and Carboxymethyl Chitosan/β-Cyclodextrin Microspheres

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Wuhan University Journal of Natural Sciences 2009年第4期14卷 362-368页

作者： LI Ruobao ZHAO Chunling ZHANG Weifen SHI Lihong TANG Jinbao Department of Basic Medicine Weifang Medical UniversityWeifang 261053Shandong China Shandong Provincial Key Laboratory of Applied Pharmacology Weifang Medical University Weifang 261053 Shandong China

To compare two microspheres of chitosan/β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin loaded theophylline as pulmonary sustained drug delivery carriers, the characteristics and ciliotoxicity were studied. The drug loadings of chitosan/ β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin micro- spheres were 21.09% and 21.42%, and the encapsulation efficiencies were 91.40% and 92.80%. The distributions of 50% （d0.5） of chitosan/β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin microspheres were 4.89 and 5.83 μm, respectively. Both micro- spheres showed spherical shape with smooth or wrinkled surfaces. FT-IR of chitosan/β-cyclodextrin microspheres demonstrated that theophylline had formed hydrogen bonds with chitosan and β-cyclodextrin, while for the carboxymethyl chitosan/β-cyclodextrin microspheres theophylline had interaction with carboxymethyl chitosan. The moisture absorption showed that an equilibrium was reached within 24 h. The two microspheres possessed better adaptability. in vitro release of theophylline from chitosan/ β-cyclodextrin microspheres was slower than that from carboxy- methyl chitosan/β-cyclodcxtrin microspheres at pH 6.8.

关键词： theophylline chitosan carboxymethyl chitosan microspheres in vitro release

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丙氨瑞林微球包封率和体外释放研究

丙氨瑞林微球包封率和体外释放研究

Realgar Nanoparticle-based Microcapsules:Preparation and In vitro and In Vivo Characterizations

第十一届全国青年药学工作者最新科研成果交流会

作者：张敏高静朱全刚武鑫王晓宇叶丽华高申第二军医大学长海医院药学部第二军医大学药学院

目的:研究由不同制备工艺、不同pH值释放介质对丙氨瑞林微球的包封率和体外释放趋势的影响。方法:由溶剂挥发法-复乳法（W/O/W）制备丙氨瑞林微球,内水相分别采用0%、8%、16%明胶水溶液,微球的挥干固化分别由常温挥发和真空低温挥发完... 详细信息

目的:研究由不同制备工艺、不同pH值释放介质对丙氨瑞林微球的包封率和体外释放趋势的影响。方法:由溶剂挥发法-复乳法（W/O/W）制备丙氨瑞林微球,内水相分别采用0%、8%、16%明胶水溶液,微球的挥干固化分别由常温挥发和真空低温挥发完成。体外释放实验中,采用pH=4.5,pH=7.0,pH=10.0三种释放介质,于1、7、14、21、28、35d取样,残余法测定体外释放微球突释量及释放度。使用电子扫描电镜和凝胶渗透色谱法记录微球释放期间各取样点微球降解程度。结果:内水相为8%明胶、低温真空挥发制备的微球的包封率最高,有机溶剂挥发方法会影响微球的体外释放模式,不同浓度的内水相的微球的体外释放模式有区别和突释量有不同,微球在释放介质pH=10.0中释放速率最快,在pH=4.5中,微球中的阿拉瑞林不能完全释放,最适宜的释放介质是pH=7.0缓冲液。结论:真空低温挥发固化的微球的突释量大,但对体外释放趋势没有显著影响,内水相浓度对体外释放的趋势有影响,不同pH值的释放介质对阿拉瑞林微球药物的释放有很大影响。

关键词： Alarelin Microspheres PLGA in vitro release

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Realgar Nanoparticle-based Microcapsules:Preparation and In ...