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1. Pharmacokinetics of membrane-moderated granulated pellet-containing tablets in beagles | |||
LI Lu,LIN Shiqi,HUANG Ying,ZHU Chune,QUAN Guilan,PAN Xin,WU Chuanbin | |||
Pharmacy 21 May 2016 | |||
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Abstract:Granulated pellet-containing tablets (GPCT) were prepared via a novel granulation technique, which laid the excipients on coated pellets and then compressed into GCPT after mixing with the cushioning fillers. The pharmacokinetics of doxycycline hydrochloride GPCT were evaluated to confirm the integrity of the coating film after compaction, with the coated pellets as a reference, containing equivalent doxycycline hydrochloride in the two formulations. The study was performed on six healthy beagles by a randomized-sequence, open-label, single-dose, two-period, crossover design with a 2-week washout period. Blood samples were collected and analyzed to calculate several pharmacokinetics parameters. The mean maximum plasma concentration (Cmax) for the test formulation and reference formulation were 2.73±0.22 mg/L and 2.94±0.47 mg/L, the mean time to reach Cmax (Tmax) were 6.67±0.47 h and 6.33±0.42 h, the AUC0-t were 68.42±6.94 mgoh/L and 72.87±12.51 mgoh/L, and the mean residence time (MRT) were 15.62±0.53 h and 15.26±0.79 h respectively. The pharmacokinetics analysis suggested that there was no significant difference regarding drug release properties, and the granulated pellet-containing tablets met the regulatory criteria for bioequivalence to the reference formulation of coated pellets in the healthy fasting beagles, from which the novel granulation technique might be proposed as an effective approach to prepare pellet-containing tablets without compromising the integrity of coating films. | |||
TO cite this article:LI Lu,LIN Shiqi,HUANG Ying, et al. Pharmacokinetics of membrane-moderated granulated pellet-containing tablets in beagles[OL].[21 May 2016] http://en.paper.edu.cn/en_releasepaper/content/4693621 |
2. Preparation, characterization and antitumor activity of six polysaccharides isolated from natural sources | |||
CEN Yihong,WU Huaping,YAN Xiaorong,Qi Wenwen,GUO Hui,WANG Xiaoqian,XIAO Yuling | |||
Pharmacy 24 February 2016 | |||
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Abstract:The carboxymethylated derivatives of six kinds of polysaccharides isolated from natural Angelica sinensis, Lentinus edodes, Ganoderma lucidum, Poria cocos, Astragalus membranaceus and Maitake were synthesized and characterized. In vitro anti-tumor activity results showed that derivatives of the six polysaccharides showed more effective anti-tumor activities than their original polysaccharides. Also, their water solubility was highly improved. Moreover, Angelica sinensis which showed the best antitumor effect were carboxymethylated with five different degree of carboxymethylation substitution in order to study the correlations between the antitumor activity, the water solubility and the degree of substitution (DS) of the polysaccharide. Experimental results showed that the water solubility of the carboxymethylated derivatives of Angelica sinensis (CASP) was highly improved with increasing of DS. However, the anti-tumor activity was not just enhanced with the increasing of water solubility. A relatively moderate DS (0.187) was found to have the best anti-tumor activities of CASP. Therefore, it can be concluded that carboxymethylation of polysaccharides can effectively enhance their water solubility and in vitro anti-tumor activity. | |||
TO cite this article:CEN Yihong,WU Huaping,YAN Xiaorong, et al. Preparation, characterization and antitumor activity of six polysaccharides isolated from natural sources[OL].[24 February 2016] http://en.paper.edu.cn/en_releasepaper/content/4678512 |
3. Prepatation, hydrolysis and antitumor activities of pachyman and their derivatives | |||
YANG Ming,YU Haiyan,CEN Yihong,RAO Zhigang,ZHOU Yi,ZHANG Fang,XIAO Yuling | |||
Pharmacy 05 May 2015 | |||
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Abstract:Water-soluble pachyman (WSP) was prepared by enzymatic hydrolysis of water-insoluble pachyman extracted from the fresh sclerotium of Poria cocos. Carboxymethylated, sulfated, methylated and hydroxyethylated derivatives of WSP were synthesized, respectively. Their chemical structure were confirmed by infrared spectra and molecular mass were determined by gel permeation chromatography. The antitumor activities against Hela tumor cell and Sarcoma 180 tumor cell (S180) of WSP and all the derivatives were tested in vitro. It is showed that effective chemical components with lower molecular weight of pachyman contribute to the enhancement of antitumor activity. | |||
TO cite this article:YANG Ming,YU Haiyan,CEN Yihong, et al. Prepatation, hydrolysis and antitumor activities of pachyman and their derivatives[OL].[ 5 May 2015] http://en.paper.edu.cn/en_releasepaper/content/4640939 |
4. The Peraration of Self-Microemulsifying Drug Delivery System for Elemene and Its In vitro Evaluation | |||
GU Mancang,QIAN Yafang,CHEN Jing | |||
Pharmacy 02 February 2014 | |||
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Abstract:Our study developed a noval self-microemulsifying drug delivery system (SMEDDS) to enhance oral absorption of elemene and evaluated its oral bioavailability in rats. Pseudo-ternary phase diagrams were constructed to identify the efficient self-microemulsification region. SMEDDS formulations were further optimized by measurement of mean droplet size and emulsification time. The in vitro release profile of SMEDDS was determined in different aqueous media. The optimal formulation consisted of 10%Miglyol? 812, 41.7%Cremophor? EL, 8.3%Labrasol? ,20%Transcutol? P as well as 200 mg/g elemene, and demonstrated a higher release rate in simulated gastric fluid than emulsion and pure drug. Our results indicate that SMEDDS is a potential and promising drug delivery system for lipophilic Chinese herbal medicines, such as elemene. | |||
TO cite this article:GU Mancang,QIAN Yafang,CHEN Jing. The Peraration of Self-Microemulsifying Drug Delivery System for Elemene and Its In vitro Evaluation[OL].[ 2 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4584449 |
5. Preparation and evaluation of Angiopep-2 peptide grafted micelle for brain targeting delivery | |||
QUAN Yi,JIN Mingji,LI Yunfei,WANG Qiming,SHAO Rongguang,GAO Zhonggao | |||
Pharmacy 20 January 2014 | |||
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Abstract:In this paper, a novel drug-loaded micelle for brain targeting delivery was developed by conjugating the targetable moiety Angiopep-2 peptide on the surface of micelle. In order to monitoring the size of the tumor inside of the brain after treatment, the technique of bioluminescence imaging in living rats was developed. The luciferase-labelled glioma cell line C6-Luc was firstly constructed through cell transfection and monoclone screening, and then evaluated by luciferase reporter assay. The anti-glioma effect of Doxorubicin-loaded targetable micelle was assessed through cell MTT assay and determining the survival time of glioma bearing rats. The results demonstrated that such Doxorubicin-loaded targetable micelle showed a strong anti-glioma effect, and it could significantly prolong the life span of glioma bearing rats, which suggested that Angiopep-2 modified micelles is a promising carrier for drug brain targeting delivery. | |||
TO cite this article:QUAN Yi,JIN Mingji,LI Yunfei, et al. Preparation and evaluation of Angiopep-2 peptide grafted micelle for brain targeting delivery[OL].[20 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4583312 |
6. Influence of Liquid Lipid Content on the Properties of Puerarin-loaded Lipid Nanoparticles | |||
HU Xiaofen | |||
Pharmacy 08 January 2014 | |||
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Abstract:The present study described the fabrication and characterization of puerarin-loaded lipid nanoparticles with blends of glyceryl monostearate (solid lipid phase) and DELIOS? MCT (liquid lipid phase) as the lipid matrices. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were prepared via controlling the ratio of liquid lipid to solid lipid. The drug-lipid compatibility was evaluated via theoretical calculation of solubility parameters and X-ray diffraction analysis. The influence of liquid lipid content on the particle size, morphology, stability, drug loading properties of the lipid nanoparticles and in vitro release behavior of puerarin was investigated. Both SLN and NLC exhibited well stability and spherical shapes, and no significant difference in particle size occurred for the NLC series. The drug loading capacity (LC) and entrapment efficiency (EE) of the lipid nanoparticles were affected as increasing the liquid lipid content, and the presence of liquid lipid had a positive effect on improved drug payload. The in vitro release behavior of puerarin was intimately associated with the constituent of the lipid matrix. A sustained release of puerarin from NLC was observed in the selected experimental time window. The results of the current study displayed the application potential of NLC as nano-sized delivery carriers for puerarin. | |||
TO cite this article:HU Xiaofen. Influence of Liquid Lipid Content on the Properties of Puerarin-loaded Lipid Nanoparticles[OL].[ 8 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4581343 |
7. Cell uptake of paclitaxel solid lipid nanoparticles modified by cell-penetrating peptides in A549 cells | |||
ZHANG Yinlong,LV Huixia,ZHOU Jianping,ZHANG Zhenhai | |||
Pharmacy 08 January 2013 | |||
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Abstract:The aim of this study was to investigate the cytotoxicity of paclitaxel solid lipid nanoparticles(SLN) modified with stearic acid octaarginine (SA-R8-C6-SLN ) as well as the cellular uptake of Coumarin-6-loaded SLN modified with SA-R8 (SA-R8-C6-SLN) in human lung cancer cells, A549. SLN were prepared using a film dispersion method; and then their particle size, zeta potential, morphology, bound efficiency of SA-R8, drug loading efficiency, and in vitro release were characterized. SA-R8-PTX-SLN and SA-R8-C6-SLN were incubated with A549 cells to measure their cytotoxicity and cellular uptake, respectively. The results indicated that the cytotoxicity of SA-R8-PTX-SLN was enhanced significantly with the increasing amount of SA-R8 and the cellular uptakes of SLN increased with the incubated concentrations and the incubated time of SLN. In contrast, SA-R8-SLN could significantly enhance the cellular uptake of SLN and the cytotoxicity of PTX in A549 cells. These in vitro results suggest that SA-R8-SLN could be proposed as alternative drug delivery system | |||
TO cite this article:ZHANG Yinlong,LV Huixia,ZHOU Jianping, et al. Cell uptake of paclitaxel solid lipid nanoparticles modified by cell-penetrating peptides in A549 cells[OL].[ 8 January 2013] http://en.paper.edu.cn/en_releasepaper/content/4511164 |
8. Overcoming drug-resistance with copolymer micelles in delivering anti-cancer drug to breast tumor cells. | |||
Min Han | |||
Pharmacy 20 September 2012 | |||
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Abstract:Drug resistance is one of the critical reasons leading to failure in chemotherapy. We developed PEG-PCL polymer micelle encapsulating Doxorubicin (DOX) as a novel drug delivery system to inhibit the drug-resistance of adriamycin-resistant K562 tumor cells(K562/ADR) in present study, and the physico-chemical properties of the micelles, accumulation and cytotoxicity of DOX in K562/ADR cells were further studied. The micelles loading DOX were prepared by solvent evaporation method with a diameter of 36 nm and a Zeta potential of 13.8 mV. The entrapment efficiency of DOX was (48.6±2.3)%. The micelles showed sustained release, and increased uptake and cellular cytotoxicity as well as decreased efflux of DOX in K562/ADR cells. This study suggested that PEG-PCL micelles possess a potential prospect in reversing the multidrug resistance of the tumor cells. | |||
TO cite this article:Min Han. Overcoming drug-resistance with copolymer micelles in delivering anti-cancer drug to breast tumor cells.[OL].[20 September 2012] http://en.paper.edu.cn/en_releasepaper/content/4489616 |
9. Preparation and characterization of novel pH-sensitive N-succinyl-chitosan/poly(vinyl alcohol) hydrogel | |||
FAN Lihong,WEN Feng,WU Penghui,WANG Libo,TAN Chang,SHA Mingming | |||
Pharmacy 15 January 2012 | |||
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Abstract:Blended hydrogels have been widely used in biomedical fields due to their biocompatibility and biodegradability. In order to get a new kind of blended hydrogel using as deliver system for drugs, we prepared N-succinyl-chitosan (NSCS) and Poly (vinyl alcohol) blended hydrogels by freezing-thawing method. The hydrogels were characterized by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy. Antibacterial activity of hydrogels composite within nanosilver was also investigated. The swelling degree of hydrogels was increased with the amount of NSCS. Protein release studies were performed in different pH solutions. The results showed that the release rate was slower under acid than under basic conditions, which could be attributed to the pH-sensitive of NSCS. It is suggesting that the NSCS/PVA hydrogels could be potentially applied as oral delivery systems for protein drugs. | |||
TO cite this article:FAN Lihong,WEN Feng,WU Penghui, et al. Preparation and characterization of novel pH-sensitive N-succinyl-chitosan/poly(vinyl alcohol) hydrogel[OL].[15 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4462334 |
10. Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery | |||
Zou Aifeng ,Meirong Huo,Yong Zhang,Jianping Zhou,Xiaoqiang Yin,Chengli Yao,Qinnv Zhu | |||
Pharmacy 09 October 2011 | |||
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Abstract:Octreotide (OCT) was recently found to have high binding affinity to the positive tumor cells of somatostatin receptors (SSTRs). In this study, octreotide-polyethene glycol-stearic acid (OCT-Phe-PEG-SA) was first successfully synthesized and used as a targeting molecule for N-octyl-O, N-carboxymethyl chitosan (OCC). Doxorubicin (DOX) was loaded into OCT-modified OCC micelles (DOX-OCC-OCT). The drug-loaded micelles obtained exhibited spherical shape, small particle sizes and negative zeta potentials. The cytotoxicity of DOX-OCC-OCT micelles against MCF-7 cells (SSTRs expressing) was found to significantly increase with the increased amount of OCT modification, while no significant difference was observed against WI-38 cells (no SSTRs expressing). Results of flow cytometry, fluorescence microscopy and confocal laser scanning microscopy confirmed DOX-OCC-OCT micelles could remarkably increase the uptake of DOX in MCF-7 cells. All the results indicated that OCC-OCT micelles may be a promising intracellular targeting carrier for efficient delivery of antitumor drugs into tumor cells. | |||
TO cite this article:Zou Aifeng ,Meirong Huo,Yong Zhang, et al. Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery[J]. |
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