Scientific Reports
·
2019
·Vol. 9
·期 1
·1-7
·
IF 4.011
Li Zhen,Peng Ying,Xia Xingyu,Cao Zhe,Deng Yuqing,Tang Bin
A Sr-based metal-organic framework (MOF) is introduced as ketoprofen carrier to form a comprehensive system for treating osteoarthritis (OA), and the drug loading amount and release rate is investigated. Structural characterization of the samples showed that Sr/PTA-MOF had good crystal morphology and structure, and chemical and thermal stability. Ketoprofen was successfully loaded on the MOF carrier, which had been identified by high performance liquid chromatography (HPLC) and thermogravimetric analysis (TGA). The release experiment manifested that more than 90% of ketoprofen released from Sr/PTA-MOF after 24 h, and ketoprofen delivery was mainly governed by the Higuchi model. Furthermore, cytotoxicity experiment manifested that synthesized MOF carrier had no poisonous effect on OA chondrocytes, which provided a preliminary foundation for the realization of comprehensive treating OA.
研究领域:
材料科学
·
医学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2014
·
IF 3.785
Chenxi Li,Chunyan Li,Zheshuo Liu,Qiuhong Li,Xueying Yan,Yu Liu,Weiyue Lu
The objective of this study was to construct a new in situ gel system based on the combination of poloxamer 407 and carrageenan (carrageenan–poloxamer 407 hydrogel, CPH) for intranasal delivery of ketorolac tromethamine . CPH showed potassium ion concentration - dependent erosion characteristics which ensured slow erosion in aqueous environment containing potassium ion at the physiological level. Loading with ketorolac tromethamine influenced erosion, drug release and thermosensitive properties of CPH. CPH containing 15% ketorolac tromethamine showed suitable gelation temperature (near 35 °C) and in vitro sustained release profiles. Pharmacokinetic study of intranasal CPH containing 15% ketorolac tromethamine in rats demonstrated enhanced absolute bioavailability (68.8 ± 23.3%) and prolonged mean residence time (8.8 ± 3.5 h) in comparison with the intranasal solution group (24.8 ± 13.8%, 3.9 ± 0.6 h). Nasal ciliotoxicity evaluation on an in situ toad palate model preliminarily showed the safety of CPH for intranasal use. All results suggested the potential of CPH as a new sustained - release platform for the intranasal delivery of ketorolac tromethamine.
研究领域:
药剂学
·
药物递送系统
·
药代动力学
✓ 已验证
DOI
高影响因子
JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY
·
2014
·Vol. 80
·期 3
·209-215
·
IF 1.426
Huang Lizhen,Wang Haixia,Li Bo,Li Erdong,Zhou Yehong,Yang Yonggang,Dong Chuan,Shuang Shaomin
β-Cyclodextrin (β-CD) and its derivatives carboxymethyl-β-CD (CM-β-CD) and 2,6-dimethyl-β-CD (DM-β-CD) modified magnetic nanoparticles (CD-MNPs) were synthesized via layer-by-layer method. CDs grafted onto Fe 3 O 4 MNPs were demonstrated by transmission electron microscopy, Fourier transform infrared and Zeta potential. Magnetic properties of CM-β-CD-MNPs, DM-β-CD-MNPs and β-CD-MNPs were characterized by vibrating sample magnetometer and the magnetic saturation values were 47, 46 and 44 emu g −1 , respectively. CD-MNPs as drug carriers were investigated by inclusion behavior and in vitro release using ketoprofen (KP) as a model drug. The maximum adsorption quantities of CM-β-CD-MNPs, DM-β-CD-MNPs and β-CD-MNPs for KP were 37.03, 7.63 and 25.12 mg g −1 , respectively, and the loading behaviors followed the Langmuir adsorption isotherm model with monolayer adsorption. The release profiles of KP released from KP-loaded CD-MNPs were rapid in initial 60 min and then gradually tend to level off, the release efficiency order was CM-β-CD-MNPs > β-CD-MNPs > DM-β-CD-MNPs, which was consistent with the order of inclusion capability. Therefore, the CD-MNPs were promising candidates for drug delivery.
研究领域:
药剂学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
Separation Science Plus
·
2018
·Vol. 1
·期 5
·351-358
·
IF 0
Yunchao He,Yaling Wu,Lingping Cheng,Shanshan He,Qiuhua Wang,Huiying Wang,Yanxiong Ke
Ketorolac has been widely applied in clinical medicine for its antipyretic, analgesic and anti-inflammatory pharmacological activity. Research showed that the analgesic effect of the S enantiomer is 230 times stronger than that of the R enantiomer. Getting the high-purity S enantiomer of Ketorolac has profound significance but still remains a challenging topic. In this work, the separation of the R and S enantiomers of Ketorolac was investigated on polysaccharide-based chiral stationary phases. Chiralcel AD-H, OD-H, OJ-H and AS-H columns were evaluated using polar organic and normal phase mode, respectively, in which the OJ-H column showed the best performance with high selectivity and resolution for Ketorolac with α = 2.43 and R S = 9.04 by using methanol/formic acid (100:0.1, v/v) as the mobile phase. The influences of acid additive, composition of mobile phase and temperature were examined. The coating amount of cellulose tris- (4-methylbenzoate) has significant influence on the sample loadability. The high loadability of chiral stationary phases coated with 40% of cellulose tris- (4-methylbenzoate) allows preparative separation up to 16 mg on an analytical column of 250 × 4.6 mm id in a single run for Ketoroac using methanol/formic acid (100:0.1, v/v) as mobile phase, which shows a potential application in industrial preparation.
研究领域:
药物化学
·
分析化学
✓ 已验证
产品关联
DOI
危险品化学品经营许可证（带存储）