MOLECULES
·
2024
·Vol. 29
·期 3
·715
·
IF 4.2
Zhe Li,Xiaosui Luo,Qiong Li,Zhengji Jin,Abid Naeem,Weifeng Zhu,Lihua Chen,Yi Feng,Liangshan Ming
Porous materials are widely used as an effective strategy for the solubilization of insoluble drugs. In order to improve the solubility and bioavailability of low water-solubility drugs, it is necessary to prepare porous materials. Mannitol is one of the most popular excipients in food and drug formulations. In this study, porous mannitol was investigated as a drug carrier for low water solubility drugs. Its fabrication, drug loading, and drug release mechanisms were investigated. Porous mannitol was fabricated using the co-spray–antisolvent process and utilizing polyvinylpyrrolidone K30 (PVP K30) as the template agent. Porous mannitol particles were prepared by changing the proportion of the template agent, spraying the particles with mannitol, and eluting with ethanol in order to regulate their pore structure. In subsequent studies, porous mannitol morphology and characteristics were determined systematically. Furthermore, curcumin and ibuprofen, two poorly water-soluble drugs, were loaded into porous mannitol, and their release profiles were analyzed. The results of the study indicated that porous mannitol can be prepared using PVP K30 as a template and that the amount of template agent can be adjusted in order to control the structure of the porous mannitol. When the template agent was added in amounts of 1%, 3%, and 5%, the mannitol pore size increased by 167.80%, 95.16%, and 163.98%, respectively, compared to raw mannitol. Molecular docking revealed that mannitol and drugs are adsorbents and adhere to each other by force interaction. The cumulative dissolution of curcumin and ibuprofen-loaded porous mannitol reached 69% and 70%, respectively. The release mechanism of curcumin and ibuprofen from drug-loaded mannitol was suitable for the Korsmeyer–Peppas kinetic model. In summary, the co-spray–antisolvent method proved effective in fabricating porous materials rapidly, and porous mannitol had a remarkable effect on drug solubilization. The results obtained are conducive to the development of porous materials.
研究领域:
药剂学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF HAZARDOUS MATERIALS
·
2011
·
IF 3.723
Hua Chen,Hanjin Luo,Yuecun Lan,Tingting Dong,Bingjie Hu,Yiping Wang
The interactions of tetracycline (TC) with nanoscale zerovalent iron (NZVI) modified by polyvinylpyrrolidone (PVP-K30) were investigated using batch experiments as a function of reactant concentration, pH, temperature, and competitive anions. Transmission electron micrographs (TEM), BET surface area and Zeta (ζ)-potential analyses indicated that the mean particle size was 10–40 nm with a surface area of 36.90 m 2 /g, and a iso-electric point of PVP-NZVI was 7.2. The results of X-ray diffraction (XRD) and high-resolution X-ray photoelectron spectroscopy (HR-XPS) of modified nanoscale zerovalent iron (PVP-NZVI) revealed that the iron nanoparticles likely have a core of zero-valent iron (Fe 0 ), while a shell is largely made of iron oxides . Degradation of TC was strongly dependent on pH and temperature. The presence of silicate and phosphate strongly inhibited the removal of TC, whereas acetate and sulfate only caused slight inhibition. LC–MS analysis of the treated solution showed that the degradation products from TC resulted from the removal of functional groups from the TC ring. The degradation products were detected both in the treated solution (initial pH of 3.0 and 6.5) and on the surface of PVP-NZVI after 4-h interaction, indicating that PVP-NZVI can adsorb both TC and its degradation products.
研究领域:
环境科学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL CHEMISTRY JOURNAL
·
2024
·Vol. 57
·期 10
·1627-1636
·
IF 0.8
Liu Lang,Ouyang Fenfen,Li Ting,Wen Min,Zha Guodong,Chen Libo,Fu Xue,Zhu Li qing
Celecoxib, the first cyclooxygenase-2 selective nonsteroidal anti-inflammatory drug, has a wide range of pharmacological effects, including anti-inflammatory, antirheumatic and antitumor effects. However, celecoxib’s poor solubility severely limits its clinical application. Thus, a novel ternary solid dispersion system was developed using PVP K30 and hydroxypropyl-β-cyclodextrin (HPβCD) as carrier materials in order to improve its solubility and dissolution behavior. The solid dispersion system was characterized by SEM, XRD, FT-IR, DSC, in vitro dissolution, saturated solubility, and contact angle test; the stability of the samples under extreme environments was investigated as well. The results showed that the novel ternary solid dispersion doped with PVP K30 and HPβCD has enhanced solubility around 6.28-fold, an almost 13.94-fold increase in the dissolution rate (120 min) compared with celecoxib’s active pharmaceutical ingredient. The substantial improvement in its dissolution performance is attributed to the fact that celecoxib is dispersed in the carrier material in an amorphous form and has hydrogen bonding interactions with the carrier materials. In addition, the improvement of wettability is one of the reasons for its increased solubility. In conclusion, the combination of PVP K30 and HPβCD can significantly improve the solubility of celecoxib and this novel solid dispersion system provides new ideas and methods to further improve the solubility of insoluble drugs.
研究领域:
药剂学
·
药物技术
·
药物传递
·
材料科学
·
生物药剂学
✓ 已验证
DOI
高影响因子
BIOPHARMACEUTICS & DRUG DISPOSITION
·
2021
·Vol. 42
·期 9
·435-443
·
IF 1.627
Hui Qiu,Zhengbing Guo,Qian Xu,Shengfang Mao,Wenming Wu
The present study was aimed to systemically assess the absorption risks of amentoflavone (AMF). Physicochemical properties of AMF were evaluated using in vitro assays including water solubility and stability in both simulated gastric and intestinal fluids, as well as logD, pka and permeability studies in a monolayer Caco-2 model. The results together suggested that AMF was a compound with moderate intestinal absorption and the poor solubility was the key rate-limiting step for the oral absorption of AMF, and PVP-K30 were thus used as a solubilizer to improve its solubility and oral bioavailability. Furthermore, studies on pharmacokinetics and biliary excretion of AMF with tween 80 or PVP-K30 were performed after oral administration, and the results showed that the percentage of AMF conjugates in bile was determined up to be 96.73% and no AMF conjugates were detected in rat plasma. The above results revealed that the poor oral absorption of AMF may probably be attributed to the low solubility, high level of metabolism and hepatic first-pass effects. The relative bioavailability of AMF solubilized by PVP-K30 was about 2-fold than that of AMF suspended in 1% tween 80. The present study may help provide scientific insights to guide the rational design of AMF into more efficient formulation systems.
研究领域:
药理学
·
药物递送系统
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）