COLLOIDS AND SURFACES B-BIOINTERFACES
·
2024
·
IF 5.4
Wei Gu,Qinfu Zhao,Ye He,Shengyu Wang,Yuanqi Yang,Yian Li,Shuaipeng Feng,Siling Wang
Mesoporous carriers have gained significant attention for enhancing the solubility and bioavailability of Biopharmaceutics Classification System (BCS) Class II drugs. However, the contribution of mesoporous carriers with varying morphologies to the physical stability of these drugs is not well-defined. In this work, mesoporous carbon nanoparticles (MCN) and hollow carbon mesoporous nanoparticles (HMC) were prepared, while the weakly acidic Indomethacin (IMC) and alkaline Celecoxib (CXB) were incorporated into these carriers in the amorphous state by the solvent evaporation method. Notably, HMC demonstrated superior drug loading efficiencies (approximately 43 %) for both IMC and CXB owning to its hollow structure. The mesoporous drug loading systems significantly enhanced dissolution rates in comparison with both self-made amorphous drugs and raw drugs. Furthermore, under accelerated and long-term storage conditions, the mesoporous carriers effectively prevented drugs loaded from crystallization, maintaining constant dissolution profiles for over 12 months. Intriguingly, CXB exhibited a slower rate of crystallization after loading into the mesoporous carriers, likely due to the formation of hydrogen bonds between the carbonaceous carrier material and the amino groups of CXB. Compared with loaded drugs, the self-made amorphous drugs exhibited a crystallinity increase beyond 60 % within the initial month. Collectively, these findings highlighted the potential of mesoporous carbon carriers to elevate the dissolution behaviors of BCS Class II drugs while preserving the physical stability of the loaded amorphous drugs.
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
CHEMICAL ENGINEERING RESEARCH & DESIGN
·
2025
·
IF 3.9
Ying Zhang,Jingjing Liu,Ling Yin,Chengyun Yan,Bingli Jiang,Yueyi Deng
The cocrystals of Indomethacin (Imc) with isonicotine (Iso), isoniazid (Inh), and salicylic acid (Sa) were prepared to improve solubility, dissolution rate, and in vivo intestinal absorption. The prepared cocrystals were characterized by X-ray diffraction (XRPD), differential scanning calorimetry (DSC), thermogravimetric analysis (TG), and Fourier infrared spectroscopy (FTIR). Subsequently, the equilibrium solubility and in vitro dissolution of the cocrystals were evaluated. The results indicate that the equilibrium solubility of the Imc-Inh cocrystal is 3.2 times that of Imc, and the maximum dissolution of the Imc-Iso cocrystal is approximately 4 times that of Imc. The mechanism underlying the formation of the Imc-Iso, Imc-Inh, and Imc-Sa cocrystals was investigated through the thermodynamics of the cocrystal formation and the calculation of DFT-D. The results demonstrate that the Gibbs free energy change (ΔG), the formation enthalpy change (ΔH) of the Imc cocrystals with Iso, Inh, and Sa are less than zero, indicating that the formation of cocrystals is spontaneous and driven by enthalpy. As the temperature rises, the values of ΔG of the cocrystals formation demonstrate a gradual increase, indicating that elevated temperatures are not favorable to cocrystal formation. In vivo single-pass intestinal perfusion experiments (SPIP) reveal that the Imc-Iso cocrystals can enhance the permeability of Imc.
研究领域:
药学
·
物理化学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2019
·
IF 4.561
Li Yang,Yan Zhang,Jingcai Cheng,Chao Yang
The significant effect of solvent mixtures on the dissolution behavior of indomethacin (IMC) was systematically studied. Experimental measurements were carried out using an in-situ attenuated total reflection Fourier transform infrared (ATR-FTIR) spectrometer. Three thermodynamic models were used to correlate the experimental data to determine the solubilities of α- and γ-form IMC in three representative systems, including acetone–heptane, acetone–water and ethanol–water at temperatures ranging from 293 K to 318 K under atmospheric pressure. The acetone–water mixture has the largest dissolving capacity for IMC among the three studied solvent mixtures, and generates “cosolvent effect”. This effect is associated with the strong hydrogen-bond interaction between acetone and water. Notably, it is found that solvent–cosolvent mixtures with solubility parameters of 21 MPa 0.5 –24 MPa 0.5 are suitable for solubility improvement in the design of pharmaceutical formulations of IMC. The solvent and antisolvent can be chosen in this order: δ antisolvent < δ solvent < 21 MPa 0.5 or δ antisolvent > δ solvent > 24 MPa 0.5 for the antisolvent crystallization of IMC. Our analysis strongly demonstrates that the solubility parameter can be a simple and efficient tool in preliminary solvent screening. However, the relationship between the solubility parameter and the resulting polymorphic form in antisolvent crystallization requires further study to achieve its potential applicability in polymorphic control.
研究领域:
药学
·
物理化学
✓ 已验证
产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2017
·
IF 6.216
Ruobai Li,Jing Kong,Haijin Liu,Ping Chen,Yuehan Su,Guoguang Liu,Wenying Lv
The extensive production and use of non-steroidal anti-inflammatory drugs (NSAIDs) has increased the volume of downstream residues that contaminate the environment, which pose great threats to ecosystems and human health. The decomposition of peroxydisulfate (PDS), which is activated by UV–vis to produce a potent oxidizing sulfate radical, comprises a new type of advanced oxidation technology. The degradation of indomethacin (IM) by the UV–vis activation of peroxydisulfate was investigated. The results demonstrated that IM degradation followed pseudo-first-order reaction kinetics. UV–vis irradiation led to the direct albeit slight photolysis of IM, whereas the addition of an oxidant significantly enhanced the removal efficiency. The IM degradation efficiency was increased when the pH was elevated from 5 to 7; however, the elimination of IM was reduced when the pH was elevated from 7 to 9 due to the conversion of SO 4 − to HO . A low concentration of Cl − had a dual effect, while a high concentration led to a dramatic inhibitory effect. Fulvic acid (SRFA) inhibited the decomposition of IM through the light screening effect and the quenching of radicals. A quenching experiment revealed that SO 4 − was the primary free radical, which is confirmed by electron spin resonance spectroscopy. The second-order rate constants of IM and SO 4 − were also determined. The luminescent bacteria Vibrio fischeri was selected to assess the toxicity of the transformation products, which was further confirmed by quantitative structure-active relationship analysis. The cleavage of the bond between C on the benzene ring and N on the indole group, the hydroxylation of the benzene ring, and the decarboxylation of the aliphatic chain were the main pathways for the degradation of IM in the UV–vis/peroxydisulfate system.
研究领域:
环境科学
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
TENSIDE SURFACTANTS DETERGENTS
·
2024
·
IF 1.2
Shengnan Kong,Zheng Ji,Ya Xu,Bangchang Wei,Chuanrun Li,Huchuan Wang
In recent years, the massive use of pharmaceuticals has led to the detection of a large number of relevant residues in water. As emerging contaminants, pharmaceuticals residues in the environment pose a major threat to human health and ecosystems. Covalent organic polymers (COPs) possess high stability, uniform pore size, and easy functionalization, which have attracted great attention in water treatment. In this study, a novel covalent organic polymer was successfully studied by a simple synthesis method, combining p -phenylenediamine (Pd) and isophthalaldehyde (Is) via a Schiff-base (referred to PdIs-COP), which was used as an absorbent for the removal of indomethacin from aqueous solutions. The composite was characterized with scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) specific surface area and thermogravimetric (TGA) analysis. The effect of changes in the pH values and the adsorption time on the adsorption capacity was also investigated. The results of this study indicated that the absorbent had a high adsorption capacity for indomethacin. The adsorption capacity of PdIs-COP for indomethacin is 92.86 mg g −1 at pH of five and a contact time of 2 min. This shows that PdIs-COP is a novel material with good affinity for pharmaceuticals.
研究领域:
环境科学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2021
·
IF 13.273
Li Yang,Yan Zhang,Peng Liu,Chongqing Wang,Yanli Qu,Jingcai Cheng,Chao Yang
This work focuses on an important problem that is the modeling and control of polymorphic crystallization of indomethacin (IMC) in which one of the crystal forms consists of hair-like crystals. The lack of kinetic knowledge impedes the seeking for methods of efficient polymorph control of IMC. Herein, kinetics of antisolvent crystallization of α-IMC and γ-IMC were first time determined on the basis of experiments and the population balance equation (PBE). It was found that γ-IMC has an advantage in the secondary nucleation rate. A higher temperature was more unfavorable for obtaining γ-IMC under the same supersaturation because the γ-IMC was at a disadvantage in both primary nucleation and growth rates. According to the results of population balance modeling, the primary nucleation rate of γ-IMC only affected the polymorphic composition at the early stage of antisolvent crystallization. The growth rate of α-IMC is the key in effectively controlling the polymorph outcome.
研究领域:
化学工程
·
制药科学
✓ 已验证
DOI
高影响因子
POLYMER TESTING
·
2021
·
IF 4.282
Yanping Huang,Ye Dan,Nianhua Dan,Yining Chen
An inflammatory-responsive intelligent controlled-release drug-loaded membrane (polycaprolactone/poly (hydroxyethyl methacrylate hydroxyethyl-methacrylate -2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol -3-yl) acetoxy) ethyl meth acylate) PCL/P(HEMA-HEIn) was prepared. Drug precursors HEIn was synthesized by the esterification reaction between indomethacin (Indo) and hydroxyethyl methacrylate (HEMA) and the structure of HEIn was confirmed by 13 C NMR and ESI-MS. Through in-situ crosslinking polymerization and solvent evaporation, the drug-loaded membranes were fabricated. Furthermore, the morphology, chemical and physical properties demonstrated that HEIn and HEMA were copolymerized and well dispersed in the film. The drug released from PCL/P(HEME-HEIn) could be triggered by inflammation environment and the release amount increased along with the degree of inflammation. Results of in vivo evaluation proved that the PCL/P(HEME-HEIn) film had the capacity of inhibiting inflammation, which was beneficial to wound healing. The proposed strategy towards PCL/P(HEME-HEIn) opened new window for drug controlled-releasing via inflammatory response.
研究领域:
药学
·
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
DRUG DELIVERY
·
2022
·
IF 6.819
Ming Yuan,Jiangxiu Niu,Qinghan Xiao,Huiyuan Ya,Yansong Zhang,Yanli Fan,Lingmei Li,Xueke Li
Hyaluronic acid (HA), as a hygroscopic and biocompatible molecule, has displayed unique permeation enhancement in transdermal delivery systems. Hence, indomethacin (IND) was encapsulated in HA-modified transfersomes (IND-HTs) to enhance transdermal IND delivery to reduce adverse effects in this study. The physiochemical properties of IND-HTs were characterized. Results showed that the prepared IND-HTs were spherical and revealed good entrapment efficiency (87.88 ± 2.03%), with a nanometric particle size (221.8 ± 93.34 nm). Then, IND-HTs were further incorporated into a carbopol 940 hydrogel (IND-HTs/Gel) to prolong retention capacity on the skin. The in vitro release and skin permeation experiments of IND-HTs/Gel were carried out with the Franz diffusion cells. It was found that IND-HTs/Gel exhibited sustained drug release, as well as superior drug permeation and flux across the skin. Confocal laser scanning microscopy showed improved penetration of HTs/Gel with a wider distribution and higher fluorescence intensity. The hematoxylin–eosin stained showed that HA improved the transdermal effect by changing the microstructure of skin layers and decreasing skin barrier function. In addition, IND-HTs/Gel showed significant analgesic activity in hot plate test and no potentially hazardous skin irritation. This study indicated that the developed IND-HTs/Gel could be a promising alternative to conventional oral delivery of IND by topical administration.
研究领域:
药剂学
·
皮肤科学
·
生物材料
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2011
·
IF 3.463
Xiujuan Huang,Yan Xiao,Meidong Lang
Micelles/sodium-alginate composite gel beads (micelles/SA beads) were constructed from SA matrix and indomethacin (IND) loaded six-arm block copolymer poly( ɛ -caprolactone)- block -(dimethylamino)ethyl methacrylate (S(PCL- b -PDMA) 6 ) micelles. The morphology, swelling property and drug loading level of the beads were investigated. The release behavior of IND from three matrices including micelles, SA beads and micelles/SA beads was evaluated at pH 1.2, 6.8 and 7.4, as well as in the simulated gastrointestinal (GI) tract. Significant differences in the release of IND from each matrix were observed in the acidic and near neutral pH fluids. The results suggested that IND could be protected by the micelles/SA beads from being released under acidic conditions in the stomach and would be mainly delivered to the small intestine and the colon. The release behavior was dependent on the initial concentrations of SA and calcium chloride (CaCl 2 ) due to the different crosslinking densities. The results demonstrated that these micelles/SA beads could represent a promising oral drug delivery system for drugs with poor water solubility.
研究领域:
药剂学
·
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
·
2016
·Vol. 37
·期 8
·1173-1179
·
IF 0.793
Yuxia Liu,Zhenfa Zhang,Cuizong Zhang,Wei Huang,Caiyun Liang,Jinyun Peng
Excess amount of analgesic and anti-inflammatory drug, such as indomethacin, often leads to serious gastrointestinal complications; therefore, amount of such active compound should be regulated in commercial drugs. This study proposes an efficient analytical technique to detect indomethacin selectively. We prepared and investigated electrochemical properties of a manganese dioxide-graphene nanocomposite film modified glassy carbon electrode (MnO 2 -Gr/GCE). The behavior of the modified electrode as electrocatalyst towards indomethacin oxidation was also examined. The cyclic voltammetric results reveal that the electrocatalytic activity for the oxidation of indomethacin can significantly be enhanced on the MnO 2 -Gr/GCE. Indomethacin exhibited a sensitive anodic peak at about 0.90 V at MnO 2 -Gr/GCE. The data obtained from differential pulse voltammetry showed that the anodic peak currents were linearly dependent on the indomethacin concentrations in the range of 1.0 × 10 −7 to 2.5 × 10 −5 mol/L with a detection limit of 3.2 × 10 −8 mol/L ( S / N = 3). Most importantly, the proposed method shows efficient and selective sensing of indomethacin in commercial pharmaceutical formulations. This is the first report of a voltammetric sensor for indomethacin using MnO 2 -Gr/GCE. We believe that this new method can be commercialized for routine applications in laboratories.
研究领域:
分析化学
·
药物分析
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF CHEMICAL THERMODYNAMICS
·
2015
·
IF 2.679
Xiaowei Sun,Qiuxiang Yin,Suping Ding,Zhiming Shen,Ying Bao,Junbo Gong,Baohong Hou,Hongxun Hao,Yongli Wang,Jingkang Wang,Chuang Xie
(Solid + liquid) equilibrium data for indomethacin (IMC) and nicotinamide (NCT) in both methanol (MeOH) and methanol/ethyl acetate (EA) mixture were determined using a static method at T = (298.15 and 313.15) K under atmospheric pressure. The 1:1 (IMC + NCT) co-crystal and IMC·MeOH were found in both systems under conditions investigated. The solubility of the 1:1 (IMC + NCT) co-crystal was correlated using a mathematical model consisting of both solubility product and a complexation process. Solubility of (IMC + NCT) co-crystals as a function of co-former (NCT) concentration was evaluated. It was found that temperature has a significant effect on the formation of methanol solvate in the systems investigated. Solvate formation could be suppressed either by increasing temperature or using solvent mixtures. Additionally, the solvent mixture could level out the solubility differences between IMC and NCT , resulting in larger and more symmetric regions for the (IMC + NCT) co-crystal, which would be helpful to the development of the co-crystallization process for the 1:1 (IMC + NCT) co-crystal.
研究领域:
药学
·
物理化学
✓ 已验证
DOI
高影响因子
Pharmaceutics
·
2018
·Vol. 11
·期 1
·4
·
IF 3.746
Wei Zhang,Nan Zheng,Lu Chen,Luyao Xie,Mingshu Cui,Sanming Li,Lu Xu
The use of mesoporous silica nanoparticles (MSNs) in the field of oral drug delivery has recently attracted greater attention. However, there is still limited knowledge about how the shape of MSNs affects drug delivery capacity. In our study, we fabricated mesoporous silica nanorods (MSNRs) to study the shape effects of MSNs on oral delivery. MSNRs were characterized by transmission electron microscopy (TEM), nitrogen adsorption/desorption, Fourier transform infrared spectroscopy (FTIR), and small-angle X-ray diffraction (small-angle XRD). Indomethacin (IMC), a non-steroidal anti-inflammatory agent, was loaded into MSNRs as model drug, and the drug-loaded MSNRs resulted in an excellent dissolution-enhancing effect. The cytotoxicity and in vivo pharmacokinetic studies indicated that MSNRs can be applied as a safe and efficient candidate for the delivery of insoluble drugs. The use of MSNs with a rod-like shape, as a drug delivery carrier, will extend the pharmaceutical applications of silica materials.Keywords:mesoporous silica nanoparticles;shape effect;drug delivery;indomethacin
研究领域:
药剂学
·
纳米医学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）