JOURNAL OF MOLECULAR STRUCTURE
·
2015
·
IF 1.602
Xiaoming Zhang,Yuyang Tian,Jiangtao Jia,Tingting Zhang,Guangshan Zhu
In this paper we present three new cocrystals based on deferiprone which is the first oral medicine as iron chelator . Solitary deferiprone possesses some known problems due to its good solubility and frequent dosing side effects. For these three novel co crystals, deferiprone is the active pharmaceutical ingredient (API), p -hydroxybenzoic acid (1, C 7 H 9 NO 2 ·C 7 H 6 O 3 ), 2, 5-dihydroxybenzoic acid (2, C 7 H 9 NO 2 ·C 7 H 6 O 4 ) and maleic acid (3, C 7 H 9 NO 2 ·C 4 H 4 O 4 ) are used as cocrystal formers (CCFs), respectively. Their structures were characterized by single crystal X-ray diffraction, powder X-ray diffraction (PXRD) analysis, thermogravimetric analyses (TGA), differential thermal analysis (DTA), elemental analysis (EA) and infrared spectral analysis (IR). Single crystal X-ray diffraction demonstrates that all three cocrystals (1–3) possess strong hydrogen-bondings assembled through hydroxyl of API and carboxylic acids of CCFs. The PXRD results indicate their high purity of as-synthesized samples. TGA, DTA, EA, IR and dissolution study of API and cocrystals were also measured and discussed, respectively. The results suggest that the cocrystals exhibit low dissolution rates comparing with solitary deferiprone, which is very advantageous for the oral medicine with frequent dosing side effects.
研究领域:
药学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
Nature Communications
·
2025
·Vol. 16
·期 1
·1-19
·
IF 15.7
Wang Zhi-Hao,Zeng Xuejiao,Huang Wanting,Yang Yanbo,Zhang Shuhao,Yang Mingzhu,Liu Hua,Zhao Fengqin,Li Airong,Zhang Zhenzhong,Liu Junjie,Shi Jinjin
Oral drug delivery systems had natural potential for colorectal cancer drug therapy. While the drug delivery efficiency is severely hindered by the complex intestinal barriers, especially mucus and epithelium barriers, resulting in unsatisfactory therapeutic effects and limited clinical translation. In this work, a bioactive self-thermophoretic and gas dual-driven nanomotor is developed for colorectal cancer therapy through efficient intestinal mucus and epithelial barrier penetration. The nanomotor shows intestinal mucus barrier penetration and the paracellular pathway reversibly opening properties of intestinal epithelium barrier, increasing the delivery efficiency of cisplatin by 3.5 folds. Owing to the targeted delivery of cisplatin and the reduced side effects on normal intestinal tissues, the therapeutic efficiency of the nanomotor for colorectal cancer in vivo is as high as 98.6%. With autonomous and reversible intestinal barriers penetration property, the nanoplatform may innovate the current oral drug delivery.
研究领域:
药剂学
·
肿瘤学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2017
·
IF 6.216
Yuanyuan Li,Xueqing Qiu,Yong Qian,Wenlong Xiong,Dongjie Yang
We developed a simple and practical method to prepare pH-responsive lignin-based complex micelles in green solvents using purified alkali lignin. Alkali lignin (AL) was quaternized and further self-assembled into lignin-based complex micelles with sodium dodecyl benzenesulfonate (SDBS) in an ethanol/water mixture. The FT-IR and 1 H NMR spectra indicated the successful grafting of quaternary ammonium groups on AL. TEM images showed that the complex micelles were uniform spherical nanoparticles. The complex micelles also exhibited rich phase behaviors responding to pH changes. Ibuprofen (IBU) was used as a drug model and more than 74.44% could be encapsulated via hydrophobic interactions. The in vitro release behavior of IBU was pH-dependent and exhibited controlled release properties. Therefore, more than 75% of IBU could be preserved in simulated gastric fluid (SGF, pH 1.2), and over 90% could be released smoothly in simulated intestinal fluid (SIF, pH 7.4). This work suggests a novel strategy for fabricating an oral drug delivery carrier and is of significance for the value-added utilization of lignin.
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
高影响因子
ACS Applied Materials & Interfaces
·
2019
·
IF 8.456
Xuefeng Li,Chunchen Zhang,Shuting Wu,Xing Chen,John Mai,Ming-Wei Chang
Advances in personalized medicine will require custom drug formulations and delivery mechanisms. Herein, we demonstrate a new type of personalized capsule comprising of printed concentric cylindrical layers with each layer having a distinctive functional drug component. Poly ε-caprolactone (PCL) with paracetamol (APAP) and chlorpheniramine maleate (CM), synergistic drugs commonly used to alleviate influenza symptoms, are printed as an inner layer and outer layer, respectively, via microscaled electrohydrodynamic (EHD) printing. Polyvinylpyrrolidone (PVP) nanofibers are embedded as interlayers between the two printed PCL-drug layers using electrospinning (ES) techniques. The complete concentric cylindrical capsule with a 6 mm inner diameter and 15 mm length can be swallowed for oral drug delivery. After dissolution of the PVP interlayer, the capsule separates in two, with inner and outer capsules for continuous drug dosing and targeting. Imaging was achieved using a 3T MRI system which allowed temporal observations of the targeted release through the incorporation of nanoparticles (Fe3O4). The morphology and structure, chemical composition, mechanical properties, and biocompatibility of the capsules were studied in vitro. In summary, this new type of custom printed and electrospun capsule that enabled component separation, targeted drug release may advance personalized medicine via multidrug oral delivery.
研究领域:
药剂学
·
生物医学工程
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Bioengineering-Basel
·
2023
·Vol. 10
·期 4
·402
·
IF 4.6
Fan Wang,Ling Li,Xiaolong Zhu,Feng Chen,Xiaoxiao Han
The low bioavailability of orally administered drugs as a result of the instability in the gastrointestinal tract environment creates significant challenges to developing site-targeted drug delivery systems. This study proposes a novel hydrogel drug carrier using pH-responsive materials assisted with semi-solid extrusion 3D printing technology, enabling site-targeted drug release and customisation of temporal release profiles. The effects of material parameters on the pH-responsive behaviours of printed tablets were analysed thoroughly by investigating the swelling properties under both artificial gastric and intestinal fluids. It has been shown that high swelling rates at either acidic or alkaline conditions can be achieved by adjusting the mass ratio between sodium alginate and carboxymethyl chitosan, enabling site-targeted release. The drug release experiments reveal that gastric drug release can be achieved with a mass ratio of 1:3, whilst a ratio of 3:1 allows for intestinal release. Furthermore, controlled release is realised by tuning the infill density of the printing process. The method proposed in this study can not only significantly improve the bioavailability of oral drugs, but also offer the potential that each component of a compound drug tablet can be released in a controlled manner at a target location.
研究领域:
药剂学
·
生物医学工程
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2010
·
IF 3.151
Yanzhuo Zhang,Tongying Jiang,Qiang Zhang,Siling Wang
Spherical mesocellular foam (MCF) with a continuous 3-D pore system was synthesized using Pluronic 123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB) as a co-surfactant. The feasibility of the prepared MCF nanoparticles for oral drug delivery was studied. A model drug, telmisartan (TEL), was loaded onto MCF via a procedure involving a combination of adsorption equilibrium and solvent evaporation. The drug-release rate and the drug loading efficiency of spherical MCF were compared with those of fibrous SBA-15. Investigations using nitrogen adsorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), wide-angle X-ray scattering (WXRS), differential scanning calorimetry (DSC) and HPLC demonstrated the successful incorporation of TEL into the MCF host. It is found that spherical MCF has a high drug loading efficiency up to 42.9% (drug weight/total weight) and higher than that of SBA-15 with a pore diameter of 6.5 nm. It is shown that a fast release rate of TEL was obtained from MCF compared with SBA-15 and pure crystalline TEL using enzyme-free simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8). We believe that the present study will help in the design of oral drug delivery systems for the dissolution enhancement of water-insoluble drugs.
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
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
POLYMER BULLETIN
·
2013
·Vol. 70
·期 10
·2675-2689
·
IF 1.332
Cao Zhi-Feng,Jin Yong,Miao Qing,Ma Chun-Yan,Zhang Biao
Novel of temperature and pH sensitive hydrogels composed of polyampholyte (casein) and poly( N -isopropylacrylamide) were successfully synthesized via free radical polymerization. The swelling behavior of the obtained hydrogel was investigated and it was found that the synthesized hydrogel has a sensitivity to temperature, pH, and the crosslinker content. The drug release of this hydrogel was determined with salicylic acid employed as the model drug. It found that the release of salicylic acid from the hydrogel particles was affected by temperature, pH, and the crosslinker content in the copolymer hydrogels. Therefore, the novel pH and temperature sensitive hydrogel seem to be of great promise in pH and temperature sensitive oral drug release systems.
研究领域:
材料科学
·
药学
·
生物医学工程
✓ 已验证
DOI
高影响因子
Gels
·
2025
·Vol. 11
·期 9
·700
·
IF 5.3
Shuhan Feng,Patrick Laurén,Jacopo Zini,Zahra Gounani,Jinfeng Bi,Jianyong Yi,Timo Laaksonen
Cellulose nanofibers and pectin are promising candidates for polysaccharide-based gel carriers. However, their integration into a structurally modified hybrid gel system has not been extensively investigated. In this study, hybrid cryogels with a pH-responsive release profile favoring small intestinal delivery were prepared by freeze-drying various ratios of anionic nanofibrillar cellulose (aNFC) and amidated pectin (AP). Under acidic conditions, carboxylate protonation reduced intermolecular electrostatic repulsion, promoting the formation of the aNFC/AP hybrid gel network. Increasing the AP content enhanced the mechanical strength of the hydrogels and resulted in larger pore sizes after freeze-drying. The hybrid cryogels prolonged the release of a model drug for up to 20–30 min at pH 3.0, while exhibiting rapid release within 1–2 min when the pH exceeded 6.5, due to gel network collapse. The release behavior was governed by both the porous morphology and the crosslinking density of the cryogel scaffolds. These findings demonstrate that aNFC/AP hybrid cryogels possess a well-defined pH-responsive functional window (pH 6.5–7.0) and hold strong potential as oral drug delivery systems targeting the small intestine.
研究领域:
药剂学
·
生物材料
·
高分子科学
·
药物递送系统
·
胃肠药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Nano
·
2024
·
IF 15.8
Yumei Wang,Wei Li,Zhenwei He,Wencai Yin,Xuchun Chen,Jianxiang Zhang,Heran Li
In the harsh gastrointestinal tract, helical bacteria with hierarchical chiral architectures possess strong abilities. Taking inspirations from nature, we developed a multichiral mesoporous silica nanoscrew (L/D-MCNS) as an efficient oral drug delivery platform by modifying the structural chiral silica nanoscrew (CNS) with L/D-alanine (L/D-Ala) enantiomers via the sequential application of a chiral template and postmodification strategies. We demonstrated that L-MCNS showed differential biological behaviors and superior advantages in oral adsorption compared to those of CNS, D-MCNS, and DL-MCNS. During the delivery, helical L/D-MCNS presenting distinctive topological structures, including small section area, large rough external surface, and a screw-like body, displayed multiple superiorities in mucus diffusion and mucosal adhesion. Meanwhile, the grafted chiral enantiomers enabled positive or negative chiral recognition with the biosystems. Once racemic flurbiprofen (FP) was encapsulated into the nanopores of L/D-MCNS (FP@L/D-MCNS), L/D-MCNS providing highly cross-linked and mesoscopic chiral nanochannels was beneficial for controlling the drug loading/release kinetics with chiral microenvironment sensitivity. Particularly, we noticed enantioselective absorption of FP in vivo, which could be attributed to the differential biological behaviors of L/D-MCNS. By simple design and regulation of the multilevel chirality of nanocarriers, L/D-MCNS can be employed for efficient oral drug delivery from the perspectives of material science, pharmacy, and bionics.
研究领域:
材料科学
·
药学
·
仿生学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Haoyu Qiu,Lisha Gong,Paul Slezak,Shixiong He,Fei Lu,Kun Yu,Jing Xie,Zhen Geng,Enling Hu,Zhihang Zhou,Guangqian Lan,Ruiqi Xie
The Helicobacter pylori infection in the stomach is the key reason for gastric mucosal bleeding. Eliminating gastric Helicobacter pylori by oral treatment remains difficult due to the presence of the gastric mucosal layer, which acts as a physical barrier to drugs via oral administration. In this study, a magnetic-navigable microneedle drug delivery platform (MNs D) for oral administration, featuring differential dual-mode drug release rate, was designed to fulfil rapid gastric hemostasis and overcome the gastric barriers for long-lasting Helicobacter pylori inhibition in stomach. MNs-D was created by rationally loading the carrier substrate, which was composed of silk fibroin with variable solubility, with antibiotics and hemostats. In vitro experiments showed MNs-D may sustainably eradicate Helicobacter pylori in stimulated gastric juices with long-lasting drug release (79 % in 24 h) and quickly establish hemostasis with instant drug release (92 % within 60 s). Most importantly, in vivo studies demonstrated MNs-D overcame the unsettling gastric mucosal barrier in traditional therapies of oral administration by insertion into the GML under magnetic navigation, resulting in sustained antibiotic release for long-lasting Helicobacter pylori eradiation (99 %). For differential dual-mode medication release against gastric Helicobacter pylori infections, this study may have firstly examined the effects of magnetic navigated microneedles administered orally.
研究领域:
药学
·
生物医学工程
·
胃肠病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2024
·
IF 6.9
Cheng Wang,Lihua Ji,Jianhao Wang,Jiaxing Zhang,Lin Qiu,Shaoqing Chen,Xinye Ni
Amifostine (AMF) as the first-line radiation protection drug, usually suffered from low compliance and short half-life upon clinical applications. The development of oral drug delivery system (DDS) for AMF is a promising solution. However, the inherent shortages of AMF present significant challenges in the design of suitable oral DDS. Here in this study, we utilized the ability of calcium ions to bind with AMF and prepared AMF loaded calcium carbonate (CC) core, CC/AMF, using phase transferred coprecipitation method. We further modified the CC/AMF using phospholipids to prepare AMF loaded lipid-calcium carbonate (LCC) hybrid nanoparticles (LCC/AMF) via a thin-film dispersion method. LCC/AMF combines the oral advantages of lipid nanoparticles with the drug-loading capabilities of CC, which was shown as uniform nano-sized formulation with decent stability in aqueous solution. With favorable intestinal transport and absorption effects, it effectively enhances the in vivo radiation protection efficacy of AMF through oral administration. More importantly, we further investigated the cellular accumulation profile and intracellular transport mechanism of LCC/AMF using MDCK and Caco-2 cell lines as models. This research not only alters the current administration method of AMF to enhance its convenience and compliance, but also provides insights and guidance for the development of more suitable oral DDS for AMF in the future.
研究领域:
药剂学
·
生物医学工程
·
放射生物学
✓ 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）