JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2019
·
IF 2.606
Nana Chen,Jing'e Niu,Qian Li,Jianyin Li,Xinping chen,Yuan Ren,Guotai Wu,Yingqian Liu,Yanbin Shi
To better treat gastric diseases and lower systemic side effect, it is essential to design new vectors to control drug release in stomach. Aiming to this challenge, we developed a new gastroretentive drug delivery system : nanomicelles-loaded gastroretentive beads. Firstly, the chitosan-coated emodin-loaded nanomicelles were developed and characterized. In vitro cytotoxicity of emodin-loaded nanomicelles, emodin suspensions and blank nanomicelles was evaluated with human gastric carcinoma SGC-7901 cells by MTT , indicating that the blank nanomicelles had null cytotoxicity and emodin-loaded nanomicelles had better antitumor efficacy compared with emodin suspensions. Secondly, nanomicelles-loaded floating mucoadhesive beads (NFM-Beads) were prepared, and the swelling, degradation, mucoadhesion and floating ability in vitro were separately investigated. FT-IR spectroscopy was applied to identify the formation of nanomicelles and NFM-Beads. Emodin release from NFM-Beads in vitro was fitted to anomalous transport mechanism. In vivo gastroretention behavior of NFM-Beads was evaluated by BaSO 4 -based X-ray imaging exams, showing that NFM-Beads can be retained in rabbit stomach for at least 8 h. Overall, the new NFM-Beads system could be an effective approach to improve the therapeutic potency of drug against gastric cancer.
研究领域:
药学
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药物递送系统
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
Pharmaceutics
·
2023
·Vol. 15
·期 3
·816
·
IF 5.4
Ajkia Zaman Juthi,Fenfen Li,Bo Wang,Md Mofasserul Alam,Md Eman Talukder,Bensheng Qiu
Super-porous hydrogels are considered a potential drug delivery network for the sedation of gastric mechanisms with retention windows in the abdomen and upper part of the gastrointestinal tract (GIT). In this study, a novel pH-responsive super-porous hybrid hydrogels (SPHHs) was synthesized from pectin, poly 2-hydroxyethyl methacrylate (2HEMA), and N, N methylene-bis-acrylamide (BIS) via the gas-blowing technique, and then loaded with a selected drug (amoxicillin trihydrate, AT) at pH 5 via an aqueous loading method. The drug-loaded SPHHs-AT carrier demonstrated outstanding (in vitro) gastroretentive drug delivery capability. The study attributed excellent swelling and delayed drug release to acidic conditions at pH 1.2. Moreover, in vitro controlled-release drug delivery systems at different pH values, namely, 1.2 (97.99%) and 7.4 (88%), were studied. These exceptional features of SPHHs—improved elasticity, pH responsivity, and high swelling performance—should be investigated for broader drug delivery applications in the future.Keywords:super-porous hybrid hydrogels;gastroretentive;controlled-release drug delivery
研究领域:
药剂学
·
生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN POLYMER JOURNAL
·
2022
·
IF 5.546
Xin Jin,Chengxiong Wei,Chengwei Wu,Wei Zhang
The metformin hydrochloride is the only oral guanidine anti glycemic agent and is used as the first-line drug for the treatment of type II diabetes. Owing to its high water solubility and short half-life, however, this drug is difficult to be released sustainedly. Here, a core–shell structured hydrogel assembly as gastroretentive carrier is proposed for the sustained release of metformin hydrochloride. The hydrogel assembly can be ingested orally into the stomach. On contact with the gastric juice, the shell rapidly swells to prevent the hydrogel to be expelled from the pylorus, and the core serves as a drug reservoir for loading metformin hydrochloride. The core–shell structure can decrease the driving force of drug release and extend the drug diffusion pathway. As a result, the hydrogel assembly can release metformin hydrochloride sustainedly for 72 h in vitro and maintain stable blood drug concentration for nearly 80 h in vivo. Moreover, the hydrogel assembly can be biodegraded by the gastric environment.
研究领域:
药剂学
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药物递送系统
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Materials Chemistry B
·
2025
·
IF 5.7
Yu Fu,Wenjing Liu,Lihang Jiang,Huili Yuan,Xiaoqian Tong,Huiwen He,Yanqin Shi,Meng Ma,Si Chen,Xu Wang
Traditional natural polysaccharide-based hydrogels, when used as drug carriers, often struggle to maintain long-term stability in the extremely harsh gastric environment. This results in unstable drug release and significant challenges in bioavailability. To address this issue, this study utilized inexpensive and safe natural polysaccharides—chitosan (CS) and high methoxyl pectin (HM)—as raw materials. Dynamic chemical bonds and anion–cation electrostatic interactions were employed to successfully prepare a super absorbent gel bead substrate (CS–HM), which serves as the “core” structure. Subsequently, another low-density hydrophilic polysaccharide, sodium carboxymethyl cellulose (CMCNa), was used to coat and crosslink the outer layer of the core, increasing the number of ionic groups. This enhancement raises the osmotic pressure inside the gel network, improving its absorption capacity. At the same time, the core–shell structure provides an energy dissipation mechanism, allowing the material to remain more stable in a strong acid environment. Due to its super absorption, high modulus, and continuous floating release properties, CS–HM@CMCNa—as a new type of acid-resistant super absorbent core–shell material-possesses the key characteristics required for gastric retention sustained-release systems. It is expected to become an ideal drug carrier for the treatment of clinical chronic diseases.
研究领域:
生物材料学
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2022
·
IF 5.062
Saige Meng,Shuangqing Wang,Ming Guan Piao
The synergistic gastroretentive drug delivery systems are capable of delivering drugs with a narrow absorption window. The purpose of this study is to prepare furosemide hollow-bioadhesive microspheres to improve bioavailability. The emulsion solvent volatilization method was adopted, through Box-Behnken design, with polymer ratio (X 1 ), dosage (X 2 ), organic solvent volume (X 3 ) and PVA concentration (X 4 ) as independent variables, and drug loading (Y 1 ), encapsulation rate (Y 2 ), yield rate (Y 3 ) and 8 h floating rate (Y 4 ) were response variables. The interaction effects of the independent and response variables were explored. The optimized hollow-bioadhesive microspheres showed the in vitro floating rate of 93.33 ± 5.24% for 8 h, the in vitro retention rate of 90.67 ± 3.21%, and the sustained drug release of 93.79 ± 4.90% for 12 h. Compared with the hollow microspheres, the hollow-bioadhesive microspheres significantly increase the retention time in the stomach. The results of Differential Scanning Calorimetry , Fourier Transform InfraRed, and X-ray diffraction showed that furosemide had good biocompatibility with excipients. Compared with commercial tablets, the relative bioavailability of hollow-bioadhesive microspheres was increased by 163.84%, and the long-term therapeutic concentration was maintained. The safety evaluation proved the oral safety of microspheres. In conclusion, the safe and economical furosemide hollow-bioadhesive microsphere is a valuable preparation for development, which can improve clinical application.
研究领域:
药剂学
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药物递送系统
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2018
·
IF 3.466
Qingguo Li,Wenhai Huang,Juan Yang,Jianfeng Wang,Min Hu,Jianmei Mo,Yuzhu Cheng,Zhanlun Ou,Zhenyu Jason Zhang,Shixia Guan
Absorption mechanism of edaravone (EDR) was studied to inform the preparation of gastric retention pellets with the aim to enhance its oral bioavailability. Three different models, namely, Caco-2 cells model, in situ single-pass intestinal perfusion model, and everted gut sac model in rats, were employed to characterize the gastrointestinal absorption kinetics of EDR. And it was found that passive transfer plays a vital role for the transport of EDR, and acidic condition is preferable for EDR absorption. Further, it is likely that EDR acts as a substrate for P-glycoprotein and multidrug-resistance protein. And hence, an orally available gastric retention pellets were developed accordingly. Pharmacokinetic experiments performed with rats and beagles showed that the absolute bioavailability of EDR solution and enteric-coated pellets following oral administration were 33.85% ± 2.45% and 7.64% ± 1.03%, indicating that stomach absorption is better than intestinal adsorption for EDR. However, the gastric retention pellets resulted in 68.96% absolute bioavailability and about 200% relative bioavailability in comparison to EDR solution, which was 9 times that of enteric-coated pellets. The present work demonstrates that gastric retention pellets has excellent potential as oral administration route for EDR.
研究领域:
药剂学
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药物代谢动力学
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生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
Pharmaceutics
·
2024
·Vol. 16
·期 10
·1242
·
IF 4.9
Da Hun Kim,Sa-Won Lee,Jun Hak Lee,Jin Woo Park,Sung Mo Park,Han-Joo Maeng,Tae-Sung Koo,Kwan Hyung Cho
Background/Objectives:The aim of this work was to prepare and characterize gastroretentive floating combination tablets (GRCTs) containing 500 mg of amoxicillin trihydrate (AMX) and 125 mg of levofloxacin (LVX) that provide sustained drug release and stability at gastric pH levels for the eradication of resistantHelicobacter pylori.Method:GRCTs were prepared with low-density excipients and hydrophilic swellable polymers, including hydroxypropyl methylcellulose (HPMC) of various viscosities, polyethylene oxide (PEO), and carboxymethylcellulose (CMC), by the direct compression method. The prepared GRCTs were investigated and optimized in terms of pH stability, tablet hardness, floating lag time and total floating time, drug release rate, gel strength.Results:AMX and LVX in GRCT were stable at the HP eradication target pH above 4.0. The effervescent GRCT composition (AMX/LVX/HPMC [4000 cP]/CMC/microcrystalline cellulose/citric acid/sodium bicarbonate/calcium silicate/silicon dioxide/magnesium stearate = 500/125/50/50/125/40/60/30/10/10,w/w) yielded acceptable hardness (>6 kp), reduced floating lag time (<5 s), a long floating duration (>12 h), and sustained release rates of AMX and LVX (>90% until 12 h). This optimized GRCT had a gel strength of 107.33 ± 10.69 g and pH > 4.0, which maintained the tablets’ shape and AMX stability for 12 h.Conclusions:Collectively, the formulated effervescent GRCTs combining AMX and LVX represented a promising candidate dosage form for eradicating resistantH. pylori.
研究领域:
药剂学
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微生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2019
·
IF 4.784
Yujia Wu,Wen Zhang,Jianyu Huang,Zichen Luo,Junsong Li,Lingchong Wang,Liuqing Di
As polysaccharide from Bletilla striata (BSP) was anticipated with mucoadhesive improvement in sodium alginate (SA) microspheres, BSP was mixed with SA to construct a composite microsphere to retain in the gastrointestinal tract for a long time. The morphological properties, particle size and thermodynamic properties of the microspheres in combination with comprehensive evaluations in the swelling properties, mucin adsorption, ex vivo and in vivo gastric retention were determined to characterize the mucoadhesion of SA-BSP blend microspheres. Results showed that the prepared microspheres were discrete and spherical. The addition of BSP increased flexibility and reduced rigidity of SA microsphere. Furthermore, the swelling property, mucin adsorption ability and the retention rate on the gastric mucosa of SA matrix were increased after blending with BSP. Mucoadhesion tests showed the SA-BSP microspheres stayed much longer in rats' stomach than the SA microsphere did. Above all, the SA-BSP microspheres with the enhanced mucoadhesion suggested being a potential drug carrier in developing the gastroretentive drug delivery system.
研究领域:
药学
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药物递送系统
·
生物药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Biomaterials Science & Engineering
·
2023
·
IF 5.8
Qikun Cheng,Mingzhi Xie,Guowei Li,Wei Xue,Lexiang Zeng,Dong Ma
Alcohol abuse is harmful to human health, and many strategies have been developed to retard this harm through protecting liver or activating relative enzymes. In this study, a new strategy of decreasing the alcohol absorption directly depending on the dealcoholization by the bacteria in the upper gastrointestinal (GI) tract was reported. To realize this, a bacteria-loaded gastro-retention oral delivery system with pore structure was constructed through emulsification/internal gelation, which could relieve acute alcohol intoxication in mice successfully. It was found that this bacteria-loaded system kept the above 30% suspension ratio in the simulated gastric fluid for 4 min, displayed good protection effect for the bacteria, and decreased the alcohol concentration from 50 to 30% below within 24 h in vitro. The in vivo imaging results demonstrated that it remained in the upper GI tract until 24 h and reduced 41.9% alcohol absorption. The mice with oral administration of the bacteria-loaded system were found with normal gait, smooth coat, and less liver damage. Although the intestinal flora distribution was influenced slightly during the oral administration, it could restore to normal levels only one day after stopping oral administration quickly, suggesting good biosafety. In conclusion, these results revealed that the bacteria-loaded gastro-retention oral delivery system might intake alcohol molecules rapidly and has huge potential in the treatment of alcohol abuse.
研究领域:
药理学
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生物技术
·
胃肠病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Advanced Healthcare Materials
·
2024
·
IF 10
Huayuan Chen,Li Pan,Chengyu Zhang,Lin Liu,Bin Tu,Ergang Liu,Yongzhuo Huang
Gastric ulcers are characterized by damage to the stomach lining and are often triggered by substances such as ethanol and non-steroidal anti-inflammatory drugs. Patchouli alcohol (PA) has demonstrated effectiveness in treating gastric ulcers through antioxidative and anti-inflammatory effects. However, the water insolubility of PA and rapid gastric emptying cause low drug concentration and poor absorption in the stomach, resulting in limited treatment efficacy of PA. This study develops an oral gastroretentive raft forming system (GRFDDS) containing the aminated hollow mesoporous silica nanoparticles (NH 2 -HMSN) for PA delivery. The application of NH 2 -HMSN can enhance PA-loading capacity and water dispersibility, promoting bio-adhesion to the gastric mucosa and sustained drug release. The incorporation of PA-loaded NH 2 -HMSN (NH 2 -HMSN-PA) into GRFDDS can facilitate gastric drug retention and achieve long action, thereby improving therapeutic effects. The results reveal that NH 2 -HMSN-PA protects the gastric mucosa damage by inhibiting NLRP3-mediated pyroptosis. The GRFDDS, optimized through orthogonal design, demonstrates the gastric retention capacity and sustained drug release, exhibiting significant therapy efficacy in an ethanol-induced acute gastric ulcers model and an aspirin-induced chronic gastric ulcers model through antioxidation, anti-pyroptosis, and anti-inflammation. This study provides a potential strategy for enhancing druggability of insoluble natural compounds and therapeutic management of gastric ulcers.
研究领域:
药学
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药物递送系统
·
胃肠病学
·
纳米技术
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Yue Zhou,Ning Gu,Fang Yang
Organic and inorganic nanomaterials have shown great potential in drug delivery applications due to their unique physical and chemical properties. Orally administered nanoparticles have attracted great attention because it is acceptable, convenient, and safe. However, nanoparticles need to overcome numerous hurdles such as acidic gastric environment, the continuous secretion of mucus, and fast gastric emptying after being delivered via an oral route. Here, we used a stimuli-responsive and triggered release strategy for superparamagnetic iron oxide nanoparticles (SPIONPs)-loaded gastro-retentive tablets for in situ bubbles generation. These materials realize SPIOs controlled release and delivery specific to the stomach. The tablet formulation contains a foaming agent (sodium bicarbonate, NaHCO 3 ), adhesive component (HPMC/carbomer 934 P (1:1)), filler (lactose/mannitol (10:1)) and SPIONPs. The in vitro bubble generation and SPIONPs released from the tablets were characterized. The ex vivo gastric adhesive ability, acoustic stimuli performance, and tissue penetration were further evaluated. The results show that when the fabricated tablets interacted with the acidic microenvironment, the carbon dioxide (CO 2 ) could be generated and be captured by ultrasound (US) imaging. Simultaneous with bubble production, SPIONPs are released from the tablets to further control ultrasound-mediated force and deliver SPIONPs entering through the mucus layer. The SPIONPs were loaded in the tablets and could be released in a controllable way; thus, the magnetic resonance imaging (MRI) could also be used to monitor the tablet status and SPIONP delivery process. Therefore, SPIONPs-loaded gastro-retentive effervescent tablets offer effective release and absorption of nanoparticles in the gastric area and be imaged by MRI and US.
研究领域:
药学
·
纳米技术
·
药物递送系统
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Nano Today
·
2020
·
IF 16.907
Xinqi Cai,Yiting Xu,Lina Zhao,Jiamei Xu,Shengkai Li,Chaoqi Wen,Xin Xia,Qian Dong,Xiaoxiao Hu,Xiaofeng Wang,Long Chen,Zhuo Chen,Weihong Tan
Gastric environment is an extreme pH and enzyme-rich condition, which together with gastric mucus barrier and short retention time of oral medicine militate against effective oral drug delivery to lesion areas of gastric diseases. Assembly, especially shape-control assembly of magnetic nanoparticles potentially helps the site-selective drug molecule delivery. However, the harsh gastric condition, and cumbersome and strict requirements make the in situ reversible assembly remain challenging. Herein, synergistically pepsin-bridged and magnetic field-mediated morphological control of magnetic-graphitic-nanocapsules (MGNs) needle assembly (MNA) is developed in stomach for prolonged gastric retention and enhanced mucus penetration. The MNAs with good biocompatibility, large magnetic moments and unique needle-shape are formed with the help of pepsin , demonstrating superior magnetic-driven capability to overcome gastric mucus barrier. Molecular dynamics simulations reveal binding modes between MGN and amino acid residues on either side of the pepsin, indicating pepsin acts as “bridge” allowing sufficient contact among MGNs and further facilitates the needle assembly. Moreover, anticancer drug doxorubicin (DOX)-loaded MNAs demonstrate superior targeted cancer cell killing ability and boosted DOX penetration in a mouse model, which promises good bioavailability of drug molecules. The versatile MNA-based platform offers a robust strategy for effective oral drug delivery and site-selective therapy of gastric diseases.
研究领域:
药学
·
纳米技术
·
生物医学工程
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）