JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2019
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IF 2.606
Ya-Nan Xia,Xiang-Hui Li,Jie-Hong Xu,Li-Qing Chen,Atef Mohammed Qasem Ahmed,Dingyun Cao,Huan-Huan Du,Yibin Deng,Qing-Ri Cao
Traditional dosage forms of dexibuprofen extremely limit their clinical applications because of the bitter taste and the frequent drug administration caused by the relatively short half-life of the drug. This study aims to design novel sustained release (SR) supermicro-pellet based dry suspensions that load dexibuprofen, and also optimize the formulations in terms of morphology, release rate, flowability, and physicochemical stability of dosage forms. Drug-loaded pellets were prepared by using a bottom spray fluid bed coating technique using microcrystalline cellulose supermicro-pellets as the core and PVP K30 or Poloxamer 188 as the binder. The drug-loaded pellets were further coated with Kollicoat SR 30D to form SR pellets. The optimal SR dry suspensions are composed of SR pellets, diluent granules, and suspending agents. PVP K30- and Poloxamer 188-based SR pellets release the drug molecules in a SR manner over 8 h and show a high release profile for Poloxamer 188-based pellets. The drug release profile is not affected by the rotation speed of the paddle but shows a distinct pH-responsive behavior. The physical property of dexibuprofen has been changed during the preparation process. The SR dry suspensions (F5, with high amount of xanthan gum in suspending agents and low amount of poloxamer 188 in diluent granules) show high physical stability with the sedimentation rate of 0.8 (Hu/H) within 5 min and good flowability with the angle of repose (θ) at 27°. Low content variations were observed with a value of A+1.80SD ≤ 15, and no significant change was found in the drug content under high humidity and strong light. In conclusion, novel SR supermicro-pellet based dry suspensions have been successfully prepared, and the optimal formulation shows excellent SR, good flowability, content uniformity, and physicochemical stability.
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Journal of Nanomaterials
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2019
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IF 2.233
Hui Zhang,Jiangying Zhu,Yanqiang Hu,Aonan Chen,Liang Zhou,Hui Gao,Yamei Liu,Shengquan Liu
A novel cellulose/TiO2/β-CD hydrogel with high photocatalytic antibacterial activity and sustained release of drug was prepared. TiO2 sol with a diameter of about 9 nm in this hydrogel was the photoantibacterial agent. β-CD can significantly enhance photoantibacterial activity and the sustained-release effect of this hydrogel. The structure and property of this hydrogel composite were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). Escherichia coli and Staphylococcus aureus were selected as model bacteria to evaluate the antibacterial activity of the composite hydrogel under natural light irradiation and darkness, respectively. The in vitro release experiment used curcumin as a model drug in PBS buffer solution. The influence of β-CD on the antibacterial activity and sustained-release effect of the composite hydrogel was investigated. The results showed that the hydrogel composite presented a good photoantibacterial property, while the antibacterial activity can be neglected under the condition of no light. The complete release of curcumin from the composite was achieved after 120 h. Therefore, the hydrogel system has the characteristics of low cost and high effect, which could be used for an antibacterial sustained-release material.
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Journal of Cleaner Production
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2019
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IF 6.395
Longzheng Wang,Gaobo Yu,Jiacheng Li,Yuhong Feng,Yang Peng,Xinyu Zhao,Yiyuan Tang,Quan Zhang
In agritechnology applications, the sustained release of pesticides plays significant roles in efficient bioavailability and environmental protection. In this study, hydrophobic derivate of sodium alginate (Ugi-SA), polyacrylamide (PAM) and montmorillonite (MMT) were utilized to construct several stretchable double-network nanocomposite hydrogels, which were used to control the release of λ-cyhalothrin. These nanocomposite hydrogels were fully characterized by Fourier transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffraction (XRD). The adoption of Ugi-SA and appropriate incorporation of MMT could significantly improve the tensile properties , pesticide-loading efficiency and sustained release performances of the hydrogels. The swelling behavior of all the hydrogels well fits into the Fickian diffusion model. The maximum fracture strain and loading efficiency of the hydrogels reached 2000% and 81.30%, respectively. The hydrogel with 5% MMT content shows the lowest cumulative release percentage of 6.68% over 87 h, and the pesticide release curves well fit into the Weibull model. These novel nanocomposite hydrogels take advantages of both the gelation property of alginate derivatives and the adsorption capacity of clays, to serve as promising potential carriers and to improve the utilization efficiency of water-insoluble pesticides.
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Materials Science & Engineering C-Materials for Biological Applications
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2018
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IF 5.08
Xiuyan Wang,Yanyan Cao,Husheng Yan
Chlorambucil, a chemotherapeutic agent, is usually administered orally to treat chronic lymphocytic leukemia and some other types of cancers in regimens of conventional and metronomic chemotherapies. However, the hydrolytic instability of chlorambucil is a major limitation in achieving the optimum therapeutic performance. In this work, mesoporous polymeric microspheres were prepared by free radical suspension copolymerization of methyl acrylate and divinylbenzene in the presence of porogen. Chlorambucil was loaded into the mesoporous polymeric microspheres through adsorption of the drug in aqueous media with high loading capacity up to more than 350 mg/g. Chlorambucil-loaded mesoporous polymeric microspheres showed sustained release property in media simulating gastrointestinal fluids, with nearly zero order release kinetics. Furthermore, the mesoporous polymeric microspheres as carriers greatly stabilized chlorambucil against its hydrolysis. The hydrolyzation percentage of chlorambucil that was adsorbed on the microspheres after incubation for 36 h in media simulating gastrointestinal fluids was less than 10%, while more than 90% of free chlorambucil hydrolyzed after incubation in the same media for 4 h. The chlorambucil-loaded mesoporous polymeric microspheres may be used as oral sustained release formulations, especially as oral formulations for the application in metronomic chemotherapy.
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JOURNAL OF MATERIALS SCIENCE
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2015
·Vol. 50
·期 14
·4914-4925
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IF 2.371
Cheng Cui,Xia Dandan,Zhang Xiuli,Chen Li,Zhang Qiqing
The therapeutic concentration of cisplatin (CDDP) is usually associated with dose-limiting side effects. To avoid these harmful effects, a biocompatible hydrogel carrier which consisted of poly( N -isopropylacrylamide) and carboxymethyl chitosan was designed to deliver CDDP to the local environment of a solid tumor. The poly( N -isopropylacrylamide)-g-carboxymethyl chitosan hydrogels were synthesized by chemical crosslinking. Scanning electronic microscopy images showed that the hydrogels exhibited a cross-linked structure with the average pore size from 100 to 200 µm. Water contact angles and swelling studies suggested that the hydrogels had good hydrophilicity and the lower critical solution temperature lay in the vicinity of 32 °C. The MTT assays implied that the hydrogels were non-cytotoxic on NIH3T3 cells. In vitro release experiment demonstrated that the release of CDDP was controllable and sustained over a long period. Moreover, the released CDDP retained its anticancer activity on A549 cells. The hydrogels are promising carriers for sustained release of cisplatin.
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BIOMATERIALS
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2016
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IF 8.387
Ming Lei,Zihang Peng,Qian Dong,Yuanfeng He,Zhaoguo Zhang,Xuefei Zhang,Mina Yan,Chunshun Zhao
One of the most important and challenging goals in pharmaceutical prevention for posterior capsule opacification is to preserve an effective drug concentration in capsular bag for a long period without affecting the patients' vision. Here, a novel kind of composite, which was prepared by 2-hydroxyethyl methacrylate (HEMA) and methyl methacrylate (MMA) via a two-step process, was applied for capsular tension ring (CTR) as an implant that could deliver docetaxel (DTX) over a long period of time. The drug release rate of the composite could be controlled by the ethyleneglycol dimethacrylate (EGDMA) content and the ratio of HEMA/MMA as well as the structure of porous PMMA framework. The CTR could continuously release DTX for up to 6 weeks in vitro and maintain DTX in effective concentration in the aqueous humor after 42 days. Docetaxel-load capsular tension ring (DTX–CTR) presented strong inhibition on the lens epithelial cells in-vivo without obvious damage to normal tissues. These results indicate that the drug sustained-release CTR can provide a promising application in posterior capsule opacification prevention.
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LANGMUIR
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2024
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IF 3.7
Jiahui Zhang,Dongxin Zhao,Kui Lu,Libo Yuan,Heng Du
Based on the typical similar repeat units (abcdefg)n of α-helical structure, the peptide H was designed to self-assemble into an organohydrogel in response to pH. Depending on the different pH, the proportions of secondary structure, microstructure, and mechanical properties of the gel were investigated. Circular dichroism (CD) and Fourier transform infrared (FT-IR) showed that the proportion of α-helical structure gradually increased to become dominant with the increase of pH. Combining transmission electron microscopy (TEM) and atomic force microscopy (AFM), it was found that the increase of the ordered α-helix structure promoted fiber formation. The further increase in pH changed the intermolecular forces, resulting in an increase in the α-helix content and the enhancement of helix–helix interaction, causing the gel fibers to converge into thicker and more dense ones. The temperature test showed the stable rheological properties of the organohydrogel between 20–60 °C. Drug release and cytotoxicity showed that the DOX-loaded organohydrogel could have a better release in an acidic environment, indicating its potential application as a drug local delivery carrier.
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ACS Applied Materials & Interfaces
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2025
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IF 8.2
Vinayak Hegde,Mahesh P. Bhat,Jae-Ho Lee,Cheol Soo Kim,Kyeong-Hwan Lee
Pesticide delivery carriers provide protection against pathogens but face significant challenges, including limited loading capacity, rapid release rates, and inconsistent performance. To address these issues, this study develops a dual-stimuli-responsive pesticide delivery carrier, featuring an iron–copper bimetal–organic framework (Fe–Cu MOF) supported on diatomaceous earth (DE) and coated with lauric acid (LA). Here, DE serves as a biocompatible scaffold, enhancing the adhesion and retention of MOF particles at target sites, thereby improving the pesticide localization and delivery efficiency. The carrier exhibits a high thiabendazole (Tbz) loading capacity of 38.14% owing to its nanoporous structure. The LA coating functions as a pH- and temperature-responsive barrier, regulating pesticide release to prolong the treatment duration and minimizing the need for repeated applications. The carrier demonstrates controlled release rates of 80.73% at pH 5 and 96.55% at 40 °C, confirming its dual-stimuli responsiveness. In vitro assays reveal 92.26% inhibition of Botrytis cinerea at 1 μg mL–1, while in vivo experiments on tomato plants and fruits show complete inhibition at 200 μg mL–1. Additionally, the developed composites adhere strongly to leaves through electrostatic and hydrogen-bonding interactions, reducing the loss of pesticide due to rain erosion. Overall, DE-MOF-Tbz-LA presents a promising and efficient alternative to conventional pesticide applications.
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Biomaterials Research
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2024
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IF 8.1
Chenyang Li,Shuai Wang,Chenghui Liao,Ying Li,Yunfeng Zhou,Haiqiang Wu,Wei Xiong
Klotho (KLO) is an anti-fibrotic protein expressed in the kidneys and has been decreasing in the development of renal fibrosis (RF). However, restoring the decline in KLO levels remains a great challenge during RF treatment. Herein, an injectable KLO-loaded chitosan (CS) hydrogel (KLO-Gel) is designed to achieve localized and prolonged release of KLO in the RF treatment. KLO-Gel was prepared by cross-linking CS with β-glycerophosphate (β-GP), followed by rapid (within 3 min) thermosensitive gelation at 37 °C. Furthermore, KLO-Gel exhibited a slow and sustained release (over 14 d) of KLO both in PBS and in the kidneys of mice with unilateral ureter obstruction (UUO). A single local injection of KLO-Gel into the renal capsule of UUO mice was more effective at reducing RF (i.e., maintaining renal function and tissue structure, alleviating extracellular matrix accumulation, and inhibiting the TGF-β1/Smad2/3 signaling pathway) over a 14-d period than daily intraperitoneal injections of free KLO or captopril. Crucially, CS was found to induce endogenous KLO secretion, highlighting the added value of using CS in RF treatment. Overall, this study demonstrated that KLO-Gel enhanced the anti-fibrotic efficacy of KLO while minimizing its off-target toxicity, and its clinical potential awaits further validation.
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COLLOIDS AND SURFACES B-BIOINTERFACES
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2024
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IF 5.4
Li Li,Fengting Xiang,Fan Wang,Anqi Chen,Yu Liu
The current situation of diabetes prevention and control is extremely severe. For instance, glimepiride (GLM), a third-generation sulfonylurea, demonstrates suboptimal clinical efficacy in oral dosage forms, which underscores the pressing need for the development of a new dosage form. Recently, in situ gel subcutaneous implants have garnered considerable attention. Hydroxybutyl chitosan (HBC) can spontaneously crosslink to form a thermosensitive hydrogel and has good biocompatibility. However, its application is hindered by its limited mechanical properties. Graphene oxide (GO), known for its stable dispersion in water, can load GLM through π–π stacking interactions. When combined with HBC, GO enhances the mechanical properties and stability of the hydrogel. Therefore, an HBC–GO@GLM hydrogel was prepared. Rheological analysis revealed that the incorporation of GO increased the critical gelation temperature of the 5 wt% HBC hydrogel from 19.1°C to 27.2°C, considerably enhancing the mechanical properties of the hydrogel. Using encapsulation efficiency as an evaluation index, the optimal encapsulation efficiency of GO@GLM was determined to be 73.53% ± 0.45% with a drug loading capacity of 27.39 ± 0.17% using the Box–Behnken design model. Computer simulation technology validated the interaction between the materials and the drug release mechanism. Pharmacokinetic results showed that compared to the HBC@GLM group, the half-life (t1/2), mean residence time and the area under the curve for the HBC–GO@GLM group were approximately 3 times those of the HBC@GLM group. Subcutaneous implantation of the HBC–GO@GLM hydrogel for drug delivery considerably extended the drug’s action time in the body, thereby maintaining blood sugar levels within a normal and stable range for an extended period.
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ACS Sustainable Chemistry & Engineering
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2024
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IF 7.1
Qingyin Dai,Ruijing Jia,Han Li,Jisheng Yang,Zhiyong Qin
Silver nanoparticles (AgNPs) are broad-spectrum antibacterial agents that are safe for the environment and the human body. To achieve a balance between material functionality, degradability, and safety of AgNPs, the peanut red skin (PSE)/polyphenol-hydroxypropyl-β-cyclodextrin (HPβCD)/AgNPs were prepared for the first time by ultrasound-triggered molecular encapsulation and biosynthesis for hydrophilic fusion of medicine and small molecules. Additionally, a novel “controlled release” sodium alginate (SA)-based hydrogel was developed and medicine/small-molecule self-assembled PSE/HPβCD/AgNPs were introduced into the three-dimensional network structure of the SA hydrogels. The SA-based hydrogels exhibited excellent mechanical and rheological properties. In different pH conditions, the hydrogels exhibit differing release and expansion behaviors, and the maximum cumulative release of AgNPs was 98.21% at pH > 6.8. Furthermore, the hydrogels exhibited strong antibacterial effects against pathogenic bacteria. They also showed excellent antioxidant properties and cytocompatibility. These advantages highlight the potential utility of the developed hydrogels for biomedical applications and agricultural fields.
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Expert Opinion on Drug Delivery
·
2024
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IF 5
Zhutian Zhang,Qian Ma,Zhaoxing Dai,Jiaxu Hong,Jifeng Gu,Rong Shi,Jianjiang Xu,Yaling Ma,Xinghuai Sun,Jianguo Sun
Background Glaucoma is one of the major irreversible blinding eye diseases in the world. Reducing intraocular pressure (IOP) is the primary treatment option, and taking eye drops daily is the common method. However, short drug duration and poor bioavailability of eye drops may lead to unsatisfied therapeutic effects and inadequate patient compliance.Methods A brimonidine-loaded silicone rubber insert (BRI@SR@PT) was prepared by loading brimonidine into a surface-modified silicone rubber ring, followed by polydopamine/thermoplastic polyurethane coatings. The physical properties, in vitro cytocompatibility and drug release of BRI@SR@PT were investigated. The BRI@SR@PT was administrated in the conjunctival sac of rabbit eyes, and its in vivo drug release, IOP-lowering efficacy and biosafety were assessed.Results The BRI@SR@PT presented great thermal stability and excellent elasticity. The BRI@SR@PT was able to release BRI sustainably for 28 days with little toxicity in vitro. Compared to BRI eye drops, the BRI@SR@PT effectively lowered IOP for 21 days based on the sustained BRI release with great biosafety when administrated in conjunctival sac of rabbit eyes in a noninvasive fashion.Conclusions The conjunctival sac insert (BRI@SR@PT), as a promising drug-delivery platform, may provide a sustained IOP-lowering treatment for patients with ocular hypertension or glaucoma, without the need for invasive procedures.
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