INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2019
·
IF 4.213
Jiaxin Liu,Shuang Li,Ge Li,Xiang Li,Changhui Yu,Zhijiang Fu,Xiangyu Li,Lesheng Teng,Youxin Li,Fengying Sun
Bevacizumab, a vascular endothelial growth factor (VEGF)-targeting drug, is widely used as an off-label therapeutic for age-related macular degeneration (AMD). To reduce the monthly administration frequency, this study investigated microspheres comprising a poly( d , l -lactide-co-glycolide)/poly(cyclohexane-1,4-diyl acetone dimethylene ketal) (PLGA/PCADK) blend that could be loaded with bevacizumab-dextran particles using solid-in-oil-in-water (S/O/W) emulsification. Control microspheres were also prepared through water-in-oil-in-water (W/O/W) emulsification. The structural stability of bevacizumab in the polymer monomers was analyzed using dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), size exclusion chromatography (SEC-HPLC), circular dichroism (CD) and fluorescence spectroscopy. Subsequently, microspheres were prepared and evaluated in terms of their morphology, encapsulation efficiency and release behavior. PLGA/PCADK microspheres prepared by the S/O/W method with <20% PCADK showed a smooth spherical structure with a uniform distribution of bevacizumab. The microspheres exhibited a release behavior comprising a slight initial burst and an increasing total release over 50 days both in vitro and in vivo . Additionally, the microspheres were well tolerated by ocular tissue. Finally, a chorioallantoic membrane (CAM) assay revealed that the bioactivity of bevacizumab was retained by PCADK. In conclusion, these results suggest the potential for bevacizumab-loaded PLGA/PCADK microspheres prepared by the S/O/W method as a means of intravitreal therapy for ocular diseases.
研究领域:
药物学
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眼科学
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药物递送系统
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PubMed
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Foods
·
2026
·Vol. 15
·期 1
·147
·
IF 5.1
Wenjie Qu,Zhuoyuan Zhang,Yiran Guo,Yan Chen,Linpeng Wang,Jian Huang,Jiyong Yin
Polygonatum sibiricumpolysaccharide (PsP), one of the main components ofPolygonatumsibiricumused in traditional Chinese food and medicine, has important bioactive functions, but it is difficult to fully utilize PsP because of the degradative effect of digestive gastric juices. This study aimed to innovatively synthesize a new food formulation for PsP, namely, a PsP–hydroxyapatite (HAP) sustained-release system, so as to reduce its degradation. The new food formulation was optimized and evaluated by the response surface method (RSM) and by in vitro experiments. The optimal stirrer temperature, reaction pH, etching pH, and loading time for synthesizing PsP-HAP were 85.62 °C, pH 11.12, pH 8.40, and 5.10 h, respectively, all of which were different from the findings of other similar research studies. The average encapsulation rate of PsP-HAP reached (40.16 ± 1.54)%, and the content of PsP was 8.98%. Additionally, PsP-HAP appeared to be pH-responsive, and its continuous antioxidative effect was first proven by the DPPH assay and then cytologically by a total antioxidative capacity assay. The CCK-8 assay indicated that PSP-HAP did not induce toxicity. This study successfully developed a new food formulation for PsP which appears to have the potential to reduce the degradative effect of digestive gastric juices. Thus, it is possible to achieve full utilization of PsP by using this new sustained-release food formulation.
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International Journal of Polymer Science
·
2018
·Vol. 2018
·期 1
·7584281
·
IF 1.718
Zhichuan Shen,Xinhua Zhou,Huina Qiu,Hua Xu,Huayao Chen,Hongjun Zhou
By using dopamine (DA) as the monomer, the model drug avermectin (AVM) was loaded on polydopamine microspheres (AVM/PDAMS) and polydopamine microcapsules (AVM@PDAMC) by the method of impregnation and encapsulation, respectively. The materials’ structures were systematically characterized using Fourier transform infrared spectroscopy (FTIR), zeta potential analysis, scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC). The comparison of antiultraviolet capability as well as release behaviors under different pH values of the materials were studied. The results showed that a spherical appearance was observed from both materials. The use of AVM/PDAMS and AVM@PDAMC made the decomposition temperature of AVM increase to 235°C and 245°C, respectively. After being exposed to ultraviolet light for 1400 min, the residual ratios of AVM of AVM/PDAMS and AVM@PDAMC were 42% and 54%, respectively. Both AVM/PDAMS and AVM@PDAMC showed acid sensitivity. AVM/PDAMS and AVM@PDAMC took about 13 h and 60 h to reach the release rate of 50% under pH 3. The release process of AVM/PDAMS could be explained by the Weibull model at pH 3, while the release behavior of AVM@PDAMC fitted the Baker–Lonsdale equation. At pH 7 and pH 9, both of the delivery materials followed the Korsmeyer–Peppas model and belonged to the Fick diffusion.
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Current Drug Delivery
·
2019
·Vol. 16
·期 4
·331-340
·
IF 1.645
Hanmei Li,Yuling Xu,Yuna Tong,Yin Dan,Tingting Zhou,Jiameng He,Shan Liu,Yuxuan Zhu
Objective: In this study, an injectable Sucrose Acetate Isobutyrate (SAIB) drug delivery system (SADS) was designed and fabricated for the sustained release of Ropivacaine (RP) to prolong the duration of local anesthesia. Methods: By mixing SAIB, RP, and N-methyl-2-pyrrolidone, the SADS was prepared in a sol state with low viscosity before injection. After subcutaneous injection, the pre-gel solution underwent gelation in situ to form a drug-released depot. Result: The in vitro release profiles and in vivo pharmacokinetic analysis indicated that RP-SADS had suitable controlled release properties. Particularly, the RP-SADS significantly reduced the initial burst release after subcutaneous injection in rats. Conclusion: In a pharmacodynamic analysis of rats, the duration of nerve blockade was prolonged by over 3-fold for the RP-SADS formulation compared to RP solution. Additionally, RP-SADS showed good biocompatibility in vitro and in vivo. Thus, the SADS-based depot technology is a safe drug delivery strategy for the sustained release of local anesthetics with long-term analgesia effects.
研究领域:
药剂学
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药物递送
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麻醉学
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生物材料
·
控释系统
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高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2018
·
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.
研究领域:
药剂学
·
肿瘤学
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PubMed
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Journal of Cleaner Production
·
2019
·
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.
研究领域:
农业技术
·
材料科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Qianyu Sun,Tianzhong Yuan,Gang Yang,Daliang Guo,Lizheng Sha,Rendang Yang
The solubility of cyclodextrin metal-organic frameworks (CD-MOFs) in aqueous media making it not suitable as sustained-release drug carrier. Here, curcumin-loaded CD-MOFs (CD-MOFs-Cur) was embedded in chitosan- graft -poly(lactic acid) (CS-LA) via a solid-in-oil-in-oil (s/o/o) emulsifying solvent evaporation method forming the sustained-release composite microspheres . At CS-LA concentration of 20 mg/mL, the composite microspheres showed good sphericity. The average particle size of CS-LA/CD-MOFs-Cur (2:1), CS-LA/CD-MOFs-Cur (4:1) and CS-LA/CD-MOFs-Cur (6:1) composite microspheres was about 9.3, 12.3 and 13.5 μm, respectively. The above composite microspheres exhibited various degradation rates and curcumin release rates. Treating in HCl solution (pH 1.2) for 120 min, the average particle size of above microspheres reduced 28.19 %, 24.34 % and 6.19 %, and curcumin released 86.23 %, 78.37 % and 52.57 %, respectively. Treating in PBS (pH 7.4) for 12 h, the average particle size of above microspheres reduced 30.56 %, 26.56 % and 10.66 %, and curcumin released 68.54 %, 54.32 % and 31.25 %, respectively. Moreover, the composite microspheres had a favorable cytocompatibility, with cell viability of higher than 90 %. These composite microspheres open novel opportunity for sustained drug release of CD-MOFs.
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Journal of Materials Chemistry B
·
2023
·
IF 7
Wei Xiong,Lingmei Yuan,Jinyang Huang,Bin Pan,Ling Guo,Guowen Qian,Cijun Shuai,Zhikui Zeng
ABSTRACT： Many traditional Chinese medicines monomers, such as naringin (NG), can regulate the local immune microenvironment to benefit osteogenesis. However, the rapid release of NG in scaffolds severely influences the osteogenesis-promoting effect. Herein, NG was loaded into mesoporous bioglass (MBG) to achieve sustained release through physical adsorption and the barrier role of mesoporous channels, then MBG loaded with NG was added to poly (L-lactic acid) (PLLA) to fabricate composite scaffolds by selective laser sintering (SLS) technology. The results showed that the NG-MBG/PLLA scaffolds could continuously slow-release NG for 14 days compared with the NG/PLLA scaffolds, the cumulative release amount for the NG-MBG/PLLA scaffolds was 44.26%. In addition, the NG-MBG/PLLA scaffolds can promote the proliferation and osteogenesis differentiation of mouse bone marrow mesenchymal stem cells (mBMSCs). Meanwhile, the composite scaffolds declined the reactive oxygen species (ROS) level of RAW264.7 under the stimulation of lipopolysaccharide (LPS) and significantly suppressed Interleukin- 6 (IL-6) and enhanced Arginase-1 (Arg-1) protein expressions. Moreover, calcium nodules and alkaline phosphatase productions of mBMSCs under macrophages-conditioned medium for the NG-MBG/PLLA group also evidently increased compared with the PLLA and MBG/PLLA groups. The NG sustained-released composite scaffolds with osteo-immunomodulation function have a great application prospect in the clinic.
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FOOD CHEMISTRY
·
2023
·
IF 8.8
Dongyang Zhu,Wuchao Ma,Meilian Yang,Shuzhen Cheng,Ling Zhang,Ming Du
This study prepared osteogenic peptides (OPs) from cod meat by hydrolysis and subsequently encapsulated them in nanoliposomes (NLP) to enhance bioaccessibility. The characterization, stability, controlled release behavior and bioactivity of OPs-loaded nanoliposomes (OPs-NLP) were investigated as well. The highest loading capacity (27.32%) was achieved in NLP loaded with 6 mg/mL of OPs. The particle size, zeta potential, and encapsulation efficiency of OPs-NLP were 70.59 nm, −11.98 mV, and 75.24%, respectively. The interaction between OPs and empty NLP was through hydrogen bonding and hydrophobic. The OPs-NLP showed the greatest stability during storage at 4 °C. The in vitro release profile of OPs from OPs-NLP fitted a one-level kinetic model best. The osteogenic activity of OPs was unaffected by NLP encapsulation, and the bioaccessibility of OPs was notably improved. These findings suggest that OPs-NLP has the potential to be used in functional foods.
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JOURNAL OF MATERIALS SCIENCE
·
2015
·Vol. 50
·期 14
·4914-4925
·
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.
研究领域:
生物医学工程
·
药剂学
·
肿瘤学
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BIOMATERIALS
·
2016
·
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.
研究领域:
眼科
·
药学
·
生物医学工程
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DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2023
·
IF 5.6
Peng Xiong,Yang Yuping,Guo Chenqi,He Qin,Li Yan,Gong Tao,Li Jia
Berberine (BBR) has a long history of use in the treatment of Rheumatoid arthritis (RA) and is considered one of the most promising natural product for the treatment of RA. However, oral administration of berberine has low bioavailability and requires frequent administration, resulting in poor patient compliance. In this study, we developed a BBR-loaded phospholipid-based phase separation gel (BBR-PPSG) to achieve sustained drug release and long-term therapeutic effect. The stability of BBR-PPSG was verified and it was found that it can be stored for a long time. The pharmacokinetic study on rats and rabbits showed that BBR-PPSG not only achieved 1-month of sustained release, but also significantly increased the area under the curve (AUC) by nearly 9-fold and prolonged the half-life (t1/2) by 10-fold. By constructing rat and rabbit models of RA, we also proved that BBR-PPSG administration once a month effectively alleviated joint swelling, and significantly reduce TNF-α levels in AIA rats and OIA rabbits. Histopathological analysis of rabbit joint sections revealed that after intra-articular injection of BBR-PPSG, the synovial cell layer remained intact, while in the model group, the synovial cells were significantly reduced and exhibited necrosis. MicroCT data analysis showed that the values of Tb.N and Tb. Sp in the BBR-PPSG group were significantly better than those in the model group (p < 0.05). This study addressed the limitations of frequent administration of BBR by developing a phospholipid-based phase separation gel system for berberine delivery, achieving long-term sustained release. The BBR-PPSG demonstrated good biocompatibility, simple preparation and excellent stability, thus holding potential as a novel pharmaceutical formulation for RA treatment.
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