ACS Applied Polymer Materials
·
2026
·Vol. 8
·期 17
·15593-15610
·
IF 5.2
Luo Zidan,Liang Siwei,Chen Chen,Mukwana Sonia,Yao Shun
In this study, a dual sustained-release injectable gel
loaded with Periplaneta americana ( P. americana ) protein–polysaccharide complex
(PPc) microspheres was developed
to achieve prolonged protein release and promote chondrocyte proliferation.
The system was constructed by encapsulating PPc-loaded microspheres
within a cationic guar gum gel matrix. PPc extracted from P. americana residues were fabricated into microspheres
via ionic emulsification cross-linking followed by glutaraldehyde
fixation. The cationic guar gum gel incorporating these PPc microspheres
was subsequently prepared through sequential acid–base neutralization,
exhibiting favorable injectability, rheological behavior, and self-healing
capacity. The optimized formulation (MS-6-gel) demonstrated excellent
encapsulation efficiency and enabled sustained release of P. americana PPc, with a maximum cumulative release
rate of 73.4%, indicating its potential for controlled and efficient
local delivery. Kinetic analysis using Korsmeyer–Peppas and
Weibull models revealed that the dual-barrier structure of the microsphere-in-gel
system substantially retarded protein diffusion, thereby extending
the release duration. Furthermore, MS-6-gel functioned as a multifunctional
platform, not only exhibiting remarkable coagulation ability and potent
antibacterial activity against both Staphylococcus aureus (100.0 ± 1.8%) and Escherichia coli (85.8 ± 2.8%), but also effectively supporting
ATDC5 chondrocyte proliferation. In summary, this dual sustained-release
gel system (MS-6-gel) integrates prolonged protein delivery, chondrocyte
proliferation promotion, antibacterial, and hemostatic functions.
Its unique microsphere-in-gel architecture enables controlled release
kinetics, highlighting a promising nature-derived strategy for cartilage
tissue engineering and biomedical applications.
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2021
·
IF 3.232
Hongfei Liu,Xiaoya Xie,Chao Chen,Caleb Kesse Firempong,Yingshu Feng,Limin Zhao,Xuezhi Yin
Objective The purpose of the present study was to prepare a clonidine hydrochloride (CH) sustained-release suspension.Methods The processes involved in the drug formulation included drug loading, impregnating, and suspension preparation. Clonidine hydrochloride drug–resin complexes (CH-DRC) were prepared using the bath method and the CH-DRC impregnated before the microencapsulation process. Based on the bottom spray fluidized bed coating method, the CH microencapsulated drug–resin complexes (CH-MC) were also prepared using Surelease® (the suspension of ethyl cellulose aqueous dispersion) as the coating material. The effects of coating (process/formulation) on the in vitro release of coating microcapsule were evaluated via single factor investigation and orthogonal design optimization. The CH-MC with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. Rats were given commercial CH ordinary tablets and the CH sustained-release suspension via intragastric administration. The plasma concentration–time curve and related pharmacokinetic parameters were investigated using the non-compartment model.Results The Tmax of the CH sustained-release suspension was delayed from 2 h to 5 h compared with the CH ordinary tablets. Similarly, the Cmax was reduced from 32.138 µg·mL−1 to 18.150 µg·mL−1 with the concentration–time curve being more gentle compared with the commercially CH ordinary tablets. After oral administration, the relative bioavailability of CH sustained-release suspension (AUC0–24 of 137.703 µg·h·mL−1) to its CH ordinary tablets (AUC0–24 of 123.337 µg·h·mL−1) was 111.65%.Conclusions The findings showed that the CH sustained-release suspension for oral administration was successfully formulated.
研究领域:
药剂学
·
药物递送系统
·
生物药剂学
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Biomaterials Science
·
2020
·Vol. 8
·期 22
·6190-6203
·
IF 6.183
Cheng-guang Wu,Xiang Wang,Yun-feng Shi,Bin-cheng Wang,Wei Xue,Yi Zhang
Supramolecular hydrogels derived from natural biomolecules have promising applications for drug delivery due to their inherent biocompatibility and tunable responsiveness to various stimuli. However, conventional hydrogels only modulate the release kinetics roughly to achieve sustained drug release, exhibiting fast-then-slow release behavior without on/off control. Herein, a guanosine (G)-quartet·Na+-borate supramolecular hydrogel (GB hydrogel) cross-linked via a guanosine–borate diester and intertwined by G4-nanofibres formed by π–π stacking of G4-quartets stabilized by Na+ is developed for on-demand release of Acyclovir (Acv). This GB hydrogel is facilely prepared by a one-pot hierarchical assembly involving hydrogen bonds, dynamic borate ester bonds and cation coordination, which endow it with tunable mechanical properties, excellent self-healing properties and reversible degradation behavior in response to pH, glucose and ion concentration. Benefiting from that the guanosine analog Acv is able to assemble into a G4-quartet by replacing guanosine via reversible hydrogen bonding, the Acv-loaded GB hydrogel showed favorable stability in physiological medium without undesired release and achieved external stimulus-triggered on-demand release with switchable on/off control and tunable release kinetics. Moreover, the GB hydrogel also exhibited excellent in vitro and in vivo biocompatibility. Such a natural nucleoside-based supramolecular hydrogel with on-demand drug release, self-healing property, biodegradability and biocompatibility provides a precisely controlled paradigm to overcome early burst release behavior of conventional hydrogels for the development of injectable hydrogel delivery systems.
研究领域:
药物递送
·
生物材料
·
化学
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FOOD CONTROL
·
2021
·
IF 5.548
Ying Lin,Ran Huang,Xiuxiu Sun,Xi Yu,Ying Xiao,Ling Wang,Wenzhong Hu,Tian Zhong
In order to develop a biodegradable agent for food preservation, β-cyclodextrin (β-CD) inclusion complexes containing p -Anisaldehyde (PAA) were prepared using co-precipitation method. Physical properties including moisture content, bulk density, hygroscopicity, entrapment efficiency and loading capacity of the inclusion complexes showed considerable results for food applications. SEM and particle size test showed notably difference between the prepared inclusion complexes and the other formulations including the raw β-CD, physical mixture, and the recrystallized β-CD in both shape and size distribution. FTIR , XRD, TGA and DTA were also carried out and confirmed the formation of inclusion complexes and inhibition of the volatility of encapsulated PAA. As a potential preservation agent, inclusion complexes demonstrated a sustained released behavior in phosphate buffer saline (PBS). Comparing with pure PAA, the inclusion complexes presented a better storage stability in low humidity environment, a higher antioxidant activity , and equal MICs against Escherichia coli and Staphylococcus aureus .
研究领域:
食品科学
·
药学
·
材料科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Huan Liu,Xinyu Meng,Lei Li,Yongmei Xia,Xueyi Hu,Yun Fang
Assemblies of as called “chitosan hydrogel-liposome” are expected for overcoming the burst effect in drug release from chitosan (CS) hydrogels. Herein, a hydrogel delivery system made of chitosan incorporated fatty acid vesicles was constructed for protective sustained release of curcumin (Cur). The curcumin was encapsulated in the prepared oligo-conjugated linoleic acid vesicles (OCLAVs), and then the drug-embedded vesicles were constructed to Cur-OCLAVs-CS hydrogels with CS solution. The fabricated Cur-OCLAVs-CS hydrogel was fluidic at room temperature and could be rapidly gelled at 37 °C. Morphology study proves that the OCLAVs stayed as nano-vesicles in the gel. The Cur-OCLAVs-CS hydrogels effectively declined the burst effect with enhanced antioxidant activity. The Cur (400 μM)-OCLAVs-CS gel presented a cumulative release rate of 51.23 % of curcumin in 96 h, comparing to 93.37 % of that from the Cur-CS gel. Moreover, the corporation of OCLAVs and CS made the gel exhibited strong synergistic effect on the antioxidant activity, with an enhancement of up to 148.1 % on the ferric reducing power. Therefore, the hydrogel carrier made of incorporated fatty acid vesicles-chitosan can be served as an injectable or 3D printable drug delivery system, which may provide a hint to overcome the burst effect that existed in chitosan and other polysaccharide-based gels.
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Rongtai Zuo,Jingjing Shi,Susu Jiang,Min Chu,Qiyang Wang,Lingchi Kong,Qinglin Kang,YaPing Guo,Junjie Guan
Diabetic skin disorders are lingering and refractory clinical diseases. In this study, a genipin-crosslinked porous chitosan fiber (CSF) hydrogel was fabricated to achieve rapid wound healing. By embedding clemastine fumarate (CF) in the CSF hydrogel pores, we synthesised a CSF/CF hydrogel for the treatment of diabetic wounds. The microstructure, chemical elements, spectral variation, mechanical properties, swelling ratios, degradability, and toxicity of the CSF/CF hydrogels were studied. Compared with the typical CS power hydrogel, the porous CSF hydrogel crosslinked with genipin possesses a stable structure and improved physicochemical properties. Moreover, CF was slowly released from the CSF hydrogel. Molecular simulation also showed that CF was evenly embedded inside the cavity formed by the novel CSF hydrogel. The results suggested that CF can resist damage from high glucose levels and promote proliferation, tube formation, and migration of endothelial cells (ECs) and fibroblasts. The CSF/CF hydrogel promoted wound healing in a rat model. Mechanistically, the beneficial effect of CF on wound healing may be related to activation of the MEK/ERK and PI3K/Akt signalling pathways. In conclusion, genipin-crosslinked CSF/CF hydrogel can accelerate wound healing and may be an effective therapeutic method for treating diabetic skin lesions.
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2022
·
IF 3.571
Gugu Hao,Rong Hu,Xiaoqin Wang,Pan Gao,Lin Wang,Manhua Jiang,Libo Xin,Guoying Tan,Yanping Zhao,Fuzhou Sun,Dexin Chu,Jinqian Lv,Jinsong You,Fangfang Huang,Xuezhi Song
In recent years, nitrosamines have been discovered in some types of drug products that becomes a current regulatory hotspot, and have attracted a lot attention from both regulatory authorities and industry. This manuscript provided an industry perspective on the nitrosamines research. A liquid chromatography coupled with tandem mass spectrometry（LC-MS/MS）method was developed and applied for the quantification of N-nitrosodimethylamine (NDMA) in metformin hydrochloride sustained-release tablets (MET). The key factors resulting in the NDMA formation in MET were identified through forced degradation and drug-excipient studies, which included high temperature, dimethylamine , strong alkali and oxidation conditions, peroxide and alkaline components contained in the formulation as well as the nitrite and nitrate impurities that might be presented in certain excipients. Further, API particle size and water content of the drug product would also affect the growth rate of NDMA. Therefore, the following mitigation strategies to reduce the risk of nitrosamines in the finished drug product are proposed in this manuscript: 1) avoid the use of excipients containing nitrite, nitrate and peroxide impurities; 2) avoid high temperature and strong alkaline environment in the production and storage condition; 3) maintain an appropriate water content level in the formulation. Based on the above principles, it was recommended to add antioxidant or incorporate excipient such as Na 2 CO 3 to modify the formulation pH to weak basic environment in the formulation of MET, which can could effectively prevent formation of NDMA in the stability process.
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MOLECULES
·
2022
·Vol. 27
·期 13
·4268
·
IF 4.927
Jie Wang,Yuntian Xing,Yang Dai,Yingnan Li,Wenyan Xiang,Jianrong Dai,Fei Xu
Pomacea canaliculata, one of the 100 most destructive invasive species in the world, and it is an important intermediate host ofAngiostrongylus cantonensis. The molluscicides in current use are an effective method for controlling snails. However, most molluscicides have no slow-release effect and are toxic to nontarget organisms. Thus, these molluscicides cannot be used on a large scale to effectively act on snails. In this study, gelatin, a safe and nontoxic substance, was combined with sustained-release molluscicide and was found to reduce the toxicity of niclosamide to nontarget organisms. We assessed the effects of gelatin and molluscicide in controllingP. canaliculatasnails and eggs. The results demonstrated that the niclosamide retention time with 1.0% and 1.5% gelatin sustained-release agents reached 20 days. Additionally, the mortality rate ofP. canaliculataand their eggs increased as the concentration of the niclosamide sustained-release agents increased. The adult mortality rate ofP. canaliculatareached 50% after the snails were exposed to gelatin with 0.1 mg/L niclosamide for 48 h. The hatching rate ofP. canaliculatawas only 28.5% of the normal group after the treatment was applied. The sustained-release molluscicide at this concentration was less toxic to zebrafish, which means that this molluscicide can increase the safety of niclosamide to controlP. canaliculatain aquatic environments. In this study, we explored the safety of using niclosamide sustained-release agents with gelatin againstP. canaliculata. The results suggest that gelatin is an ideal sustained-release agent that can provide a foundation for subsequent improvements in control ofP. canaliculata.Keywords:invasive species;biological material carrier for sustained drug;Pomacea canaliculatacontrol;environmental safety
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JOURNAL OF POROUS MATERIALS
·
2022
·Vol. 29
·期 5
·1489-1505
·
IF 2.523
Chang Ziling,Li Huafei,Yang Yuxiang,Yuan Hongming,Huang Yan,Yao Pingping,Ni Chaoying
Herein, we developed the dual-function template method to fabricate hollow magnetic nano-spheres (denoted as HMFe–Si–C n , n = 16, 18) with a mesoporous shell and hollow interior structure using alkyl chain trimethoxysilane templating. The shorter chain template directed formation of HMFe–Si–C 16 with size of 119 nm, having disordered inkbottle type mesopores and saturation magnetization of 50.01 emu/g higher than that of HMFe–Si–C 18 with cylindrical type mesopores. In addition, the HMFe–C n loaded with MMC diaplays a pH and magnetic dual responsive drug release behavior. By contrast, Mitomycin C (MMC) loading efficiency of HMFe–Si–C 16 was higher owing to the fact that the pore size, surface area, and pore volume of HMFe–Si–C 16 were larger than those of HMFe–Si–C 18 . Besides, MMC loaded HMFe–Si–C n hollow spheres showed a clear pH-dependent drug release behavior, having a higher release rate in acidic environments of pH 5.7. For the pH 5.7 and 7.4 release, the release kinetic for HMFe–Si–C 16 –MMC composites follows pseudo-first-order attributable to its special pore structure. With Fe(0) as a core, HMFe–Si–C n is distinguished for higher magnetic properties, and it is more conducive to magnetic targeted treatment of cancer cells and can release drugs through external magnetic field. In addition, HMFe–Si–C n has lower cytotoxicity and better biocompatibility. For this reason the inner cavity of HMFe–Si–C 16 could be labeled with radioisotope 99 Tc m to study the magnetic targeting distribution of HMFe–Si–C 16 in vivo, and its cytotoxicity against in vitro HeLa cells was also studied. These results indicate the potential of HMFe–Si–C 16 in the magnetic targeted drug delivery system.
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MACROMOLECULAR MATERIALS AND ENGINEERING
·
2022
·Vol. 307
·期 10
·2200262
·
IF 4.402
Zhiwen Zeng,Cuiping Guo,Daohuan Lu,Zhijie Geng,Dating Pei,Shan Yu
Infection and chronic inflammation caused by oxidative stress are the main challenges in chronic wound healing. In this study, a silk fibroin/kappa-carrageenan ( k CA)-based hydrogel functionalized with epigallocatechin-3-gallate (EGCG) and Cu 2+ is fabricated for chronic wound healing. Polyphenol–metal functional complexes and ionic-covalent entanglement networks are prepared by introducing Cu 2+ . Cu 2+ coordinates with k CA to enhance the mechanical properties and chelates with EGCG to form an EGCG-Cu 2+ complex that continuously releases EGCG. The sustained release of EGCG enhances the antibacterial properties by synergizing with the effects of Cu 2+ . Furthermore, the prepared hydrogel exhibits a potent ability to scavenge excessive intracellular reactive oxygen species, controllable antioxidant bioactivity, and reliable biocompatibility. Ultimately, the resulting multifunctional hydrogel dressing provides a potential and effective strategy for chronic wound care management with increased mechanical strength and antibacterial and antioxidant properties.
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APPLIED SURFACE SCIENCE
·
2021
·
IF 6.707
Xiang Gao,Rui Huang,Yanpeng Jiao,Thomas Groth,Wufeng Yang,Chenlin Tu,Hailong Li,Fan Gong,Jiaqi Chu,Mingyan Zhao
The healing of wounds in diabetes mellitus patients remains a critical clinical challenge globally. To promote healing, the development of bioactive dressings that not only provide physical protection but also supply a favorable microenvironment for healing at the wound interface is urgently required. Herein, Michael addition reaction was first used for intrinsic-crosslinking of bioactive maleilated chitosan/thiolated hyaluronan (mCH/tHA) multilayer coatings on poly (L-lactic acid) (PLLA) nanofibrous mats (P-mCH/tHA) for a sustained release of insulin (IN) and compared that with pure PLLA and PLLA mats coated with native CH/HA (P-CH/HA) multilayers. The physicochemical studies showed that P-mCH/tHA have higher tensile strength, an accelerated degradation rate, more antibacterial activity and sustained release of insulin when compared to P-CH/HA and pure PLLA mats. Studies on bioactive properties of PLLA mats coated with either mCH/tHA or CH/HA indicated an improved adhesion, spreading and proliferation of mesenchymal stem cells on P-mCH/tHA_IN in comparison to the other PLLA mats. Most interestingly, in vivo investigations with a diabetes mouse model demonstrated fastest wound closure when using P-mCH/tHA_IN among all groups with facilitated re-epithelization, angiogenesis, and increased collagen deposition in the wounds, which makes this coating in combination with IN promising for development of new bioactive wound dressings.
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2021
·
IF 3.517
Jianfeng Guo,Juhui Liu,Haoran Qie,Feng Zhao,Catherine Hui Niu
Folate-modified carboxymethyl chitosan (FCMC) was made by folate acid as targeted group and attaching folate to carboxymethyl chitosan, and then, targeted FCMC/CaCO3 hybrid nanosphere were formed by self-assembly of calcium carbonate in FCMC solution. The physicochemical properties of the nanospheres were investigated by Fourier transform infrared spectroscopy, X-ray diffraction analysis, Brunauer–Emmett–Teller measurement and thermogravimetric analysis (TGA). The results showed that the FCMC/CaCO3 hybrid nanospheres were composed of calcite, vaterite and polysaccharides, and the content of organic compounds was 12.17%. Also, the structure performance of the hybrid nanospheres was analyzed. Besides, the effects of the hybrid nanospheres on the encapsulation efficiency, the drug loading content and the release behavior were also analyzed with the metformin (MET) as a model drug. Scanning electron microscope, Zeta potential analysis and UV–Vis were used to characterize the hybrid nanospheres. Under the conditions of FCMC/Ca2+ molar ratio of 4: 1 and reaction for 24 h, the achieved results showed that the spherical aggregates with regular morphology were obtained and the average particle size of the nanospheres was 207 nm. The specific surface area of the hybrid nanosphere is 27.06 m2·g−1 and the average pore diameter of the sample is 3.84 nm, indicating the presence of mesoporous structure in the sample. This mesoporous structure can supply potential space for adsorption of anticancer drugs. Additionally, the surface charge of the nanoparticles was positive and the entrapment efficiency was 83.32%. The hybrid nanospheres have a capability of effective pH-sensitivity controlled drug release. All the drug loaded hybrid nanospheres successfully sustained the release of MET at pH 7.4, only about 44.58% of the drug released in 6 days. While under acidic condition (pH 5.0) drug release was significantly accelerated, being over 98.85% of the drug released. The hybrid nanospheres demonstrated an excellent smart drug delivery behavior.
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