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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2022 · IF 8.025

Fabrication of phenylalanine amidated pectin using ultra-low temperature enzymatic method and its hydrogel properties in drug sustained release application

Chenmin Zheng,Wanping Huang,Yuping Zou,Wensi Huang,Peng Fei,Guoguang Zhang

In this study, pectin was modified with phenylalanine by ultra-low temperature enzymatic method to improve its gel properties. The grafting ratio of phenylalanine amidated pectin was studied under different reaction conditions. The highest value (29.21 %) was reached a reaction temperature of −5 °C and time of 12 h. Further analysis indicated that phenylalanine and high methoxyl pectin combined at the solid-liquid two phase interface under the catalysis of papain to form phenylalanine amidated pectin. Moreover, the physicochemical properties of pectin hydrogel and its feasibility as a sustained-release drug carrier were discussed. The results showed that phenylalanine amidated pectin can form hydrogel with a certain strength under acidic conditions, and there is no need to add a lot of soluble solids and divalent cations. Besides, the phenylalanine amidated pectin hydrogel as a sustained release carrier of drugs showed more sustained and complete drug release.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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AAPS PHARMSCITECH · 2021 ·Vol. 23 ·期 1 ·1-11 · IF 3.246

Preparation and Evaluation of rhINF-α-2b Sodium Hyaluronate Cross-Linked Porous Microspheres: Characterization, Sustained-Release Properties, and Antitumor Activity

Liu Hongfei,Zou Yi,Zhu Jie,He Haibing,Feng Yingshu,Firempong Caleb Kesse,Yu Yang,Sun Changshan

Recombinant human interferon α-2b (rhINF-α-2b), like most proteins, has several shortcomings such as relatively short half-life, low therapeutic index, high circulating drug fluctuations, and rapid degradation which could hinder its effective delivery. Novel electrostatic spray and ion exchange drug-loading techniques were combined to formulate rhINF-α-2b sodium hyaluronate cross-linked porous sustained-release microspheres (rhINF-α-2b-SHCPM), a protein delivery system. The different properties of rhINF-α-2b-SHCPM including the physicochemical nature, in vitro release behavior, and antitumor activity were evaluated. The loading rate (10.31 ± 0.94%) and encapsulation efficiency (89.09 ± 2.37%) of rhINF-α-2b-SHCPM produced acceptable values. The in vitro cumulative release rate of rhINF-α-2b-SHCPM within 24 h was also 86.26 ± 2.11% with a much better sustained release effect. Thus, the half-life (10.763 h) and retention time (14.067 h) of rhIFNα-2b-SHCPM were significantly prolonged with enhanced bioavailability (43,198.387 ng/L*h) and decreased peak concentration (15,266.4 ngL -1 ) compared with the free rhIFNα-2b protein (0.912 h, 0.952 h, 34,749.048 ng/L*h, and 48,870.2 ngL -1 , respectively). The in vitro anti-proliferative activity and in vivo tumor inhibitory rate of rhIFNα-2b-SHCPM also increased by 90 and 55.86%, respectively, compared with the free rhIFNα-2b solution. The findings significantly supported a well-developed protein delivery system with improved sustained release, acceptable bioavailability, and increased antitumor activities. Graphical Abstract

CAS / MDL: 25322-68-3
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Enhanced antimicrobial activity and pH-responsive sustained release of chitosan/poly (vinyl alcohol)/graphene oxide nanofibrous membrane loading with allicin

Yongxu Liu,Rong Song,Xiaohong Zhang,Dawei Zhang

Herein, the natural extract of garlic, allicin (Alli), was added into chitosan (CS)/polyvinyl alcohol (PVA)/graphene oxide (GO) composites to develop the nanofibrous membranes with strong antibacterial activity and sustained-release properties by electrospinning technology. Vitro Alli release test showed that the release rate and amount of Alli could be regulated by the content of GO in the nanofibrous membrane. The antibacterial activity test against Staphylococcus aureus was performed and revealed the antibacterial activity of nanofibrous membranes loading with Alli. Compared with the nanofibrous membrane without GO, the CS/PVA/Alli nanofibrous membrane with 0.1 wt% GO still had nice antibacterial activity after 48 h. The water contact angle of nanofibrous membranes dropped significantly with the addition of GO and Alli, which showed the nanofibrous membrane had highly hydrophobic. The CS/PVA/GO nanofibrous membrane loading with Alli had great hygroscopicity and moisture-retention capacity. The essential characteristics of nanofibrous membranes were evaluated by SEM, FTIR , XRD. The above results indicate that the membrane has a strong antimicrobial activity and long-lasting efficacy, so the developed natural nanofibrous membranes hold potential as promising antibacterial wound dressing and tissue engineering.

CAS / MDL: 67-68-5 9002-89-5
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2020 · IF 4.389

Stimulation of in vitro and in vivo osteogenesis by Ti-Mg alloys with the sustained-release function of magnesium ions

Luxin Liang,Qianli Huang,Hong Wu,Zhengxiao Ouyang,Tang Liu,Hao He,Jian Xiao,Guanghua Lei,Kun Zhou

Magnesium (Mg) is well-known for its bioactivity and degradability. However, due to its low evaporation temperature and limited solubility in titanium (Ti), the fabrication of Ti-Mg alloys remains a huge challenge. In this study, Ti-xMg (x = 0.312, 0.625, 1.25 and 2.5 wt.%) alloys were fabricated by the combination of mechanical alloying (MA) and spark plasma sintering (SPS). Mg mainly existed as a solid solute element in the Ti matrix, while it also existed as second-phase particles due to its precipitation and dispersion during the SPS process. At a low content of 0.625 wt.%, Mg could increase the mechanical strength of Ti by the solid solution strengthening. However, it was detrimental to material mechanical properties when the Mg content increased to 1.25 wt.%. Being immersed in phosphate buffered solution (PBS), Ti-Mg alloys exhibited a burst Mg 2+ release behavior within the first day, and then the rates of Mg 2+ release gradually decreased within the following 27 days. The results suggested that the cell viability was dependent on the content of Mg in the Ti-Mg alloys. The high Mg content (2.5 wt.%) in the Ti-Mg alloys could lead to significant cytotoxicity. However, appropriate Mg content (0.312∼0.625 wt.%) could promote cell attachment, proliferation and differentiation. The Ti-0.625Mg alloy exhibited the best in vitro biological performance among all groups. In vivo results obtained by implanting the Ti-0.625Mg alloy in the femurs of rats further revealed its enhanced regenerative potential and osteointegration compared to pure Ti implants.

CAS / MDL: 7439-95-4
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DRUG DELIVERY · 2020 · IF 4.902

Long-term sustained release Poly(lactic-co-glycolic acid) microspheres of asenapine maleate with improved bioavailability for chronic neuropsychiatric diseases

Junqiu Zhai,Yu-e Wang,Xiangping Zhou,Yan Ma,Shixia Guan

Schizophrenia and bipolar disorder are severe chronic neuropsychiatric diseases, affecting hundreds of millions of people worldwide. Asenapine maleate (ASM) has been demonstrated as a safe and effective therapeutic agent under twice-daily administration. However, lower compliance is observed when patients are treated with ASM, which significantly limits its application in schizophrenia and bipolar disorder. Moreover, the low bioavailability of ASM caused by first-pass metabolism and poor aqueous solubility also impairs the treatment effect. A formulation of ASM with the property of long-term sustained release and improved bioavailability can be a solution to overcome these weaknesses. In this article, we prepared ASM-loaded poly(lactic-co-glycolic acid) (ASM-PLGA) microspheres through different techniques, including emulsification-solvent evaporation (ESE), Shirasu porous glass membrane emulsification (SPG-ME), and microfluidic method. In vitro and in vivo assessments demonstrated that uniform-sized microspheres generated by the microfluidic process sustainably released ASM throughout 40-days, showing low burst release and significantly improved bioavailability. The results suggest that ASM-PLGA microspheres prepared by the microfluidic method provide an efficient strategy to enhance the drug exposure of ASM as the treatment of chronic neuropsychiatric diseases. It is also evident that this microfluidic strategy has the potential to construct with other drugs, establishing long-acting formulations.

✓ 已验证 DOI PubMed 高影响因子
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Journal of Materials Chemistry B · 2013 ·Vol. 1 ·期 25 ·3202-3208 · IF 0

A new type of pH-responsive coordination polymer sphere as a vehicle for targeted anticancer drug delivery and sustained release

Peng Fei Gao,Lin Ling Zheng,Li Jiao Liang,Xiao Xi Yang,Yuan Fang Li,Cheng Zhi Huang

A new type of coordination polymer sphere prepared by combining 1,1′-(1,4-butanediyl)bis(imidazole) (bbi) and ferrous ions has been demonstrated as a targeted delivery system for in situ encapsulating anticancer drugs. These stable coordination polymer spheres can be fabricated simply by a deposition method. Drugs, doxorubicin hydrochloride (DOX·HCl) for example, can be easily in situ encapsulated by simply mixing the drug with bbi ligand through the deposition method and results in a high drug loading efficiency up to 98% and a drug loading content of nearly 40%, which is remarkably high for not only metal–organic but also other materials. A noticeable feature of the drug loaded coordination polymer spheres is that they show sustainable drug release for several days due to their superior stability, and are sensitive to external pH owing to the coordination bonds. The drug can be released faster in mild acidic conditions in comparison to physiological acidity. By conjugating folic acid to the surface of the coordination polymer spheres, the vehicles can be taken up selectively by cancer cells through cell surface receptor-mediated mechanisms. Cell viability experiments with HeLla cells demonstrated the low toxicity of the delivery vehicles and the good anticancer efficacy of the drug-loaded coordination polymer spheres.

✓ 已验证 产品关联 DOI PubMed
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PLoS One · 2015 ·Vol. 10 ·期 11 ·e0141467 · IF 3.234

Application of 5-Fluorouracil-Polycaprolactone Sustained-Release Film in Ahmed Glaucoma Valve Implantation Inhibits Postoperative Bleb Scarring in Rabbit Eyes

Xiu-Zeng Bi,Wei-Hua Pan,Xin-Ping Yu,Zong-Ming Song,Zeng-Jin Ren,Min Sun,Cong-Hui Li,Kai-Hui Nan

This study was designed to investigate whether 5-fluorouracil (5-Fu)-polycaprolactone sustained-release film in Ahmed glaucoma valve implantation inhibits postoperative bleb scarring in rabbit eyes. Eighteen New Zealand white rabbits were randomly divided into three groups (A, B and C; n = 6 per group). Group A received combined 5-Fu-polycaprolactone sustained-release film application and Ahmed glaucoma valve implantation, group B received local infiltration of 5-Fu and Ahmed glaucoma valve implantation, and group C received Ahmed glaucoma valve implantation. Postoperative observations were made of the anterior segment, intraocular pressure, central anterior chamber depth, blebs, drainage tube, and accompanying ciliary body detachment. The pathology of the blebs and surrounding tissues were observed at month 3 postoperatively. We revealed that the 5-Fu-polycaprolactone sustained-release film maintained a release concentration range of 13.7 ± 0.12 to 37.41 ± 0.47 μg/ml over three months in vitro . Postoperatively, diffuse blebs with ridges were found in all eyes in group A, two blebs were observed in group B, and no bleb formation was present in group C. The postoperative central anterior chamber depth in group A was significantly less than that of the other two groups. The postoperative intraocular pressure of group A stabilized at 6.33–8.67 mmHg, whereas that of group C gradually remained at 7.55–10.02 mmHg. The histopathology showed that the fibrous tissue thickness of the blebs in group A was significantly thinner than that of the other groups. We conclude that the 5-Fu-polycaprolactone sustained-release film had a sustained drug release effect, which promoted the inhibition of bleb scarring after Ahmed glaucoma valve implantation.

CAS / MDL: 51-21-8
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2024 · IF 4.9

Bi-layered oil encapsulates formed by polydopamine-supported in situ complex coacervation: Investigation of structure formation and sustained release performance

Qirui Tian,Weiqing Zhou,Qiong Cai,Xiaoyun Pan,Guanghui Ma,Guoping Lian

In polydopamine (PDA)-supported in situ complex coacervation, PDA is pre-coated onto emulsion droplets, and further applied as an interlayer to support the interfacial immobilization of coacervates biopolymers. In the current research, the stepwise immobilization of gelatin (GE) and gum Arabic (GA) onto PDA layer is monitored to in-depth investigate the mechanism of PDA layer as coating material and functional substrates. GE and GA were applied as adsorbates, with different forms of PDA (spherical shell, planar solid, and nanoparticles) as substrates. Real-time observations of the binding steps were performed using quartz crystal monitor with dissipation (QCM-D) and isothermal titration calorimetry (ITC). Meanwhile, using PDA-supported coacervates as encapsulating material, sustained release of essential oil volatiles was also evaluated, either dispersed in detergent solution or freeze dried in open air. The anti-oxidation performance was determined by measuring the absorbance of lipid hydroperoxide using UV spectrophotometer. The results revealed that PDA enabled synergistic immobilization of biopolymers through chemical bonding and adhesive force during the processing of in situ complex coacervation, thus enhanced protection of core compounds with two-stage releasing kinetics and prevented hyperoxidation. Also, PDA-based colloids and substrates also exhibit controllable conformation characteristic, provide a promising prospect as versatile intermediate functional biomaterials for encapsulation.

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Advanced Science · 2025 · IF 14.1

3D-Printed Biomimetic Vascular Scaffold Crosslinked with Heparan Sulfate for Sustained Release of PDGFB-LG4 Fusion Protein Promotes Bone Regeneration

Jiahua Duan,Gaofei Qian,Huikang Zhang,Feifan Wang,Qiang Tian,Dong Lei,Jianning Zhao

A central focus of bone tissue engineering is the construction of vascular systems, which provide nutrients for cell survival, remove metabolic waste, and accelerate tissue regeneration. Platelet-derived growth factor-BB (PDGFB) has the ability to stimulate both vascularization and bone regeneration; however, its clinical application has been hindered by side effects and low efficacy due to suboptimal delivery systems. In this study, a biomimetic vascular scaffold crosslinked with heparan sulfate (HS) is developed to enable sustained delivery of the PDGFB-LG4 fusion protein, targeting the regeneration of critically sized bone defects. The scaffold is designed with a vascular-like hierarchical structure, incorporating a customized 3D framework, multibranched microchannels, and permeable porous walls, which facilitates mass exchange and cell infiltration. PDGFB-LG4 exhibits superior osteoinductive and angiogenic activity compared to PDGFB. In a calvarial defect model, the composite scaffold (PCLHS-PDGFB-LG4) significantly enhances both vascularization and bone regeneration, demonstrating improved efficacy at lower doses compared to PDGFB. This approach may be applicable to other growth factors and gelatin-based materials, offering the potential for a wide range of applications in regenerative medicine.

CAS / MDL: 9050-30-0 57459-72-0
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Preparation and characterization of high-methoxyl pectin/glycerides emulsion for pH-responsive, targeting, and sustained release of fat-soluble substances

Yinghong Pei,Zhonghao Zhang,Zhihao Duan,Tao Gao,Qingye Jiang,Shenglin Hu,Zizhong Tang,Yanger Chen,Shu Yuan,Xiaorong Yan,Ming Yuan

In this study, a pH-responsive emulsion system was prepared, combining high-methoxyl pectin (HMP) with camellia oil glycerides (CG). The emulsion was characterized as O/W type, with HMP serving as the wall material and CG as the oil phase. The physicochemical properties, pH responsiveness, digestion stability, and encapsulated delivery capabilities of the HMP-CG emulsion were investigated. The emulsion showed an average droplet size of 480.47 ± 76.19 nm, possessing a negative charge and a pronounced core-shell structure. HMP package CG enhanced hydrophilic ability and enabled targeted release within the small intestine through the structural changes of HMP. The presence of HMP and CG increased droplet dispersion and target digestibility of the emulsion system, leading to sustainable small intestine-specific release. Overall, HMP-CG emulsion system, composed of natural materials, exhibited the ability to achieve targeted and controllable release via pH-responsive mechanisms, offering an alternative for developing gel materials incorporating fat-soluble substances.

CAS / MDL: 12501-23-4
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Food Chemistry-X · 2025 · IF 8.2

Preparation and application of modified Aronia melanocarpa pectin-whey protein stabilized clove essential oil pickering emulsion sustained-release preservative pads

Liu Yang,Zhipeng Jiang,Xinyu Zhang,Xue Ding,Rui Xiao,Wenwen Chen,Shengyu Xu,Hongyuan Zhang

Aronia melanocarpa Pectin (AP) was modified via alkaline/enzymatic/high-pressure enzymatic methods. High-pressure enzymatic pectin (HPP-AP) exhibited the lowest esterification degree with galacturonic acid content, optimal shear-thinning behavior, and emulsification performance. HPP-AP complexed with whey protein isolate (WPI) through hydrophobic interactions (exposed galacturonic acid–WPI residues) and hydrogen bonding (amide–hydroxyl groups), forming stable composite particles. These particles stabilized Pickering emulsions (20 % oil phase) encapsulating clove essential oil (CEO), demonstrating uniform interfacial adsorption (oil-in-water type), high encapsulation efficiency, and stability under diverse conditions (pH, temperature, centrifugation). The emulsions showed sustained CEO release (87.8 % at 7 days) and inhibited aspergillus Niger ( A. niger ) effectively. Coated onto non-woven fabrics, the emulsion formed a gel-network coating. During 12 d storage (4 °C), preservative pads delayed strawberry weight loss, texture/color deterioration, and moisture migration, extending shelf life by 6 d while maintaining quality in transport simulation. This work provides a novel strategy for plant essential oil-based active packaging

CAS / MDL: 7758-02-3
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Materials Science & Engineering C-Materials for Biological Applications · 2016 · IF 3.42

Lipid-coated hollow mesoporous silica nanospheres for co-delivery of doxorubicin and paclitaxel: Preparation, sustained release, cellular uptake and pharmacokinetics

Yang Qiu,Chao Wu,Jie Jiang,Yanna Hao,Ying Zhao,Jie Xu,Tong Yu,Peng Ji

A carrier consisting of lipid-coated hollow mesoporous silica nanospheres (L-HMSN) was produced for the combination of the water-insoluble drug (paclitaxel, PTX) and the water-soluble drug (doxorubicin, DOX). DOX was adsorbed into the nanoscale hollow structure of the hollow mesoporous silica nanospheres (HMSN) by adsorption and PTX was wrapped in the phospholipid layer of the HMSN surface by lipid film hydration method. The characterization results showed that DOX and PTX were present in the nanopheres in an amorphous state. The loaded L-HMSN (DOX/PTX@L-HMSN) in vitro drug release showed a sustained release in phosphate buffered solution (PBS) at pH   6.8 and 0.001%SDS. The cellular uptake experiment indicated that L-HMSN was successfully taken up by A549 cells. In addition, the combination of DOX and PTX in L-HMSN exhibited a marked synergistic effect in inhibiting the proliferation of A549 cells. The pharmacokinetic study demonstrated that L-HMSN could significantly improve the relative bioavailability of DOX and PTX. These results confirm that L-HMSN is a promising carrier for successful drug combination.

CAS / MDL: 94-26-8
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