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FOOD CHEMISTRY · 2026 · IF 9.8

Anthocyanins-quercetin copigmentation enhances liposomal encapsulation: Mechanisms, bilayer interactions, and sustained release performance

Bowen Luo,Xiang Li,Xiuyu Jiang,Jianwei Liu,Huiji Zhou,Bo Wang,Benu Adhikari,Xianwu Peng,Wanping Zhang,Zijia Zhang

Conventional liposome preparation techniques often show poor encapsulation efficiency (EE) for hydrophilic compounds. In this study, copigmentation was employed as a hydrophobic modification strategy to improve the liposomal delivery of anthocyanins (ACNs). ACNs formed stable copigmentation complexes with quercetin (QTI), primarily through π–π stacking and hydrophobic interactions. These interactions enhanced the hydrophobicity of ACNs and promoted their redistribution from the aqueous phase toward the bilayer interfacial region. Liposomes prepared by the polyol dilution method encapsulated ACNs@QTI complexes more efficiently than free ACNs, achieving an EE of 81.5 ± 0.6% and a particle size of 166.4 ± 7.9 nm. FTIR, DSC, and fluorescence analyses confirmed stronger interactions between ACNs@QTI complexes and phospholipid membranes, while in-vitro release experiments demonstrated its superior sustained-release performance. These findings highlight copigmentation as a practical non-covalent strategy to enhance liposomal encapsulation of hydrophilic bioactives, offering a basis for enhancing the stability and delivery of ACNs and other water-soluble compounds in food and pharmaceutical applications.

✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF CLUSTER SCIENCE · 2023 ·Vol. 35 ·期 2 ·419-428 · IF 2.8

Preparation and Characterization of Titanium Oxide Nanocapsules Containing Retinoic Acid for Sustained Release

Yu Xuecheng,Zhao Yunhe,Chen Gang,Yu Jing,Wang Ruolan,Deng Yuhao,Wang Xiaoying,Yuan Xinru,Yu Xue-Feng,He Rui

Retinoic acid (RA) is widely used in cosmetics and medicine. However, high concentrations of RA may cause adverse effects, and carcinogenic substances can be generated by light degradation. Herein, a convenient and eco-friendly method was developed to achieve the sustained release of RA by TiO 2 nanocapsules. The surface morphologies, crystalline properties, and chemical structures were studied by SEM, XRD, FT-IR, NMR. The particle size is ~ 200 nm. The synthesis conditions, photostability and biological properties were also investigated. The XRD results indicated that the low crystallinity of anatase TiO 2 shell contributed to the sustained release of inner RA. The sustained release properties were investigated by the elution process. It confirmed that the RA was encapsulated in the TiO 2 shell with loose structures. Light irradiation experiments showed that the irradiation time was extended from ~ 30 s to ~ 120 s when the concentration of residual RA was reduced to half under the same conditions. This showed that inner RA was well protected and continuously released. The RA-TiO 2 nanocapsules showed good dispersion in water and oil phases, sustained release properties, extended effect time, long-acting antibacterial properties and photostability.

研究领域: 纳米技术 · 药学 · 材料科学 · 生物医学工程
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COLLOID AND POLYMER SCIENCE · 2024 ·Vol. 302 ·期 5 ·819-828 · IF 2.2

Molecularly imprinted polymers based on attapulgite and sustained-release properties for 5-FU

Ji Xinyuan,Yang Zhe,Fang Jiahui,Hu Sheng

In this study, a novel molecularly imprinted polymer (MIP) was synthesized with attapulgite (ATP) and acrylamide (AM) and ethyl methacrylate (MMA) for controlled release carrier of 5-fluorouracil (5-FU). The MIPs (PAM-PMMA) were characterized by XRD, FESEM, HRTEM, and FTIR. The drug loading and in vitro controlled release ability of MIP on 5-FU was investigated by adsorption property analysis and in vitro release analysis. MIPs (PAM-PMMA) reached a maximum drug loading of 12 mg/g and a maximum release of 80% at an ATP dosage of 0.2 g (0.4%), an initial concentration of 5-FU of 100 mg/L, and an adsorption time of 240 min. Cytotoxicity analysis showed that the maximum inhibition of cells could reach 25% at 72 h of cell culture time under the above conditions. The results showed that MIPs synthesized with ATP as the substrate and AM and MMA as the functional monomers were successfully synthesized and could be used as a drug delivery system for 5-FU. Graphical

研究领域: 材料科学 · 高分子科学 · 药剂学 · 纳米技术
✓ 已验证 DOI 高影响因子
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Drug Delivery and Translational Research · 2021 ·Vol. 12 ·期 3 ·589-602 · IF 4.617

Preparation of olmesartan medoxomil solid dispersion with sustained release performance by mechanochemical technology

Zhang Qihong,Feng Zongmiao,Ren Wei,Zhao Yunchun,Dushkin Alexandr V.,Su Weike

Hypertension is a common disease for human with high morbidity and mortality, and olmesartan medoxomil (OM) is widely used in the therapy of hypertension. However, poor water solubility and low bioavailability limit its widespread use. To improve the effect of OM, a ternary OM solid dispersion consisting of hydroxypropyl- β -cyclodextrin (HP- β- CD) and hydroxypropyl methylcellulose (HPMC) was prepared by mechanochemical method. The best preparation parameters were OM/HP- β -CD/HPMC-E5 with mass ratio of 1:2.6:1 and milling time of 4 h. Under the optimal preparation conditions, the solubility of the ternary solid dispersion could be increased by 12 times as compared with pure OM. Due to the addition of HPMC-E5, the solid dispersion had sustained release performance with prolonged release time of 12 h. Furthermore, in vivo study demonstrated that the prepared solid dispersion could afford significantly improved bioavailability of ~ 3-fold in comparison with pure drug. Hence, the prepared ternary solid dispersion of OM may be a promise delivery system for clinical application. Graphical abstract

研究领域: 药剂学 · 高血压治疗 · 药物递送系统
✓ 已验证 DOI 高影响因子
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INDUSTRIAL CROPS AND PRODUCTS · 2023 · IF 5.9

Dual-responsive bagasse cellulose/PVA hydrogels for sustained release of plant growth regulator

Mei Chen,Pingxiong Cai,Yuanfeng Pan

Agrochemicals play an irreplaceable role in the process of agricultural production. However, unreasonable use of agrochemicals can cause serious harm to the environment. Therefore, the controlled release of agrochemicals is critical in the sustainable development of agriculture and benefiting the environment. In this work, a composite hydrogel was prepared from dialdehyde cellulose and reinforced by polyvinyl alcohol (PVA) while cysteamine dihydrochloride acted as a cross-linking agent to render the hydrogel pH and redox-responsive for the controlled release of a model agrochemical, i.e., salicylic acid (SA). The aldehyde content in the modified cellulose reached 10.65 mmol/g while the yield of oxidized cellulose was 55%. The structure, morphology and properties of the composite hydrogels were characterized by Fourier transform infrared (FTIR), X-ray diffraction (XRD), thermal gravimetric analysis (TGA) and scanning electron microscopy (SEM). In addition, the release behavior of SA loaded in the hydrogels under various different conditions was also studied. The results showed that the addition of PVA could improve the mechanical properties of hydrogels, and the cumulative release of SA could be modulated by varying release conditions or environmental stimuli; and the release kinetics was well fitted with the Korsmeyer-Peppas model. Moreover, the release of SA could be promoted under acidic conditions and in the presence of reducing agent glutathione (GSH). The findings from this work particularly benefit the agricultural production.

✓ 已验证 产品关联 DOI 高影响因子
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ACS Applied Nano Materials · 2023 · IF 5.9

Ibuprofen-Loaded ZnO Nanoparticle/Polyacrylonitrile Nanofibers for Dual-Stimulus Sustained Release of Drugs

Shushu Chao,Yiqiu Zhang,Shihong Cheng,Xinzhe Shao,Songlin Liu,Wenjuan Lu,Yanfeng Wang,Pingping Zhang,Qingqiang Yao

Based on the opportunities of ibuprofen administration innovation and challenges associated with the construction of transdermal drug delivery systems using medicated nanoparticles and electrospun nanofiber membranes, we developed a transdermal drug delivery system comprising ibuprofen-loaded ZnO nanoparticles/polyacrylonitrile electrospun nanofiber membranes (ZnO-ibuprofen/PAN), which was dual-stimulus responsive, wherein both pH and temperature triggered drug release. ZnO-ibuprofen nanoparticles with high drug loading capacity (17.7%) were prepared at room temperature by a one-step method involving 4,4′-((4-(4H-1,2,4-triazol-4-yl) phenyl) azanediyl)dibenzoic acid, Zn(NO3)2·6H2O, and ibuprofen, following which electrospinning was conducted to generate the ZnO-ibuprofen/PAN nanofibers. The transdermal drug release behavior of the ZnO-ibuprofen/PAN electrospun nanofiber membranes in the normal (pH = 7.4, 37 °C) and inflammatory (pH = 6.5, 42 °C) tissue environment exhibited increased drug release rate at higher ambient temperatures and decreased pH following 24 h of drug release. The cumulative drug release rate of ZnO-ibuprofen/PAN electrospun fibers through porcine skin under inflammatory conditions reached 71.35% ± 2.96% after 24 h, thereby demonstrating their favorable transdermal permeation behavior. The cytotoxicity assays revealed that the nanofibers possessed excellent biocompatibility. Thus, the dual stimulus-responsive ZnO-ibuprofen/PAN can be an effective transdermal drug delivery carrier.

CAS / MDL: 109-89-7
✓ 已验证 产品关联 DOI 高影响因子
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DRUG DELIVERY · 2022 · IF 6.819

Sustained release of brimonidine from BRI@SR@TPU implant for treatment of glaucoma

Yujin Zhao,Chang Huang,Zhutian Zhang,Jiaxu Hong,Jianjiang Xu,Xinghuai Sun,Jianguo Sun

Glaucoma is the leading cause of irreversible vision loss worldwide, and reduction of intraocular pressure (IOP) is the only factor that can be interfered to delay disease progression. As the first line and preferred method to treat glaucoma, eye drops have many shortcomings, such as low bioavailability, poor patient compliance, and unsustainable therapeutic effect. In this study, a highly efficient brimonidine (BRI) silicone rubber implant (BRI@SR@TPU implant) has been designed, prepared, characterized, and administrated for sustained relief of IOP to treat glaucoma. The in vitro BRI release from BRI@SR@TPU implants shows a sustainable release profile for up to 35 d, with decreased burst release and increased immediate drug concentration. The carrier materials are not cytotoxic to human corneal epithelial cells and conjunctival epithelial cells, and show good biocompatibility, which can be safely administrated into rabbit’s conjunctival sac. The BRI@SR@TPU implant sustainably released BRI and effectively reduced IOP for 18 d (72 times) compared to the commercial BRI eye drops (6 h). The BRI@SR@TPU implant is thus a promising noninvasive platform product for long-term IOP-reducing in patients with glaucoma and ocular hypertension.

CAS / MDL: 919-30-2
✓ 已验证 产品关联 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2022 · IF 5.999

A bifunctional zoledronate sustained-release system in scaffold: Tumor therapy and bone repair

Wu Di,Yang Shuai,Wang Bo,Tan Wei,He Jinpeng,Guowen Qian,Youwen Deng

It is of great challenges to repair bone defect and prevent tumor recurrence in bone tumors postoperative treatment. Bone scaffolds loaded with zoledronate (ZOL) are expected to solve these issues due to its osteogenesis and anti-tumor ability. Furthermore, ZOL needs to be sustained release to meet the requirement of long-term therapy. In this study, ZOL was loaded into amination functionalized mesoporous silicon (SBA15NH 2 ), and then incorporated into poly ( L -lactic acid) to prepare PLLA/SBA15NH 2 -ZOL scaffold via selective laser sintering technology. On one hand, ZOL of local release not only can inhibit growth and proliferation of bone tumor cells but also inhibit osteoclast differentiation through competitive binding of receptor activator of nuclear factor (NF)-kB (RANK) in osteoclast precursors. On the other hand, amination function could change the surface charge of mesoporous silica to positive charge to enhance the absorption of ZOL, mesoporous structure and abundant amino groups of SBA15NH 2 play a barrier role and form hydrogen bond with phosphate groups of ZOL, respectively, thereby achieving its sustained release. The results showed that the loading amount of ZOL was 236.53 mg/g, and the scaffold could sustainedly release ZOL for more than 6 weeks. The scaffold inhibited proliferation of osteosarcoma cells through inducing apoptosis and cell cycle arrest . TRAP staining and F-actin ring formation experiment showed the scaffold inhibited differentiation and mature of osteoclast. Pit formation assay indicated that bone resorption activity was inhibited strongly.

CAS / MDL: 919-30-2 78-10-4
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Advanced Healthcare Materials · 2023 · IF 10

Transdermal Sustained Release Properties and Anti-Photoaging Efficacy of Liposome-Thermosensitive Hydrogel System

Sijie Wu,Gaodan Liu,Ping Shao,Xingyu Lin,Jiahao Yu,Hanchi Chen,Huiliang Li,Simin Feng

Drug delivery systems have become a research priority in the biomedical field. The incorporation of liposomes to hydrogels further forms more robust multifunctional systems for more effective and sustained topical drug delivery. In this study, carboxymethyl-modified chitosan/hyaluronic acid (CMC/HA, CMH) thermosensitive hydrogel is developed for sustained transdermal delivery of liposomes. Hydrogels are crosslinked by hydrogen bonding, hydrophobic interaction and electrostatic interaction. The gel properties can be regulated by substitution degree (DS), and when DS = 18.20 ± 0.67% (CMH2), the gel temperature is 37.8 °C, allowing rapid gelation at body temperature (315 s). Moreover, CMH2 hydrogel has suitable spreadability (17.7–57.2 cm 2 ), viscosity (2133.4 mPa s) and porous structure, which facilitated its adhesion and application on the skin and liposomes delivery. The hydrogel can retard the liposomes release, and the release rate of ascorbyl glucoside (AA2G) is 33.92–49.35% in 24 h. Hydrogel avoids the rapid clearance of liposomes from the skin and improved the skin retention, achieving the long-term release of bioactive components. Liposome-hydrogel system more efficiently promotes the anti-photoaging effect of AA2G on skin, reducing epidermal thickness, melanin deposition and lipid oxidative damage and increasing collagen density. Therefore, liposome-hydrogel systems are proposed as multifunctional delivery systems for sustained transdermal delivery.

CAS / MDL: 9012-76-4 129499-78-1
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Environmental Sciences · 2022 · IF 6.796

A sustained-release microcarrier effectively prolongs and enhances the antibacterial activity of lysozyme

Mei Du,Jingzhang Liu,Fengbang Wang,Lei Bi,Chunyan Ma,Maoyong Song,Guibin Jiang

Bacterial infections have become a great threat to public health in recent years. A primary lysozyme is a natural antimicrobial protein; however, its widespread application is limited by its instability. Here, we present a poly (N-isopropylacrylamide) hydrogel inverse opal particle (PHIOP) as a microcarrier of lysozyme to prolong and enhance the efficiency against bacteria. This PHIOP-based lysozyme (PHIOP-Lys) formulation is temperature-responsive and exhibits long-term sustained release of lysozyme for up to 16 days. It shows a potent antibacterial effect toward both Escherichia coli and Staphylococcus aureus , which is even higher than that of free lysozyme in solution at the same concentration. PHIOPs-Lys were demonstrated to effectively inhibit bacterial infections and enhance wound healing in a full-thickness skin wound rat model. This study provides a novel pathway for prolonging the enzymatic activity and antibacterial effects of lysozyme.

CAS / MDL: 10043-52-4 7664-39-3
✓ 已验证 产品关联 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2022 · IF 5.518

Sustained-release system based on BTA@MOF-5 for self-healing coating application

Chengbin Guo,Yubo Lian,Chen Huang,Zhenyu Chen

A novel sustained-release system was designed on the basis of metal–organic framework-5 (MOF-5) as a nanocontainer to load benzotriazole (BTA). Furthermore, the fabricated BTA/MOF-5 (BTA@MOF-5) was doped to the epoxy coating to improve the anticorrosion performance of copper. UV spectrophotometry proved the sustained-release behavior of BTA@MOF-5. Salt spray tests and electrochemical measurements demonstrated the self-healing ability of the composite coating . This novel sustained-release system provides a new strategy for metal protection.

✓ 已验证 产品关联 DOI 高影响因子
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2022 · IF 5.589

Platensimycin-berberine chloride co-amorphous drug system: Sustained release and prolonged half-life

Zhe Wang,Xin Chen,Duanxiu Li,Enhe Bai,Hailu Zhang,Yanwen Duan,Yong Huang

Co-amorphous technology is an emerging approach for pharmaceutical engineering of drugs and drug leads with improved physicochemical properties and bioavailability. Platensimycin (PTM) is a promising natural antibiotic lead that acts on bacterial fatty acid synthase and exhibits excellent antibacterial activity . Despite great strides to improve its poor pharmacokinetics by medicinal chemistry and nanotechnology, there are no convenient oral delivery systems developed. Here, a co-amorphous system of PTM and berberine chloride (BCL) was developed for oral delivery of PTM. Co-amorphous PTM-BCL was prepared by rotary vacuum evaporation method, and systematically characterized by powder X-ray diffraction, temperature modulated differential scanning calorimetry , Fourier transform infrared spectroscopy (FTIR), and X-ray photoelectron spectroscopy (XPS). Compared with PTM or BCL alone, the equilibrium solubility and dissolution rate of both of them in the co-amorphous systems decreased significantly, showing the characteristics of sustained release . The molecular interactions between PTM and BCL were mediated by strong charged-mediated hydrogen bonds , based on FTIR, XPS, and NMR-based techniques. The co-amorphous PTM-BCL system showed excellent physiochemical stability at room and elevated (40 °C) temperature under dry conditions. The combination of PTM and BCL showed increased killing of a clinical isolated methicillin-resistant Staphylococcus aureus strain in killing checkerboard assays. Finally, co-amorphous PTM-BCL exhibited 2- or 3-fold longer half-life in rats than that of crystalline and amorphous PTM upon oral administration, respectively. Our study suggests a rational approach to realize the full potential of potent antibiotic PTM, which may be conveniently adapted for engineering of other important pharmaceutics.

CAS / MDL: 9004-32-4 9085-26-1
✓ 已验证 产品关联 DOI PubMed 高影响因子
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