Expert Opinion on Drug Delivery
·
2024
·
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.
研究领域:
药剂学
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眼科医学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2022
·
IF 5.999
Xu-Chun Song,Ya-Lan Yu,Gui-Yuan Yang,A.-Li Jiang,Ying-jie Ruan,Shang-hua Fan
A simple and versatile strategy for controlled production of monodisperse ethyl cellulose (EC) microcapsules by a single-stage emulsification method has been developed. Monodisperse oil-in-water emulsions, obtained by a microfluidic device, are used as templates for preparing EC microcapsules. Oil-soluble ethyl acetate (EA) is miscible with water, so the interfacial mass transfer between EA and water occurs sufficiently, which leads to water molecules pass through the phase interface and diffuse into emulsion interior. Water molecules aggregate at the interface, and some merge into a large water drop in the central position of the emulsion. After evaporation of EA solvent, monodisperse EC microcapsules create large numbers of pits on the surface with a hollow structure. Curcumin is used as a model drug and embedded in the hollow structure. EC microcapsules have good, sustained drug release efficacy in a simulated intestinal environment, and the release process of EC microcapsules containing 6.14% drug-loaded capacity is fully consistent with the vitro drug release model. Such simple techniques for making EC microcapsules may open a window to the controlled preparation of other multifunctional microcapsules. Besides, it offers theoretical guidance for the study of EC microcapsules as drug carriers and expanding clinical application of curcumin.
研究领域:
药剂学
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材料科学
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DOI
PubMed
高影响因子
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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DOI
PubMed
高影响因子
JOURNAL OF PHYSICS D-APPLIED PHYSICS
·
2020
·Vol. 53
·期 24
·245401
·
IF 3.169
Jingyi Xue,Xiaolei Li,Qianli Li,Jiahong Lyu,Wei Wang,Lin Zhuang,Yue Xu
A novel magnetic drug-loaded osteoinductive Fe3O4/CaCO3 hybrid microspheres system (MDHMs) with excellent drug delivery property has been fabricated by a modified coprecipitation method. The MDHMs are uniform vaterite microspheres with well-defined mesoporous nanostructures. The formation of vaterite is based on the templating effect of casein micelles, which is promising in bone tissue engineering. Cyclodextrins (CDs) increase the porosity of the microspheres with a pore size of about 7.3 nm and a surface area of about 50.73 m2 g−1. The mesoporous structure gives the MDHMs great drug loading efficiency of about 80.75–88.74% and the minocycline-loaded MDHMs display a sustained drug release property (about 95% in 5 d). Moreover, the MDHMs also possess stable magnetic property with a saturation magnetization of about 4.41 emu g−1 and a remarkable magnetism-responsive behavior. These results demonstrate that with superior drug delivery property, osteoinductive potential and magnetic property, the MDHMs have a great potential in the treatment of peri-implantitis.
研究领域:
材料科学
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药剂学
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生物医学工程
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DOI
高影响因子
CELLULOSE
·
2021
·Vol. 28
·期 3
·1587-1597
·
IF 5.044
Liu Xiaohong,Li Ming,Zhang Haichuan,Chen Liheng,Fu Shiyu
A cellulose- grafted -poly( N -isopropylacrylamide) (cellulose- g -PNIPAAm) copolymer with thermo-responsivity was synthesized using homogeneous activators regenerated by electron transfer for atom transfer radical polymerization (ARGET-ATRP). The prepared copolymer dispersed at low concentration in water or phosphate-buffered saline (PBS) at 25 °C could self-assembly into micelles at 37 °C. The size and morphology of these micelles were determined by dynamic light scattering and transmission electron microscopy. The copolymer at a concentration over 4.2% by weight in water formed an injectable thermo-responsive hydrogel that was composed of micelles when the temperature increased to 37 °C. This hydrogel was used to load the anticancer drug doxorubicin (DOX). In vitro release studies demonstrated that this hydrogel released DOX in a sustained manner. Furthermore, this cellulose-based injectable thermo-responsive hydrogel was used in cytotoxicity tests, revealing that it was very biocompatible. Based on the above results, this cellulose- g -PNIPAAm injectable thermo-responsive hydrogel has strong potential for application in smart drug delivery systems.
研究领域:
材料科学
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生物医药
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高分子化学
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DOI
高影响因子
ACS Applied Materials & Interfaces
·
2021
·
IF 9.229
Huali Li,Shuwen Luo,Liuqin Zhang,Zilong Zhao,Min Wu,Weihua Li,Fa-Qian Liu
Marine biofouling is one of the technical bottlenecks restricting the development of the global marine economy. Among the commercial self-polishing antifouling coatings, cuprous oxide is an irreplaceable component because of its efficiency and broad-spectrum antibacterial activity. However, one of the biggest obstacles to achieving long-term antifouling is the “initial burst and final decay” of cuprous oxide in the coating. Here, we lock the copper ions by establishing an antifouling unit composed of Cu2O (core) and Cu-based metal–organic framework (Cu-MOF, shell). Cu-MOF is densely grown in situ on the periphery of Cu2O by acid proton etching. The shell structure of Cu-MOF can effectively improve the stability of the internal Cu2O and thus achieve the stable and slow release of copper ions. Furthermore, Cu2O@Cu-MOF nanocapsules can also achieve active defense by rapid and complete dissolution of Cu2O@Cu-MOF at local acidic microenvironment (pH ≤ 5) where the adhesion of fouling organisms occurs. Super-resolution fluorescence microscopy is used to explain the sterilization mechanism. Relying on the water- and acid-sensitive properties of Cu-MOF shell, the stable, controlled and efficient release of copper ions has been achieved for the Cu2O@Cu-MOF nanocapsules in the self-polishing antifouling coatings. Thus, these controlled-release nanocapsules make long-term antifouling promising.
研究领域:
材料科学
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海洋生物学
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化学工程
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DOI
PubMed
高影响因子
Journal of Orthopaedic Surgery and Research
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2021
·Vol. 16
·期 1
·1-9
·
IF 2.359
Li Jiyou,Liu Ning,Huang Zhipeng,Wang Wantao,Hou Donghua,Wang Wenbo
Background Osteoarthritis is a chronic inflammatory disease of the joints associated with significant morbidity and lower quality of life. Current treatment strategies focus on reducing cartilage degeneration but fail to restore their proliferative ability. Super-activated platelet lysate (sPL) is an enhanced form of platelet-rich plasma that can be easily inactivated. The purpose of this study is to evaluate whether sPL-loaded PLGA/chitosan/gelatin microspheres can prevent and treat osteoarthritis. Methods Features of biological microspheres were detected by SEM and ELISA. Osteoarthritis chondrocytes were co-cultured with hydrogel loaded with sPL. The effect of biological microspheres on chondrocyte proliferation was evaluated using a CCK-8 cell proliferation test. Cell morphology and cell necrosis were measured with a microscope. The gene expression levels of cartilage-related markers type 2 collagen, aggrecan (ACAN), and SRY type high mobility group box-9 (SOX9) were determined by real-time quantitative polymerase chain reaction (Rt-PCR). A rat osteoarthritis model was established. Micro-CT was used to characterize cartilaginous changes after the injection of biological microspheres. Histopathological HE staining, Safranin-O Fast Green staining and staining scores, type II collagen staining, and proteoglycan staining were used to evaluate the degree of cartilaginous repair. Results Biological microspheres were able to continuously release biological factors. Exposure to loading sPL microspheres significantly increased chondrocyte proliferation, reduced cell necrosis, and increased the expression of cartilage markers type 2 collagen, ACAN, and SOX9 in osteoarthritic chondrocytes. In vivo experiments found that biological microspheres also smoothen cartilage surfaces, promote the expression of proteoglycan and type 2 collagen while also increasing cartilaginous integrity as evaluated using Safranin-O Fast Green staining. Conclusions PLGA/chitosan/gelatin hydrogel loaded with sPL is a promising tool for effective and non-invasive articular cartilage repair in osteoarthritis. Graphic abstract Biological microspheres loaded with sPL release various biological factors to promote chondrocyte proliferation and upregulate chondrocyte functionalization genes (SOX9, CoX II, ACAN), leading to an overall enhanced cartilaginous matrix.
研究领域:
骨科
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生物医学工程
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药理学
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DOI
PubMed
高影响因子
CHEMICAL PAPERS
·
2026
·
IF 2.7
Weng Xuling,Guo Fang,Zhong Yu,Feng Wanyun,Shang Xiaoqiang,Chen Yufeng
A drug delivery system based on magadiite for gemcitabine (namely GEM-Mag) has been constructed by protonation, intercalation with tetrabutylammonium ions (TBA + ), and ion exchange. Various measurements were used to characterize the samples. XRD results showed that the basal spacing of Na-magadiite (15.17 Å) decreased to 11.40 Å after protonation. Following intercalation with TBA + , the basal spacing increased to 25.79 Å. After further ion exchange with the positively charged GEM, the basal spacing reduced to 18.21 Å. FT-IR and TG-DTG indicated that the GEM was incorporated into the magadiite. Based on CHN elemental analysis and EDS results, the chemical formula of GEM-Mag was estimated to be H 1.59 (C 9 H 12 F 2 N 3 O 4 ) 0.41 Si 14 O 29 ·2.33H 2 O. According to the chemical formula, the loading capacity of GEM-Mag for GEM was 10.74%. Drug release tests were carried out either in phosphate buffered solution (PBS, pH = 7.40) or in HCl solution (pH = 1.35). Results revealed that the GEM-Mag exhibited sustained-release of GEM. While the drug released for 96 h in the PBS, the cumulative release percentage of GEM from drug delivery system was only 53.46%; whereas in the HCl solution (pH = 1.35), the cumulative release percentage was 52.15% after 700 min. Cytotoxicity assay confirmed that the magadiite-based drug delivery system for GEM exhibited stronger inhibitory effects on HepG2 cells compared with that of the free GEM. In addition, the drug-loading process and mechanisms have been discussed in detail.
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DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2026
·
IF 5.9
Jiji Fan,Yanan Bu,Lei Huang,Xiuqiong Chen,Huiqiong Yan,Qiang Lin
The inherent molecular rigidity of alginate, which limits chain flexibility and prevents effective entanglement, has long hindered its direct electrospinning into uniform nanofibers from aqueous solutions. To overcome this limitation and expand the application of alginate in infection-prone wound repair, this study introduces a novel antibacterial alginate derivative (RA-OSA-APA) synthesized via oxidation-reductive amination using 6-aminopenicillanic acid (6-APA) as a hydrophobic modifier. Leveraging this functional polymer, RA-OSA-APA was blended with water-soluble polyvinyl alcohol (PVA) to successfully fabricate RA-OSA-APA/PVA composite nanofibers through electrospinning. Furthermore, a sequential multilayer electrospinning strategy was employed to sequentially co-spun chitosan (CS) and gelatin (GT) onto the surface of RA-OSA-APA/PVA composite nanofibers, resulting in RA-OSA-APA/PVA/CS/GT electrospun multilayer composite nanofibers. Comprehensive characterization results demonstrated that chemical modification disrupted alginate’s hydrogen bonding network, enhanced molecular flexibility, and facilitated chain entanglement with PVA, significantly improving electrospinnability. Although bead-free nanofibers could not be electrospun from pure RA-OSA-APA aqueous solution, its content was effectively increased within the uniform RA-OSA-APA/PVA composite nanofibers. Furthermore, the sequential layering of CS and GT onto the RA-OSA-APA/PVA composite nanofibers via multilayer electrospinning not only yielded uniform fibrous morphologies stabilized by intermolecular hydrogen bonding but also created a unique physical barrier effect. This architectural innovation effectively reduced water absorption, achieved the effective loading and controlled release of triclosan (TCA), and synergized with the inherent antibacterial functions and robust cytocompatibility of CS and GT to enhance biological performance. With their favorable physicochemical and controlled-release properties, the RA-OSA-APA/PVA/CS/GT composite nanofibers represent a promising multifunctional wound dressing platform for managing infected wounds.
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Shiyu Chen,Jingjing Chang,Yawen Yin,Xiaoyan Mu,Anchi Diao,Xinyi Wang,Lei Liu,Zhaozhu Zheng,Gang Li,Xiaoqin Wang
Chronic wounds have persistent oxidative stress impairing tissue regeneration, necessitating antioxidant strategies that are both biologically effective and durable. While silk fibroin (SF) exhibits intrinsic antioxidant activity, how its molecular weight governs antioxidant performance across chemical and cellular contexts remains unclear. We systematically elucidate SF's molecular-weight-dependent antioxidant behavior and translate these insights into designing a sustained-release composite gel. SF fragments spanning ultra-low to high molecular weights were prepared and characterized. Ultra-low-molecular-weight silk fibroin (∼10.7 kDa) exhibited the strongest chemical antioxidant activity, achieving >60% DPPH scavenging and > 95% hydroxyl radical elimination, attributed to enriched tyrosine content and reduced β-sheet crystallinity. However, this superior radical-scavenging capacity did not translate directly to cellular repair. Instead, low-molecular-weight silk fibroin (L-SF, ∼27 kDa) provided the most robust and concentration-stable cellular protection, significantly restoring viability in oxidatively damaged fibroblasts and enhancing intracellular antioxidant defenses, including catalase (CAT) and superoxide dismutase activities ( p < 0.01). Building on this divergence, a composite high-molecular-weight silk fibroin/sodium carboxymethyl cellulose (H-SF/CMC-Na) hydrogel was engineered using H-SF for mechanical reinforcement and L-SF surface coating to impart sustained antioxidant activity. The optimized formulation (H-SF: CMC-Na = 2: 1, 40% solids) satisfied mechanical and conformability requirements for wound dressing applications and enabled sustained release of bioactive SF over 24 h. Gel extracts significantly improved cellular antioxidant indicators, increasing CAT activity 7.6-fold. This work establishes molecular-weight-guided design as a unifying principle for SF-based antioxidant biomaterials, demonstrating that effective wound dressing candidates must balance radical-scavenging capacity with cellular compatibility and sustained biological function.
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DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2026
·
IF 5.4
Fengrui Li,Dingshi Guo,Tingyu Zhang,Yuhang Jiang,Xinran Wang,Yanyan Liu,Shuang Gao
Conventional pesticides are often plagued by poor controlled-release performance, hydrophobic nature, posing risks to nontarget organisms. The development of nano-delivery carriers with hydrophilicity on crop surfaces and sustained-release function within crops remains challenging. Inspired by host-guest recognition in supramolecular chemistry, we developed a molecular recognition-driven engineering strategy that exploits the pesticide structure to modulate its release performance and mechanism. The two structurally distinct fungicides azoxystrobin (AZO) and dimethomorph (DIM) as guests were encapsulated in methylated β -cyclodextrin cavity (M β CD) towards preparing nanofibers using electrospinning techniques to target crop diseases. SEM, Zeta potential, molecular simulations, DFT calculations, release kinetics and mechanism collectively confirmed that pesticide structure affected the host-guest inclusion behavior, nanofiber morphology, and ultimately the sustained-release feature. Both pesticide/M β CD inclusion complex nanofiber (pesticide/M β CD-IF) displayed highly water-soluble and good antifungal efficacy against Rhizoctonia solani and Haematonectria haematococca relative to the corresponding free pesticides. The LC 50 value of DIM/M β CD-IF was higher than that of DIM SC, indicating improved safety for soil nontarget organisms. This study presents a pesticide architecture-centered paradigm for nanofiber design, aiming to provide a feasible method for sustainable crop protection. Download: Download high-res image (194KB) Download: Download full-size image
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高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2024
·
IF 10.5
Ying Qin,Yi Wei,Zejing Gao,Jingxuan Liu,Donglin Sui,Yuning Hu,Fangling Gong,Guanghui Ma
Sustained release microspheres loaded with goserelin are regarded as a promising candidate for treating prostate cancer and other sex hormone diseases. However, their widespread adoption has been hindered by issues such as wide particle size distribution and unstable release characteristics. To address these challenges, we employed a combination of the solid-in-oil-in-water microspheres preparation approach (S/O/W) and innovative premix membrane emulsification technology and deeply investigated the effects of four key parameters on the loaded performance of microspheres and the microscopic mechanisms behind them. With this approach, we successfully produced goserelin-loaded sustained release microspheres of narrow particle size distribution (Span 0.642), remarkable encapsulation efficiency (DL = 4.23 %, EE = 93.98 %), low initial burst release (about 0.50 % within 2 h), and compatibility with small injection needles (23-G, inner diameter 0.33 mm, outer diameter 0.64 mm, maximal force 59 N). In the animal model(administered dose, 2.4 mg·Kg −1 ), goserelin long-acting sustained release microspheres sustained release for over 32 days, maintaining effective concentrations above 2 ng·mL −1 , and effectively reduced serum testosterone concentrations to castration levels (<1.0 ng·mL −1 ) by day 4, maintaining this inhibition for up to 21 days, exhibiting comparable efficacy to the positive control group. In vivo release kinetics analysis revealed that goserelin-loaded sustained release microspheres exhibited a release pattern dominated by diffusion with corrosion assistance in vivo. In summary, the systematic and comprehensive evaluation of uniform-sized goserelin-loaded sustained release microspheres has highlighted their excellent translational potential, and the study herein may provide new strategies and ideas for the development of microsphere dosage forms.
研究领域:
药剂学
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生物医学工程
·
肿瘤学
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DOI
PubMed
高影响因子
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