JOURNAL OF CONTROLLED RELEASE
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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
ACS Applied Bio Materials
·
2025
·
IF 4.7
Boying Li,Ran Zhang,Nana Wang,Xiaoning Liu,Ning Li,Jintong Ding,Zhanshuo Cao,Xiongwei Qu,Chengfen Xing
Acute myeloid leukemia (AML) is extremely difficult to cure due to the challenges in accurately targeting it, as it is characterized by rapid progression, high aggressiveness, and high drug resistance. In this study, biomimetic sustained release nanoparticles (PLGA-C-M) were designed and prepared to inhibit the survival and resistance pathways of AML. PLGA-C-M targeted AML cells by wrapping leukemia cell membranes, achieving sustained slow drug release in the blood, and then progressively affecting intracellular Ca2+ signaling by targeting TRPM2 ion channels that were highly expressed in AML in a step-by-step manner. PLGA-C-M can inhibit the growth of AML cells from three aspects: destroying mitochondrial function, reducing autophagy, and overcoming the drug resistance of cancer cells. Biomimetic nanoparticles achieved simultaneous regulation of intracellular ROS and Ca2+ signals to inhibit the growth of leukemia cells and provided ideas for the regulation of ion channel-related signal transduction in AML.
研究领域:
纳米技术
·
癌症生物学
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药理学
·
生物化学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Yushen Ma,Xiaoming Zhu,Hui Chen,Lixiao Ni,Yalun Pang,Cunhao Du,Chu Xu,Jiahui Shi,Yiping Li,Shiyin Li
Climate change has made on-site bloom control increasingly challenging. Therefore, it is necessary to study whether it is possible to control the outbreak of summer cyanobacterial blooms by early prevention of cyanobacterial recovery. This study used artemisinin sustained-release algaecides (ASAs), a typical allelochemical for in-situ cyanobacterial control, to evaluate recovery effects and microbial-ecological impacts through microcosm experiments. All doses inhibited the recovery and bloom of cyanobacteria (Chl-a < 66μg/L), prevented spore germination to varying degrees (especially at the low and high doses), and reduced the ecological niche of cyanobacteria (1.6–2.6). The results demonstrated that low-dose ASAs effectively prevented cyanobacterial recovery with minimal microbial-ecological impacts. Higher ASAs doses reduced bacterial diversity (shannon index dropped from 5 to around 2.8), enhanced environmental selection (the proportion increased from 15 % to 67 %), and loss of native species. The bacterial community underwent a pronounced shift: dominant cyanobacterial genera such as Limnothrix declined substantially, whereas Proteobacteria increased to 60–95 % phylum-level relative abundance. Conversely, eukaryotes enhanced heterogeneous selection (the proportion = 50 %–83 %), smaller diversity changes (Chao1 = 1000–1600), moderate community succession, and widespread microbial cooperation. The effects of ASAs on microbial networks were limited, but the effects of high doses were not negligible, especially the low occupancy module, which accounted for only 8.79 %, was more affected by the DOC/pH changes caused by high-dose. Moreover, ASAs prevented cyanobacterial recovery through bacterial-eukaryotic cooperation and functional microbes, provided the microbial community had not undergone severe environmental stress. Our findings emphasize the importance of considering the nonlinear microbial-ecological responses to dosing and the necessity of low-dose strategies during both in-situ control and prevention, as low-dose result in less changes in microbial community structure and lower risk of secondary cyanobacterial blooms.
研究领域:
环境科学
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微生物学
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生态毒理学
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藻类学
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水处理
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产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2025
·
IF 9.8
Linyan Chen,Haohan Jing,Yuhe Dong,Yuantong Cao,Tong Wu,Wanying Zhu,Fanwei Dai,Minhui Chen,Yao Liu,Nan He,Ran Huang,Tian Zhong
The traditional method of generating chlorine dioxide (ClO 2 ) involves reacting sodium chlorite with acid on-site, posing high safety risks of concentrated ClO 2 . This study encapsulates ClO 2 molecules directly in α-cyclodextrin (α-CD) to form inclusion complexes (ClO 2 @α-CD). This approach enables stable storage and safe handling of gaseous ClO 2 , while its sustained-release property also provides long-term microbial inhibition. Fumigation with 0.25 g of ClO 2 @α-CD completely inhibited Aspergillus niger growth on potato dextrose agar (PDA). A 0.5 g dose reduced the 6-day decay incidence of A. niger -inoculated strawberries from 91.67 % (control) to 5.00 % and the severity from 58.75 % (control) to 1.25 %. In commercial storage simulations, 5 g of ClO 2 @α-CD reduced the natural incidence from 53.33 % (control) to 26.67 %, while preserving the weight, color, firmness, and total soluble solids (TSS)/titratable acidity (TA) ratio of strawberries. These findings suggest that ClO 2 @α-CD is a viable approach for controlling postharvest diseases and prolonging fruit shelf-life.
研究领域:
食品科学
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植物病理学
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化学工程
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产品关联
DOI
PubMed
高影响因子
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
·
眼科医学
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产品关联
DOI
PubMed
高影响因子
LANGMUIR
·
2020
·
IF 3.557
Ya Wang,Chaonan Li,Ting Wang,Xinwen Li,Xiaogang Li
A pesticide carrier system can offer advantages to active components, such as improving shelf life, extending the lasting period, and reducing toxicity, all of which could reduce the adverse effects of pesticides on the environment. Graphene oxide (GO) is a promising medical drug carrier material, and its research in the field of pesticides is still in the exploration stage. Herein, in order to load water-insoluble pesticides, a series of polylactic acid–graphene oxides (PLA–GOs) were produced incorporating small amounts (0.1–1 wt %) of GO using acetone–chloroform and N,N-dimethylformamide–dichloromethane, two dual-solvent systems. The prepared PLA–GO carrier materials were characterized by FT-IR, Raman spectroscopy, and differential scanning calorimetry analysis, and their effects on rice growth within 20 days were also evaluated. When the amount of GO added was 0.5% and the solvent system was acetone–chloroform, the amount of pyraclostrobin (Pyr) loaded on PLA–GO (A-0.5%) was very high (39.89%). The PLA–GO pesticide microsphere showed a significantly sustained release of Pyr (up to 30 d). Furthermore, the indoor bioassay results showed that the PLA–GO pesticide microsphere (EC50 = 1.2682) had the best fungicidal activity against Rhizoctonia solani, followed by Pyr technical (EC50 = 2.3137) and commercial Pyr microcapsule suspension (EC50 = 3.4570). In conclusion, it was found that PLA–GOs prepared using the acetone–chloroform system were more suitable as a pesticide carrier, which provided a preliminary basis for GO to realize the coating of water-insoluble pesticides.
研究领域:
材料科学
·
农业科学
·
环境科学
✓ 已验证
DOI
高影响因子
SN Applied Sciences
·
2020
·Vol. 2
·期 12
·1-11
·
IF 0
Chen Huayao,Zhan Jinghui,Zhou Hongjun,Hao Li,Xu Hua,Pu Xia,Zhou Xinhua
Developing effective sustained release system is an efficient way to prevent the pollution from overused pesticide. Hence, a highly efficient sustained release system was developed using zinc (II) modified montmorillonite (Zn–Mt) prepared by ion exchange from sodium montmorillonite (Na–Mt) with zinc nitrate. Zn–Mt was modified by sodium alginate (ALG) to further improve its sustained release performance and pH-sensitivity. The results indicated that triazolone was supported on the zinc modified montmorillonite through the coordination bond from zinc ion. The zinc ion in the Mt also played a similar role as calcium ion to induce ALG crosslinking which made ALG highly dispersed in the pores of Mt. ALG interacted with Zn 2+ from Mt through electrostatic interaction and winded with triazolone to form a barrier for the sustained release system. As a result, the adsorption capacity of ALG–Zn–Mt (17.75 mg/g) was improved comparing with Na–Mt without modification (14.52 mg/g). The sustained release performance of ALG–Zn–Mt showed also significant pH-sensitivity in accordance with the stability of ALG.
研究领域:
环境科学
·
农药化学
·
材料科学
✓ 已验证
DOI
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
·
眼科学
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
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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产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
DOI
高影响因子
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
·
麻醉学
·
生物材料
·
控释系统
✓ 已验证
DOI
高影响因子
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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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）