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Materials · 2019 ·Vol. 12 ·期 22 ·3780 · IF 2.972

Loading and Sustained Release of Benzyl Ammonium Chloride (BAC) in Nano-Clays

Xianfeng Yue,Rong Zhang,Huairui Li,Minglei Su,Xiaobei Jin,Daochun Qin

Benzyl ammonium chloride (BAC) is a broad-spectrum bactericide, but vulnerable to leaching by water. In this paper, halloysite nanotubes (HNT) and montmorillonite (MMT) were used as drug carriers to load BAC, in order to achieve good anti-mildew activity and long-term sustained release properties. The HNT and MMT nano-composites were characterized by transmission electron microscope (TEM), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and nitrogen adsorption/desorption. XRD results showed that BAC intercalated the interlayer of MMT, and expanded the interlayer spacing from 1.15 nm to 1.75 nm. Pore analysis showed that BAC decreased the cavity of halloysite nanotubes to a certain extent, which indicated that BAC loaded inside the lumen of HNT successfully. TG analysis showed that the loading capacity of MMT to BAC was higher than HNT. The accelerated-release experiments revealed both two clays have significant sustained-release effects on BAC, and the releasing rate of HNT was relatively lower. Both HNT and MMT have promising application prospects as sustained-release carriers. The inhibition test showed that BAC in nano-clay has good anti-mildew resistance performance.Keywords:Benzyl ammonium chloride;halloysite nanotubes;montmorillonite;sustained release;anti-mildew

CAS / MDL: 3287-99-8
研究领域: 材料科学 · 微生物学
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Materials Today Communications · 2022 · IF 3.662

Solid particles surface-modified with beta-cyclodextrin for sustained release of flavor

Yipeng Zhang,Jianping Zhang,Zechun Liu,Yanjun Huang,Xiaopeng Xiong

Beta-cyclodextrin (β-CD) has promising applications in many fields based on its hydrophobic cavity at the central of the cyclic molecule, which can form inclusion complex with specific molecule via a host-guest interaction. However, the water solubility of β-CD limits its application. Herein, attempts have been made to graft β-CD onto two kinds of solid particles while retaining the function of β-CD, so as to expand its application. First, SiO 2 nanoparticles were modified with silane coupling agent KH-560 to offer epoxy groups. Then, the epoxy groups of the modified SiO 2 and the hydroxyl groups of β-CD were simultaneously esterified by a dicarboxylic acid of succinic acid in a non-toxic solvent medium to obtain the β-CD modified SiO 2 (SiO 2 @β-CD). On the other hand, microcrystalline cellulose (MCC) particles were also modified with β-CD (MCC@β-CD) through co-esterification of their hydroxyl groups with succinic acid. The syntheses were monitored by Fourier transform infrared (FT-IR) spectroscopy, and the obtained materials were characterized by X-ray diffraction (XRD), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). The degrees of β-CD modification for the particles have been measured and analyzed to optimize the synthesis conditions. The results indicate that the degree of β-CD modification for the SiO 2 @β-CD is relatively low, but the material exhibits over 60 ºC elevation of the thermal stability. In comparison, the degree of β-CD modification for MCC@β-CD reached as high as 422 mg/g. Due to the much higher content of β-CD, the synthesized MCC@β-CD was employed to load a flavor compound of D -limonene, and its sustained release was investigated to suggest the potential of the β-CD modified particles.

CAS / MDL: 2530-83-8 77-09-8
研究领域: 材料科学 · 食品科学
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JOURNAL OF APPLIED POLYMER SCIENCE · 2023 · IF 3

A sustained-release gel film based on chitosan for treating cutaneous candidiasis

Hudie Fu,Li Kang,Lanjun Yu,Yanping Fu,Zhijie Wen,Shengpeng Zhu,Mohan Zhao,Yuqing Wang,Qi Chen,Qinxiong Lin,Xinzhou Yang,Yan Hu

Hydrogels have been widely used in wound dressings owing to their biocompatibility and bacteriostatic properties. In this study, a chitosan-citric acid gel film was prepared using chitosan as the raw material and citric acid as the acid solvent and cross-linking agent. In addition, to increase the antibacterial effect of the gel film, ketoconazole/β-cyclodextrin inclusion complex was prepared by inclusion technology and added to the gel film to prepare a chitosan-citric acid sustained-release gel film loaded with ketoconazole/β-cyclodextrin inclusion complex for treating cutaneous candidiasis. The physical and chemical properties of the chitosan-citric acid gel films were investigated using infrared spectroscopy, x-ray diffraction, water vapor transmittance test, thermal analysis, and swelling tests. Drug release, antibacterial, and toxicity tests of the chitosan-citric acid gel film loading with ketoconazole/β-cyclodextrin inclusion complex were carried out in vitro. The composite film showed good sustained drug release behavior, antibacterial effects, and biocompatibility in vitro. These results support that the chitosan-citric acid hydrogel has great potential as a gel wound dressing for the treatment of cutaneous candidiasis.

CAS / MDL: 7585-39-9 65277-42-1
研究领域: 药剂学 · 材料科学 · 生物医学工程 · 微生物学
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AAPS PHARMSCITECH · 2023 ·Vol. 24 ·期 6 ·1-10 · IF 3.3

Transdermal Delivery of Estradiol Simultaneously Possessing Rapid Release and Sustained Release Effect

Tang XiaoFei,Qin Huaiying,Yang Jianhua,Zhang XiaoYun

Dissolving microneedle (DMN) has been researched as a drug delivery technology that improves drug molecule transportation through the skin with little discomfort. However, the sluggish drug absorption, poor skin dissolution, and lengthy time lags of DMN have limited its potential uses. The aim of this study was to design a novel DMN system for the administration of the poorly water-soluble drug, estradiol (E2), with fast skin penetration and a stable release rate for a long time. DMN containing E2 emulsion (E2-EM-DMN) and traditional DMN (T-DMN) were prepared. Rat skin was used for penetration test and guinea pig skin was used for skin irritation experiment. The drug release profiles and stability properties of these two kinds of DMNs were also investigated. High performance liquid chromatography was employed to determine the E2 content in DMN. The E2 concentration in rat plasma was achieved by a newly developed liquid chromatography-mass spectrometry method that was fast, reproducible, and specific. The height of E2-EM-DMN and T-DMN was 600 μm. The drug loading of the E2-EM-DMN and T-DMN was 667.30 ± 7.21 μg/patch and 672.56 ± 6.98 μg/patch. E2-EM-DMN possessed enough mechanical strength to penetrate the skin and caused no irritation to the skin. E2-EM-DMN could release the drug more rapidly and more continuously than T-DMN. E2-EM-DMN had good pharmaceutical stability. In summary, the E2-EM-DMN showed reliable quality and superior release performance. Emulsion-embedded DMN is an ideal transdermal delivery system for drugs. Graphical Abstract

CAS / MDL: 25322-68-3
研究领域: 药剂学 · 药物递送系统 · 药学
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JOURNAL OF APPLIED POLYMER SCIENCE · 2023 ·Vol. 140 ·期 15 ·e53716 · IF 3

A pesticide sustained-release microcapsule from cellulose nanocrystal stabilized Pickering emulsion template

Cai-xia Yang,Jun Li,Yu-qing Zhang,Chao Wu,De-qiang Li

Efficient utilization of pesticides has presented various advantages in the ecological environment, food safety, and agricultural sustainability. Pesticide microcapsule could significantly improve the pesticide utilization ratio, and thus, we prepared a sustained-release microcapsule from cellulose nanocrystal (CNCs) stabilized Pickering emulsion template. The NaCl was added to overcome the strong electrostatic repulsion among CNCs for forming a stable oil-in-water (O/W) CNCs-based Pickering emulsion template, followed by crosslinking with hexamethylene diisocyanate on the interface. UV–vis and zeta-potential were used to characterize the as-prepared Pickering emulsion, and the stability and emulsion fraction were calculated. Results indicated that NaCl contributed to the stability of Pickering emulsion, even at a low concentration. The obtained CNCs-based microcapsule was characterized by FT-IR, XRD, SEM, TG-DTG, and three-phase contact angles. The microcapsule presented an encapsulation efficiency of 96.76% and sustained release of the imidacloprid for more than 82 h. Results indicated the potential for loading and sustained release of imidacloprid, which is beneficial to the environment, food, and agriculture.

CAS / MDL: 822-06-0 138261-41-3
研究领域: 农业科学 · 材料科学 · 环境科学
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LANGMUIR · 2025 · IF 3.9

Microfluidic Regulation of Core–Shell PLGA Microspheres for Sustained Release of Leuprolide Acetate

Ruoxin Wei,Jiaze Dou,Yihui Wu,Jinjin Li,Lian Cen,Zhenhao Xi

Microsphere formulations represent a promising drug delivery system for proteins and peptides with short half-lives as they effectively mitigate drug degradation in vivo. This study aimed to develop poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with leuprolide acetate (LA) using microfluidic technology and to investigate key factors that could have a significant effect on the LA encapsulation and loading. A glass capillary microfluidic device for a water-in-oil-in-water (W/O/W) emulsion system was developed. Gelatin (Gel) of varying concentrations was introduced in the internal aqueous phase, and different collecting solutions for W/O/W emulsions were investigated. The effect of the LA concentration in the inner phase was also explored. It was shown that LA-loaded PLGA microspheres (LA–PLGA–MS) by microfluidics were monodisperse with a uniform particle size of 80 μm and exhibited a distinguished core–shell structure. At a Gel concentration of 7.5 mg/mL, the microspheres reached a maximum encapsulation efficiency (EE) of 80.28% and a drug loading (DL) of 4.24%. The in vitro release could last for around 28 days. The DL of microspheres was found to be increased with the increase in LA concentration in the inner water phase. The incorporation of Gel within the inner water phase and the collecting solution with a suitable pH value were the main factors that affected the EE of microspheres. Briefly, LA–PLGA–MS could be successfully prepared and regulated using microfluidics and sustained LA release as monodispersed microsphere formulations. The developed technological strategy could provide a precise strategy and experimental reference for applications in delivery systems for water-soluble peptides and proteins.

研究领域: 药剂学 · 生物医学工程 · 纳米技术 · 药物递送
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Polymers · 2024 ·Vol. 16 ·期 24 ·3451 · IF 4.7

Sustained Release of Curcumin from Cur-LPs Loaded Adaptive Injectable Self-Healing Hydrogels

Caixia Wu,Xiaoqun Ning,Qunfeng Liu,Xiaoyan Zhou,Huilong Guo

Biological tissue defects are typically characterized by various shaped defects, and they are prone to inflammation and the excessive accumulation of reactive oxygen species. Therefore, it is still urgent to develop functional materials which can fully occupy and adhere to irregularly shaped defects by injection and promote the tissue repair process using antioxidant and anti-inflammatory mechanisms. Herein, in this work, phenylboronic acid modified oxidized hyaluronic acid (OHAPBA) was synthesized and dynamically crosslinked with catechol group modified glycol chitosan (GCHCA) and guar gum (GG) into a hydrogel loaded with curcumin liposomes (Cur-LPs) which were relatively uniformly distributed around 180 nm. The hydrogel possessed rapid gelation within 30 s, outstanding injectability and tissue-adaptive properties with self-healing properties, and the ability to adhere to biological tissues and adapt to tissue movement. Moreover, good biocompatibility and higher DPPH scavenging efficiency were illustrated in the hydrogel. And a more sustainable release of curcumin from Cur-LPs-loaded hydrogels, which could last for 10 days, was achieved to improve the bioavailability of curcumin. Finally, they might be injected to fully occupy and adhere to irregularly shaped defects and promote the tissue repair process by antioxidant mechanisms and the sustained release of curcumin for anti-inflammation. And the hydrogel would have potential application as candidates in tissue defect repair.

研究领域: 生物材料学 · 组织工程 · 药剂学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2024 · IF 6

Sustained release behavior of lysozyme based on konjac glucomannan/κ-carrageenan composite hydrogels

Guanchen Wu,Yongpeng Yin,Cuiping Li,Ruijie Hao,Jiaxiang Zang,Mengyao Kang,Denglin Luo,Wei Xu

In this study, the gelation mechanism of konjac glucomannan (KGM)/κ-carrageenan (KC) composite hydrogels at different mass ratios and its controlled release ability to lysozyme (Ly) were investigated. With the increase of KGM proportion, water holding capacity (WHC) and hardness first increased and then decreased, and reached the maximum when the mass ratio of KGM to KC was 1:2. Rheological tests showed that the viscoelasticity of the composite hydrogels can be effectively adjusted by changing the mixing ratio of KGM and KC. Fourier transform infrared spectroscopy (FTIR) and thermogravimetry confirmed that the thermal stability of the composite hydrogels was enhanced by hydrogen bonding as the main interaction force between KGM and KC. The porous gel network was observed by scanning electron microscope (SEM). With the increase of KGM ratio, the pore size first decreased and then increased. In addition, adjusting the ratio of KGM and the pH of release environment can enhance the controlled release effect of KC on Ly by the in vitro release experiment of Ly. Overall, these findings provide a theoretical basis for the development of performance-enhanced composite hydrogels for drug-controlled release.

CAS / MDL: 11114-20-8
研究领域: 食品科学 · 生物材料学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2023 · IF 5.8

Rapidly separable microneedle patch for the controlled and sustained release of 5-fluorouracil

Lijing Zhang,Jiatong Lv,Yannan Yin,Guixia Ling,Peng Zhang

5-Fluorouracil (5-FU) is frequently used in the treatment of tumors and swollen tissues. However, traditional administration methods can result in poor patient compliance and require to administrate frequently due to the short T 1/2 of 5-FU. Herein, the [email protected] loaded nanocapsules were prepared using multiple emulsion solvent evaporation methods to enable the controlled and sustained release of 5-FU. To decrease the drug release rate and enhance patient compliance, the obtained pure nanocapsules were added to the matrix to fabricate rapidly separable microneedles (SMNs). The entrapment efficiency (EE%) of [email protected] loaded nanocapsules was in the range of 41.55–46.29 %, and the particle size of ZIF-8, [email protected] , and [email protected] loaded nanocapsules were 60  nm , 110 nm, and 250 nm respectively. According to the release study in vivo and in vitro, we concluded that [email protected] nanocapsules could achieve the sustained release of 5-FU and that the burst release of nanocapsules could be elegantly handled by incorporating nanocapsules into the SMNs. What's more, the use of SMNs could improve patient compliance due to the rapid separation of needles and backing of SMNs. The pharmacodynamics study also revealed that the formulation would be a better choice for the treatment of scars due to the advantages of painlessness, separation ability, and high delivery efficiency. In conclusion, the SMNs containing [email protected] loaded nanocapsules could serve as a potential strategy for some skin diseases therapy with controlled and sustained drug release behavior.

研究领域: 药剂学 · 药物递送系统 · 纳米技术 · 药理学
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RSC Advances · 2022 ·Vol. 12 ·期 26 ·16444-16453 · IF 4.036

A sustained-release Trametinib bio-multifunction hydrogel inhibits orthodontically induced inflammatory root resorption

Hang Yu,Zhina Wu,Xingfu Bao,Xiaoduo Tang,Junhu Zhang,Yi Zhang,Min Hu

Orthodontic tooth movement (OTM) is a bone reconstruction process. In most cases, OTM could induce root resorption as a common side effect, called orthodontically induced inflammatory root resorption (OIIRR). OIIRR affects tooth health and interferes with the stability of orthodontic treatment. Osteoclasts, which perform bone resorption in OTM, attack cementum, causing OIIRR. Many signaling pathways are involved in the maturation and differentiation of osteoclasts, among which the ERK1/2 is one of the important pathways. In this experiment, we added Trametinib (Tra), a specific inhibitor of ERK1/2, to catechol-modified chitosan (CHI-C) and oxidized dextran (ODex) to form a CCOD–Trametinib composite hydrogel (CCOD–Tra) to prevent OIIRR. CCOD–Tra exhibited good biocompatibility, injectability, strong adhesion, good hemostatic function and sustained release of Tra. We performed local injection of CCOD–Tra into the periodontal tissues of rats. CCOD–Tra firmly adhered to the periodontal tissues and then released Tra to establish a good biological environment and maintain a drug concentration at a high level around the roots for a long time. H&E, TRAP, immunochemistry staining and micro-CT indicated that CCOD–Tra had a good effect in terms of preventing OIIRR. Cell experiments showed that CCOD–Tra reduced the expression of TRAP, MMP-9 and C-FOS in osteoclast cells through the ERK1/2 signaling pathway to inhibit the differentiation and maturation of osteoclasts. Based on the above results, we concluded that CCOD–Tra had the ability to prevent OIIRR, the high adhesion and injectability of CCOD may provide better therapeutic ideas for clinical prevention of OIIRR.

研究领域: 牙科学 · 药学 · 生物材料 · 组织工程
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REGIONAL ANESTHESIA AND PAIN MEDICINE · 2024 · IF 5.1

Magnetically targeted lidocaine sustained-release microspheres: optimization, pharmacokinetics, and pharmacodynamic radius of effect

Ling-xi Zheng,Qian Yu,Lin Peng,Qiang Li

Objective This study aimed to optimize the formulation of magnetically targeted lidocaine microspheres, reduce the microsphere particle size, and increase the drug loading and encapsulation rate of lidocaine. The optimized microspheres were characterized, and their pharmacokinetics and effective radii of action were studied. Methods The preparation of magnetically targeted lidocaine microspheres was optimized using ultrasonic emulsification-solvent evaporation. The Box-Behnken design method and response surface method were used for optimization. The optimized microspheres were characterized and tested for their in vitro release. Blood concentrations were analyzed using a non-compartment model, and the main pharmacokinetic parameters (half-life ( t 1/2 ), maximum blood concentration, area under the blood concentration-time curve (AUC), time to peak ( T max ), and mean retention time (MRT) were calculated. Pathological sections were stained to study the safety of the microsphere tissues. A rabbit sciatic nerve model was used to determine the “standard time ( t 0 )” and effective radius of the microspheres. Results The optimized lidocaine microspheres exhibited significantly reduced particle size and increased drug loading and encapsulation rates. Pharmacokinetic experiments showed that the t 1/2 , T max , and MRT of magnetically targeted lidocaine microspheres were significantly prolonged in the magnetic field, and the AUC 0-48 and AUC 0-∞ were significantly decreased. Its pharmacodynamic radius was 31.47 mm. Conclusion Magnetically targeted lidocaine microspheres provide sustained long-lasting release, neurotargeting, nerve blocking, and high tissue safety. This preparation has a significantly low blood concentration and a slow release in vivo, which can reduce local anesthetic entry into the blood. This may be a novel and effective method for improving postoperative comfort and treating chronic pain. This provides a countermeasure for exploring the size of the magnetic field for the application of magnetic drug-carrying materials.

CAS / MDL: 1317-61-9
研究领域: 药剂学 · 生物医学工程 · 神经科学
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RSC Advances · 2024 ·Vol. 14 ·期 10 ·7195-7205 · IF 3.9

Nanomicrosphere sustained-release urokinase systems with antioxidant properties for deep vein thrombosis therapy

Shun Xiao,Xiaozhi Sun,Chong Wang,Jianlie Wu,Kun Zhang,Mingjin Guo,Bing Liu

Deep vein thrombosis (DVT) is a venous return disorder caused by abnormal clotting of blood in deep veins. After thrombosis, most of the thrombus will spread to the deep vein trunk throughout the limb. If DVT is not treated in time, most of them will develop into thrombosis sequelae and even threaten life. Intravenous thrombolytic drugs are the most promising strategy for treating DVT, but current drugs used for thrombolysis suffer from short half-lives and narrow therapeutic indexes. To effectively manage DVT, it is necessary to develop a novel multifunctional drug-loading system to effectively prolong the treatment time and improve the therapeutic efficacy. In this study, a urokinase-loaded protocatechuic aldehyde-modified chitosan microsphere drug-loading platform was constructed for the treatment of DVT. This microsphere adsorbed urokinase well through electrostatic interaction, and the introduction of bovine serum albumin conferred stability to the microspheres. Therefore, the microsphere drug delivery system could achieve slow drug release to effectively dissolve blood fibrin. In addition, chitosan grafted with protocatechuic aldehyde imparted excellent antioxidant activity to the system to reduce free radicals in the blood vessels. Effective management of oxidative stress could avoid abnormal platelet activation and new thrombus formation. The experimental results showed that this microsphere had good biocompatibility, anti-inflammatory properties, and considerable thrombolytic activity. In conclusion, this study provided a new direction and developed a novel multi-functional nano microsphere drug delivery platform for the treatment of DVT.

研究领域: 药剂学 · 药理学 · 生物医学工程 · 材料科学 · 治疗学
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