BIOINORGANIC CHEMISTRY AND APPLICATIONS
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2021
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IF 7.778
Wen Liu,Tong-Tong Wang,Xiao-Luan Tang,Fei-Ya Jiang,Xiao Yan,Jun Deng
In this work, quercetin was loaded in the highly-porous lactose via the adsorption of quercetin molecules in ethanol. The method aims to improve the quercetin solubility and the loading capacity of lactose. The method relates to the synthesis of the highly-porous lactose with a particle size of ∼35 μm, a mean pore width of ∼30 nm, a BET surface area of 35.0561 ± 0.4613 m2/g, and a BJH pore volume of ∼0.075346 cc/g. After the quercetin loading in ethanol, BET surface area and BJH pore volume of porous lactose were reduced to 28.8735 ± 0.3526 m2/g and 0.073315 cc/g, respectively. The reduction rate was based on the quercetin loading efficiency of highly-porous lactose. DSC analysis and XRD analysis suggest that the sediments of quercetin in the nanopores of porous lactose are crystalline. FTIR spectroscopy results suggest that there is no significant interaction between quercetin and lactose. The highly-porous lactose had a higher loading efficiency of 20.3% (w/w) compared to the α-lactose (with 5.2% w/w). The release rates of quercetin from the highly-porous lactose tablets were faster compared to the conventional α-lactose carrier.
研究领域:
药剂学
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食品科学
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材料科学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2019
·
IF 3.973
Ce Cheng,Zhihua Wu,David Julian McClements,Liqiang Zou,Shengfeng Peng,Wei Zhou,Wei Liu
A novel cholesterol-free curcumin delivery system was fabricated by rhamnolipids modified liposomes (RL-Lps). The incorporation of the rhamnolipids increased the sphericity, reduced the size, and decreased the polydispersity of the liposomes compared with pure liposomes (Lps). Analysis of the environmental stability of the RL-Lps showed they have good long-term stability over a wide range of pH (2–3 and 5–8), ionic strengths (0–200 mM), and accelerated centrifugal conditions. The curcumin-loaded rhamnolipids modified liposomes (Cur-RL-Lps) could be prepared with a relatively high loading efficiency (LE > 90%) and loading capacity (LC > 3.5%). The thermal and photochemical stability of the curcumin was improved after encapsulation in the Cur-RL-Lps. In vitro release studies indicated that the sustained release of the curcumin was prolonged when rhamnolipids were incorporated into the liposomes. This study shows that rhamnolipids have great potential for liposomal delivery system suitable for utilization in functional foods, dietary supplements, and pharmaceutical preparations.
研究领域:
药学
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药物递送系统
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生物技术
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
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2017
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IF 4.159
Hong Wang,Guangxing Zhang,Xueqin Ma,Yanhua Liu,Jun Feng,Kinam Park,Wenping Wang
Poly (lactide-co-glycolide) (PLGA) microparticles are widely used for controlled drug delivery. Emulsion methods have been commonly used for preparation of PLGA microparticles, but they usually result in low loading capacity, especially for drugs with poor solubility in organic solvents . In the present study, the nanocrystal technology and a water-soluble polymer template method were used to fabricate nanocrystal-loaded microparticles with improved drug loading and encapsulation efficiency for prolonged delivery of breviscapine . Breviscapine nanocrystals were prepared using a precipitation-ultrasonication method and further loaded into PLGA microparticles by casting in a mold from a water-soluble polymer. The obtained disc-like particles were then characterized and compared with the spherical particles prepared by an emulsion-solvent evaporation method. X-ray powder diffraction (XRPD) and confocal laser scanning microscopy (CLSM) analysis confirmed a highly-dispersed state of breviscapine inside the microparticles. The drug form, loading percentage and fabrication techniques significantly affected the loading capacity and efficiency of breviscapine in PLGA microparticles, and their release performance as well. Drug loading was increased from 2.4% up to 15.3% when both nanocrystal and template methods were applied, and encapsulation efficiency increased from 48.5% to 91.9%. But loading efficiency was reduced as the drug loading was increased. All microparticles showed an initial burst release, and then a slow release period of 28 days followed by an erosion-accelerated release phase, which provides a sustained delivery of breviscapine over a month. A relatively stable serum drug level for more than 30 days was observed after intramuscular injection of microparticles in rats. Therefore, PLGA microparticles loaded with nanocrystals of poorly soluble drugs provided a promising approach for long-term therapeutic products characterized with preferable in vitro and in vivo performance.
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
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2023
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IF 5.9
Xiaowen Li,Dongdong Ye,Zhongrun Xiang,Huai Wang,Huiqing Wang,Yun Lu,Risheng Yao
Biocompatible cellulose has been used as a pharmaceutical excipient for several decades. However, there are still shortcomings, such as low drug loading, slow disintegration, and easy drug extraction. Herein, we describe a novel process for manufacturing cellulose nanomesh (CNM), a new structured nanocellulose with a high surface area of 98.37 m 2 g −1 and a high yield above 88%. This process combines mild acid vapor with a dilute enzymatic hydrolysis preparation method. The unique nanomesh structure clearly demonstrates benefits as superior drug carriers, including a high drug loading rate (>81.2%), miniaturizing volume, ultrafast disintegration time (<7 s), long-term sustained release (22 h), and also a strong drug-abuse deterrent effect. Our work suggests that the CNM produces great potential as a promising multi-functional drug carrier to realize tablet miniaturization, drug abuse-deterrent, and drug slow and controlled release.
研究领域:
制药工程
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材料科学
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生物医学工程
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产品关联
DOI
高影响因子
Chemical Engineering and Processing-Process Intensification
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2024
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IF 3.8
Senlin Li,Yifan Zheng,Zhihao Zhang,Shengao Xu,Yuan Pu,Dan Wang
Supercritical carbon dioxide was used as the solvent for manufacturing of ibuprofen loaded gelatine sponges with high loading capacity and fast release performance toward healthcare materials in the treatment of postoperative dental pain. The solubility of ibuprofen in supercritical CO 2 was first determined at 313 K under different pressure conditions. The micronisation of ibuprofen drugs were successfully adsorbed onto the surface of network pore system of gelatine sponges via supercritical CO₂ processing. The loading capacity of ibuprofen in gelatine sponges obtained by using supercritical CO₂ as the solvent can be up to 19.86 wt%, which was double that of the sample prepared by direct soaking in ethanol. The dissolution of ibuprofen was determined and higher instantaneous dissolution rate was observed for the ibuprofen loaded gelatine sponges synthesized by supercritical CO₂ processing.
研究领域:
制药工程
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材料科学
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药物递送
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产品关联
DOI
高影响因子
International Journal of Nanomedicine
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2023
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IF 8
Conglian Yang,Tingting Wu,Yuting Qin,Yan Qi,Yu Sun,Miao Kong,Xue Jiang,Xianya Qin,Yaqi Shen,Zhiping Zhang
Background Doxorubicin (DOX) is an effective chemotherapeutic agent but severe side effects limit its clinical application. Nanoformulations can reduce the toxicity while still have various limitations, such as complexity, low drug loading capability and excipient related concerns.Methods An amphiphilic conjugate, doxorubicin-dichloroacetate, was synthesized and the corresponding nanoparticles were prepared. The in vitro cytotoxicity and intracellular uptake, in vivo imaging, antitumor effects and systemic toxicities of nanoparticles were carried out to evaluate the therapeutic efficiency of tumor.Results Doxorubicin-dichloroacetate conjugate can self-assemble into nanoparticles with small amount of DSPE-PEG2000, leading to high drug loading (71.8%, w/w) and diminished excipient associated concerns. The nanoparticles exhibited invisible systemic toxicity and high maximum tolerated dose of 75 mg DOX equiv./kg, which was 15-fold higher than that of free DOX. It also showed good tumor targeting capability and enhanced antitumor efficacy in murine melanoma model.Conclusion This work provides a promising strategy to simplify the drug preparation process, increase drug loading content, reduce systemic toxicity as well as enhance antitumor efficiency.
研究领域:
药剂学
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肿瘤学
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纳米医学
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DOI
PubMed
高影响因子
RSC Advances
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2019
·Vol. 9
·期 5
·2371-2378
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IF 3.049
Nan Wang,Xiao-Chuan Chen,Ruo-Lin Ding,Xian-Ling Yang,Jun Li,Xiao-Qi Yu,Kun Li,Xi Wei
Stimulus-responsive, controlled-release systems are of great importance in medical science and have drawn significant research attention, leading to the development of many stimulus-responsive materials over the past few decades. However, these materials are mainly designed to respond to external stimuli and ignore the key problem of the amount of drug loading. In this study, exploiting the synergistic effect of boronic esters and N-isopropylacrylamide (NIPAM) pendant, we present a copolymer as an ROS and esterase dual-stimulus responsive drug delivery system that has a drug loading of up to 6.99 wt% and an entrapment efficiency of 76.9%. This copolymer can successfully self-assemble into polymer micelles in water with a narrow distribution. Additionally, the measured CMC hinted at the good stability of the polymeric micelles in water solution, ensuing long circulation time in the body. This strategy for increasing the drug loading on the basis of stimulus response opens up a new avenue for the development of drug delivery systems.
研究领域:
医学
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材料科学
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药剂学
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产品关联
DOI
PubMed
高影响因子
POLYMER
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2012
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IF 3.438
Liang Sun,Jianzhong Du
Polymer vesicles have been widely explored as drug delivery carriers. However, there are still several notable problems in the determination of the drug loading content (DLC) and the drug loading efficiency (DLE) of the drug delivery vehicles . Presented in this paper is the reconsideration of various important factors in the measurement of the DLC and DLE based on an ‘instant’ biocompatible and biodegradable polymer vesicle which can be directly dissolved in water, with a focus on the study on the time for removing the free drug. Firstly, an anti-cancer drug, doxorubicin (DOX), was successfully encapsulated into a highly biocompatible and biodegradable poly( ε -caprolactone)- block -poly[2-(methacryloyloxy)ethyl phosphorylcholine] (PCL- b -PMPC) diblock copolymer vesicle. Secondly, a specific methodology for removing the unencapsulated drug by dialysis method before the drug release experiment has been established to verify the DLC and the DLE of DOX. A number of important factors have been investigated, such as the period of time for removing the free drug, the temperature and the volume of water outside the dialysis tube, etc. Finally, the DOX release experiment was carried out at pH 5.0 and pH 7.4 with the cumulative release percentages of 55% and 35% after 24 h when the DOX feeding was 1.0 mg. As PCL- b -PMPC vesicles absorb UV light, the DOX encapsulated in polymer vesicles was calculated by subtracting the UV absorbance of vesicle solution from the UV absorbance of DOX-loaded vesicle solution at different DOX feedings of 1.0, 3.0 and 5.0 mg. We also found the appropriate calibration curves at different solution conditions were of great significance for the calculation of DLC and DLE.
研究领域:
药剂学
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生物材料学
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DOI
高影响因子
POLYMER INTERNATIONAL
·
2021
·Vol. 71
·期 4
·487-494
·
IF 2.99
Si Dong,Yue Tang,Pan He,Sheng Ma,Wantong Song,Mingxiao Deng,Zhaohui Tang
Self-assembled polymeric nanoparticle (NP) drug carriers are capable of encapsulated and controlled delivery, facilitating improvements in the therapeutic efficiency of drugs. Here we report a series of poly( l -glutamic acid)- g -methoxy poly(ethylene glycol)/4-phenylbutyl ester (PLG- g -mPEG/PB) copolymers, which were synthesized by esterification of 4-phenylbutanol (PB) and PLG- g -mPEG in different feed ratios. The copolymers obtained form into nano-sized micelles in aqueous solution by a self-assembly process, with lower critical micelle concentration value for higher PB ratio in the copolymers. Variable temperature infrared spectroscopy and circular dichroism were used to prove the breaking of intermolecular hydrogen bonds after PB modification. Podophyllotoxin (PPT), an effective anticancer agent, was incorporated into the inner core of the micelle system by physical entrapment through hydrophobic interaction between the drug and the PB-modified copolymers. Both the drug loading content and the loading efficiency increased with PB content in the PLG- g -mPEG/PB copolymers and reached an ultrahigh value of 28.2 wt% and 94%, respectively. The PPT-encapsulated micelles (PPT-NPs) were stable at pH 7.4 but dissociated and released 80% of loaded PPT in a weak acidic environment (pH 5.0). The in vitro proliferation of non-small-cell lung cancer cells (A549) was significantly inhibited by PPT-NPs in a cytotoxicity assay. These results demonstrate that hydrophobic modification is an efficient route for tuning the self-assembly behaviour and drug encapsulation of PLG- g -mPEG copolymers, and our PLG- g -mPEG/PB will serve as a promising carrier for hydrophobic anticancer drug delivery. © 2021 Society of Industrial Chemistry.
研究领域:
生物材料
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药物递送
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
APPLIED SURFACE SCIENCE
·
2018
·
IF 4.439
Ang Liu,Huiwen Tian,Weihua Li,Wei Wang,Xiang Gao,Peng Han,Rui Ding
Layered double hydroxides (LDHs) nanocontainers intercalating with corrosion inhibitors are considered as a great platform to deliver corrosion inhibitors to the corroding sites. However, the small interlayer spacing and strong interaction between hydrotalcite laminates and interlayer anions impede the loading of macromolecular species into LDHs via a conventional anion-exchange process. This work devises a new paradigm for the preparation of LDHs in corrosion protection. A new method combining delamination and self-assembly to increase the loading of the organic corrosion inhibitor —5-Methyl-1,3,4-thiadiazole-2-thiol (MTT) into LDHs is applied and exhibits remarkable corrosion protection effects. The SEM, EDS, TEM, XRD, XPS and FT-IR were used to characterize the LDHs and LDH nanosheets. UV–vis absorption spectra and thermogravimetric analysis (TGA) experiments indicate an enhanced loading of MTT which is slowly released to the chloride media. The electrochemical experiments indicate that the release of MTT from their LDHs host can efficiently inhibit the corrosion on the surface of mild steel in 3.5 wt% NaCl solution. Furthermore, surface analysis experiments were carried out to probe into the anticorrosion mechanism of LDHs.
研究领域:
材料科学
·
腐蚀与防护
✓ 已验证
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2019
·
IF 3.973
Huijia Song,Chaofeng Wang,Haipin Zhang,Lu Yao,Junjie Zhang,Ruixia Gao,Xiaoshuang Tang,Tie Chong,Wenpin Liu,Yuhai Tang
To overcome the limited drug loading capacity of magnetic nanopharmaceuticals arising from the relatively large mass of the metal core, a high-loading drug delivery system based on amino-functionalized Fe 3 O 4 magnetic nanospheres modified by hyperbranched phenylboronic acid (HPBA-Fe 3 O 4 ) were prepared for the first time. The obtained nanomaterials were characterized by transmission electron microscopy, Fourier transform infrared, zeta potential, elemental analysis, vibrating sample magnetometry and X-ray diffraction analysis, and the results showed that hyperbranched phenylboronic acid (HPBA) were successfully grafted onto the surface of the magnetic nanospheres. The polymerization conditions, adsorption and desorption performance, and tumor-targeting ability of HPBA-Fe 3 O 4 was investigated in detail through chemical and biological experiments. The drug loading amount and capacity of HPBA-Fe 3 O 4 are 271.3 mg/g and 27.13%, respectively, which are 2.26 and 3.27 times greater than those of PBA-Fe 3 O 4 and PEI-Fe 3 O 4 , and the thermodynamic fitting results further demonstrate the high drug loading ability of HPBA-Fe 3 O 4 . In vitro studies performed in U-87 MG malignant glioma cells and astrocytes via light and fluorescence microscopy analyses, cell counting kit-8 assays, and HPLC tests confirm the pH-sensitive release and tumor-targeted drug delivery capabilities of HPBA-Fe 3 O 4 . The facile fabrication of hyperbranched magnetic nanomaterials could be an alternative solution for designing high-loading, tumor cell-targeting and pH-responsive DDSs with high-mass cores.
研究领域:
生物医学工程
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纳米医学
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
MATERIALS CHEMISTRY AND PHYSICS
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2019
·
IF 2.781
Li-li Lu,Wen-ya Xiong,Jun-bin Ma,Tian-fang Gao,Si-yuan Peng,Wang Xiao
Pores and framework dual responsive controlled release systems with high drug loading capacity based on HMONs (DOX@HMONs/CD) have been prepared. The DOX@HMONs/CD show high loading capacity (1060 mg/g) for anticancer drug. The cumulative release of drug diffusing from pore channels or degraded framework could be tuned by varying the pH or the concentration of dithiothreitol (DTT), and the systems exhibited an obvious enhanced release capacity in the combination of two stimulus.
研究领域:
生物材料学
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药物递送系统
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肿瘤治疗
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）