Regenerative Biomaterials
·
2021
·Vol. 8
·期 2
·
IF 6.353
Li Yue,Leng QingQing,Pang XianLun,Shi Huan,Liu YanLin,Xiao SuSu,Zhao Ling,Zhou Ping,Fu ShaoZhi
Dermal injury, including trauma, surgical incisions, and burns, remain the most prevalent socio-economical health care issue in the clinic. Nanomedicine represents a reliable administration strategy that can promote the healing of skin lesions, but the lack of effective drug delivery methods can limit its effectiveness. In this study, we developed a novel nano-drug delivery system to treat skin defects through spraying. We prepared curcumin-loaded chitosan nanoparticles modified with epidermal growth factor (EGF) to develop an aqueous EGF-modified spray (EGF@CCN) for the treatment of dermal wounds. In vitro assays showed that the EGF@CCN displayed low cytotoxicity, and that curcumin was continuously and slowly released from the EGF@CCN. In vivo efficacy on wound healing was then evaluated using full-thickness dermal defect models in Wistar rats, showing that the EGF@CCN had significant advantages in promoting wound healing. On day 12 post-operation, skin defects in the rats of the EGF@CCN group were almost completely restored. These effects were related to the activity of curcumin and EGF on skin healing, and the high compatibility of the nano formulation. We therefore conclude that the prepared nano-scaled EGF@CCN spray represents a promising strategy for the treatment of dermal wounds.
研究领域:
药学
·
纳米技术
·
伤口愈合
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2012
·
IF 3.628
Jinsong Liu,Lihua Xu,Chuantong Liu,Dafeng Zhang,Siqian Wang,Zhennan Deng,Weiwei Lou,Haihong Xu,Qing Bai,Jianfeng Ma
In the present paper, cationic nanoparticles of curcumin, chitosan and poly(ɛ-caprolactone) were developed by a simple nano-precipitation method. The developed curcumin loaded chitosan/poly(ɛ-caprolactone) (chitosan/PCL) nanoparticle showed almost spherical shape and its diameter was varied between 220 nm and 360 nm and zeta potential was varied between +30 mV and 0 mV as a function with pH value. The encapsulation of curcumin into nanoparticles was confirmed by fluorescence spectral analysis. In vitro release study showed the sustained release behavior of curcumin from nanoparticles during the period of 5 days study. In vitro cytotoxicity test revealed the drug concentration dependent on the cell viability against Hela cells and OCM-1 cells after 48 h co-incubation. Furthermore, in vitro cell uptake study revealed that the cell uptake of curcumin was greatly enhanced by encapsulated curcumin into cationic chitosan/PCL nanoparticles. Therefore, the developed cationic chitosan/PCL nanoparticles might be a promising candidate for curcumin delivery to cancer cells.
研究领域:
药剂学
·
生物医学工程
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2015
·
IF 2.858
Ming Ying,Fengwen Huang,Haidong Ye,Hong Xu,Liangliang Shen,Tianwen Huan,Shitong Huang,Jiangfeng Xie,Shengli Tian,Zhangli Hu,Zhendan He,Jun Lu,Kai Zhou
The interaction between curcumin and pepsin was investigated by fluorescence, synchronous fluorescence, UV–vis absorption, circular dichroism (CD), and molecular docking. Under physiological pH value in stomach, the fluorescence of pepsin can be quenched effectively by curcumin via a combined quenching process. Binding constant ( K a ) and binding site number ( n ) of curcumin to pepsin were obtained. According to the theory of Förster's non-radiation energy transfer, the distance r between pepsin and curcumin was found to be 2.45 nm within the curcumin–pepsin complex, which implies that the energy transfer occurs between curcumin and pepsin, leading to the quenching of pepsin fluorescence. Fluorescence experiments also suggest that curcumin is located more closely to tryptophan residues than tyrosine residues. CD spectra together with UV–vis absorbance studies show that binding of curcumin to pepsin results in the extension of peptide strands of pepsin with loss of some β-sheet structures. Thermodynamic parameters calculated from the binding constants at different temperatures reveal that hydrophobic force plays a major role in stabilizing the curcumin–pepsin complex. In addition, docking results support the above experimental findings and suggest the possible hydrogen bonds of curcumin with Thr-77, Thr-218, and Glu-287 of pepsin, which help further stabilize the curcumin–pepsin complex.
研究领域:
生物化学
·
药物化学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Regenerative Biomaterials
·
2015
·Vol. 2
·期 2
·97-105
·
IF 0
Li Xiaomeng,Qin Jinli,Ma Jun
A silk fibroin/poly (vinyl alcohol) porous scaffold with a water vapor transmission rate of 2125 ± 464 g/m2/day has been developed via thermally induced phase separation (gelation) and freeze-drying process. A hierarchical architecture of micropores and nanofibers was observed inside the scaffolds, and the related structures were analyzed. The viability and proliferation of 3T3 fibroblasts were examined, which indicated that the scaffolds exerted low cytotoxicity. After loading curcumin, the scaffolds can suppress the growth of 3T3 fibroblasts. The release behavior of curcumin from the scaffolds was investigated. At pH = 7.2, the release profiles showed no significant difference for the loading amounts of 0.5 mg and 0.25 mg per sample. Meanwhile, the cumulative amount of released drug at pH = 5.7 was significantly more than that in neutral solution due to more degradation of the scaffolds. It was suggested that the silk fibroin/poly (vinyl alcohol) blend scaffolds could be potentially used as wound dressing materials.
研究领域:
生物材料学
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
RSC Advances
·
2014
·Vol. 4
·期 103
·59211-59217
·
IF 3.708
Qiyu Huang,Lili Zhang,Xiaoyi Sun,Ke Zeng,Juan Li,You-Nian Liu
In this work, carboxymethyl dextran (CMD), a polysaccharidic dextran derivative with well-known biocompatibility and biodegradability, was used to modify curcumin-loaded liposomes for improving the anticancer efficacy of curcumin. The CMDylated curcumin-loaded liposomes (CMD-Cur-Lip) were successfully prepared and characterized in comparison with unmodified and two PEGylated curcumin-loaded liposomes. The results showed that: (1) the encapsulation efficiency of curcumin in the liposomes was improved after being modified with CMD; (2) all the curcumin-loaded liposomes displayed controlled release characteristics; (3) the CMD-Cur-Lip demonstrated improved cell cytotoxicity against cancer cells, as compared to other liposomal formulations and free curcumin; (4) CMD-Cur-Lip exhibited the highest cellular uptake as compared to other liposomal formulations.
研究领域:
药学
·
肿瘤学
·
纳米技术
✓ 已验证
产品关联
DOI
高影响因子
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
·
2018
·Vol. 34
·期 2
·203-211
·
IF 1.248
Song Shengmei,Li Minglu,Gong Xiaojuan,Han Hui,Zhou Yehong,Wang Li,Shuang Shaomin,Dong Chuan
In the paper, folic acid(FA)-mediated and β -cyclodextrin( β -CD) derivatives functionalized magnetic Fe 3 O 4 nanoparticles(MNPs) were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticancer drug. FA-sulfobutyl ether- β -CD-MNPs(FA-SBE- β -CD-MNPs), FA-hydroxypropyl- β -CD-MNPs(FA-HP- β -CD-MNPs) and FA-carboxymethyl- β -CD-MNPs(FA-CM- β -CD-MNPs) were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE- β -CD-MNPs, 9.6 mg/g, 81.63% for FA-HP- β -CD-MNPs and 7.88 mg/g, 85.28% for FA-CM- β -CD-MNPs, respectively. Meanwhile, at pH=5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE- β -CD-MNPs in 5 h. Cellular uptake indicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE- β -CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE- β -CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.
研究领域:
药剂学
·
生物医学工程
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2018
·
IF 3.862
Lijun Hu,Min Li,Zhipeng Zhang,Yuanyuan Shen,Shengrong Guo
Paclitaxel (PTX), one of the most potent anticancer agents , has showed a remarkable activity against varieties of tumors. However, the bioavailability of PTX is quite low due to its poor aqueous solubility. Moreover, the emerging multidrug resistance (MDR) in cancer to PTX remains a major obstacle for successful chemotherapy. In order to address these problems, we developed self-assembly of biotinylated poly(ethylene glycol)-poly(curcumin) (Biotin-PEG-PCDA) for PTX delivery (termed as PTX-BPC NPs) with the application of mPEG 2K -P(CL-co-LLA) as an emulsifier . The loading content and encapsulation efficiency of PTX were 13.2% and 92.0%, respectively. In vitro drug release study showed that PTX-BPC NPs could degrade rapidly and then release the PTX payload in a 10 mM glutathione (GSH) environment. Compared with free PTX, PTX-BPC NPs exhibited enhanced anticancer efficacy (IC 50(MCF-7/ADR cells) , 17.28 µg/mL vs. 1.15 µg/mL). In addition, these biotin-modified nanoparticles could also significantly reverse PTX resistance by suppressing the over-expression of P-gp, thus resulting in increased intracellular drug accumulation and reduced drug efflux in MCF-7/ADR cells, which showed a great anticancer effect.
研究领域:
药学
·
纳米技术
·
癌症研究
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CELLULAR PHYSIOLOGY AND BIOCHEMISTRY
·
2017
·Vol. 44
·期 2
·618-633
·
IF 5.104
Qi Zhangyang,Wu Meihao,Fu Yun,Huang Tengfei,Wang Tingting,Sun Yanjie,Feng Zhibo,Li Changzheng
Background/Aims: The generation of reactive oxygen species (ROS) caused by amyloid-β (Aβ) is considered to be one of mechanisms underlying the development of Alzheimer’s disease. Curcumin can attenuate Aβ-induced neurotoxicity through ROS scavenging, but the protective effect of intracellular curcumin on neurocyte membranes against extracellular Aβ may be compromised. To address this issue, we synthesized a palmitic acid curcumin ester (P-curcumin) which can be cultivated on the cell membrane and investigated the neuroprotective effect of P-curcumin and its interaction with Aβ. Methods: P-curcumin was prepared through chemical synthesis. Its structure was determined via nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). An MTT assay was used to assess Aβ cytotoxicity and the protective effect of P-curcumin on SH-SY5Y cells. The effect of P-curcumin on Aβ-induced ROS production in vitro and in vivo were assessed based on changes in dichlorofluorescein (DCF) fluorescence. A spectrophotometric method was employed to detect lipid peroxidation. To mimic the interaction of P-curcumin on cell membranes with Aβ, liposomes were prepared by thin film method. Finally, the interactions between free P-curcumin and P-curcumin cultivated on liposomes and Aβ were determined via spectrophotometry. Results: A novel derivative, palmitic acid curcumin ester was prepared and characterized. This curcumin, cultivated on the membranes of neurocytes, may prevent Aβ-mediated ROS production and may inhibit the direct interaction between Aβ and the cellular membrane. Furthermore, P-curcumin could scavenge Aβ-mediated ROS as curcumin in vitro and in vivo, and had the potential to prevent lipid peroxidation. Morphological analyses showed that P-curcumin was better than curcumin at protecting cell shape. To examine P-curcumin’s ability to attenuate direct interaction between Aβ and cell membranes, the binding affinity of Aβ to curcumin and P-curcumin was determined. The association constants for free P-curcumin and curcumin were 7.66 × 104 M-1 and 7.61 × 105 M-1, respectively. In the liposome-trapped state, the association constants were 3.71 × 105 M-1 for P-curcumin and 1.44× 106 M-1 for curcumin. With this data, the thermodynamic constants of P-curcumin association with soluble Aβ (ΔH, ΔS, and ΔG) were also determined. Conclusion: Cultivated curcumin weakened the direct interaction between Aβ and cell membranes and showed greater neuroprotective effects against Aβ insult than free curcumin
研究领域:
神经科学
·
药理学
·
生物化学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2021
·
IF 7.514
Xueyan Hou,Jinying Liang,Xue Yang,Jintao Bai,Mingbo Yang,Ning Qiao,Zilong Hu,Xiqing Yan,Yongli Shi
Curcumin (CUR) is a food additive approved by World Health Organization. But the shortcomings, such as poor water solubility, easy oxidation and degradation, limit its application. In this study, the CUR-loaded poloxamer 188 -based nanoparticles (CUR/PTT NPs) were fabricated to improve the stability and water solubility of CUR . Studies found the spherical CUR/PTT NPs had an average size of 98.71 ± 0.64 nm. Stability experiments displayed CUR/PTT NPs were extremely stable in different conditions. XRD analysis indicated the changes of crystal structures of CUR might be the main cause of the improved water solubility. Reducing power and anti-degradation tests suggested CUR/PTT NPs could improve the anti-oxidation and anti-degradation of CUR. Additionally, the results of body weight gains, hematological examination, organ coefficients, hematoxylin and eosin staining demonstrated CUR/PTT NPs bearing the excellent in vivo bio-security. Therefore, this study may provide a new idea for the combination of food industry and nanoparticles.
研究领域:
食品科学
·
纳米技术
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Bioengineering and Biotechnology
·
2022
·
IF 6.064
Jiang Mingyue,Chen Le,Chen Bo,Yu Qinghua,Zhang Xianming,Jing Weihong,Ma Limei,Deng Tao,Yang Zhangyou,Yu Chao
Curcumin (CUR) is a natural bioactive compound that has attracted attention as a “golden molecule” due to its therapeutic properties against several types of tumors. Nonetheless, the antitumor application of CUR is hampered due to its extremely low aqueous solubility and chemical instability. Herein, a novel type of CUR-loaded polymeric micelles with intracellular K+-responsive controlled-release properties is designed and developed. The polymeric micelles are self-assembled by poly (N-isopropylacrylamide-co-acryloylamidobenzo-15-crown-5-co-N, N-dimethylacrylamide)-b-DSPE (PNDB-b-DSPE) block copolymers, and CUR. CUR is successfully loaded into the micelles with a CUR loading content of 6.26 wt%. The proposed CUR-PNDB-DSPE polymeric micelles exhibit a significant CUR release in simulated intracellular fluid due to the formation of 2 : 1 ‘‘sandwich’’ host–guest complexes of 15-crown-5 and K+, which lead to the hydrophilic outer shell of micelles to collapse and the drug to rapidly migrate out of the micelles. In vitro, the B16F10 cell experiment indicates that CUR-PNDB-DSPE micelles exhibit a high cellular uptake and excellent intracellular drug release in response to the intracellular K+ concentration. Moreover, CUR-PNDB-DSPE micelles show high cytotoxicity to B16F10 cells compared to free CUR and CUR-PEG-DSPE micelles. The polymeric micelles with intracellular K+-responsive controlled release properties proposed in this study provide a new strategy for designing novel targeted drug delivery systems for CUR delivery for cancer treatment.
研究领域:
药学
·
纳米技术
·
癌症研究
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
·
2022
·
IF 3.784
Jiawei Han,Yuanfeng Wei,Luyuan Li,Yutong Song,Zunting Pang,Shuai Qian,Jianjun Zhang,Yuan Gao,Weili Heng
In the previous study, the development of amorphous curcumin (CUR) aimed to enhance the solubility/dissolution of CUR by disrupting its crystal lattice, but it unexpectedly showed a decreased dissolution than its crystalline counterpart on account of gel formation in its dissolution process. Whether such gelation could be eliminated by co-amorphous strategy was answered in this study. Herein, CUR by co-amorphization with chlorogenic acid (CHA) was successfully prepared using quench cooling. The formed co-amorphous material (namely CUR-CHA CM) eliminated the gelation and hence performed superior dissolution performance than crystalline/amorphous CUR. Meanwhile, it exhibited higher physical stability than amorphous CUR during dissolution as well as under long-term/accelerated conditions. To further study the such enhancement mechanism, the internal molecular interactions were investigated for CUR-CHA CM in the solid state as well as in aqueous solution. FTIR and solid-state 13 C NMR spectra confirmed that intermolecular hydrogen bonds formed between CUR and CHA after co-amorphization. Furthermore, the nucleation of CUR was significantly inhibited by CHA in an aqueous solution, thus maintaining the supersaturated dissolution for a long time. The present study offers a feasible strategy to eliminate gelation and enhance stability of amorphous solids by co-amorphization and crystallization inhibition.
研究领域:
药剂学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2021
·
IF 4.384
Jiawei Han,Luyuan Li,Zunting Pang,Meiling Su,Xiaoshuang He,Shuai Qian,Jianjun Zhang,Yuan Gao,Yuanfeng Wei
Amorphous curcumin (CUR) exhibited a decreased dissolution rate in comparison with the crystalline counterpart due to its gel formation during dissolution. The main purpose of the present study is to explore the mechanism of such gelation phenomenon. It was found that the dissolution of amorphous CUR and gel properties were influenced by the temperature and pH of the media. The formed gels were characterized by TPA, SEM, DSC, XRPD, FTIR and PLM. The results indicated that the gelation process led to the formation of a porous structure in which water molecules infiltrate, and entered into its supercooled liquid state with high viscosity when contacting aqueous media, accompanied by decreased T g and crystalline transformation. In addition, mixing with hydrophilic excipients (such as hydrophilic silica) accelerated the gel formation of amorphous CUR, while the addition of hydrophobic excipients (such as hydrophobic silica and magnesium stearate) could effectively weaken and even eliminate the gelation, hence significantly improving its dissolution. Furthermore, according to contact angle measurement and fluorescence microscope observation, hydrophilic excipients were found to be able to accelerate water entering into the interior of amorphous CUR, hence facilitating the gelation, while hydrophobic excipients would hinder water infiltration into the powder and thus achieve degelation. In conclusion, it is important to recognize that the gelation potential of some amorphous materials should be considered in developing robust amorphous drug product of high quality and performance.
研究领域:
药剂学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）