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JOURNAL OF NANOPARTICLE RESEARCH · 2021 ·Vol. 23 ·期 5 ·1-14 · IF 2.253

Biotin-modified oligochitosan-F127 micelles for honokiol’s encapsulation

Zhu Li,Song Zhimei,Feng Sijia,Xu Hongmei,Chen Shiyu,Feng Runliang

In the study, biotin-modified oligochitosan-F127 conjugate (F127-CS-BIO) was synthesized as a carrier to prepare honokiol-loaded micelles via dialysis method. The encapsulation efficiency and drug loading were 70.79 ± 2.70% and 9.70 ± 0.57%, respectively. The mean particle size and zeta potentials were 210.9 ± 4.65 nm and 12.9 ± 7.22 mV, respectively. In vitro release studies showed that the release of honokiol from the micelles was slow and steady. MTT evaluation and cellular uptake results demonstrated that F127-CS-BIO was more easily absorbed by tumor cells and resulted in low IC 50 value of honokiol due to biotin’s targeting guidance when compared with biotin-unmodified F127-CS. In conclusion, F127-CS-BIO polymer was expected as an effective nanocarrier to encapsulate chemotherapeutic drugs. Graphical abstract

CAS / MDL: 298-93-1
研究领域: 药剂学 · 纳米医学 · 肿瘤学
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International Journal of Nanomedicine · 2017 · IF 4.3

Redox-sensitive Pluronic F127-tocopherol micelles: synthesis, characterization, and cytotoxicity evaluation

Yuling Liu,Sai Fu,Longfei Lin,Yuhong Cao,Xi Xie,Hua Yu,Meiwan Chen,Hui Li

Pluronic F127 (F127), an amphiphilic triblock copolymer, has been shown to have significant potential for drug delivery, as it is able to incorporate hydrophobic drugs and self-assemble into nanosize micelles. However, it suffers from dissociation upon dilution owing to the relatively high critical micelle concentration and lack of stimuli-responsive behavior. Here, we synthesized the α-tocopherol (TOC) modified F127 polymer (F127-SS-TOC) via a redox-sensitive disulfide bond between F127 and TOC, which formed stable micelles at relatively low critical micelle concentration and was sensitive to the intracellular redox environment. The particle size and zeta potential of the F127-SS-TOC micelles were 51.87±6.39 nm and -8.43±2.27 mV, respectively, and little changes in both particle size and zeta potential were observed within 7 days at room temperature. With 10 mM dithiothreitol stimulation, the F127-SS-TOC micelles rapidly dissociated followed by a significant change in size, which demonstrated a high reduction sensitivity of the micelles. In addition, the micelles showed a high hemocompatibility even at a high micelle concentration (1,000 μg/mL). Low cytotoxicity of the F127-SS-TOC micelles at concentrations ranging from 12.5 μg/mL to 200 μg/mL was also found on both Bel 7402 and L02 cells. Overall, our results demonstrated F127-SS-TOC micelles as a stable and safe aqueous formulation with a considerable potential for drug delivery.

CAS / MDL: 1119-62-6
研究领域: 药剂学 · 生物材料学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2019 · IF 2.367

Preparation and evaluation of isoliquiritigenin-loaded F127/P123 polymeric micelles

Yu-Jiao Xie,Qi-Long Wang,Michael Adu-Frimpong,Jian Liu,Kang-Yi Zhang,Xi-Ming Xu,Jiang-Nan Yu

Isoliquiritigenin (ISL) possesses a variety of pharmacological activities amid poor solubility in water which has restricted its clinical application. In this study, isoliquiritigenin-loaded F127/P123 polymeric micelles (ISL-FPM) were successfully prepared and evaluated in vitro and in vivo. The particle size, polydispersity index, and zeta potential of the selected formulation were 20.12 ± 0.72 nm, 0.183 ± 0.046, and −38.31 ± 0.33 mV, respectively, coupled with high encapsulation efficiency of 93.76 ± 0.31%. Drug-loading test showed the solubility of ISL after formulating into micelles was 232 times higher than its intrinsic solubility. Moreover, critical micelle concentration (CMC) was tested with fluorescence probe method and turned out to be quite low, which implied high stability of ISL-FPM. Release profile in HCl (pH 1.2), double distilled water, and PBS (pH 7.4) of ISL-FPM reached over 80%, while free ISL was around 40%. Pharmacokinetic research revealed that formulated ISL-FPM significantly increased bioavailability by nearly 2.23-fold compared to free ISL. According to the results of in vitro antioxidant activity, scavenging DPPH activity of ISL was significantly strengthened when it was loaded into polymeric micelles. Altogether, ISL-FPM can act as a promising approach to improve solubility as well as enhance bioavailability and antioxidant activity of ISL.

研究领域: 药剂学 · 药物化学
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MATERIALS SCIENCE FORUM · 2020 · IF 0

Preparation and Characterization of Oligopeptide/M-Pluronic F127 Composite Membranes

Chuan Jun Xia,Ping Deng Ming,Ya Song Hu,Cong Cong Zhan,An Duo Zhou,He Yi Mao,Xia Huang

In the present study, oligopeptide (TEA) and modified Pluronic F127 (M-Pluronic F127) with different mass fraction composited by intermolecular forces. And the oligopeptide/M-Pluronic F127 composite membranes were prepared and investigated. The structural parameters of the membranes were characterized by fourier transform-infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and differential scanning calorimetry (DSC) measurements. It was found that there had strong interaction between TEA and M-Pluronic F127 and the composite films with different proportions had different surface morphology and thermal stability. The characteristics of the membranes were related to the significant changes of the self-assembly behavior of the TEA modified by M-Pluronic F127.

研究领域: 生物材料学 · 分子生物学
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EUROPEAN POLYMER JOURNAL · 2019 · IF 3.621

Single component Pluronic F127-lipoic acid hydrogels with self-healing and multi-responsive properties

Li Song,Bao Zhang,Ge Gao,Chunsheng Xiao,Gao Li

Herein, Pluronic F127 (PEO 99 -PPO 65 -PEO 99 ) end functionalized with α-lipoic acid (LA) (F127-LA) was synthesized and used for preparation of “single-component, multi-responsive” hydrogels through the photo cross-linking of LA components. The F127-LA hydrogels not only possessed thermo- and reduction- double responsiveness, but also demonstrated self-healing properties under UV irradiation due to the existence of dynamic disulfide bonds. The rheological and mechanical properties of the hydrogels can be adjusted by their concentration. The F127-LA hydrogels presented a swelling ratio decrease from 25 °C to 37 °C due to a lower critical solution temperature (LCST)-type thermo-responsive volume phase transition. The bovine serum albumin (BSA) was loaded into F127-LA hydrogels, and their drug release behavior can be regulated by surrounding temperature and reducing agent concentration. The volume shrinkage of the hydrogels promoted the sustained release of BSA above volume phase transition temperature. Cytocompatibility assay of L929 mouse fibroblasts showed that cellular metabolic activity were merely affected by F127-LA, even at concentrations up to 1000 mg L −1 . This study thus provided a very promising route for the preparation of multifunctional hydrogels.

CAS / MDL: 1122-58-3
研究领域: 材料科学 · 生物医学工程 · 药物递送
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JOURNAL OF NANOPARTICLE RESEARCH · 2018 ·Vol. 20 ·期 10 ·1-11 · IF 2.127

Pluronic F127-cyclodextrin conjugate micelles for encapsulation of honokiol

Feng Runliang,Deng Peizong,Zhou Feilong,Feng Sijia,Song Zhimei

To overcome honokiol’s poor water solubility and investigate its antifungal activity and pharmacokinetic property, Pluronic® F-127 (F127)-cyclodextrin conjugate was synthesized and employed to prepare honokiol-loaded micelles through emulsion-solvent evaporation method. The drug-loaded micelles were obtained with 92.30 ± 3.28% of encapsulation efficiency being higher than that obtained from F127 due to additional cyclodextrin inclusion. Fourier transformation infrared spectrometry and diffraction scanning calorimetry analysis tests demonstrated that honokiol was successfully encapsulated into the conjugate micelles in the amorphous or solid solution state because of their interactions. Meanwhile, in vitro antifungal activity experiment indicated that the MIC 90 of drug-loaded micelles was 64 μg/mL, showing the same antifungal activity as pure honokiol although it obviously retarded honokiol’s release. In vivo pharmacokinetic results confirmed that in vivo area under curve and apparent distribution volume of honokiol in drug-loaded micelles were 2- and 1.69-folds higher than that for pure honokiol, with its obvious prolonged mean retention time and half-life period, respectively. The clearance rate of honokiol was also shortened about 2-fold in comparison with pure honokiol when encapsulated into the micelles. These results suggest that the developed F127-cyclodextrin micellar formulation is a promising drug delivery system for antifungal drugs. ᅟ

CAS / MDL: 106-95-6 111689-03-3
研究领域: 药剂学 · 生物医学 · 药物递送系统
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RSC Advances · 2017 ·Vol. 7 ·期 74 ·47091-47098 · IF 3.108

Preparation, characterization and anticancer activities of resveratrol loaded redox-sensitive F127-SS-TOC micelles

Yuling Liu,Longfei Lin,Jizheng Song,Ye Zhao,Zhimao Chao,Hui Li

Resveratrol (RES), a natural polyphenolic compound existing in plants, exhibits anticancer potential in inhibiting growth of various types of human cancers especially breast cancer. However, the poor aqueous solubility and low bioavailability limit its clinical application. Pluronic F127 (F127)-SS-Tocopherol (TOC) polymer is a redox-sensitive conjugate which has been synthesized by our previous study. Due to the amphiphilic properties of block copolymer F127-SS-TOC, RES was encapsulated by the F127-SS-TOC polymer and formed RES-loaded micelles (F127-SS-TOC/RES) in aqueous solution by self-assembly via a solvent evaporation method. The drug loading of F127-SS-TOC/RES micelles was 13.25 ± 2.29%, which remained stable for 7 days at 25 °C. The particle size and zeta potential of the above-mentioned micelles measured by dynamic light scattering (DLS) were 39.50 ± 1.39 nm and −4.55 ± 0.39 mV, respectively. Besides, F127-SS-TOC/RES micelles have significant cytotoxicity in human breast cancer cells MCF-7 and MDA-MB-231 compared to free RES and non-redox-sensitive F127-TOC/RES micelles. The results also showed that redox-sensitive F127-SS-TOC/RES micelles could induce apoptosis and elevate the intracellular reactive oxygen species (ROS) level against MDA-MB-231 cells. Hence, our results indicated that RES loaded F127-SS-TOC micelles hold potential in improving the treatment of breast cancer.

研究领域: 药剂学 · 肿瘤学 · 生物材料学
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Frontiers in Bioengineering and Biotechnology · 2021 · IF 5.89

Pluronic F127-Modified Electrospun Fibrous Meshes for Synergistic Combination Chemotherapy of Colon Cancer

Xie Dengchao,Ma Panpan,Ding Xin,Yang Xiao,Duan Lian,Xiao Bo,Yi Shixiong

Colon cancer ranks as the third most common malignancy in the world. Combination chemotherapy, resorting to electrospun fibrous technology, has been considered as a promising strategy to exert synergistic effects in colon cancer treatment. Herein, we manufactured various pluronic F127 (PF127)-modified electrospun fibrous meshes with different weight ratios of camptothecin (CPT) and curcumin (CUR). The fluorescence characterization of the obtained PF127-CPT-meshes, PF127-CUR-meshes, and PF127-CPT/CUR-meshes (2:1) showed that CPT and CUR were evenly distributed within individual fibers of these meshes. Drug release experiments revealed that both types of drugs could be released from fibrous meshes simultaneously and sustainably. Importantly, these meshes exhibited strong in vitro anti-colon cancer activities, compared with the control meshes without drugs. Moreover, the combination index values of the PF127-CPT/CUR-meshes (CPT/CUR weight ratio = 5:1, 3:1, or 2:1) were <0.5 after incubation for respective 24 and 36 h, indicating the synergistic anti-colon cancer effects of CPT and CUR in fibrous meshes. Collectively, these results demonstrate that PF127-CPT/CUR-meshes can be developed as an efficient implantable system for effective synergistic treatment of colon cancer.

研究领域: 肿瘤学 · 药剂学 · 生物材料学
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

Cadmium removal from rice protein via synergistic treatment of rhamnolipids and F127/PAA hydrogels

Chong Shen,Shi Tang,Qin Meng

Heavy metal ions can accumulate in the area’s crop harvest, such as rice, via a tight binding with protein. Such binding paves great difficulties to remove heavy metal ions. This study aims to remove cadmium from contaminated rice protein using rhamnolipid biosurfactant together with Pluronic F127/poly (acrylic acid) (i.e., F127/PAA) hydrogels. The two-step consequential washing removed 92% of cadmium in rice protein, making the residual cadmium content below the safety level (<0.2 mg/kg) without impairing the main components and structure of rice protein. Interestingly, the washing by either rhamnolipids or hydrogels failed to effectively remove cadmium, indicating the synergistic effect of the two materials. Mechanistically, rhamnolipids with higher Cd 2+ binding constant compete with protein on binding with cadmium and then deliver it to F127/PAA hydrogels that present highest Cd 2+ adsorptive capability for immobilization. In considering that the F127/PAA hydrogels are reusable, this treatment is low-cost, safe and effective for removal of cadmium from polluted rice products.

CAS / MDL: 10022-68-1
研究领域: 环境科学 · 食品科学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF MICROENCAPSULATION · 2020 · IF 2.287

Novel folated pluronic F127 modified liposomes for delivery of curcumin: preparation, release, and cytotoxicity

Ziling Li,Xiangyuan Xiong,Shengfeng Peng,Xing Chen,Wei Liu,Chengmei Liu

Aim: A novel folated pluronic F127 (FA-F127) was synthesised, so as to modify liposomes with FA group on the surface, and evaluate the effects of FA-F127 modification on the properties of the modified liposomes.Methods: FA was linked to one end of pluronic F127, via the terminal OH group, to obtain FA-F127 and the structure was characterised. FA-F127 modified curcumin liposomes (cur-FA-F127-Lps) were prepared. The physicochemical characteristics of cur-FA-F127-Lps, including morphology and particle size, were studied. The in vitro cytotoxicity of cur-FA-F127-Lps against KB cancer cells was determined by MTT tests.Results: The effects of FA-F127 modification on the average particle size, PDI, curcumin encapsulation efficiency and microstructure were not significant. Compared with nonfolated F127 liposomes (cur-F127-Lps), cur-FA-F127-Lps exhibited significantly higher cytotoxicity towards KB cells.Conclusions: Folic acid modified liposomes provide a novel strategy to improve the chemotherapeutic efficacy of hydrophobic bioactive compounds.

CAS / MDL: 458-37-7
研究领域: 药剂学 · 药物递送系统 · 纳米技术 · 肿瘤学
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JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY · 2020 · IF 1.701

Liposomes consisting of pluronic F127 and phospholipid: Effect of matrix on morphology, stability and curcumin delivery

Ziling Li,Yousheng Huang,Shengfeng Peng,Xing Chen,Liqiang Zou,Wei Liu,Chengmei Liu

We prepared liposomes consisting of different ratios of phospholipid and pluronic F127 (F127-Lps), then evaluated the effect of matrix on the morphology, stability and carriers’ property of liposomes. The particle size of liposomes was significantly decreased after pluronic F127 modification. Pluronic F127 at low ratio may incorporate into liposomes and form spherical and lamellar structure, while pluronic F127 at high ratio can form mixed aggregates with spherical micelles and lamellar vesicles. The membrane stability of liposomes was enhanced with increasing of pluronic F127 ratio. Curcumin was encapsulated into F127-Lps (cur-F127-Lps) with an entrapment efficiency of 89%. The higher the ratio of pluronic F127 was, the slower the release rate of curcumin. First order model was the main release mechanism for curcumin loaded liposomes. These results are useful for designing liposome-based food delivery systems that can be used in functional foods.

CAS / MDL: 458-37-7
研究领域: 食品科学 · 药剂学
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RSC Advances · 2020 ·Vol. 10 ·期 41 ·24507-24514 · IF 3.119

Dual responsive oligo(lysine)-modified Pluronic F127 hydrogels for drug release of 5-fluorouracil

Peihong Li,Xueyan Dai,Lijie Qu,Yanlong Sui,Chunling Zhang

Peptide-containing hydrogels have become a research hotspot due to their unique secondary structure and biocompatibility. Herein, we used amino-terminated F127 as a macroinitiator to initiate the ring-opening polymerization of L-lysine(z)-NCA, and the obtained oligo(lysine)-modified F127 (FL) had degrees of polymerization of lysine of 2, 5, and 8. The results showed that the FL hydrogels had reversible temperature-dependent sol–gel transitions, and the introduction of lysine increased the critical gel temperature. In the dilute solution of FL, the micelle size increased and aggregated as the pH increased; the micelle grew into a rod-like shape under alkaline conditions. Scanning electron micrographs showed that the interior of the FL hydrogel had a more complete porous structure. The FL-2 hydrogel loaded with 5-fluorouracil exhibited an approximately linear release trend within 12 h and has good biocompatibility. Therefore, FL hydrogels have potential applications in the field of biomedicine.

研究领域: 生物材料 · 药剂学 · 高分子化学
✓ 已验证 DOI PubMed 高影响因子
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