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Poloxamer
Pharmaceutics · 2020 ·Vol. 12 ·期 6 ·574 · IF 4.421

Controlled Delivery of Insulin-like Growth Factor-1 from Bioactive Glass-Incorporated Alginate-Poloxamer/Silk Fibroin Hydrogels

Qing Min,Xiaofeng Yu,Jiaoyan Liu,Yuchen Zhang,Ying Wan,Jiliang Wu

Thermosensitive alginate–poloxamer (ALG–POL) copolymer with an optimal POL content was synthesized, and it was used to combine with silk fibroin (SF) for building ALG–POL/SF hydrogels with dual network structure. Mesoporous bioactive glass (BG) nanoparticles (NPs) with a high level of mesoporosity and large pore size were prepared and they were employed as a vehicle for loading insulin-like growth factor-1 (IGF-1). IGF-1-loaded BG NPs were embedded into ALG–POL/SF hydrogels to achieve the controlled delivery of IGF-1. The resulting IGF-1-loaded BG/ALG–POL/SF gels were found to be injectable with their sol-gel transition near physiological temperature and pH. Rheological measurements showed that BG/ALG–POL/SF gels had their elastic modulus higher than 5kPa with large ratio of elastic modulus to viscous modulus, indicative of their mechanically strong features. The dry BG/ALG–POL/SF gels were seen to be highly porous with well-interconnected pore characteristics. The gels loaded with varied amounts of IGF-1 showed abilities to administer IGF-1 release in approximately linear manners for a few weeks while effectively preserving the bioactivity of encapsulated IGF-1. Results suggest that such constructed BG/ALG–POL/SF gels can function as a promising injectable biomaterial for bone tissue engineering applications.Keywords:alginate–poloxamer copolymer;silk fibroin;dual network hydrogel;mesoporous bioactive glass;insulin-like growth factor-1

研究领域: 材料科学 · 生物医学工程 · 组织工程 · 药物递送系统
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2019 · IF 4.784

The utilization of low molecular weight heparin-poloxamer associated Laponite nanoplatform for safe and efficient tumor therapy

Jinyu Li,Hao Pan,Sen Qiao,Yunjian Li,Jie Wang,Wei Liu,Weisan Pan

In the present investigation, we have synthesized the dalteparin which is a kind of low molecular weight heparin (LMWH) and possess the antitumor and antiangiogenic efficacy with carboxylates poloxamer 407 to form a heparin-poloxamer nanogel (HP copolymer). The complex HP is capable of enhancing the efficacies, minimizing the side effects of dalteparin and exhibiting a good thermosensitivity. Therewith, the synthetic Laponite RDS (LR) nanosilicate embarked with doxorubicin (DOX) at a satisfactory high drug entrapment efficiency was integrated with the complex HP and thus constituted a newfangled biocompatible injectable temperature-sensitive hydrogel. To our delight, consociation with 2.5 w/v % of LR nanodisks, HP at the concentration of 5 w/v % was sufficient to execute the solution-gel transition at animal heat, while 17.5 w/v % of P-407 was needed for fabricating the LR-P hydrogel. Simultaneously, LR-HP possesses a more preferable syringeability. Furthermore, the release behavior in vitro for the DOX@LR-HP demonstrated as extended and controlled manner, wherein, the drug-eluting profile was regulated by the LR nanocomposites. Moreover, based on synergic action of heparin and drug, DOX@LR-HP hydrogels demonstrated the best antitumor efficacy in vitro and in vivo. What is noteworthy is that through the course of treatment, the reflected anticancer efficacy direct at the established xenograft S180 sarcoma tumor was provided by the single administration of the DOX@LR-HP hybrid gel. This excellent long-term sustainable-anticancer function in vivo demonstrating the prospect of this nanohybrid-gel combination as an estimable focal drug delivery vehicle for treatment of cancer.

CAS / MDL: 25316-40-9 25952-53-8
研究领域: 药学 · 生物材料 · 肿瘤学
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CHEMICO-BIOLOGICAL INTERACTIONS · 2023 · IF 5.1

A novel self-assembled nanoplatform based on retrofitting poloxamer 188 for triple-negative breast cancer targeting treatment

Xueyan Hou,Yalin Guan,Sisi He,Zeqing Wu,Jintao Bai,Jingjing Xu,Jingwen Wang,Suyue Xu,Huiqing Zhu,Yanyan Yin,Xue Yang,Yongli Shi

Poloxamer 188 is a widely used pharmaceutical excipient, which can be found in a variety of drug formulations. In this study, a novel self-assembled nanoplatform was developed for active targeting of folate receptor-overexpressing triple-negative breast cancer. This platform, FPP NPs, was prepared by the retrofitted poloxamer 188 derivatives, resulting in nanoparticles with an appropriate size (< 100 nm), good stability, and satisfactory biocompatibility. Cellular uptake and in vivo distribution studies showed that the FPP NPs had strong tumor cell uptake and active targeting capabilities. Furthermore, docetaxel (DTX) was loaded into FPP NPs in this research. The resulting DTX/FPP NPs exhibited high drug encapsulation efficiency and drug loading capacity, and could rapidly release DTX under slightly acidic conditions, significantly increasing the antitumor activity of the encapsulated drug both in vitro and in vivo. In addition, DTX/FPP NPs could significantly decrease the hepatotoxicity and nephrotoxicity of DTX. Therefore, this drug delivery nanoplatform, based on retrofitted poloxamer 188 with self-assembly properties in aqueous solution and active targeting capabilities to tumors, may provide a promising approach for targeted treatment of triple-negative breast cancer.

研究领域: 药学 · 纳米技术 · 癌症研究 · 药物递送系统
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2023 · IF 5

A novel boronate-linked polydopamine-poloxamer 407 loaded zinc phthalocyanine nanoparticles for photothermal and photodynamic synergy therapy

Dan Ma,Hai Zhang,Mao Zhao,An-ru Liao,Qian-rong Peng,Wen-wen Jiang,Min Yang

Combination therapy and the drug delivery in response to the tumor microenvironment can effectively improve the efficacy of anticancer therapy. Polymeric nanoparticles can increase the solubility of water-insoluble drugs and have been evaluated as carriers for anti-cancer drugs in several clinical trials . In this paper, zinc phthalocyanine-encapsulated with a boronate-linked polydopamine-poloxamers 407 nanoparticles were developed for pH response and reactive oxygen species (ROS) response release, as well as synergistic photothermal and photodynamic effects. These nanoparticles exhibited a favorable size of 75.02 ± 1.12  nm , stability within 28 days, pH and ROS release up to 57.29% within 84 h, and 73.5% inhibition of A549 cells at a concentration of 5 μg/mL. Overall, our work provides an effective strategy for the encapsulation of hydrophobic photosensitizers , combined PDT and PTT therapy.

研究领域: 纳米技术 · 癌症治疗 · 药物递送系统 · 生物医学工程
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2025 · IF 5.2

Thermosensitive-based synergistic antibacterial effects of novel LL37@ZPF-2 loaded poloxamer hydrogel for infected skin wound healing

Zixuan Wang,Yingxiao Sun,Peijie Dong,Jinhu Wang,Lijie Wang,Aili Zhao,Guangmin Qu,Hang Li,Kannapathirage Dilini Maheshika Gunarathne,Wen Zhang,Yao Chen,Xin Meng

Trauma healing is the process of healing after the body has been subjected to an external force and the skin and other tissues have become dissected or defective, showing the synergistic effect of various processes. Therefore, the investigation of innovative wound dressings has significant research and clinical implications. In this study, we constructed a zinc based metal–organic framework (MOF) and loaded with antimicrobial peptide LL37 to prepare LL37@ZPF-2 (ZPF = zeolite pyrimidine backbone), which was subsequently integrated with Poloxamer 407 to fabricate LL37@ZPF-2 thermosensitive hydrogel. Our study showed that in-situ packaging method can achieve encapsulation rate of 98 % and 15 % of drug loading for LL37. LL37@ZPF-2 demonstrated a higher inhibitory potency against S.aureus compared to E.coli . The Poloxamer 407-gel exhibits thermo-responsive sol–to–gel phase transition behaviors with a phase transition temperature (Tsol/gel) of ∼ 28.01℃, making it an appropriate material for wound healing. The composite hydrogel has excellent biocompatibility and hemocompatibility. A full-thickness skin defect model was built to confirm that LL37@ZPF-2 thermosensitive hydrogel dressing could inhibit bacterial growth, reduce the risk of wound infection, and stimulate angiogenesis and collagen deposition, resulting in a wound healing rate of 94.4 % on day 7 and complete healing on day 10. Our findings demonstrate that the novel thermosensitive LL37@ZPF-2 hydrogel confers good antibacterial activity, promoting cell migration and infected-wound healing properties, providing a promising platform for wound healing.

研究领域: 生物医学工程 · 药剂学 · 伤口愈合 · 抗菌研究 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF MATERIALS RESEARCH · 2022 ·Vol. 38 ·期 2 ·337-349 · IF 2.909

Assembling drug-loaded-layered double hydroxide nanohybrids with poloxamer 188 for improved cellular uptake and in vitro efficacy

Ren Jin,Liang Liang,Yang Yongqing,Liu Xiang,Li Weidong,Liu Wenbo,Wang Yali,Yu Jingmou

Layered Double Hydroxide (LDHs) requires surface functionalization to achieve desirable colloidal and biological stability for effective drug delivery. The present work reported a new functionalized approaches to construct drug-loaded nanohybrids (2:1E and 2.8:1E) by co-assembling LDH sheets, penta-fluorouracil (5Fu) and poloxamer 188 through exfoliation reassembling. Some analysis showed that more poloxamer 188 were needed to prepare 2:1E with appropriate particle size than 2.8:1E. Besides, 2.8:1E shows advantages in drug loading rate and dispersion as compared with ion exchange method. In addition, these nanohybrids can improve the sudden release of 5Fu in naked drug-loaded LDH. Most importantly, significant enhanced cell uptake and better cytotoxicity were seen in these nanohybrids in contrast to naked drug-loaded LDH. Lastly, the results reveal that assembling drug-loaded LDH with poloxamer 188 is a promising strategy to improve cellular uptake and in vitro efficacy of LDHs for biomedical applications. Graphical abstract Drug-loaded nanohybrids were synthesised by co-assembling LDH sheets, penta-fluorouracil (5Fu) and poloxamer 188 through exfoliation reassembling, and showed advantages in dispersion, enhanced cell uptake and better cytotoxicity as compared with naked drug-loaded-LDH prepared by ion exchange method.

研究领域: 药剂学 · 生物材料 · 纳米医学
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AAPS PHARMSCITECH · 2024 ·Vol. 25 ·期 6 ·1-15 · IF 3.4

Effects of Commonly used Surfactants, Poloxamer 188 and Tween 80, on the Drug Transport Capacity of Intestinal Glucose Transporters

Chen Jiasheng,Chen Zhenzhen,Wang Wentao,Wang Liyang,Zheng Jiaqi,Wu Shiqiong,Pan Yuru,Li Sai,Zhao Jie,Cai Zheng

Some glycoside drugs can be transported through intestinal glucose transporters (IGTs). The surfactants used in oral drug preparations can affect the function of transporter proteins. This study aimed to investigate the effect of commonly used surfactants, Poloxamer 188 and Tween 80, on the drug transport capacity of IGTs. Previous studies have shown that gastrodin is the optimal drug substrate for IGTs. Gastrodin was used as a probe drug to evaluate the effect of these two surfactants on intestinal absorption in SD rats through pharmacokinetic and in situ single-pass intestinal perfusion. Then, the effects of the two surfactants on the expression of glucose transporters and tight-junction proteins were examined using RT-PCR and western blotting. Additionally, the effect of surfactants on intestinal permeability was evaluated through hematoxylin-eosin staining. The results found that all experimental for Poloxamer 188 (0.5%, 2.0% and 8.0%) and Tween 80 (0.1% and 2.0%) were not significantly different from those of the blank group. However, the AUC (0-∞) of gastrodin increased by approximately 32% when 0.5% Tween 80 was used. The changes in IGT expression correlated with the intestinal absorption of gastrodin. A significant increase in the expression of IGTs was observed at 0.5% Tween 80. In conclusion, Poloxamer 188 had minimal effect on the drug transport capacity of IGTs within the recommended limits of use. However, the expression of IGTs increased in response to 0.5% Tween 80, which significantly enhanced the drug transport capacity of IGTs. However, 0.1% and 2.0% Tween 80 had no significant effect. Graphical Abstract

研究领域: 药剂学 · 药理学 · 肠道吸收
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PHARMACEUTICAL CHEMISTRY JOURNAL · 2021 ·Vol. 54 ·期 10 ·1033-1039 · IF 0.837

Preparation and In Vitro/Vivo Evaluation of New Celecoxib Solid Dispersions with Co-Carrier Containing Aerosil and Poloxamer 188

Shi Xiangjun,Ding Zejie,Bao Jiayin,Wang Chao

Solid dispersions (SDs) containing co-carrier were developed to improve in vitro dissolution and in vivo pharmacokinetics of celecoxib (CXB). Various polymers, including PVP K30, PEG4000, PEG6000, Poloxamer 188, Eudragit E100 and colloidal SiO 2 , were studied in the preparation of CXB-containing SDs. Poloxamer 188 and Aerosil stood out in preliminary characterization. Further study was focused on the selection and characterization of optimum ratio of CXB and polymer in solid dispersions (CXB-Poloxamer 188-Aerosil, 1:5:1). Results exhibited remarkable enhancement of both the dissolution and bioavailability of CXB which retained an amorphous form in SD samples.

研究领域: 药学 · 药理学 · 药物递送系统
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MICROCHEMICAL JOURNAL · 2020 · IF 3.594

Silver sulfide nanoparticles on MWCNTs stabilized by poloxamer: An enhanced electrochemical sensor for high sensitivity detection of 2,4,6-trinitrotoluene

Xin Li,Ya Ma,Xiao-Lin Zhong,Li-Shi Wang

In this manuscript, an electrochemical sensor modified with multi-walled   carbon nanotubes (MWCNTs) and silver sulfide (Ag 2 S) was prepared by means of potentiostatic deposition method for the detection of 2,4,6-trinitrotoluene. The poloxamer (Px) was then electrodeposition onto the surface of MWCNTs and Ag 2 S as a film-forming material to prevent the leakage of nanomaterial, to improve the stability of the modified electrode and then enhance the current signal, which contributed to the high sensitivity of the electrode. During the electrodeposition process, some influence factors, such as the deposition cycle number, deposition time, and applied potential of silver sulfide, and the deposition time and applied potential of Px have been inspected. Under optimal conditions, the obtained sensor showed good catalytic performance for the reduction reaction of 2,4,6-trinitrotoluene. The proposed sensor also exhibited excellent stability and reproducibility, providing a wide linear ranges from 0.22 to 15.4 μmol L -1 and a low detection limit of 3.23 nmol L -1 (S/N = 3). It also provides a satisfactory result when applied to the actual sample detection.

研究领域: 材料科学 · 分析化学 · 环境科学
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PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY · 2023 · IF 3.4

Layered double hydroxides - poloxamer 188 nanocomposites based on exfoliation reassembling for improved cellular uptake and controlled delivery of methotrexate

Liang Liang,Jin Ren,Jun Dai,Jianyun Liu,Lifang Zhang,Donglin Li,Chao Yang,Jingmou Yu

Exploitation of advanced methotrexate (MTX) delivery with nanocomposites has important clinical application value. Poloxamer 188 micelle and layered double hydroxide loaded with MTX (LDH-MTX) by exfoliation reassembling were used to prepare LDH-MTX-poloxamer 188 nanocomposites with good dispersibility and efficient cellular uptake for controlled drug delivery. The LDH-MTX-poloxamer 188 nanocomposites with sphere-like morphology, of which the average hydrodynamic diameter was <100 nm, were shown to have better dispersion state than naked LDH-MTX. Importantly, the LDH-MTX-poloxamer 188 nanocomposites could achieve significant sustained drug release and have obvious pH dependent responsive release ability. In addition, these nanocomposites also exhibited long-term and excellent in vitro antitumor efficacy as opposed to pure MTX or LDH-MTX as evident from cell viability. More interestingly, compared to pure FITC used to simulate MTX, LDH nanocomposites labeled with FITC were considered to have better cell adhesion through cell uptake. Therefore, the studied nanocomposites of LDH-MTX-poloxamer 188 can be further used as a new advanced MTX delivery nanovehicles with desired properties in future therapeutic aspects.

研究领域: 药剂学 · 纳米医学 · 肿瘤学
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CARBOHYDRATE POLYMERS · 2025 · IF 12.5

The comparison of anticrystallization effects of cellulose derivatives with polyvinylpyrrolidone and poloxamer on andrographolide: In vitro and in vivo characterization

Xiaoyi Zhang,Peixia Luo,Jiaming Wang,Lei Yang,Zipei Pang,Shufeng Chen,Yi Zhou,Linghao Qin

Cellulose derivatives play important roles in the development of pharmaceutical oral solid formulations. Owing to their high molecular weight and functional groups, these polymers can interact with water-insoluble drug crystals, influencing not only the drug's physicochemical properties but also its absorption efficiency. In this study, an anticrystallization experiment was designed to compare the inhibitory effects of cellulose derivatives (methylcellulose (MC), hydroxypropyl cellulose (HPC) and hydroxypropyl methyl cellulose (HPMC)) with those of polyvinylpyrrolidone (PVP) and poloxamer (F68) on the crystallization of model drugs (andrographolide, AG). Both in vitro characterization experiments and in vivo pharmacokinetic studies were conducted to evaluate the interaction patterns between andrographolide crystals and polymers. The results indicated that cellulose derivatives exhibited stronger anticrystallization effects, with HPMC showing the most pronounced interaction with drug crystals among all the tested polymers. HPMC significantly prolonged the crystallization time and increased the degree of supersaturation. By adsorbing onto specific crystal surfaces, HPMC was able to modulate the crystal growth orientation, reduce the contact angle, and improve the wettability of drug crystals. Furthermore, andrographolide crystals adsorbed by HPMC exhibited rapid in vitro drug release behavior and upgraded in vivo absorption efficiency, demonstrating its potential to improve the utilization of water-insoluble drugs.

CAS / MDL: 540-69-2 7758-02-3
研究领域: 药剂学 · 药物化学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2016 · IF 3.994

Tissue distribution and enhanced in vivo anti-hyperlipidemic-antioxidant effects of perillaldehyde-loaded liposomal nanoformulation against Poloxamer 407-induced hyperlipidemia

Emmanuel Omari-Siaw,Qilong Wang,Congyong Sun,Zengquan Gu,Yuan Zhu,Xia Cao,Caleb Kesse Firempong,Rita Agyare,Ximing Xu,Jiangnan Yu

An optimized perillaldehyde-loaded liposomal nanoformulation (PAH-LNF) was successfully applied to improve the pharmacological effect of perillaldehyde (PAH) in poloxamer 407-induced hyperlipidemia . Oral administration of PAH-LNF (240   mg/kg per body weight) in rats significantly enhanced solubility and relative bioavailability (270.7%) compared to the free PAH with about 2.7-, 1.5-, 1.3-, 1.3- and 1.5-fold increase in AUC, T 1/2 , MRT, C max and T max , respectively. Tissue distribution study also revealed the accumulation of PAH in the liver, lungs, spleen, kidney, brain and heart in order of decreasing affinity. Moreover, a significant decrease in serum total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) with simultaneous increase in high-density lipoprotein cholesterol (HDL-C) level was observed in the chemically-induced hyperlipidemic mice which further confirmed PAH’s anti-hyperlipidemic properties. Additionally, PAH-LNF also significantly increased the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) with a concurrent decrease in malondialdehyde (MDA) to affirm the antioxidant and hepatoprotective effects of PAH. Thus, liposomal nanoformulation promises to be a useful drug delivery system for the development of PAH.

CAS / MDL: 49562-28-9
研究领域: 药理学 · 纳米医学 · 生物化学
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