FOOD AND CHEMICAL TOXICOLOGY
·
2020
·
IF 4.679
Congyong Sun,Wenjing Li,Ping Ma,Yang Li,Yuan Zhu,Huiyun Zhang,Michael Adu-Frimpong,Wenwen Deng,Jiangnan Yu,Ximing Xu
Syringic acid (SA), a natural polyphenol found in fruits and vegetables, is claimed to show notable hepatoprotection . Nevertheless, low solubility and bioavailability hamper the application of SA. This study aimed to investigate the potential of TPGS/F127/F68 mixed polymeric micelles as a sustained and liver-targeting nanocarrier for SA. Herein, the prepared SA-loaded TPGS/F127/F68 mixed polymeric micelles (SA-TPGS-Ms) were spherically-shaped and homogeneously-distributed nanoparticles with high entrapment efficiency (94.67 ± 2.05%) and sustained release. Besides, in-vitro cell culture studies revealed that SA-TPGS-Ms substantially promoted cellular uptake with excellent biocompatibility . After oral administration, SA-TPGS-Ms demonstrated an increased bioavailability (2.3-fold) and delayed in-vivo elimination compared with the free SA. Furthermore, the alleviation of oxidative stress and amelioration of hepatic injury in CCl 4 -induced hepatotoxicity mice further demonstrated the excellent hepatoprotection of SA-TPGS-Ms. Collectively, SA-TPGS-Ms could be a promising nanocarrier for the utilization of SA in functional foods, with enhanced bioavailability and hepatoprotection.
研究领域:
药理学
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纳米技术
·
肝病学
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DOI
PubMed
高影响因子
Journal of Biomedical Nanotechnology
·
2017
·Vol. 13
·期 12
·1631-1646
·
IF 4.521
Wang Jiao,Liu Qiang,Yang Linnan,Xia Xiaofei,Zhu Rongrong,Chen Shengguang,Wang Mei,Cheng Liming,Wu Xianzheng,Wang Shilong
Cervical cancer is the fourth most common cancer in women worldwide, and existing treatments cause severe side effects and great burdens. Thus, the development of safe, inexpensive therapeutic agents is necessary. Curcumin (Cur), a well-known natural product, exerts promising anti-cancer
activities against various cancer types. However, its therapeutic efficacy is severely restrained due to rapid degradation, poor aqueous solubility, and low bioavailability. The objective of this study was to investigate the therapeutic potential of novel curcumin-loaded TPGS/F127/P123 mixed
polymeric micelles (Cur@NPT100) for cervical cancer treatment. The Cur@NPT100 exhibited an average size of approximately 19 nm, a zeta potential of around –4 mV, a drug loading of 8.18 ± 0.36%, and an encapsulation efficiency of 79.38 ± 4.65%. Unlike free Cur, Cur@NPT100
are readily dispersed in aqueous medium, showing enhanced stability and a sustained release profile over a 6-day period. In vitro cell culture experiments revealed that TPGS/F127/P123 mixed polymeric micelles (NPT100) based nanocarriers substantially promoted the selective cellular
uptake of Cur into HeLa cells rather than by non-cancerous NIH3T3 cells, inducing higher cytotoxicity and greater apoptosis and significantly increasing the percentage of cells arrested at the G2/M phase of the cell cycle. Additionally, the Cur@NPT100 facilitated more Cur accumulation in the
mitochondria and decreased the mitochondrial membrane potential. In addition, western blot assays demonstrated that Cur@NPT100 were more potent than free Cur at activating the mitochondria-mediated apoptosis pathway. In vivo results further confirmed that Cur@NPT100 exhibited a much higher
antitumor efficacy than free Cur and had excellent biocompatibility. In conclusion, Cur@NPT100 might be an effective therapeutic agent for cervical cancer.
研究领域:
药学
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肿瘤学
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纳米技术
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药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2022
·
IF 3.915
Xiaoli Xia,Jian Zhang,Michael Adu‑Frimpong,Xiaoxiao Li,Xinyi Shen,Qing He,Wanjing Rong,Hao Ji,Elmurat Toreniyazov,Ximing Xu,Jiangnan Yu,Qilong Wang
Hyperoside (Hyp) self-assembled polymeric micelles (Hyp-PMs) were purposely developed to enhance aqueous solubility, in vivo availability and anti-oxidative effect of Hyp. In preparing Hyp-PMs, we employed the thin film dispersion method with the micelles consisting of TPGs and mPEG2000-PDLLA3000. The particle size, polydispersity index and zeta potential of Hyp-PMs were 67.42 ± 1.44 nm, 0.229 ± 0.015 and −18.67 ± 0.576 mV, respectively, coupled with high encapsulation efficiency （EE）of 90.63 ± 1.45% and drug loading (DL) of 6.97 ± 1.56%. Furthermore, the value of critical micelle concentration (CMC) was quite low, which indicated good stability and improved self-assembly ability of Hyp-PMs. Also, trend of in vitro Hyp release from Hyp-PMs demonstrated enhanced solubility of Hyp. Similarly, in comparison with free Hyp, oral bioavailability of Hyp-PMs was improved (about 8 folds) whilst half-life of Hyp-PMs was extended (about 3 folds). In vitro anti-oxidative effect showed obvious strong scavenging DPPH capability of Hyp-PMs, which may be attributed to its smaller size and better solubility. Altogether, Hyp-PMs may serve as a possible strategy to potentially enhance aqueous solubility, bioavailability and anti-oxidative effect of Hyp, which may play a key role in Hyp application in the pharmaceutical industries.
研究领域:
药学
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纳米技术
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药物递送系统
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药代动力学
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产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2020
·Vol. 21
·期 5
·1-13
·
IF 2.401
Liu Dandan,Qiao Sen,Cheng Bingchao,Li Dongyang,Chen Jisuan,Wu Qingyin,Pan Hao,Pan Weisan
Despite that either non-covalent or covalent attachment of hydrophilic polymers or surfactants onto nanodiamonds (NDs) could overcome the shortcomings of being a drug delivery system, it is hard to draw a definite conclusion which strategy is more effective. Hence, with the purpose of comparing the influence of different coating approach of NDs on the oral delivery efficiency of water-insoluble model drug curcumin (CUR), NDs were firstly modified with d -α-tocopheryl polyethylene glycol 1000 succinate (TPGS) via non-covalent or covalent conjugation method, and then loaded with CUR (CUR@NDs-COOH/TPGS or CUR@NDs-TPGS). In comparison with the core-shell-structured CUR@NDs-COOH/TPGS, CUR@NDs-TPGS were irregular in shape with dense TPGS film, and exhibited smaller size, more negatively potential, and higher drug loading efficiency. The covalent connection group also showed higher anti-cancer activity, cellular uptake, and permeability through the Caco-2 cell monolayers, as well as favorable distribution, penetration, and retention in rat intestines. The oral bioavailability study in rats demonstrated that CUR@NDs-TPGS showed significantly greater C max and AUC 0− t in contrast with CUR suspension and the TPGS-coated ones, respectively. The findings illustrated that covalent grafting TPGS onto the surface of NDs possesses better efficacy and biocompatibility on oral delivery of poorly soluble drug CUR than pristine and non-covalent coated nanoparticles.
研究领域:
药学
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药物递送系统
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纳米技术
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药代动力学
✓ 已验证
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2023
·
IF 6
Lan Tang,Kaijuan Huang,Wenhui Jiang,Lulu Fu,Ran Zhang,Liting Shen,Zhimin Ou,Ye Huang,Zhenhai Zhang
D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) is a commonly used nonionic surfactant used as a pharmaceutical carrier in different drug delivery systems. TPGS can reverse P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) and also has anticancer activities. It suggests that when designing antitumor drug preparation, it’s necessary to take into account the antitumor activity of TPGS. Our in vivo studies showed that TPGS exerted the strongest cytotoxicity in MCF-7-ADR cells when compared with seven other tumor cell lines. The further study revealed TPGS caused apoptosis and blocked MCF-7 cell growth in G2/M phase. Mechanistic insights suggested that TPGS increased intracellular calcium ion concentrations, leading to apoptosis via the mitochondrial pathway. Furthermore, two in vivo experiments were performed. One was TPGS, and DOX solution was administered by tail vein injection on MCF-7-ADR tumor bearing nude mice. The other was temperature sensitive TPGS gel (TPGS-TG) was administered by intratumoral injection on MCF-7-ADR tumor bearing nude mice combined with paclitaxel albumin nanoparticles (Abraxane®) administered by tail vein injection. The findings confirmed that TPGS could play its role in anti-tumor to reduce the toxicity of chemotherapeutic drugs and improve the efficiency of drug-resistant tumors, thereby enhancing the development of safe oncology therapeutics.
研究领域:
药理学
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肿瘤学
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药物递送系统
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癌症研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2023
·
IF 8
Ran Tao,Chengzhang Wang,Yin Lu,Changwei Zhang,Hao Zhou,Hongxia Chen,WenJun Li
Background This study demonstrated an innovative formulation including the polyprenol (GBP) lipid and vitamin E-TPGS hybrid nanoparticles (NPs) which was aimed to control the transfer of betulinic acid (BA) and low-substituted hydroxyl fullerenol (C60(OH)n). Additionally, it developed BA-C60(OH)n-GBP-TPGS-NPs delivery system and researched the anti-hepatocellular carcinoma (HCC) effects.Materials and Methods The NPs were prepared by nanoprecipitation with ultrasonic-assisted emulsification (UAE) method. It was characterized by scanning electronic microscopy (SEM), transmission electron microscopy (TEM), FTIR spectrum, size distribution and zeta potential. Physical and chemical properties were evaluated through measurement of drug release, stability studies, drug loading efficiency (DE) and encapsulation efficiency (EE). Biological activities were evaluated through measurement of MTT assay, lactate dehydrogenase leakage assay (LDH), cell proliferation assays, cell apoptosis analysis, comet assay, wound healing assay, cell invasion and Western blot analysis.Results and Conclusions The NPs exhibited clear distribution characteristics, improved solubility and stability. BA and C60(OH)n for the NPs displayed a biphasic release pattern with sustained drug release properties. The mixture of C60(OH)n with different hydroxyl groups may have a certain effect on the stability of the NPs system itself. The NPs could effectively inhibit MHCC97H cell proliferation, migration and invasion in vitro. Combined use of C60(OH)n and BA in GBP lipids may improve the inhibit effect of C60(OH)n or BA against HCC cells and reduce cytotoxicity and genotoxicity of C60(OH)n for normal cells. We concluded that one of the important mechanisms of BA-C60(OH)n-GBP-TPGS-NPs inhibiting MHCC97H cells is achieved by up-regulating the expression of Caspase-3, Caspase-8 and Caspase-9.
研究领域:
药学
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纳米技术
·
肿瘤学
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细胞生物学
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药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Bioengineering and Biotechnology
·
2021
·
IF 5.89
Wang Wenrui,Zhou Mengyang,Xu Yang,Peng Wei,Zhang Shiwen,Li Rongjie,Zhang Han,Zhang Hui,Cheng Shumin,Wang Youjing,Wei Xinyu,Yue Chengxu,Yang Qingling,Chen Changjie
Multidrug resistance (MDR) is a serious problem during cancer therapy. The purpose of the present study was to formulate D-α-Tocopheryl polyethylene glycol 1000 succinate-resveratrol-solid lipid nanoparticles (TPGS-Res-SLNs) to improve its therapeutic efficacy against breast cancer. In this study, the solvent injection method was used to prepare the TPGS-Res-SLNs. It was found that the TPGS-Res-SLNs exhibited zeta potential and drug-loading of −25.6 ± 1.3 mV and 32.4 ± 2.6%, respectively. Therefore, it was evident that the TPGS-Res-SLNs can increase cellular uptake of chemotherapeutic drugs, induce mitochondrial dysfunction, and augment tumor treatment efficiency by inducing apoptosis. Moreover, it was found that SKBR3/PR cells treated with TPGS-Res-SLNs exhibited significant inhibition of cell migration and invasion, as compared with free resveratrol. In addition, results from in vivo SKBR3/PR xenograft tumor models revealed that TPGS-Res-SLNs has better efficacy in promoting apoptosis of tumor cells owing to high therapeutic outcomes on tumors when compared with the efficacy of free resveratrol. In conclusion, the findings of the present study indicate significant potential for use of TPGS-Res-SLNs as an efficient drug delivery vehicle to overcome drug resistance in breast cancer therapy.
研究领域:
药学
·
肿瘤学
·
纳米技术
·
药物递送系统
·
癌症治疗
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2023
·
IF 5
Shuoye Yang,Yakun Niu,Siqi Li,Mingzhen Lv,Jiaxin Liu,Lu Zhang,Lan Cui,Lingbo Qu
Coenzyme Q10 (CoQ10) has a wide range of nutraceutical functions and therapeutic values, nevertheless, its biomedical application as a health product or drug is hampered by the low absorption efficiency and bioavailability. In the present study, the hybrid mesoporous silica nanoparticle-supported lipid bilayers (LMSNs) as nanocarriers for CoQ10 are prepared by fusing the phospholipid membrane onto MSNs cores. Further, LMSNs are functionalized with d -α-tocopherol polyethylene glycol 1000 succinate (TPGS), deoxycholic acid (Doca) and chitosan (CS) sequentially, to obtain the TPGS-LMSNs and DCs-TPGS-LMSNs samples, respectively. MSNs, liposomes , and unmodified LMSNs are also prepared as controls. The results reveal that various nanocarriers have a high loading capacity for CoQ10, low cytotoxicity towards Caco-2 cells, and sustained release property in different pH mediums. In contrast to other nano-formulations, [email protected] show the higher cellular uptake efficiency and the resulting ROS inhibition effect, which can be taken up by cells via caveolae-mediated route, macropinocytosis, and unique bile acid uptake pathway mediated by ASBT. Efficient delivery of DC-TPGS-LMSNs is further illustrated by in vivo intestinal uptake and pharmacokinetics study, in which [email protected] exhibit higher absorption efficiency, longer circulation time, and more enhanced bioavailability than other formulations after oral administration. The results suggest that multifunctional LMSNs might be the potent candidate for CoQ10 delivery, and the findings will contribute to the rational design of novel drug delivery vehicles .
研究领域:
纳米技术
·
药剂学
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药物递送系统
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF PHARMACY AND PHARMACOLOGY
·
2016
·Vol. 68
·期 9
·1109-1118
·
IF 2.363
Yang Lei,Xin Jin,Zhang Zhenhai,Yan Hongmei,Wang Jing,Sun E,Hou Jian,Jia Xiaobin,Lv Huixia
ObjectiveThis work aimed at preparing ginsenoside compound K (GCK)-loaded liposomes modified with TPGS (GCKT-liposomes) to enhance solubility and targeting capability of GCK, as well as inhibit the efflux of GCK from tumour cells.MethodsGCKT-liposomes were prepared by the thin-film hydration method and characterized by particle size, polydispersity, zeta potential and drug encapsulation efficiency. A549 cells were used as antitumour cell model to access the cellular uptake of the GCK and perform its antitumour function. The enhancement of in vivo antitumour efficacy of GCKT-liposomes was evaluated by nude mice bearing tumour model.Key findingsThe results showed that GCKT-liposomes achieved a comparatively high drug loading efficiency and reasonable particle size at the ratio of 7 : 3 (phospholipid: TPGS). The in vitro release demonstrated that the dissolution of GCK was remarkably improved by entrapping it into liposomes. In addition, GCKT-liposomes exhibited a great hypersensitizing effect on A549 cells, and the cellular uptake was enhanced. Compared with free GCK, the IC50 of GCKT-liposomes was significantly reduced (16.3 ± 0.8 vs 24.9 ± 1.0 μg/ml). In vivo antitumour assay also indicated that GCKT-liposomes achieved higher antitumour efficacy (67.5 ± 0.5 vs 40.8 ± 0.7%).ConclusionThe novel GCKT-liposomes significantly improved the antitumour efficacy of GCK.
研究领域:
药学
·
肿瘤学
·
药物递送系统
·
癌症研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2017
·Vol. 7
·期 41
·25694-25701
·
IF 3.108
Xiaoju Shi,Guoyue Lv,Xiaodong Sun,Dianbo Cao,Guangyi Wang,Yulei Chang
Recently, several targeted drug delivery systems have shown promising antitumor activity towards different types of cancer. However, targeting the tumor microenvironment, cellular surface and/or only one organelle may not achieve the expected therapeutic effects. Herein, a targeted drug delivery with stepwise targeting and image-guided strategy was obtained for enhancing antitumor therapy and overcoming various problems caused by the random drug distribution of traditional medicine. In this design, a multifunctional nanoplatform, TPGS/PPG2L@IONPs@DOX/TPP–DOX, based on poly(ethylene glycol)-poly(ε-caprolactone)-poly(amidoamine)-lactose acid (mPEG-PCL-G2.0 PAMAM-LA, PPG2L) copolymer and D-α-tocopherol polyethylene glycol 1000 succinate (TPGS), as a co-carrier, incorporates iron oxide nanoparticles (IONPs) as imaging agents and loads a DOX/triphenylphosphonium (TPP)–DOX drug for chemotherapy. In this nanoplatform micelle, the LA as targeting moieties to hepatocarcinoma cells is the first targeting step. After the drug is released from the hybrid micelles, the incorporated DOX and TPP–DOX target delivery to nuclei and mitochondria for the next targeting step. Furthermore, with the help of MRI contrast agents of IONPs, the distribution of hybrid micelles was monitored. As a result, the hybrid micelles demonstrated enhanced antitumor cell activity in both HepG2 and HepG2/DOX cells. The results indicated that the multifunctional hybrid micelles showed great potential in enhancing antitumor activity under image-guided and stepwise targeted chemotherapy.
研究领域:
药学
·
癌症研究
·
纳米技术
·
医学影像
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2020
·
IF 2.734
Rui Bao,Qi-Long Wang,Ran Li,Michael Adu-Frimpong,Elmurat Toreniyazov,Hao Ji,Xi-Ming Xu,Jiang-Nan Yu
6-Shogaol is one component of ginger, which has been described to possess various health-promoting effects including anticancer, antiinflammatory, antioxidant and antiatherogenic. However, poor water solubility has limited the aforementioned health benefits and clinical applications of the drug. Herein, the aforementioned drawback was circumvented by the preparation of 6-shogaol-loaded liposome through thin-film dispersion method with TPGS as the carrier, in comparison with 6-shogaol liposome and free 6-shogaol. Appropriate indices were used for the characterization of the developed liposomes viz., particle size (PS), zeta potential (Z-potential), polydispersity index (PDI), entrapment efficiency (EE) and loading capacity (LC) while their morphologies were observed under the transmission electron microscopy (TEM). In-vitro dissolution investigation showed a substantial improvement in the accumulative release rates of liposomes comparable to the free 6-shogaol. The TPGS-modified 6-shogaol and 6-shogaol liposomes had oral relative bioavailability (RBA) of 580.04% and 281.55%, respectively, with improved t 1/2 , MRT, C max , AUC 0-t and T max . Pertinently, the TPGS coated 6-shogaol liposome may enhance the targeting of the drug to the brain. Therefore, the TPGS coated 6-shogaol liposome could potentially improve oral bioavailability of lipophilic drug in-vivo . More importantly, the results of tissue distribution investigation suggest that TPGS coated 6-shogaol liposome may act as promising carrier for brain delivery in future.
研究领域:
药剂学
·
药理学
·
纳米技术
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
Asian Journal of Pharmaceutical Sciences
·
2013
·
IF 0
Ting Yuan,Lingzhen Qin,Zhouhua Wang,Jinyuan Nie,Zhefei Guo,Ge Li,Chuanbin Wu
Solid dispersion of calcitriol with lipophilic surfactants and triglycerides was developed by melt-mixing method to modify the release and enhance stability of the drug. The solid dispersions were characterized by differential scanning calorimetry (DSC), hot stage polarized optical microscopy (HSPM), infrared spectroscopy (FTIR) and stability studies. The solid dispersion significantly enhanced the stability of calcitriol, which could be attributed to the high antioxidant activity of the solid lipid dispersion. The rapid dissolution rate from the solid dispersion was attributed to the amorphous or solid solution state of drug with improved specific surface area and wettability than the drug crystals. Therefore, solid dispersion of calcitriol with d -a-tocopheryl polyethylene glycol 1000 succinate (TPGS) offers a good approach to modify the release and enhance stability of calcitriol. The influence of lipophilic solid dispersion on drug bioavailability needs further investigation.
研究领域:
药剂学
·
药物化学
✓ 已验证
产品关联
DOI
危险品化学品经营许可证（带存储）