The Experts below are selected from a list of 32628 Experts worldwide ranked by ideXlab platform
Yanbin Jiang - One of the best experts on this subject based on the ideXlab platform.
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incorporation of 10 hydroxycamptothecin nanocrystals into zein microspheres
Chemical Engineering Science, 2016Co-Authors: Guijin Liu, Yinxia Huang, Hongdi Wang, Yanbin JiangAbstract:Abstract Incorporation of drug nanocrystal (DNC) into a particulate carrier to form the DNC delivery system was conducted in this study, where 10-hydroxycamptothecin (HCPT) was selected as the model drug and zein was the carrier. The supercritical anti-solvent (SAS) process or the built-in ultrasonic dialysis process (BUDP) was applied to prepare HCPT NC-loaded zein microspheres (HCPT NC-Zein MS) at first respectively, but the results showed that the products obtained were unsatisfactory in their particle microstructures. Fortunately, by combining the SAS process with BUDP, i.e. the co-precipitation of HCPT and zein prepared using the SAS process was dispersed into ethanol–water as the dialysis solution for BUDP, the results showed that desirable HCPT NC-Zein MS were obtained. The formulations were evaluated quantitatively by an overall desirability function (DF), and the optimized HCPT NC- Zein MS was prepared according to the range analysis results of DF. Under the optimized conditions, HCPT NC-Zein MS with a mean particle size=1.10±0.12 µm, drug loading=5.98% and encapsulation efficiency=95.68% were obtained. The further characterizations of SEM, FT-IR, XRD and DSC demonstrated that HCPT NC was successfully incorporated into the interior of zein microspheres. The effects of the process parameters and the formation mechanism of HCPT NC-Zein MS were discussed in detail. Furthermore, it is presented that HCPT NC-Zein MS sustained HCPT release rate successfully, where about 50% HCPT was fast released in the first 20 h, then the release trend followed zero order kinetics and reached 70% in 82 h.
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preparation of 10 hydroxycamptothecin proliposomes by the supercritical co2 anti solvent process
Chemical Engineering Journal, 2014Co-Authors: Guijin Liu, Wei Wang, Hongdi Wang, Yanbin JiangAbstract:Abstract For this study, 10-Hydroxycamptothecin proliposomes (HCPT-PL) were prepared using the supercritical CO2 anti-solvent process. The mixture of soy lecithin and cholesterol were chosen as liposomal components. The effects of different variables, i.e., the mass ratio of soy lecithin to cholesterol, the mass ratio of HCPT to liposomal components, temperature, pressure and HCPT solution flow rate on HCPT-PL formation were investigated using an OA25 (55) orthogonal experimental design. The formulations were evaluated quantitatively using an overall desirability function, which was calculated based on four assessment indices, i.e., particle size, particle size distribution, drug loading and encapsulation efficiency. SEM and TEM images showed that spherical or clavate HCPT-PL were obtained under different processing conditions, and the drug loading has a significant effect on the morphologies. Under the optimized conditions, clavate HCPT-PL with a mass median diameter of 209.8 ± 38.4 nm, a drug loading of 5.33% and an encapsulation efficiency of 85.28% were obtained. For the optimized HCPT-PL, the residual DCM meets the ICH requirement, and part of the encapsulated HCPT still maintains its crystalline state. And the result of in vitro release rate study showed that HCPT-PL sustained the HCPT release rate successfully, where the drug release of the optimized HCPT-PL followed the first order kinetics, and the drug diffusion mainly corresponded to a Fickian diffusion mechanism during the first 10 h.
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co precipitation of 10 hydroxycamptothecin and poly l lactic acid by supercritical co2 anti solvent process using dichloromethane ethanol co solvent
Journal of Supercritical Fluids, 2013Co-Authors: Wei Wang, Guijin Liu, Yanbin JiangAbstract:Abstract In this study, 10-hydroxycamptothecin (HCPT) and poly ( l -lactic acid) (PLLA) are co-precipitated by the supercritical anti-solvent (SAS) process using a mixture of dichloromethane (DCM)/ethanol (EtOH) as co-solvent, and supercritical carbon dioxide as the anti-solvent. The effect of five operating conditions on particle morphology, mass median diameter (Dp50) and HCPT loading is investigated using the single-factor method. The results indicate that HCPT loading can be greatly increased by using DCM/EtOH co-solvent, and the suitable operating conditions for the experimental system are determined. Under suitable conditions, the HCPT loading is 13.3% and Dp50 is 794.5 nm. The drug loaded microparticles are characterized in detail. The SEM images showed that most of the particles were spherical, and PLLA concentration has a major impact on the particle shape. Results of TEM, DSC and XRD indicate that the micronized HCPT is dispersed into the PLLA matrix. For low HCPT loading, most of HCPT existed in the drug loaded microparticles in an amorphous state, but for high HCPT loading, part of the encapsulated drug existed in crystalline form. FT-IR results show that SAS process does not change the chemical structure of HCPT. The result of in vitro drug release test indicated that the crystallinity of HCPT in microparticles affects the control release performance, and the good encapsulated microparticles with higher HCPT loading and higher crystallinity are better.
Guijin Liu - One of the best experts on this subject based on the ideXlab platform.
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incorporation of 10 hydroxycamptothecin nanocrystals into zein microspheres
Chemical Engineering Science, 2016Co-Authors: Guijin Liu, Yinxia Huang, Hongdi Wang, Yanbin JiangAbstract:Abstract Incorporation of drug nanocrystal (DNC) into a particulate carrier to form the DNC delivery system was conducted in this study, where 10-hydroxycamptothecin (HCPT) was selected as the model drug and zein was the carrier. The supercritical anti-solvent (SAS) process or the built-in ultrasonic dialysis process (BUDP) was applied to prepare HCPT NC-loaded zein microspheres (HCPT NC-Zein MS) at first respectively, but the results showed that the products obtained were unsatisfactory in their particle microstructures. Fortunately, by combining the SAS process with BUDP, i.e. the co-precipitation of HCPT and zein prepared using the SAS process was dispersed into ethanol–water as the dialysis solution for BUDP, the results showed that desirable HCPT NC-Zein MS were obtained. The formulations were evaluated quantitatively by an overall desirability function (DF), and the optimized HCPT NC- Zein MS was prepared according to the range analysis results of DF. Under the optimized conditions, HCPT NC-Zein MS with a mean particle size=1.10±0.12 µm, drug loading=5.98% and encapsulation efficiency=95.68% were obtained. The further characterizations of SEM, FT-IR, XRD and DSC demonstrated that HCPT NC was successfully incorporated into the interior of zein microspheres. The effects of the process parameters and the formation mechanism of HCPT NC-Zein MS were discussed in detail. Furthermore, it is presented that HCPT NC-Zein MS sustained HCPT release rate successfully, where about 50% HCPT was fast released in the first 20 h, then the release trend followed zero order kinetics and reached 70% in 82 h.
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preparation of 10 hydroxycamptothecin proliposomes by the supercritical co2 anti solvent process
Chemical Engineering Journal, 2014Co-Authors: Guijin Liu, Wei Wang, Hongdi Wang, Yanbin JiangAbstract:Abstract For this study, 10-Hydroxycamptothecin proliposomes (HCPT-PL) were prepared using the supercritical CO2 anti-solvent process. The mixture of soy lecithin and cholesterol were chosen as liposomal components. The effects of different variables, i.e., the mass ratio of soy lecithin to cholesterol, the mass ratio of HCPT to liposomal components, temperature, pressure and HCPT solution flow rate on HCPT-PL formation were investigated using an OA25 (55) orthogonal experimental design. The formulations were evaluated quantitatively using an overall desirability function, which was calculated based on four assessment indices, i.e., particle size, particle size distribution, drug loading and encapsulation efficiency. SEM and TEM images showed that spherical or clavate HCPT-PL were obtained under different processing conditions, and the drug loading has a significant effect on the morphologies. Under the optimized conditions, clavate HCPT-PL with a mass median diameter of 209.8 ± 38.4 nm, a drug loading of 5.33% and an encapsulation efficiency of 85.28% were obtained. For the optimized HCPT-PL, the residual DCM meets the ICH requirement, and part of the encapsulated HCPT still maintains its crystalline state. And the result of in vitro release rate study showed that HCPT-PL sustained the HCPT release rate successfully, where the drug release of the optimized HCPT-PL followed the first order kinetics, and the drug diffusion mainly corresponded to a Fickian diffusion mechanism during the first 10 h.
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co precipitation of 10 hydroxycamptothecin and poly l lactic acid by supercritical co2 anti solvent process using dichloromethane ethanol co solvent
Journal of Supercritical Fluids, 2013Co-Authors: Wei Wang, Guijin Liu, Yanbin JiangAbstract:Abstract In this study, 10-hydroxycamptothecin (HCPT) and poly ( l -lactic acid) (PLLA) are co-precipitated by the supercritical anti-solvent (SAS) process using a mixture of dichloromethane (DCM)/ethanol (EtOH) as co-solvent, and supercritical carbon dioxide as the anti-solvent. The effect of five operating conditions on particle morphology, mass median diameter (Dp50) and HCPT loading is investigated using the single-factor method. The results indicate that HCPT loading can be greatly increased by using DCM/EtOH co-solvent, and the suitable operating conditions for the experimental system are determined. Under suitable conditions, the HCPT loading is 13.3% and Dp50 is 794.5 nm. The drug loaded microparticles are characterized in detail. The SEM images showed that most of the particles were spherical, and PLLA concentration has a major impact on the particle shape. Results of TEM, DSC and XRD indicate that the micronized HCPT is dispersed into the PLLA matrix. For low HCPT loading, most of HCPT existed in the drug loaded microparticles in an amorphous state, but for high HCPT loading, part of the encapsulated drug existed in crystalline form. FT-IR results show that SAS process does not change the chemical structure of HCPT. The result of in vitro drug release test indicated that the crystallinity of HCPT in microparticles affects the control release performance, and the good encapsulated microparticles with higher HCPT loading and higher crystallinity are better.
Xing-jie Liang - One of the best experts on this subject based on the ideXlab platform.
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synergistically enhanced therapeutic effect of a carrier free hcpt dox nanodrug on breast cancer cells through improved cellular drug accumulation
Molecular Pharmaceutics, 2015Co-Authors: Fei Chen, Yuanyuan Zhao, Yuanming Pan, Xiangdong Xue, Xu Zhang, Anil Kumar, Xing-jie LiangAbstract:We are interested in developing systems for simultaneous delivery of two or more chemotherapeutic agents. Simple physical mixing of drugs may reduce the therapeutic effect and cause unexpected or even dangerous side-effects. For example, when 10-hydroxycamptothecin (HCPT) and doxorubicin (DOX) injection solutions are mixed, the curative effect is actually reduced in clinical practice. In this study we demonstrated that when HCPT and DOX are combined into a single nanoparticle, their toxicity to tumor cells in vitro is synergistically enhanced. We used a simple and “green” reprecipitation method to successfully create a carrier-free dual-drug delivery system by self-nanocrystallization of the drug molecules. When HCPT and DOX were coassembled, they formed small, spherical nanodrug particles with a positive surface charge. Cellular uptake of HCPT was improved and nuclear accumulation increased as much as 1.57-fold in comparison to HCPT alone. The carrier-free HCPT/DOX nanoparticles demonstrated enhanced syn...
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Synergistically Enhanced Therapeutic Effect of a Carrier-Free HCPT/DOX Nanodrug on Breast Cancer Cells through Improved Cellular Drug Accumulation
2015Co-Authors: Fei Chen, Yuanyuan Zhao, Yuanming Pan, Xiangdong Xue, Xu Zhang, Anil Kumar, Xing-jie LiangAbstract:We are interested in developing systems for simultaneous delivery of two or more chemotherapeutic agents. Simple physical mixing of drugs may reduce the therapeutic effect and cause unexpected or even dangerous side-effects. For example, when 10-hydroxycamptothecin (HCPT) and doxorubicin (DOX) injection solutions are mixed, the curative effect is actually reduced in clinical practice. In this study we demonstrated that when HCPT and DOX are combined into a single nanoparticle, their toxicity to tumor cells in vitro is synergistically enhanced. We used a simple and “green” reprecipitation method to successfully create a carrier-free dual-drug delivery system by self-nanocrystallization of the drug molecules. When HCPT and DOX were coassembled, they formed small, spherical nanodrug particles with a positive surface charge. Cellular uptake of HCPT was improved and nuclear accumulation increased as much as 1.57-fold in comparison to HCPT alone. The carrier-free HCPT/DOX nanoparticles demonstrated enhanced synergistic cytotoxicity against breast cancer cells in vitro, while an antagonistic effect was observed when HCPT and DOX were directly mixed at high concentration
Xiangtao Wang - One of the best experts on this subject based on the ideXlab platform.
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Amphiphilic Hybrid Dendritic-Linear Molecules as Nanocarriers for Shape-Dependent Antitumor Drug Delivery
2018Co-Authors: Yifei Guo, Meihua Han, Xiangtao Wang, Ting Wang, Shuang Zhao, Zhengqi Dong, Yanhong WangAbstract:Nanoparticles based on hybrid block copolymers had been expected as effective nanocarriers for hydrophobic drug delivery. Herein, the novel dendritic-linear molecules from OEG dendron conjugated with octadecylamine (G2-C18) was designed, synthesized, and further applied as nanocarrier to prepare 10-hydroxycamptothecin (HCPT) nanoparticles via antisolvent precipitation method. It seemed that the feed weight ratio of HCPT vs G2-C18 not only affected the drug-loading content of nanoparticles but also influenced the morphology of HCPT nanoparticles; the morphology of HCPT nanoparticles was changed from nanosphere (NSs) to nanorod (NRs) with increasing the feed weight ratio. Both of HCPT nanoparticles presented good stability and similar drug release profiles, but different anticancer efficacy and cellular uptake mechanism. The cytotoxicity of HCPT NRs was enhanced significant comparing with HCPT NSs, the IC50 value was 2-fold lower than HCPT NSs (p < 0.05). More importantly, HCPT NRs showed apparently higher antitumor activity in vivo, the inhibition rate of HCPT NRs was 1.3-fold higher than HCPT NSs. Based on these results, it suggested that the antitumor activity could be influenced significantly by particle morphology, which should be considered and optimized during the nanocarrier design
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10 hydroxycamptothecin hcpt nanosuspensions stabilized by mpeg1000 hcpt conjugate high stabilizing efficiency and improved antitumor efficacy
International Journal of Nanomedicine, 2017Co-Authors: Linjie Yang, Jingyi Hong, Yifei Guo, Meihua Han, Meifeng Liu, Xiangtao WangAbstract:In this study, polyethylene glycol (PEG)ylated 10-hydroxycamptothecin (mPEG1000-HCPT) was synthesized and used as a stabilizer to prepare 10-hydroxycamptothecin (HCPT) nanosuspensions for their in vitro and in vivo antitumor investigation. The resultant HCPT nanosuspensions (HCPT-NSps) had a very high drug payload of 94.90% (w/w) and a mean particle size of 92.90±0.20 nm with narrow size distribution (polydispersity index of 0.16±0.01). HCPT-NSps could be lyophilized without the need of the addition of any cryoprotectant and then be reconstituted into nanosuspensions of a similar size by direct resuspension in water. HCPT was in crystalline form in HCPT-NSps. Using mPEG1000-HCPT as stabilizer, insoluble camptothecin and 7-ethyl-10-hydroxycamptothecin could also be easily made into nanosuspensions with similar features such as high drug payload, small particle size, and cryoprotectant-free freeze drying. The 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay indicated that the HCPT-NSps had a significantly higher cytotoxicity than HCPT injections, with 3.77 times lower IC50 value against HepG2 cells and 14.1 times lower IC50 value against MCF-7 cells. An in vivo study in H22 tumor-bearing mice after intravenous injection of HCPT-NSps demonstrated that HCPT-NSps significantly improved the antitumor efficacy compared to the commercially available HCPT injections (86.38% vs 34.97%) at the same dose of 5 mg/kg. Even at 1/4 of the dose, HCPT-NSps could also achieve a similar antitumor efficacy to that of HCPT injections. mPEG1000-HCPT may be a highly efficient stabilizer able to provide camptothecin-based drugs, and probably other antitumor agents containing aromatic structure, with unique nanosuspensions or nanocrystals for improved in vivo therapeutic efficacy.
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Hydroxycamptothecin Nanorods Prepared by Fluorescently Labeled Oligoethylene Glycols (OEG) Codendrimer: Antitumor Efficacy in Vitro and in Vivo
2016Co-Authors: Yifei Guo, Meihua Han, Ting Wang, Zhengqi Dong, Yanna Zhao, Chunyan Zhu, Xiangtao WangAbstract:Nanorods based on dendrimers were explored as excellent candidates for nanoscale drug delivery system. In this study, fluorescently labeled PAMAM-b-oligoethylene glycols codendrimer (POC) was utilized as carrier to prepare 10-hydroxycamptothecin (HCPT) loaded nanorods (HCPT NRs) via antisolvent precipitation method augmented by ultrasonication with the optimized drug-loading content (∼90.6%) and positive charged surface. The nanorods presented high stability, and the release of HCPT nanorods showed a sustained release manner and was completed within 48 h. The nanorods presented higher cytotoxicity against HepG2 and 4T1 cells than HCPT injections, and the cellular uptake mechanism was proved to involve clathrin-mediated endocytosis and macropincytosis-dependent endobytosis. Importantly, the HCPT nanorods resulted in strong antitumor efficacy on the H22 liver tumor model, and no significant adverse effects was observed. Besides, in vivo studies also showed that HCPT NRs possessed better tumor accumulation over HCPT injection at the equivalent concentration. According to the high drug-loading content, enhanced antitumor efficacy, and appropriate particle size, HCPT NRs as the safe and efficient drug delivery systems could have potential application for cancer chemotherapy in clinic
Wei Wang - One of the best experts on this subject based on the ideXlab platform.
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preparation of 10 hydroxycamptothecin proliposomes by the supercritical co2 anti solvent process
Chemical Engineering Journal, 2014Co-Authors: Guijin Liu, Wei Wang, Hongdi Wang, Yanbin JiangAbstract:Abstract For this study, 10-Hydroxycamptothecin proliposomes (HCPT-PL) were prepared using the supercritical CO2 anti-solvent process. The mixture of soy lecithin and cholesterol were chosen as liposomal components. The effects of different variables, i.e., the mass ratio of soy lecithin to cholesterol, the mass ratio of HCPT to liposomal components, temperature, pressure and HCPT solution flow rate on HCPT-PL formation were investigated using an OA25 (55) orthogonal experimental design. The formulations were evaluated quantitatively using an overall desirability function, which was calculated based on four assessment indices, i.e., particle size, particle size distribution, drug loading and encapsulation efficiency. SEM and TEM images showed that spherical or clavate HCPT-PL were obtained under different processing conditions, and the drug loading has a significant effect on the morphologies. Under the optimized conditions, clavate HCPT-PL with a mass median diameter of 209.8 ± 38.4 nm, a drug loading of 5.33% and an encapsulation efficiency of 85.28% were obtained. For the optimized HCPT-PL, the residual DCM meets the ICH requirement, and part of the encapsulated HCPT still maintains its crystalline state. And the result of in vitro release rate study showed that HCPT-PL sustained the HCPT release rate successfully, where the drug release of the optimized HCPT-PL followed the first order kinetics, and the drug diffusion mainly corresponded to a Fickian diffusion mechanism during the first 10 h.
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co precipitation of 10 hydroxycamptothecin and poly l lactic acid by supercritical co2 anti solvent process using dichloromethane ethanol co solvent
Journal of Supercritical Fluids, 2013Co-Authors: Wei Wang, Guijin Liu, Yanbin JiangAbstract:Abstract In this study, 10-hydroxycamptothecin (HCPT) and poly ( l -lactic acid) (PLLA) are co-precipitated by the supercritical anti-solvent (SAS) process using a mixture of dichloromethane (DCM)/ethanol (EtOH) as co-solvent, and supercritical carbon dioxide as the anti-solvent. The effect of five operating conditions on particle morphology, mass median diameter (Dp50) and HCPT loading is investigated using the single-factor method. The results indicate that HCPT loading can be greatly increased by using DCM/EtOH co-solvent, and the suitable operating conditions for the experimental system are determined. Under suitable conditions, the HCPT loading is 13.3% and Dp50 is 794.5 nm. The drug loaded microparticles are characterized in detail. The SEM images showed that most of the particles were spherical, and PLLA concentration has a major impact on the particle shape. Results of TEM, DSC and XRD indicate that the micronized HCPT is dispersed into the PLLA matrix. For low HCPT loading, most of HCPT existed in the drug loaded microparticles in an amorphous state, but for high HCPT loading, part of the encapsulated drug existed in crystalline form. FT-IR results show that SAS process does not change the chemical structure of HCPT. The result of in vitro drug release test indicated that the crystallinity of HCPT in microparticles affects the control release performance, and the good encapsulated microparticles with higher HCPT loading and higher crystallinity are better.
