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| 1 | A nano-cocrystal strategy to improve the dissolution rate and oral bioavailability of baicalein显示文摘Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE. | Jiaxin Pi Shuya Wang Wen Li Dereje Kebebe Ying Zhang Bing Zhang Dongli Qi Pan Guo Nan Li Zhidong Liu | 2019 | Asian Journal of Pharmaceutical Sciences2019，14，2： | 12 |
| 2 | Research progress of in-situ gelling ophthalmic drug delivery system显示文摘Blindness and vision impairment are the most devastating global health problems resulting in a substantial economic and social burden.Delivery of drug to particular parts of the anterior or posterior segment has been a major challenge due to various protective barriers and elimination mechanisms associated with the unique anatomical and physiological nature of the ocular system.Drug administration to the eye by conventional delivery systems results in poor ocular bioavailability(<5%).The designing of a novel approach for a safe,simple,and effective ocular drug delivery is a major concern and requires innovative strategies to combat the problem.Over the past decades,several novel approaches involving different strategies have been developed to improve the ocular delivery system.Among these,the ophthalmic in-situ gel has attained a great attention over the past few years.This review discussed and summarized the recent and the promising research progress of in-situ gelling in ocular drug delivery system. | Yumei Wu Yuanyuan Liu Xinyue Li Dereje Kebebe Bing Zhang Jing Ren Jun Lu Jiawei Li Shouying Du Zhidong Liu | 2019 | Asian Journal of Pharmaceutical Sciences2019，14，1： | 7 |
| 3 | 单克隆抗体OX26修饰的丹酚酸B/黄芩苷纳米结构脂质载体研究显示文摘目的制备转铁蛋白受体单克隆抗体OX26修饰的丹酚酸B/黄芩苷纳米结构脂质载体(Sal B/BA-NLC),并对其进行表征和细胞摄入研究。方法采用乳化-固化法制备Sal B/BA-NLC,用2-亚氨基硫烷盐酸盐(2-iminothiolane hydrochloride)将OX26进行硫醇化后连接于Sal B/BA-NLC表面,以形态、粒径、Zeta电位及包封率等为评价指标考察其理化性质,并用差示扫描量热法(DSC)与核磁共振波谱(NMR)进行验证。以香豆素-6(coumarin-6,C6)为荧光探针,代替黄芩苷和丹酚酸B制备制剂,利用高内涵成像仪考察脑微血管内皮细胞bEnd.3对其的摄入情况。结果所制备的OX26修饰的Sal B/BA-NLC粒径为(27.50±3.37)nm,PDI为0.39±0.04,Zeta电位为(-7.06±1.85)m V。DSC与NMR结果表明,药物是以无定形的形式存在于纳米结构脂质载体中。细胞摄入结果显示,当考察时间一致时,bEnd.3细胞摄入3组溶液体系的荧光强度为OX26-C6-NLC>C6-NLC>C6-SL。结论所制备的OX26修饰的Sal B/BA-NLC粒径较小、分布均匀,且包封率高。与溶液组和未修饰的NLC组相比,OX26修饰的NLC组具有更高的摄入量。 | 吴玉梅 李新悦 张谦 刘静静 Dereje KEBEBE 郭盼 刘志东 | 2018 | 中草药2018，49，12： | 5 |
| 4 | Pharmacokinetic study of ginsenoside Re after vaginal administration in rabbits by UPLC-MS/MS determination显示文摘Objective: A selective and sensitive ultra performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method was employed to study the pharmacokinetics of ginsenoside Re(GRe) in rabbits after vaginal administration of Xiaomi suppository to evaluate the systemic exposure of the suppository for the local treatment.Methods: Chromatographic separation was on an ACQUITY UPLC?BEH C18 column, and acetonitrile-0.1%formic acid was used as mobile phase in gradient elution. The plasma samples were deproteinized by acetonitrile, and the pharmacokinetic parameters were calculated by Winnonlin 6.4.Results: Calibration curve of GRe showed a good linearity over the concentration range from 5 ng/mL to500 ng/mL(r = 0.9999). The low limit of quantification of 5 ng/m L could satisfy the experimental requirement. The intra-day and inter-day precision of GRe at three concentrations were less than 1.96%, and the average recoveries of GRe were more than 64.0%. The pharmacokinetic parameters for vaginal administration were as follows: Tm ax, 0.5 h; C max, 20.88 ng/mL; AUC0-t, 64.71 h · ng/mL and the residence time was3.06 h. By using deconvolution calculation method, the cumulative absorption fraction of GRe was about0.89%.Conclusion: The systemic exposure of GRe was minimal after vaginal administration of Xiaomi suppository. | Xu Han Ying Zhang Jia-xin Pi Dereje Kebebe Bing Zhang Shu-ya Wang Bo-ying Liu Jing Ren Zhi-dong Liu | 2018 | Chinese Herbal Medicines2018，10，3： | 2 |
| 5 | 用于眼后段持续给药的原位pH触发凝胶系统中三七总皂苷的研制与评价显示文摘目的:为三七总皂苷(PNS)在pH敏感型原位凝胶中的研究及相关制剂的开发和改进奠定基础。方法:我们使用Carbopol■940(一种常用的pH敏感聚合物)和增稠剂羟丙基甲基纤维素(HPMC E4M)作为眼用凝胶基质来制备PNS眼用原位凝胶。此外,通过评估凝胶能力和体外释放研究结果进行配方优化。还进行了体外(角膜渗透、流变学和稳定性)和体内(眼部刺激和玻璃体的初步药代动力学)研究。结果:研究表明,含有三七总皂苷的原位凝胶系统显示出药物的缓释性,使其成为改善眼后生物利用度的理想眼部给药系统。结论:本研究为原位pH触发凝胶中PNS的研究及相关制剂的开发和改进奠定了基础。同时,它将传统中药与现代原位凝胶技术相结合,为糖尿病视网膜病变等后眼病的治疗提供了新的方向。 | 卢鹏 王仁兴 岳兴 高艳泉 张清清 邢斌 张颖 于昌祥 蔡新富 尚强 Dereje Kebebe 皮嘉欣 刘志东 | 2021 | Acupuncture and Herbal Medicine2021，1，2： | 1 |
| 6 | Construction of curcumin-loaded micelles and evaluation of the anti-tumor effect based on angiogenesis显示文摘Objective:Inhibition of tumor angiogenesis has become a new targeted tumor therapy.In this study,we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-targeting peptide NGR.Methods:The targeted polymer poly(ethylene glycol)-b-poly(lactide-co-glycolide)(PEG-PLGA)modified with Asn–Gly–Arg(NGR)peptide was prepared and characterized by 1H nuclear magnetic resonance and Fourier-transform infrared spectrometry.NGR-PEG-PLGA was used to construct curcumin(Cur)-loaded micelles by the solvent evaporation method.The physicochemical properties of the micelles were also investigated.Additionally,we evaluated the antitumor efficacy of the polymer micelles(PM)using in vitro cytology experiments and in vivo animal studies.Results:The particle size of Cur-NGR-PM was 139.70±2.51 nm,and the drug-loading capacity was 14.37±0.06%.In vitro cytological evaluation showed that NGR-modified micelles showed higher cellular uptake through receptor-mediated endocytosis pathways than did unmodified micelles,leading to the apoptosis of tumor cells.Then,in vivo antitumor experiments showed that the modified micelles significantly inhibited tumor growth and were safe.Conclusions:NGR-modified micelles significantly optimized the therapeutic efficacy of Cur.This strategy offers a viable avenue for cancer treatment. | Rui Liu Zhongyan Liu Xueli Guo Dereje Kebebe Jiaxin Pi Pan Guo | 2023 | Acupuncture and Herbal Medicine2023，3，4： | 0 |
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