• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

新型紫杉烷类 DHA-SBT-1214 在油包水纳米乳剂配方中在荷瘤和非荷瘤小鼠体内的生物分布和药代动力学评价。

Biodistribution and Pharmacokinetic Evaluations of a Novel Taxoid DHA-SBT-1214 in an Oil-in-Water Nanoemulsion Formulation in Naïve and Tumor-Bearing Mice.

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy, Northeastern University, Boston, Massachusetts, 02115-5000, USA.

Institut de Recherche en Cancérologie de Montpellier IRCM, INSERM U1194, ICM, Université de Montpellier, Montpellier, France.

出版信息

Pharm Res. 2018 Mar 8;35(4):91. doi: 10.1007/s11095-018-2349-x.

DOI:10.1007/s11095-018-2349-x
PMID:29520477
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6151135/
Abstract

PURPOSE

The main purpose of this study was to formulate an oil-in-water nanoemulsion of a next generation taxoid DHA-SBT-1214 and evaluate its biodistribution and pharmacokinetics.

METHODS

DHA-SBT-1214 was encapsulated in a fish oil containing nanoemulsion using a high pressure homogenization method. Following morphological characterization of the nanoemulsions, qualitative and quantitative biodistribution was evaluated in naïve and cancer stem cell-enriched PPT-2 human prostate tumor bearing mice.

RESULTS

DHA-SBT-1214 was successfully encapsulated up to 20 mg/ml in the nanoemulsion formulation and had an average oil droplet size of 200 nm. Using a DiR near infra-red dye encapsulated nanoemulsion, we have shown the delivery of nanoemulsion to mouse tumor region. By quantitative analysis, DHA-SBT-1214 encapsulated nanoemulsion demonstrated improved pharmacokinetic properties in plasma and different tissues as compared to its solution form. Furthermore, the nanoemulsions were stable and had slower in vitro drug release compared to its solution form.

CONCLUSIONS

The results from this study demonstrated effective encapsulation of the drug in a nanoemulsion and this nanoemulsion showed sustained plasma levels and enhanced tumor delivery relative to the solution form.

摘要

目的

本研究的主要目的是制备一种新型紫杉烷类药物 DHA-SBT-1214 的水包油纳米乳，并评价其体内分布和药代动力学。

方法

采用高压均质法将 DHA-SBT-1214 包封于含有鱼油的纳米乳中。对纳米乳进行形态学特征描述后，在未处理和富含肿瘤干细胞的 PPT-2 人前列腺肿瘤荷瘤小鼠中进行定性和定量的体内分布评价。

结果

DHA-SBT-1214 成功地包封在纳米乳制剂中，浓度高达 20mg/ml，平均油滴大小为 200nm。使用包封 DiR 近红外染料的纳米乳，我们已经证明了纳米乳向小鼠肿瘤部位的递送。通过定量分析，与溶液形式相比，DHA-SBT-1214 包封的纳米乳在血浆和不同组织中的药代动力学特性得到了改善。此外，与溶液形式相比，纳米乳在体外具有更稳定的性质和更缓慢的药物释放。

结论

本研究结果表明，该药物在纳米乳中的有效包封，与溶液形式相比，纳米乳显示出持续的血浆水平和增强的肿瘤递送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/b1e6a634226b/nihms-986609-f0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/3fb7b38d5c6d/nihms-986609-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/4da59a7a017d/nihms-986609-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/bdf174296261/nihms-986609-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/3e763aca01f3/nihms-986609-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/2258587cccff/nihms-986609-f0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/b1e6a634226b/nihms-986609-f0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/3fb7b38d5c6d/nihms-986609-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/4da59a7a017d/nihms-986609-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/bdf174296261/nihms-986609-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/3e763aca01f3/nihms-986609-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/2258587cccff/nihms-986609-f0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ee9/6151135/b1e6a634226b/nihms-986609-f0008.jpg

相似文献

1
Biodistribution and Pharmacokinetic Evaluations of a Novel Taxoid DHA-SBT-1214 in an Oil-in-Water Nanoemulsion Formulation in Naïve and Tumor-Bearing Mice.新型紫杉烷类 DHA-SBT-1214 在油包水纳米乳剂配方中在荷瘤和非荷瘤小鼠体内的生物分布和药代动力学评价。
Pharm Res. 2018 Mar 8;35(4):91. doi: 10.1007/s11095-018-2349-x.
2
Nanoemulsion formulation of a novel taxoid DHA-SBT-1214 inhibits prostate cancer stem cell-induced tumor growth.新型紫杉烷类化合物DHA-SBT-1214的纳米乳剂配方可抑制前列腺癌干细胞诱导的肿瘤生长。
Cancer Lett. 2017 Oct 10;406:71-80. doi: 10.1016/j.canlet.2017.08.004. Epub 2017 Aug 11.
3
DHA-SBT-1214 Taxoid Nanoemulsion and Anti-PD-L1 Antibody Combination Therapy Enhances Antitumor Efficacy in a Syngeneic Pancreatic Adenocarcinoma Model.DHA-SBT-1214 -taxoid 纳米乳与抗 PD-L1 抗体联合治疗增强了同种异体胰腺腺癌细胞模型的抗肿瘤疗效。
Mol Cancer Ther. 2019 Nov;18(11):1961-1972. doi: 10.1158/1535-7163.MCT-18-1046. Epub 2019 Aug 22.
4
Prostate cancer stem cell-targeted efficacy of a new-generation taxoid, SBT-1214 and novel polyenolic zinc-binding curcuminoid, CMC2.24.新一代紫杉烷 SBT-1214 和新型多烯锌结合姜黄素 CMC2.24 对前列腺癌干细胞的靶向疗效。
PLoS One. 2013 Sep 24;8(9):e69884. doi: 10.1371/journal.pone.0069884. eCollection 2013.
5
A novel camptothecin derivative incorporated in nano-carrier induced distinguished improvement in solubility, stability and anti-tumor activity both in vitro and in vivo.一种负载于纳米载体中的新型喜树碱衍生物在体外和体内均显著提高了溶解度、稳定性及抗肿瘤活性。
Pharm Res. 2009 Apr;26(4):926-35. doi: 10.1007/s11095-008-9795-9. Epub 2008 Dec 2.
6
The effects of oil-in-water nanoemulsion polyethylene glycol surface density on intracellular stability, pharmacokinetics, and biodistribution in tumor bearing mice.水包油纳米乳聚乙二醇表面密度对荷瘤小鼠细胞内稳定性、药代动力学及生物分布的影响。
Pharm Res. 2015 Apr;32(4):1475-85. doi: 10.1007/s11095-014-1553-6. Epub 2014 Oct 28.
7
Folate Modified Long Circulating Nano-Emulsion as a Promising Approach for Improving the Efficiency of Chemotherapy Drugs in Cancer Treatment.叶酸修饰的长循环纳米乳液作为提高化疗药物在癌症治疗中效率的一种有前途的方法。
Pharm Res. 2020 Nov 13;37(12):242. doi: 10.1007/s11095-020-02811-1.
8
Oral delivery of fish oil in oil-in-water nanoemulsion: development, colloidal stability and modulatory effect on in vivo inflammatory induction in mice.水包油型纳米乳中鱼油的口服递送：制剂学研究、胶体稳定性及其对小鼠体内炎症诱导的调节作用。
Biomed Pharmacother. 2021 Jan;133:110980. doi: 10.1016/j.biopha.2020.110980. Epub 2020 Nov 26.
9
Perspectives of nanoemulsion assisted oral delivery of docetaxel for improved chemotherapy of cancer.纳米乳剂辅助口服多西他赛用于改善癌症化疗的前景
Drug Deliv. 2016;23(2):479-88. doi: 10.3109/10717544.2014.920430. Epub 2014 Jun 5.
10
An optimized two-vial formulation lipid nanoemulsion of paclitaxel for targeted delivery to tumor.紫杉醇靶向递释两瓶装优化型脂纳米乳液
Int J Pharm. 2017 Dec 20;534(1-2):308-315. doi: 10.1016/j.ijpharm.2017.10.005. Epub 2017 Oct 3.

引用本文的文献

1
Design, synthesis and SAR study of Fluorine-containing 3rd-generation taxoids.含氟第三代紫杉烷的设计、合成及构效关系研究。
Bioorg Chem. 2022 Feb;119:105578. doi: 10.1016/j.bioorg.2021.105578. Epub 2021 Dec 23.
2
Design, synthesis and SAR study of 3rd-generation taxoids bearing 3-CH, 3-CFO and 3-CHFO groups at the C2-benzoate position.设计、合成和第三代 taxoids 的 SAR 研究 3-CH，3-CFO 和 3-CHFO 基团在 C2-苯甲酸酯位置。
Bioorg Chem. 2020 Jan;95:103523. doi: 10.1016/j.bioorg.2019.103523. Epub 2019 Dec 20.
3
Challenging the CNS Targeting Potential of Systemically Administered Nanoemulsion Delivery Systems: a Case Study with Rapamycin-Containing Fish Oil Nanoemulsions in Mice.挑战全身性给予的纳米乳液递送系统对中枢神经系统的靶向潜力：以载有雷帕霉素的鱼油纳米乳液在小鼠中的研究为例。
Pharm Res. 2019 Jul 11;36(9):134. doi: 10.1007/s11095-019-2667-7.
4
Nanomedicine-based formulations containing ω-3 polyunsaturated fatty acids: potential application in cardiovascular and neoplastic diseases.基于纳米医学的含 ω-3 多不饱和脂肪酸制剂：在心血管和肿瘤疾病中的潜在应用。
Int J Nanomedicine. 2019 Apr 23;14:2809-2828. doi: 10.2147/IJN.S197499. eCollection 2019.

本文引用的文献

1
Mathematical Modeling and Experimental Validation of Nanoemulsion-Based Drug Transport across Cellular Barriers.基于纳米乳剂的药物跨细胞屏障转运的数学建模与实验验证
Pharm Res. 2017 Jul;34(7):1416-1427. doi: 10.1007/s11095-017-2158-7. Epub 2017 Apr 7.
2
Colloidal Instability Fosters Agglomeration of Subvisible Particles Created by Rupture of Gels of a Monoclonal Antibody Formed at Silicone Oil-Water Interfaces.胶体不稳定性促进了由硅油 - 水界面处形成的单克隆抗体凝胶破裂产生的亚可见颗粒的聚集。
J Pharm Sci. 2016 Aug;105(8):2338-48. doi: 10.1016/j.xphs.2016.06.010. Epub 2016 Jul 13.
3
Cancer statistics, 2016.癌症统计数据，2016 年。
CA Cancer J Clin. 2016 Jan-Feb;66(1):7-30. doi: 10.3322/caac.21332. Epub 2016 Jan 7.
4
Prostate cancer incidence in 43 populations worldwide: An analysis of time trends overall and by age group.全球43个地区的前列腺癌发病率：总体及按年龄组划分的时间趋势分析。
Int J Cancer. 2016 Mar 15;138(6):1388-400. doi: 10.1002/ijc.29894. Epub 2015 Nov 27.
5
Gelation of a monoclonal antibody at the silicone oil-water interface and subsequent rupture of the interfacial gel results in aggregation and particle formation.单克隆抗体在硅油-水界面发生凝胶化，随后界面凝胶破裂，导致聚集和颗粒形成。
J Pharm Sci. 2015 Apr;104(4):1282-90. doi: 10.1002/jps.24358. Epub 2015 Jan 30.
6
Immunotherapeutic vitamin E nanoemulsion synergies the antiproliferative activity of paclitaxel in breast cancer cells via modulating Th1 and Th2 immune response.免疫治疗维生素 E 纳米乳通过调节 Th1 和 Th2 免疫应答增强紫杉醇在乳腺癌细胞中的抗增殖活性。
J Control Release. 2014 Dec 28;196:295-306. doi: 10.1016/j.jconrel.2014.10.010. Epub 2014 Oct 22.
7
Formulation development of a novel targeted theranostic nanoemulsion of docetaxel to overcome multidrug resistance in ovarian cancer.一种新型多西他赛靶向治疗诊断纳米乳剂的制剂研发，用于克服卵巢癌的多药耐药性。
Drug Deliv. 2016;23(3):968-80. doi: 10.3109/10717544.2014.923068. Epub 2014 Jun 5.
8
Cancer stem cells in prostate cancer chemoresistance.前列腺癌化疗耐药中的癌症干细胞。
Curr Cancer Drug Targets. 2014;14(3):225-40. doi: 10.2174/1568009614666140328152459.
9
Mucoadhesive microparticulate drug delivery system of curcumin against Helicobacter pylori infection: Design, development and optimization.姜黄素抗幽门螺杆菌感染的黏膜黏附微粒给药系统：设计、开发与优化。
J Adv Pharm Technol Res. 2014 Jan;5(1):48-56. doi: 10.4103/2231-4040.126996.
10
CNS delivery and pharmacokinetic evaluations of DALDA analgesic peptide analog administered in Nano-sized oil-in-water emulsion formulation.经纳米级油包水乳剂配方给药的 DALDA 镇痛肽类似物的中枢神经系统传递和药代动力学评估。
Pharm Res. 2014 May;31(5):1315-24. doi: 10.1007/s11095-013-1252-8. Epub 2013 Dec 3.