作为肿瘤治疗潜在纳米载体的白蜡修饰阿霉素脂质体的制备、体外表征及药动学评价

M. Fazel, Marjan Daeihamed, M. Osouli, Ameneh Almasi, A. Haeri, S. Dadashzadeh
{"title":"作为肿瘤治疗潜在纳米载体的白蜡修饰阿霉素脂质体的制备、体外表征及药动学评价","authors":"M. Fazel, Marjan Daeihamed, M. Osouli, Ameneh Almasi, A. Haeri, S. Dadashzadeh","doi":"10.22037/IJPR.2018.2373","DOIUrl":null,"url":null,"abstract":"The aim of current study was to investigate the effect of Brij decoration of liposomes on in-vitro and in-vivo characteristics of the nanocarriers. Two hydrophilic Brij surfactants (Brij 35 and Brij 78) with almost similar molecular weight but differing in acyl chain were incorporated into liposomal bilayers at two percentages (5% and 10%). Conventional liposomes (CL) containing egg phosphatidylcholine and cholesterol as well as Brij-enriched liposomal dispersions were prepared and characterized. In-vivo pharmacokinetics of various liposomal formulations and drug solution (six groups) was studied after intravenous administration to rats. Conventional and Brij enriched doxorubicin (DOX) liposomes had small size within 82-97 nm and showed homogenous distribution (PDI < 0.1). Drug encapsulation was higher than 97% in all liposomes. The drug release profiles proved sustained DOX release from various formulations. Based on the results of in-vivo studies, all five liposomes increased drug exposure and plasma concentration in comparison to free drug. However, DOX liposomes enriched with 5% of either Brij 35 or Brij 78 showed higher AUC values and lower clearance. Overall, Brij surfactants (5% of bilayer lipids) could be potentially used to improve liposomal pharmacokinetic parameters.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":"89 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2018-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"7","resultStr":"{\"title\":\"Preparation, In-Vitro Characterization and Pharmacokinetic Evaluation of Brij Decorated Doxorubicin Liposomes as a Potential Nanocarrier for Cancer Therapy\",\"authors\":\"M. Fazel, Marjan Daeihamed, M. Osouli, Ameneh Almasi, A. Haeri, S. Dadashzadeh\",\"doi\":\"10.22037/IJPR.2018.2373\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The aim of current study was to investigate the effect of Brij decoration of liposomes on in-vitro and in-vivo characteristics of the nanocarriers. Two hydrophilic Brij surfactants (Brij 35 and Brij 78) with almost similar molecular weight but differing in acyl chain were incorporated into liposomal bilayers at two percentages (5% and 10%). Conventional liposomes (CL) containing egg phosphatidylcholine and cholesterol as well as Brij-enriched liposomal dispersions were prepared and characterized. In-vivo pharmacokinetics of various liposomal formulations and drug solution (six groups) was studied after intravenous administration to rats. Conventional and Brij enriched doxorubicin (DOX) liposomes had small size within 82-97 nm and showed homogenous distribution (PDI < 0.1). Drug encapsulation was higher than 97% in all liposomes. The drug release profiles proved sustained DOX release from various formulations. Based on the results of in-vivo studies, all five liposomes increased drug exposure and plasma concentration in comparison to free drug. However, DOX liposomes enriched with 5% of either Brij 35 or Brij 78 showed higher AUC values and lower clearance. Overall, Brij surfactants (5% of bilayer lipids) could be potentially used to improve liposomal pharmacokinetic parameters.\",\"PeriodicalId\":416671,\"journal\":{\"name\":\"Iranian Journal of Pharmaceutical Research : IJPR\",\"volume\":\"89 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2018-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"7\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Iranian Journal of Pharmaceutical Research : IJPR\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.22037/IJPR.2018.2373\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Iranian Journal of Pharmaceutical Research : IJPR","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.22037/IJPR.2018.2373","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 7

摘要

本研究旨在探讨脂质体的Brij修饰对纳米载体体内外特性的影响。两种分子量相近但酰基链不同的亲水性Brij表面活性剂Brij 35和Brij 78分别以5%和10%的比例掺入脂质体双分子层。制备了含有卵磷脂酰胆碱和胆固醇的常规脂质体(CL)以及富含brij的脂质体分散体并进行了表征。研究了不同脂质体制剂和药物溶液(6组)在大鼠静脉给药后的体内药代动力学。常规和Brij富集的阿霉素脂质体在82 ~ 97 nm范围内体积较小,分布均匀(PDI < 0.1)。所有脂质体的药物包封率均大于97%。药物释放谱证明了各种制剂的持续DOX释放。根据体内研究的结果,与游离药物相比,所有五种脂质体都增加了药物暴露和血浆浓度。然而,含有5% Brij 35或Brij 78的DOX脂质体显示出更高的AUC值和更低的清除率。总的来说,Brij表面活性剂(占双层脂质的5%)可能潜在地用于改善脂质体药代动力学参数。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation, In-Vitro Characterization and Pharmacokinetic Evaluation of Brij Decorated Doxorubicin Liposomes as a Potential Nanocarrier for Cancer Therapy
The aim of current study was to investigate the effect of Brij decoration of liposomes on in-vitro and in-vivo characteristics of the nanocarriers. Two hydrophilic Brij surfactants (Brij 35 and Brij 78) with almost similar molecular weight but differing in acyl chain were incorporated into liposomal bilayers at two percentages (5% and 10%). Conventional liposomes (CL) containing egg phosphatidylcholine and cholesterol as well as Brij-enriched liposomal dispersions were prepared and characterized. In-vivo pharmacokinetics of various liposomal formulations and drug solution (six groups) was studied after intravenous administration to rats. Conventional and Brij enriched doxorubicin (DOX) liposomes had small size within 82-97 nm and showed homogenous distribution (PDI < 0.1). Drug encapsulation was higher than 97% in all liposomes. The drug release profiles proved sustained DOX release from various formulations. Based on the results of in-vivo studies, all five liposomes increased drug exposure and plasma concentration in comparison to free drug. However, DOX liposomes enriched with 5% of either Brij 35 or Brij 78 showed higher AUC values and lower clearance. Overall, Brij surfactants (5% of bilayer lipids) could be potentially used to improve liposomal pharmacokinetic parameters.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信