脂质体辅助给药系统的制备:阿霉素和9-(n -哌嗪基)-5-甲基-12(H)-喹诺[3,4-b][1,4]苯并噻唑氯与人血清白蛋白的包封和释放谱

IF 6.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Pharmaceutics Pub Date : 2025-02-06 DOI:10.3390/pharmaceutics17020202
Danuta Pentak, Violetta Kozik, Andrzej Zieba, Marlena Paździor-Heiske, Aleksandra Szymczyk, Josef Jampilek, Andrzej Bak
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引用次数: 0

摘要

背景/目的:本研究的主要目的是制备一种以市售药物多柔比星(DOX)为基础的脂质体给药系统和具有良好抗癌活性的出芽剂9-(n -哌嗪基)-5-甲基-12(H)-喹诺[3,4-b][1,4]苯并噻唑氯(9- pbthacl)。方法:采用分光光度法,对基于双棕榈酰磷脂酰胆碱(DPPC)的新型脂质体复合物(L)与人血清白蛋白(HSA)及其失败类似物(dHSA)的药物包封和释放特性进行了细致的研究。结果:考察了操作参数(温度和pH)对脂质体/药物(s)/(d)HSA,即[LDPPC/9-PBThACl/DOX]:(d)HSA体系以及磷脂双分子层极性的影响。为了比较实验结果,采用数学模型确定了控制脂质体药物释放/潜在药物释放过程的分析因素。所观察到的药物包封和释放谱的变化是由于脂质体偶联物与人血浆蛋白的结合。结论:环境pH值的变化直接影响药物在脂质体中的包封率和药物释放效率。此外,采用主成分分析(PCA)和层次聚类分析(HCA)对脂质体组合的分组趋势进行了研究。最后,方差分析(ANOVA)证实了pH缓冲和温度变化因素对脂质体偶联物药物释放特性的统计学影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Preparing a Liposome-Aided Drug Delivery System: The Entrapment and Release Profiles of Doxorubicin and 9-(N-Piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium Chloride with Human Serum Albumin.

Background/Objectives: The principal aim of this work was to prepare a liposomal drug delivery system based on the commercial drug doxorubicin (DOX) and a budding agent with promising anticancer activity, 9-(N-piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). Methods: A spectrophotometric methodology was used to meticulously investigate the drug entrapment and release characteristics of the new liposomal complexes (L) based on dipalmitoylphosphatidylcholine (DPPC) with human serum albumin (HSA) and its defeated analog (dHSA). Results: The impact of the operational parameters (temperature and pH) on the liposome/drug(s)/(d)HSA, namely [LDPPC/9-PBThACl/DOX ]:(d)HSA] systems, as well as the polarity of the phospholipid bilayer, was examined. In order to compare the experimental findings, mathematical models were employed to specify the analytical factors controlling the process of drug release/potential drug release from liposomes. The observed variations in the drug encapsulation and release profiles were due to the combination of liposomal conjugates with human plasma protein. Conclusions: It was proven that changes in the environmental pH directly affect the percentage of drug entrapment in liposomes and the medicine release efficiency. Moreover, the grouping tendency of the liposomal combinations was investigated using a principal component analysis (PCA) and a hierarchical clustering analysis (HCA). Finally, an analysis of variance (ANOVA) confirmed the statistical impact of pH buffering and changing temperature factors on the drug release characteristics of liposomal conjugates.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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