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

<b>Background/Objectives:</b> 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-(<i>N</i>-piperazinyl)-5-methyl-12(<i>H</i>)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). <b>Methods</b>: 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). <b>Results</b>: The impact of the operational parameters (temperature and pH) on the liposome/drug(s)/(d)HSA, namely [L<sub>DPPC/9-PBThACl/DOX</sub> ]:(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. <b>Conclusions</b>: 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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Publication Details

Journal
Pharmaceutics
Published
2025-02-06
DOI
https://doi.org/10.3390/pharmaceutics17020202
Citations
2
Primary Topic
Nanoparticle-Based Drug Delivery
Type
article
Field-Weighted Citation Impact
1.19

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article

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

Anthony Szymczyk, Andrzej Bąk, Danuta Pentak, Josef Jampílek et al.
2 citations
Pharmaceutics
Nanoparticle-Based Drug Delivery
1.19
article

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

Anthony Szymczyk, Andrzej Bąk, Danuta Pentak, Josef Jampílek, Andrzej Zięba, Violetta Kozik, Marlena Paździor-Heiske
article en
2 citations

Abstract

<b>Background/Objectives:</b> 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-(<i>N</i>-piperazinyl)-5-methyl-12(<i>H</i>)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). <b>Methods</b>: 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). <b>Results</b>: The impact of the operational parameters (temperature and pH) on the liposome/drug(s)/(d)HSA, namely [L<sub>DPPC/9-PBThACl/DOX</sub> ]:(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. <b>Conclusions</b>: 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.

PharmaceuticsVol. 17(2)
Medical University of Silesia (PL), University of Opole (PL), University of Silesia in Katowice (PL)
Śląski Uniwersytet Medyczny w Katowicach
Good health and well-being
Openalex Percentile: Top 25%
Nanoparticle-Based Drug Delivery
1.19
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