{"title":"7-Methyljuglone-Loaded Poly-(Lactide Co-Glycolide) 纳米粒子的抗结核活性。","authors":"Bianca Diedericks, Anna-Mari Kok, Vusani Mandiwana, Bhavna Gowan Gordhan, Bavesh Davandra Kana, Suprakas Sinha Ray, Namrita Lall","doi":"10.3390/pharmaceutics16111477","DOIUrl":null,"url":null,"abstract":"<p><strong>Background/objectives: </strong>Loading of natural products into poly-(lactide-co-glycolic) acid (PLGA) nanoparticles as drug delivery systems for the treatment of diseases, such as tuberculosis (TB), has been widely explored. The current study investigated the use of PLGA nanoparticles with 7-methyljuglone (7-MJ), an active pure compound, isolated from the roots of <i>Euclea natalensis</i> A. DC.</p><p><strong>Methods: </strong>7-MJ as well as its respective PLGA nanoparticles were tested for their antimycobacterial activity against <i>Mycobacterium smegmatis</i> (<i>M. smegmatis</i>), drug-susceptible <i>Mycobacterium tuberculosis</i> (<i>M. tuberculosis</i>) (H37Rv), and multi-drug-resistant <i>M. tuberculosis</i> (MDR11). The cytotoxicity of 7-MJ as well as its respective PLGA nanoparticles were tested for their cytotoxic effect against differentiated human histiocytic lymphoma (U937) cells. Engulfment studies were also conducted to determine whether the PLGA nanoparticles are taken up by differentiated U937 cells.</p><p><strong>Results: </strong>7-MJ has been shown to have a minimum inhibitory concentration (MIC) value of 1.6 µg/mL against <i>M. smegmatis</i> and multi-drug-resistant <i>M. tuberculosis</i> and 0.4 µg/mL against drug-susceptible <i>M. tuberculosis</i>. Whilst promising, 7-MJ was associated with cytotoxicity, with a fifty percent inhibition concentration (IC<sub>50</sub>) of 3.25 µg/mL on differentiated U937 cells. In order to lower the cytotoxic potential, 7-MJ was loaded into PLGA nanoparticles. The 7-MJ PLGA nanoparticles showed an 80-fold decrease in cytotoxic activity compared to free 7-MJ, and the loaded nanoparticles were successfully taken up by differentiated macrophage-like U937 cells.</p><p><strong>Conclusions: </strong>The results of this study suggested the possibility of improved delivery during TB therapy via the use of PLGA nanoparticles.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"16 11","pages":""},"PeriodicalIF":4.9000,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11597334/pdf/","citationCount":"0","resultStr":"{\"title\":\"Antitubercular Activity of 7-Methyljuglone-Loaded Poly-(Lactide Co-Glycolide) Nanoparticles.\",\"authors\":\"Bianca Diedericks, Anna-Mari Kok, Vusani Mandiwana, Bhavna Gowan Gordhan, Bavesh Davandra Kana, Suprakas Sinha Ray, Namrita Lall\",\"doi\":\"10.3390/pharmaceutics16111477\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background/objectives: </strong>Loading of natural products into poly-(lactide-co-glycolic) acid (PLGA) nanoparticles as drug delivery systems for the treatment of diseases, such as tuberculosis (TB), has been widely explored. The current study investigated the use of PLGA nanoparticles with 7-methyljuglone (7-MJ), an active pure compound, isolated from the roots of <i>Euclea natalensis</i> A. DC.</p><p><strong>Methods: </strong>7-MJ as well as its respective PLGA nanoparticles were tested for their antimycobacterial activity against <i>Mycobacterium smegmatis</i> (<i>M. smegmatis</i>), drug-susceptible <i>Mycobacterium tuberculosis</i> (<i>M. tuberculosis</i>) (H37Rv), and multi-drug-resistant <i>M. tuberculosis</i> (MDR11). The cytotoxicity of 7-MJ as well as its respective PLGA nanoparticles were tested for their cytotoxic effect against differentiated human histiocytic lymphoma (U937) cells. Engulfment studies were also conducted to determine whether the PLGA nanoparticles are taken up by differentiated U937 cells.</p><p><strong>Results: </strong>7-MJ has been shown to have a minimum inhibitory concentration (MIC) value of 1.6 µg/mL against <i>M. smegmatis</i> and multi-drug-resistant <i>M. tuberculosis</i> and 0.4 µg/mL against drug-susceptible <i>M. tuberculosis</i>. Whilst promising, 7-MJ was associated with cytotoxicity, with a fifty percent inhibition concentration (IC<sub>50</sub>) of 3.25 µg/mL on differentiated U937 cells. In order to lower the cytotoxic potential, 7-MJ was loaded into PLGA nanoparticles. The 7-MJ PLGA nanoparticles showed an 80-fold decrease in cytotoxic activity compared to free 7-MJ, and the loaded nanoparticles were successfully taken up by differentiated macrophage-like U937 cells.</p><p><strong>Conclusions: </strong>The results of this study suggested the possibility of improved delivery during TB therapy via the use of PLGA nanoparticles.</p>\",\"PeriodicalId\":19894,\"journal\":{\"name\":\"Pharmaceutics\",\"volume\":\"16 11\",\"pages\":\"\"},\"PeriodicalIF\":4.9000,\"publicationDate\":\"2024-11-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11597334/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.3390/pharmaceutics16111477\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.3390/pharmaceutics16111477","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Antitubercular Activity of 7-Methyljuglone-Loaded Poly-(Lactide Co-Glycolide) Nanoparticles.
Background/objectives: Loading of natural products into poly-(lactide-co-glycolic) acid (PLGA) nanoparticles as drug delivery systems for the treatment of diseases, such as tuberculosis (TB), has been widely explored. The current study investigated the use of PLGA nanoparticles with 7-methyljuglone (7-MJ), an active pure compound, isolated from the roots of Euclea natalensis A. DC.
Methods: 7-MJ as well as its respective PLGA nanoparticles were tested for their antimycobacterial activity against Mycobacterium smegmatis (M. smegmatis), drug-susceptible Mycobacterium tuberculosis (M. tuberculosis) (H37Rv), and multi-drug-resistant M. tuberculosis (MDR11). The cytotoxicity of 7-MJ as well as its respective PLGA nanoparticles were tested for their cytotoxic effect against differentiated human histiocytic lymphoma (U937) cells. Engulfment studies were also conducted to determine whether the PLGA nanoparticles are taken up by differentiated U937 cells.
Results: 7-MJ has been shown to have a minimum inhibitory concentration (MIC) value of 1.6 µg/mL against M. smegmatis and multi-drug-resistant M. tuberculosis and 0.4 µg/mL against drug-susceptible M. tuberculosis. Whilst promising, 7-MJ was associated with cytotoxicity, with a fifty percent inhibition concentration (IC50) of 3.25 µg/mL on differentiated U937 cells. In order to lower the cytotoxic potential, 7-MJ was loaded into PLGA nanoparticles. The 7-MJ PLGA nanoparticles showed an 80-fold decrease in cytotoxic activity compared to free 7-MJ, and the loaded nanoparticles were successfully taken up by differentiated macrophage-like U937 cells.
Conclusions: The results of this study suggested the possibility of improved delivery during TB therapy via the use of PLGA nanoparticles.
PharmaceuticsPharmacology, 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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