Ali Al-Samydai, Moath Al Qaraleh, Lidia K Al-Halaseh, Maha N Abu Hajleh, Simone Carradori, Maryam Abdulmaged, Rand Kareem, Hasanain Alzaidi, Mohamad Ak Mousa, Yusuf Al-Hiari, Hamdi Nsairat, Walhan Alshaer
{"title":"优化的芦丁聚乙二醇化纳米脂质体模型对PANK1和MCF7细胞系具有显著的选择性。","authors":"Ali Al-Samydai, Moath Al Qaraleh, Lidia K Al-Halaseh, Maha N Abu Hajleh, Simone Carradori, Maryam Abdulmaged, Rand Kareem, Hasanain Alzaidi, Mohamad Ak Mousa, Yusuf Al-Hiari, Hamdi Nsairat, Walhan Alshaer","doi":"10.2174/0118715206231749241209073759","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>This study aims to enhance the delivery of polyphenols using nanotechnology.</p><p><strong>Objective: </strong>To develop and evaluate liposomal formulations for improved delivery and stability of polyphenols, specifically focusing on Rutin.</p><p><strong>Methods: </strong>Liposomal formulations were meticulously prepared via the Thin-Film Hydration method. Comprehensive physical characterization was conducted, including stability assessments using Dynamic Light Scattering (DLS) and Thermogravimetric Analysis (TGA). The free radical scavenging activity was measured using the DPPH• assay, and MTT cell viability assays were performed to assess cytotoxicity.</p><p><strong>Results: </strong>The results demonstrated a significant reduction in nanoparticle size from 123 nm to 116 nm and an increase in charge from -14 to -22 with rising Rutin concentrations. The formulation achieved enhanced homogeneity at a Rutin concentration of 2.0 mg/mL and showed higher stability. Incorporating Rutin improved the formulation's stability over 30 days, as evidenced by a decrease in the Differential Scanning Calorimetry peak temperature from 58.65 °C to 54.42 °C. Rutin-loaded and co-loaded nanoliposomes exhibited remarkable selectivity against PANK1 and MCF7 cell lines, with IC50 values of 2.13±0.35 μg/mL and 4.75±0.19 μg/mL, respectively.</p><p><strong>Conclusion: </strong>PEGylated Rutin-loaded nanoliposomes offer a promising platform for biodegradable and biocompatible drug delivery systems, enhancing the bioavailability, solubility, and stability of the polyphenols.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6000,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Optimized Rutin-incorporating PEGylated Nanoliposomes as a Model with Remarkable Selectivity Against PANC1 and MCF7 Cell Lines\",\"authors\":\"Ali Al-Samydai, Moath Al Qaraleh, Lidia K Al-Halaseh, Maha N Abu Hajleh, Simone Carradori, Maryam Abdulmaged, Rand Kareem, Hasanain Alzaidi, Mohamad Ak Mousa, Yusuf Al-Hiari, Hamdi Nsairat, Walhan Alshaer\",\"doi\":\"10.2174/0118715206231749241209073759\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>This study aims to enhance the delivery of polyphenols using nanotechnology.</p><p><strong>Objective: </strong>To develop and evaluate liposomal formulations for improved delivery and stability of polyphenols, specifically focusing on Rutin.</p><p><strong>Methods: </strong>Liposomal formulations were meticulously prepared via the Thin-Film Hydration method. Comprehensive physical characterization was conducted, including stability assessments using Dynamic Light Scattering (DLS) and Thermogravimetric Analysis (TGA). The free radical scavenging activity was measured using the DPPH• assay, and MTT cell viability assays were performed to assess cytotoxicity.</p><p><strong>Results: </strong>The results demonstrated a significant reduction in nanoparticle size from 123 nm to 116 nm and an increase in charge from -14 to -22 with rising Rutin concentrations. The formulation achieved enhanced homogeneity at a Rutin concentration of 2.0 mg/mL and showed higher stability. Incorporating Rutin improved the formulation's stability over 30 days, as evidenced by a decrease in the Differential Scanning Calorimetry peak temperature from 58.65 °C to 54.42 °C. Rutin-loaded and co-loaded nanoliposomes exhibited remarkable selectivity against PANK1 and MCF7 cell lines, with IC50 values of 2.13±0.35 μg/mL and 4.75±0.19 μg/mL, respectively.</p><p><strong>Conclusion: </strong>PEGylated Rutin-loaded nanoliposomes offer a promising platform for biodegradable and biocompatible drug delivery systems, enhancing the bioavailability, solubility, and stability of the polyphenols.</p>\",\"PeriodicalId\":7934,\"journal\":{\"name\":\"Anti-cancer agents in medicinal chemistry\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":2.6000,\"publicationDate\":\"2025-01-21\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Anti-cancer agents in medicinal chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/0118715206231749241209073759\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anti-cancer agents in medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0118715206231749241209073759","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Optimized Rutin-incorporating PEGylated Nanoliposomes as a Model with Remarkable Selectivity Against PANC1 and MCF7 Cell Lines
Background: This study aims to enhance the delivery of polyphenols using nanotechnology.
Objective: To develop and evaluate liposomal formulations for improved delivery and stability of polyphenols, specifically focusing on Rutin.
Methods: Liposomal formulations were meticulously prepared via the Thin-Film Hydration method. Comprehensive physical characterization was conducted, including stability assessments using Dynamic Light Scattering (DLS) and Thermogravimetric Analysis (TGA). The free radical scavenging activity was measured using the DPPH• assay, and MTT cell viability assays were performed to assess cytotoxicity.
Results: The results demonstrated a significant reduction in nanoparticle size from 123 nm to 116 nm and an increase in charge from -14 to -22 with rising Rutin concentrations. The formulation achieved enhanced homogeneity at a Rutin concentration of 2.0 mg/mL and showed higher stability. Incorporating Rutin improved the formulation's stability over 30 days, as evidenced by a decrease in the Differential Scanning Calorimetry peak temperature from 58.65 °C to 54.42 °C. Rutin-loaded and co-loaded nanoliposomes exhibited remarkable selectivity against PANK1 and MCF7 cell lines, with IC50 values of 2.13±0.35 μg/mL and 4.75±0.19 μg/mL, respectively.
Conclusion: PEGylated Rutin-loaded nanoliposomes offer a promising platform for biodegradable and biocompatible drug delivery systems, enhancing the bioavailability, solubility, and stability of the polyphenols.
期刊介绍：
Formerly: Current Medicinal Chemistry - Anti-Cancer Agents.
Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents.
Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication.
Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.
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