Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study
<b>Objectives:</b> This work aimed to develop and investigate liposomes incorporating Rhein (Lip-Rh) into the liposomal membrane to enhance the compound’s water solubility and oral bioavailability. <b>Methods:</b> Liposomes were produced by the thin lipid film technique, with...
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| Format: | Article |
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MDPI AG
2025-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/17/3/307 |
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| author | Silviu Iulian Filipiuc Natalia Simionescu Gabriela Dumitrița Stanciu Adina Coroaba Narcisa Laura Marangoci Leontina Elena Filipiuc Mariana Pinteala Cristina Mariana Uritu Bogdan Ionel Tamba |
| author_facet | Silviu Iulian Filipiuc Natalia Simionescu Gabriela Dumitrița Stanciu Adina Coroaba Narcisa Laura Marangoci Leontina Elena Filipiuc Mariana Pinteala Cristina Mariana Uritu Bogdan Ionel Tamba |
| author_sort | Silviu Iulian Filipiuc |
| collection | DOAJ |
| description | <b>Objectives:</b> This work aimed to develop and investigate liposomes incorporating Rhein (Lip-Rh) into the liposomal membrane to enhance the compound’s water solubility and oral bioavailability. <b>Methods:</b> Liposomes were produced by the thin lipid film technique, with a phosphatidylcholine-to-cholesterol molar ratio of 5:1, dissolved in chloroform and methanol, and thereafter hydrated with ultrapure water and subjected to sonication. The resultant liposomes were studied from a physicochemical perspective using DLS, zeta potential, STEM, UV–Vis, and fluorescence spectroscopies, while oral bioavailability was assessed by fluorescence imaging. Additionally, cell viability assays were performed on tumour cells (MCF-7) in comparison to normal cells (HGFs). <b>Results:</b> The resultant nanoparticles exhibited relatively uniform sizes and narrow size distribution. In vivo fluorescence imaging studies performed on Wistar rats demonstrated significantly enhanced oral bioavailability for Lip-Rh, with rapid absorption into the bloodstream observed one hour after administration, in contrast to the free compound dissolved in vegetable oil. Cell viability assays demonstrated higher cytotoxicity of Lip-Rh towards MCF-7 cells compared to HGF cells, highlighting the selective therapeutic potential of the product. Moreover, we determined that the optimal dose of Rhein per kilogram of body weight, when encapsulated in liposomes, is approximately 2.5 times less than when Rhein is delivered in its unencapsulated form. <b>Conclusions:</b> Lip-Rh is a promising candidate for oncological treatments, presenting three key advantages: increased cytotoxicity towards tumour cells, protection of normal tissues, and the practicality of oral delivery. Additional investigation is required to explore its application in anticancer therapy, whether as monotherapy or as a complementary treatment. |
| format | Article |
| id | doaj-art-7dbc4b83d24d4f4987247e07a547b147 |
| institution | DOAJ |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj-art-7dbc4b83d24d4f4987247e07a547b1472025-08-20T02:42:24ZengMDPI AGPharmaceutics1999-49232025-02-0117330710.3390/pharmaceutics17030307Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution StudySilviu Iulian Filipiuc0Natalia Simionescu1Gabriela Dumitrița Stanciu2Adina Coroaba3Narcisa Laura Marangoci4Leontina Elena Filipiuc5Mariana Pinteala6Cristina Mariana Uritu7Bogdan Ionel Tamba8Centre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iasi, RomaniaCentre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iasi, RomaniaAdvanced Center for Research and Development in Experimental Medicine “Prof. Ostin C. Mungiu”, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, RomaniaCentre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iasi, RomaniaCentre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iasi, RomaniaAdvanced Center for Research and Development in Experimental Medicine “Prof. Ostin C. Mungiu”, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, RomaniaCentre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iasi, RomaniaCentre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iasi, RomaniaAdvanced Center for Research and Development in Experimental Medicine “Prof. Ostin C. Mungiu”, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, Romania<b>Objectives:</b> This work aimed to develop and investigate liposomes incorporating Rhein (Lip-Rh) into the liposomal membrane to enhance the compound’s water solubility and oral bioavailability. <b>Methods:</b> Liposomes were produced by the thin lipid film technique, with a phosphatidylcholine-to-cholesterol molar ratio of 5:1, dissolved in chloroform and methanol, and thereafter hydrated with ultrapure water and subjected to sonication. The resultant liposomes were studied from a physicochemical perspective using DLS, zeta potential, STEM, UV–Vis, and fluorescence spectroscopies, while oral bioavailability was assessed by fluorescence imaging. Additionally, cell viability assays were performed on tumour cells (MCF-7) in comparison to normal cells (HGFs). <b>Results:</b> The resultant nanoparticles exhibited relatively uniform sizes and narrow size distribution. In vivo fluorescence imaging studies performed on Wistar rats demonstrated significantly enhanced oral bioavailability for Lip-Rh, with rapid absorption into the bloodstream observed one hour after administration, in contrast to the free compound dissolved in vegetable oil. Cell viability assays demonstrated higher cytotoxicity of Lip-Rh towards MCF-7 cells compared to HGF cells, highlighting the selective therapeutic potential of the product. Moreover, we determined that the optimal dose of Rhein per kilogram of body weight, when encapsulated in liposomes, is approximately 2.5 times less than when Rhein is delivered in its unencapsulated form. <b>Conclusions:</b> Lip-Rh is a promising candidate for oncological treatments, presenting three key advantages: increased cytotoxicity towards tumour cells, protection of normal tissues, and the practicality of oral delivery. Additional investigation is required to explore its application in anticancer therapy, whether as monotherapy or as a complementary treatment.https://www.mdpi.com/1999-4923/17/3/307Rheinfluorescence imagingliposomal RheinRhein biodistributionRhein cytotoxicity |
| spellingShingle | Silviu Iulian Filipiuc Natalia Simionescu Gabriela Dumitrița Stanciu Adina Coroaba Narcisa Laura Marangoci Leontina Elena Filipiuc Mariana Pinteala Cristina Mariana Uritu Bogdan Ionel Tamba Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study Pharmaceutics Rhein fluorescence imaging liposomal Rhein Rhein biodistribution Rhein cytotoxicity |
| title | Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study |
| title_full | Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study |
| title_fullStr | Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study |
| title_full_unstemmed | Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study |
| title_short | Fluorescent Rhein-Loaded Liposomes for In Vivo Biodistribution Study |
| title_sort | fluorescent rhein loaded liposomes for in vivo biodistribution study |
| topic | Rhein fluorescence imaging liposomal Rhein Rhein biodistribution Rhein cytotoxicity |
| url | https://www.mdpi.com/1999-4923/17/3/307 |
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