Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis
<b>Background/Objectives</b>: Pentacyclic triterpenoids are increasingly studied as anticancer agents with many advantages compared to synthetic chemotherapeutics. The aim of this study was to prepare liposomal and nanostructured lipid formulations including a standardized extract of sil...
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2024-12-01
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| author | Dumitriţa Rugină Mihai Adrian Socaciu Madalina Nistor Zorita Diaconeasa Mihai Cenariu Flaviu Alexandru Tabaran Carmen Socaciu |
| author_facet | Dumitriţa Rugină Mihai Adrian Socaciu Madalina Nistor Zorita Diaconeasa Mihai Cenariu Flaviu Alexandru Tabaran Carmen Socaciu |
| author_sort | Dumitriţa Rugină |
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| description | <b>Background/Objectives</b>: Pentacyclic triterpenoids are increasingly studied as anticancer agents with many advantages compared to synthetic chemotherapeutics. The aim of this study was to prepare liposomal and nanostructured lipid formulations including a standardized extract of silver birch (<i>Betula pendula</i>) outer bark (TTs) and to evaluate their potential as anticancer agents in vitro, using Melanoma B16-F10 and Walker carcinoma cells. <b>Methods</b>: Appropriate solvents were selected for efficient TTs extraction, and original recipes were used to obtain Pegylated liposomes and nanolipid complexes with entrapped TTs, comparative to pure standards (betulinic acid and doxorubicin) in similar conditions. The composition, morphology, and sizes of all nanoformulations were checked by high-performance liquid chromatography/mass spectrometry, Transmission Electronic Microscopy, and Diffraction Light Scattering. The entrapment efficiency and its impact on cell viability, cell cycle arrest, and apoptosis by flow cytometry was also measured on both cancer cell lines. <b>Conclusions:</b> The standardized TTs, including betulin, lupeol, and betulinic acid, showed good stability and superior activity compared to pure betulinic acid. According to experimental data, TTs showed good entrapment in liposomal and NLC nanoformulations, both delivery systems including natural, biodegradable ingredients and enhanced bioavailability. The apoptosis and necrosis effects were more pronounced for TTs liposomal formulations in both types of cancer cells, with lower cytotoxicity compared to Doxorubicin, and can be correlated with their increased bioavailability. |
| format | Article |
| id | doaj-art-f2a2fd74a8f04c55b2701fbfe042d686 |
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| language | English |
| publishDate | 2024-12-01 |
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| spelling | doaj-art-f2a2fd74a8f04c55b2701fbfe042d6862025-08-20T02:43:45ZengMDPI AGPharmaceuticals1424-82472024-12-011712163010.3390/ph17121630Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells ApoptosisDumitriţa Rugină0Mihai Adrian Socaciu1Madalina Nistor2Zorita Diaconeasa3Mihai Cenariu4Flaviu Alexandru Tabaran5Carmen Socaciu6Faculty of Veterinary Medicine, University of Agricultural Sciences and Veterinary Medicine, 400372 Cluj-Napoca, RomaniaFaculty of Medicine, University of Medicine and Pharmacy “Iuliu Hatieganu”, 400347 Cluj-Napoca, RomaniaFaculty of Food Science and Technology, University of Agricultural Sciences and Veterinary Medicine, 400372 Cluj-Napoca, RomaniaFaculty of Food Science and Technology, University of Agricultural Sciences and Veterinary Medicine, 400372 Cluj-Napoca, RomaniaFaculty of Veterinary Medicine, University of Agricultural Sciences and Veterinary Medicine, 400372 Cluj-Napoca, RomaniaFaculty of Veterinary Medicine, University of Agricultural Sciences and Veterinary Medicine, 400372 Cluj-Napoca, RomaniaDepartment of Biotechnology, BIODIATECH—Proplanta Research Centre for Applied Biotechnology in Diagnosis and Molecular Therapy, 400478 Cluj-Napoca, Romania<b>Background/Objectives</b>: Pentacyclic triterpenoids are increasingly studied as anticancer agents with many advantages compared to synthetic chemotherapeutics. The aim of this study was to prepare liposomal and nanostructured lipid formulations including a standardized extract of silver birch (<i>Betula pendula</i>) outer bark (TTs) and to evaluate their potential as anticancer agents in vitro, using Melanoma B16-F10 and Walker carcinoma cells. <b>Methods</b>: Appropriate solvents were selected for efficient TTs extraction, and original recipes were used to obtain Pegylated liposomes and nanolipid complexes with entrapped TTs, comparative to pure standards (betulinic acid and doxorubicin) in similar conditions. The composition, morphology, and sizes of all nanoformulations were checked by high-performance liquid chromatography/mass spectrometry, Transmission Electronic Microscopy, and Diffraction Light Scattering. The entrapment efficiency and its impact on cell viability, cell cycle arrest, and apoptosis by flow cytometry was also measured on both cancer cell lines. <b>Conclusions:</b> The standardized TTs, including betulin, lupeol, and betulinic acid, showed good stability and superior activity compared to pure betulinic acid. According to experimental data, TTs showed good entrapment in liposomal and NLC nanoformulations, both delivery systems including natural, biodegradable ingredients and enhanced bioavailability. The apoptosis and necrosis effects were more pronounced for TTs liposomal formulations in both types of cancer cells, with lower cytotoxicity compared to Doxorubicin, and can be correlated with their increased bioavailability.https://www.mdpi.com/1424-8247/17/12/1630pentacyclic triterpenoidsPEGylated liposomesnanolipid complexesdiffraction light scatteringmelanoma B16-F10 and walker 256 carcinoma cellscell cycle arrest |
| spellingShingle | Dumitriţa Rugină Mihai Adrian Socaciu Madalina Nistor Zorita Diaconeasa Mihai Cenariu Flaviu Alexandru Tabaran Carmen Socaciu Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis Pharmaceuticals pentacyclic triterpenoids PEGylated liposomes nanolipid complexes diffraction light scattering melanoma B16-F10 and walker 256 carcinoma cells cell cycle arrest |
| title | Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis |
| title_full | Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis |
| title_fullStr | Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis |
| title_full_unstemmed | Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis |
| title_short | Liposomal and Nanostructured Lipid Nanoformulations of a Pentacyclic Triterpenoid Birch Bark Extract: Structural Characterization and In Vitro Effects on Melanoma B16-F10 and Walker 256 Tumor Cells Apoptosis |
| title_sort | liposomal and nanostructured lipid nanoformulations of a pentacyclic triterpenoid birch bark extract structural characterization and in vitro effects on melanoma b16 f10 and walker 256 tumor cells apoptosis |
| topic | pentacyclic triterpenoids PEGylated liposomes nanolipid complexes diffraction light scattering melanoma B16-F10 and walker 256 carcinoma cells cell cycle arrest |
| url | https://www.mdpi.com/1424-8247/17/12/1630 |
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