Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement
Vascularization is a highly conserved and considerably complex and precise process that is finely driven by endogenous regulatory processes at the tissue and systemic levels. However, it can reveal itself to be slow and inadequate for tissue repair and regeneration consequent to severe lesions/damag...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/2/479 |
| _version_ | 1827755901309681664 |
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| author | Nunzia Gallo Stefano Quarta Marika Massaro Maria Annunziata Carluccio Amilcare Barca Donato Cannoletta Luisa Siculella Luca Salvatore Alessandro Sannino |
| author_facet | Nunzia Gallo Stefano Quarta Marika Massaro Maria Annunziata Carluccio Amilcare Barca Donato Cannoletta Luisa Siculella Luca Salvatore Alessandro Sannino |
| author_sort | Nunzia Gallo |
| collection | DOAJ |
| description | Vascularization is a highly conserved and considerably complex and precise process that is finely driven by endogenous regulatory processes at the tissue and systemic levels. However, it can reveal itself to be slow and inadequate for tissue repair and regeneration consequent to severe lesions/damages. Several biomaterial-based strategies were developed to support and enhance vasculogenesis by supplying pro-angiogenic agents. Several approaches were adopted to develop effective drug delivery systems for the controlled release of a huge variety of compounds. In this work, a microparticulate system was chosen to be loaded with the essential amino acid L-lysine, a molecule that has recently gained interest due to its involvement in pro-angiogenic, pro-regenerative, and anti-inflammatory mechanisms. Poly (lactic-co-glycolic acid), the most widely used FDA-approved biodegradable synthetic polymer for the development of drug delivery systems, was chosen due to its versatility and ability to promote neovascularization and wound healing. This study dealt with the development and the effectiveness evaluation of a PLGA-based microparticulate system for the controlled release of L-lysine. Therefore, in order to maximize L-lysine encapsulation efficiency and tune its release kinetics, the microparticle synthesis protocol was optimized by varying some processing parameters. All developed formulations were characterized from a morphological and physicochemical point of view. The optimized formulation was further characterized via the evaluation of its preliminary biological efficacy in vitro. The cellular and molecular studies revealed that the L-lysine-loaded PLGA microparticles were non-toxic, biocompatible, and supported cell proliferation and angiogenesis well by stimulating the expression of pro-angiogenic genes such as metalloproteinase-9, focal adhesion kinases, and different growth factors. Thus, this work showed the potential of delivering L-lysine encapsulated in PLGA microparticles as a cost-effective promoter system for angiogenesis enhancement and rapid healing. |
| first_indexed | 2024-03-11T08:16:35Z |
| format | Article |
| id | doaj.art-2104a1d0469e4b30b150d8e62c7d6fe8 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T08:16:35Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-2104a1d0469e4b30b150d8e62c7d6fe82023-11-16T22:40:29ZengMDPI AGPharmaceutics1999-49232023-02-0115247910.3390/pharmaceutics15020479Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis EnhancementNunzia Gallo0Stefano Quarta1Marika Massaro2Maria Annunziata Carluccio3Amilcare Barca4Donato Cannoletta5Luisa Siculella6Luca Salvatore7Alessandro Sannino8Department of Engineering for Innovation, University of Salento, Via Monteroni, 73100 Lecce, ItalyDepartment of Biological and Environmental Sciences and Technologies (DISTEBA), University of Salento, 73100 Lecce, ItalyInstitute of Clinical Physiology (IFC), National Research Council (CNR), 73100 Lecce, ItalyInstitute of Clinical Physiology (IFC), National Research Council (CNR), 73100 Lecce, ItalyDepartment of Biological and Environmental Sciences and Technologies (DISTEBA), University of Salento, 73100 Lecce, ItalyDepartment of Engineering for Innovation, University of Salento, Via Monteroni, 73100 Lecce, ItalyDepartment of Biological and Environmental Sciences and Technologies (DISTEBA), University of Salento, 73100 Lecce, ItalyDepartment of Engineering for Innovation, University of Salento, Via Monteroni, 73100 Lecce, ItalyDepartment of Engineering for Innovation, University of Salento, Via Monteroni, 73100 Lecce, ItalyVascularization is a highly conserved and considerably complex and precise process that is finely driven by endogenous regulatory processes at the tissue and systemic levels. However, it can reveal itself to be slow and inadequate for tissue repair and regeneration consequent to severe lesions/damages. Several biomaterial-based strategies were developed to support and enhance vasculogenesis by supplying pro-angiogenic agents. Several approaches were adopted to develop effective drug delivery systems for the controlled release of a huge variety of compounds. In this work, a microparticulate system was chosen to be loaded with the essential amino acid L-lysine, a molecule that has recently gained interest due to its involvement in pro-angiogenic, pro-regenerative, and anti-inflammatory mechanisms. Poly (lactic-co-glycolic acid), the most widely used FDA-approved biodegradable synthetic polymer for the development of drug delivery systems, was chosen due to its versatility and ability to promote neovascularization and wound healing. This study dealt with the development and the effectiveness evaluation of a PLGA-based microparticulate system for the controlled release of L-lysine. Therefore, in order to maximize L-lysine encapsulation efficiency and tune its release kinetics, the microparticle synthesis protocol was optimized by varying some processing parameters. All developed formulations were characterized from a morphological and physicochemical point of view. The optimized formulation was further characterized via the evaluation of its preliminary biological efficacy in vitro. The cellular and molecular studies revealed that the L-lysine-loaded PLGA microparticles were non-toxic, biocompatible, and supported cell proliferation and angiogenesis well by stimulating the expression of pro-angiogenic genes such as metalloproteinase-9, focal adhesion kinases, and different growth factors. Thus, this work showed the potential of delivering L-lysine encapsulated in PLGA microparticles as a cost-effective promoter system for angiogenesis enhancement and rapid healing.https://www.mdpi.com/1999-4923/15/2/479L-lysinePLGAdrug delivery systemsmicrospheresangiogenesis |
| spellingShingle | Nunzia Gallo Stefano Quarta Marika Massaro Maria Annunziata Carluccio Amilcare Barca Donato Cannoletta Luisa Siculella Luca Salvatore Alessandro Sannino Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement Pharmaceutics L-lysine PLGA drug delivery systems microspheres angiogenesis |
| title | Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement |
| title_full | Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement |
| title_fullStr | Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement |
| title_full_unstemmed | Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement |
| title_short | Development of L-Lysine-Loaded PLGA Microparticles as a Controlled Release System for Angiogenesis Enhancement |
| title_sort | development of l lysine loaded plga microparticles as a controlled release system for angiogenesis enhancement |
| topic | L-lysine PLGA drug delivery systems microspheres angiogenesis |
| url | https://www.mdpi.com/1999-4923/15/2/479 |
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