Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence
Lipid-based nanocarriers (LNs) have made it possible to prolong corneal residence time and improve the ocular bioavailability of ophthalmic drugs. In order to investigate how the LNs interact with the ocular mucosa and reach the posterior eye segment, we have formulated lipid nanocarriers that were...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-08-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/15/4673 |
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| author | Carmelo Puglia Debora Santonocito Giuseppe Romeo Sebastiano Intagliata Giovanni Luca Romano Enrica Strettoi Elena Novelli Carmine Ostacolo Pietro Campiglia Eduardo Maria Sommella Rosario Pignatello Claudio Bucolo |
| author_facet | Carmelo Puglia Debora Santonocito Giuseppe Romeo Sebastiano Intagliata Giovanni Luca Romano Enrica Strettoi Elena Novelli Carmine Ostacolo Pietro Campiglia Eduardo Maria Sommella Rosario Pignatello Claudio Bucolo |
| author_sort | Carmelo Puglia |
| collection | DOAJ |
| description | Lipid-based nanocarriers (LNs) have made it possible to prolong corneal residence time and improve the ocular bioavailability of ophthalmic drugs. In order to investigate how the LNs interact with the ocular mucosa and reach the posterior eye segment, we have formulated lipid nanocarriers that were designed to bear a traceable fluorescent probe in the present work. The chosen fluorescent probe was obtained by a conjugation reaction between fluoresceinamine and the solid lipid excipient stearic acid, forming a chemically synthesized adduct (ODAF, <i>N</i>-(3′,6′-dihydroxy-3-oxospiro [isobenzofuran-1(3<i>H</i>),9′-[9<i>H</i>] xanthen]-5-yl)-octadecanamide). The novel formulation (LN-ODAF) has been formulated and characterized in terms of its technological parameters (polydispersity index, mean particle size and zeta potential), while an in vivo study was carried out to assess the ability of LN-ODAF to diffuse through different ocular compartments. LN-ODAF were in nanometric range (112.7 nm ± 0.4), showing a good homogeneity and long-term stability. A TEM (transmission electron microscopy) study corroborated these results of characterization. In vivo results pointed out that after ocular instillation, LN ODAF were concentrated in the cornea (two hours), while at a longer time (from the second hour to the eighth hour), the fluorescent signals extended gradually towards the back of the eye. From the results obtained, LN-ODAF demonstrated a potential use of lipid-based nanoparticles as efficient carriers of an active pharmaceutical ingredient (API) involved in the management of retinal diseases. |
| first_indexed | 2024-03-10T09:11:21Z |
| format | Article |
| id | doaj.art-b0ad4fb7adbe4846b0fb650bb53e595e |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T09:11:21Z |
| publishDate | 2021-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-b0ad4fb7adbe4846b0fb650bb53e595e2023-11-22T06:01:36ZengMDPI AGMolecules1420-30492021-08-012615467310.3390/molecules26154673Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo EvidenceCarmelo Puglia0Debora Santonocito1Giuseppe Romeo2Sebastiano Intagliata3Giovanni Luca Romano4Enrica Strettoi5Elena Novelli6Carmine Ostacolo7Pietro Campiglia8Eduardo Maria Sommella9Rosario Pignatello10Claudio Bucolo11Department of Drug and Health Science, University of Catania, Viale Andrea Doria 6, 95125 Catania, ItalyDepartment of Drug and Health Science, University of Catania, Viale Andrea Doria 6, 95125 Catania, ItalyDepartment of Drug and Health Science, University of Catania, Viale Andrea Doria 6, 95125 Catania, ItalyDepartment of Drug and Health Science, University of Catania, Viale Andrea Doria 6, 95125 Catania, ItalyDepartment of Biomedical and Biotechnological Sciences, Section of Pharmacology, University of Catania, 95125 Catania, ItalyCNR Neuroscience Institute, Area della Ricerca, 56124 Pisa, ItalyCNR Neuroscience Institute, Area della Ricerca, 56124 Pisa, ItalyDepartment of Pharmacy, University of Naples Federico II, 80131 Naples, ItalyDepartment of Pharmacy, University of Salerno, 84084 Fisciano, ItalyDepartment of Pharmacy, University of Salerno, 84084 Fisciano, ItalyDepartment of Drug and Health Science, University of Catania, Viale Andrea Doria 6, 95125 Catania, ItalyDepartment of Biomedical and Biotechnological Sciences, Section of Pharmacology, University of Catania, 95125 Catania, ItalyLipid-based nanocarriers (LNs) have made it possible to prolong corneal residence time and improve the ocular bioavailability of ophthalmic drugs. In order to investigate how the LNs interact with the ocular mucosa and reach the posterior eye segment, we have formulated lipid nanocarriers that were designed to bear a traceable fluorescent probe in the present work. The chosen fluorescent probe was obtained by a conjugation reaction between fluoresceinamine and the solid lipid excipient stearic acid, forming a chemically synthesized adduct (ODAF, <i>N</i>-(3′,6′-dihydroxy-3-oxospiro [isobenzofuran-1(3<i>H</i>),9′-[9<i>H</i>] xanthen]-5-yl)-octadecanamide). The novel formulation (LN-ODAF) has been formulated and characterized in terms of its technological parameters (polydispersity index, mean particle size and zeta potential), while an in vivo study was carried out to assess the ability of LN-ODAF to diffuse through different ocular compartments. LN-ODAF were in nanometric range (112.7 nm ± 0.4), showing a good homogeneity and long-term stability. A TEM (transmission electron microscopy) study corroborated these results of characterization. In vivo results pointed out that after ocular instillation, LN ODAF were concentrated in the cornea (two hours), while at a longer time (from the second hour to the eighth hour), the fluorescent signals extended gradually towards the back of the eye. From the results obtained, LN-ODAF demonstrated a potential use of lipid-based nanoparticles as efficient carriers of an active pharmaceutical ingredient (API) involved in the management of retinal diseases.https://www.mdpi.com/1420-3049/26/15/4673ocular drug deliverynanomedicinefluorescent nanoparticlefluorescence microscopyretina |
| spellingShingle | Carmelo Puglia Debora Santonocito Giuseppe Romeo Sebastiano Intagliata Giovanni Luca Romano Enrica Strettoi Elena Novelli Carmine Ostacolo Pietro Campiglia Eduardo Maria Sommella Rosario Pignatello Claudio Bucolo Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence Molecules ocular drug delivery nanomedicine fluorescent nanoparticle fluorescence microscopy retina |
| title | Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence |
| title_full | Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence |
| title_fullStr | Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence |
| title_full_unstemmed | Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence |
| title_short | Lipid Nanoparticles Traverse Non-Corneal Path to Reach the Posterior Eye Segment: In Vivo Evidence |
| title_sort | lipid nanoparticles traverse non corneal path to reach the posterior eye segment in vivo evidence |
| topic | ocular drug delivery nanomedicine fluorescent nanoparticle fluorescence microscopy retina |
| url | https://www.mdpi.com/1420-3049/26/15/4673 |
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