Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery

The present work has as its purpose the synthesis and characterization of a novel lipid material to be used in the preparation of solid lipid nanoparticles (SLNs) for the potential sustained release of progesterone in the vagina. For this reason, a material capable of ensuring the permanence of the...

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Main Authors: Roberta Cassano, Sonia Trombino
Format: Article
Language:English
Published: Wiley 2019-01-01
Series:International Journal of Polymer Science
Online Access:http://dx.doi.org/10.1155/2019/8690145
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author Roberta Cassano
Sonia Trombino
author_facet Roberta Cassano
Sonia Trombino
author_sort Roberta Cassano
collection DOAJ
description The present work has as its purpose the synthesis and characterization of a novel lipid material to be used in the preparation of solid lipid nanoparticles (SLNs) for the potential sustained release of progesterone in the vagina. For this reason, a material capable of ensuring the permanence of the formulation in the administration site for the time needed to guarantee the transmucosal absorption of the steroid was synthetized in order to reduce the number of administrations and to ensure an effective concentration of drug at the site of action. To this end, an ester, 2,3-dihydroxypropanoate of octadecyl (stearyl glycerine), containing two hydroxyl groups was initially synthesized. In particular, the hydroxyl group less sterically encumbered was functionalized with a thiol group, in a coupling reaction, with the amino acid L-cysteine. The obtained compound was characterized by FT-IR spectrometry and 1H-NMR. The functionalized lipid with L-cysteine was then used for the preparation of solid lipid nanoparticles that were loaded with progesterone. Finally, the release of progesterone from the lipid matrix based on newly synthesized ester, under conditions that simulate the vaginal physiological environment, was evaluated. All the obtained results suggest that the prepared nanoparticles could be used for the administration of progesterone, when its integration is essential, for example, in cases of threats of abortion or to increase fertility.
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spelling doaj-art-18534ccab12b4b819c16daa78d9d7c612025-02-03T01:27:48ZengWileyInternational Journal of Polymer Science1687-94221687-94302019-01-01201910.1155/2019/86901458690145Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal DeliveryRoberta Cassano0Sonia Trombino1Department of Pharmacy, Health and Nutritional Sciences, Università della Calabria, Arcavacata di Rende, Cosenza, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, Università della Calabria, Arcavacata di Rende, Cosenza, ItalyThe present work has as its purpose the synthesis and characterization of a novel lipid material to be used in the preparation of solid lipid nanoparticles (SLNs) for the potential sustained release of progesterone in the vagina. For this reason, a material capable of ensuring the permanence of the formulation in the administration site for the time needed to guarantee the transmucosal absorption of the steroid was synthetized in order to reduce the number of administrations and to ensure an effective concentration of drug at the site of action. To this end, an ester, 2,3-dihydroxypropanoate of octadecyl (stearyl glycerine), containing two hydroxyl groups was initially synthesized. In particular, the hydroxyl group less sterically encumbered was functionalized with a thiol group, in a coupling reaction, with the amino acid L-cysteine. The obtained compound was characterized by FT-IR spectrometry and 1H-NMR. The functionalized lipid with L-cysteine was then used for the preparation of solid lipid nanoparticles that were loaded with progesterone. Finally, the release of progesterone from the lipid matrix based on newly synthesized ester, under conditions that simulate the vaginal physiological environment, was evaluated. All the obtained results suggest that the prepared nanoparticles could be used for the administration of progesterone, when its integration is essential, for example, in cases of threats of abortion or to increase fertility.http://dx.doi.org/10.1155/2019/8690145
spellingShingle Roberta Cassano
Sonia Trombino
Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery
International Journal of Polymer Science
title Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery
title_full Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery
title_fullStr Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery
title_full_unstemmed Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery
title_short Solid Lipid Nanoparticles Based on L-Cysteine for Progesterone Intravaginal Delivery
title_sort solid lipid nanoparticles based on l cysteine for progesterone intravaginal delivery
url http://dx.doi.org/10.1155/2019/8690145
work_keys_str_mv AT robertacassano solidlipidnanoparticlesbasedonlcysteineforprogesteroneintravaginaldelivery
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