Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery

The poor ocular bioavailability of melatonin (MEL) limits the therapeutic action the molecule could exert in the treatment of ocular diseases. To date, no study has explored the use of nanofiber-based inserts to prolong ocular surface contact time and improve MEL delivery. Here, the electrospinning...

Full description

Bibliographic Details
Main Authors: Alessia Romeo, Adrienn Kazsoki, Safaa Omer, Balázs Pinke, László Mészáros, Teresa Musumeci, Romána Zelkó
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/15/4/1296
_version_ 1797603807238029312
author Alessia Romeo
Adrienn Kazsoki
Safaa Omer
Balázs Pinke
László Mészáros
Teresa Musumeci
Romána Zelkó
author_facet Alessia Romeo
Adrienn Kazsoki
Safaa Omer
Balázs Pinke
László Mészáros
Teresa Musumeci
Romána Zelkó
author_sort Alessia Romeo
collection DOAJ
description The poor ocular bioavailability of melatonin (MEL) limits the therapeutic action the molecule could exert in the treatment of ocular diseases. To date, no study has explored the use of nanofiber-based inserts to prolong ocular surface contact time and improve MEL delivery. Here, the electrospinning technique was proposed to prepare poly (vinyl alcohol) (PVA) and poly (lactic acid) (PLA) nanofiber inserts. Both nanofibers were produced with different concentrations of MEL and with or without the addition of Tween<sup>®</sup> 80. Nanofibers morphology was evaluated by scanning electron microscopy. Thermal and spectroscopic analyses were performed to characterize the state of MEL in the scaffolds. MEL release profiles were observed under simulated physiological conditions (pH 7.4, 37 °C). The swelling behavior was evaluated by a gravimetric method. The results confirmed that submicron-sized nanofibrous structures were obtained with MEL in the amorphous state. Different MEL release rates were achieved depending on the nature of the polymer. Fast (20 min) and complete release was observed for the PVA-based samples, unlike the PLA polymer, which provided slow and controlled MEL release. The addition of Tween<sup>®</sup> 80 affected the swelling properties of the fibrous structures. Overall, the results suggest that membranes could be an attractive vehicle as a potential alternative to liquid formulations for ocular administration of MEL.
first_indexed 2024-03-11T04:37:18Z
format Article
id doaj.art-6e1494223ed8491b89b22b2267b2930e
institution Directory Open Access Journal
issn 1999-4923
language English
last_indexed 2024-03-11T04:37:18Z
publishDate 2023-04-01
publisher MDPI AG
record_format Article
series Pharmaceutics
spelling doaj.art-6e1494223ed8491b89b22b2267b2930e2023-11-17T20:55:31ZengMDPI AGPharmaceutics1999-49232023-04-01154129610.3390/pharmaceutics15041296Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular DeliveryAlessia Romeo0Adrienn Kazsoki1Safaa Omer2Balázs Pinke3László Mészáros4Teresa Musumeci5Romána Zelkó6Department of Drug and Health Sciences, Laboratory of Drug Delivery Technology, University of Catania, Viale A. Doria 6, 95125 Catania, ItalyUniversity Pharmacy Department of Pharmacy Administration, Semmelweis University, Högyes Endre utca 7-9, H-1092 Budapest, HungaryUniversity Pharmacy Department of Pharmacy Administration, Semmelweis University, Högyes Endre utca 7-9, H-1092 Budapest, HungaryDepartment of Polymer Engineering, Faculty of Mechanical Engineering, Budapest University of Technology and Economics, Műegyetem rkp. 3, H-1111 Budapest, HungaryDepartment of Polymer Engineering, Faculty of Mechanical Engineering, Budapest University of Technology and Economics, Műegyetem rkp. 3, H-1111 Budapest, HungaryDepartment of Drug and Health Sciences, Laboratory of Drug Delivery Technology, University of Catania, Viale A. Doria 6, 95125 Catania, ItalyUniversity Pharmacy Department of Pharmacy Administration, Semmelweis University, Högyes Endre utca 7-9, H-1092 Budapest, HungaryThe poor ocular bioavailability of melatonin (MEL) limits the therapeutic action the molecule could exert in the treatment of ocular diseases. To date, no study has explored the use of nanofiber-based inserts to prolong ocular surface contact time and improve MEL delivery. Here, the electrospinning technique was proposed to prepare poly (vinyl alcohol) (PVA) and poly (lactic acid) (PLA) nanofiber inserts. Both nanofibers were produced with different concentrations of MEL and with or without the addition of Tween<sup>®</sup> 80. Nanofibers morphology was evaluated by scanning electron microscopy. Thermal and spectroscopic analyses were performed to characterize the state of MEL in the scaffolds. MEL release profiles were observed under simulated physiological conditions (pH 7.4, 37 °C). The swelling behavior was evaluated by a gravimetric method. The results confirmed that submicron-sized nanofibrous structures were obtained with MEL in the amorphous state. Different MEL release rates were achieved depending on the nature of the polymer. Fast (20 min) and complete release was observed for the PVA-based samples, unlike the PLA polymer, which provided slow and controlled MEL release. The addition of Tween<sup>®</sup> 80 affected the swelling properties of the fibrous structures. Overall, the results suggest that membranes could be an attractive vehicle as a potential alternative to liquid formulations for ocular administration of MEL.https://www.mdpi.com/1999-4923/15/4/1296nanofibersocular insertelectrospinningPLAPVAin vitro dissolution study
spellingShingle Alessia Romeo
Adrienn Kazsoki
Safaa Omer
Balázs Pinke
László Mészáros
Teresa Musumeci
Romána Zelkó
Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery
Pharmaceutics
nanofibers
ocular insert
electrospinning
PLA
PVA
in vitro dissolution study
title Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery
title_full Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery
title_fullStr Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery
title_full_unstemmed Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery
title_short Formulation and Characterization of Electrospun Nanofibers for Melatonin Ocular Delivery
title_sort formulation and characterization of electrospun nanofibers for melatonin ocular delivery
topic nanofibers
ocular insert
electrospinning
PLA
PVA
in vitro dissolution study
url https://www.mdpi.com/1999-4923/15/4/1296
work_keys_str_mv AT alessiaromeo formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery
AT adriennkazsoki formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery
AT safaaomer formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery
AT balazspinke formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery
AT laszlomeszaros formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery
AT teresamusumeci formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery
AT romanazelko formulationandcharacterizationofelectrospunnanofibersformelatoninoculardelivery