Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers
Topical application of drops containing ocular drugs is the preferred non-invasive route to treat diseases that affect the anterior segment of the eye. However, the formulation of eye drops is a major challenge for pharmacists since the access of drugs to ocular tissues is restricted by several barr...
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doaj-83dea07b72a142b59950e3955d8bc6bb2020-11-24T21:27:47ZengMDPI AGPolymers2073-43602019-07-01117121310.3390/polym11071213polym11071213Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug CarriersMiguel Gómez-Ballesteros0Vanessa Andrés-Guerrero1Francisco Jesús Parra2Jorge Marinich3Beatriz de-las-Heras4Irene Teresa Molina-Martínez5Blanca Vázquez-Lasa6Julio San Román7Rocío Herrero-Vanrell8Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid (UCM), IdISSC, 28040 Madrid, SpainDepartment of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid (UCM), IdISSC, 28040 Madrid, SpainInstitute of Polymer Science and Technology, ICTP-CSIC, and CIBER-BBN, 28006 Madrid, SpainDepartment of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid (UCM), IdISSC, 28040 Madrid, SpainOcular Pathology National Net (OFTARED) of the Institute of Health Carlos III, 28029 Madrid, SpainDepartment of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid (UCM), IdISSC, 28040 Madrid, SpainInstitute of Polymer Science and Technology, ICTP-CSIC, and CIBER-BBN, 28006 Madrid, SpainInstitute of Polymer Science and Technology, ICTP-CSIC, and CIBER-BBN, 28006 Madrid, SpainDepartment of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid (UCM), IdISSC, 28040 Madrid, SpainTopical application of drops containing ocular drugs is the preferred non-invasive route to treat diseases that affect the anterior segment of the eye. However, the formulation of eye drops is a major challenge for pharmacists since the access of drugs to ocular tissues is restricted by several barriers. Acetazolamide (ACZ) is a carbonic anhydrase inhibitor used orally for the treatment of ocular hypertension in glaucoma. However, large ACZ doses are needed which results in systemic side effects. Recently, we synthesized copolymers based on 2-hydroxyethyl methacrylate (HEMA) and a functionalized three-arm poloxamer star (Bayfit-MA). The new material (HEMA/Bayfit-MA) was engineered to be transformed into nanoparticles without the use of surfactants, which represents a significant step forward in developing new ophthalmic drug delivery platforms. Acetazolamide-loaded nanocarriers (ACZ-NPs) were prepared via dialysis (224 ± 19 nm, −17.2 ± 0.4 mV). The in vitro release rate of ACZ was constant over 24 h (cumulative delivery of ACZ: 83.3 ± 8.4%). Following standard specifications, ACZ-NPs were not cytotoxic in vitro in cornea, conjunctiva, and macrophages. In normotensive rabbits, ACZ-NPs generated a significant intraocular pressure reduction compared to a conventional solution of ACZ (16.4% versus 9.6%) with the same dose of the hypotensive drug (20 µg). In comparison to previously reported studies, this formulation reduced intraocular pressure with a lower dose of ACZ. In summary, HEMA:Bayfit-MA nanoparticles may be a promising system for ocular topical treatments, showing an enhanced ocular bioavailability of ACZ after a single instillation on the ocular surface.https://www.mdpi.com/2073-4360/11/7/1213nanoparticlesglaucomaacetazolamideHEMA/Bayfit-MAdrug deliveryophthalmology |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Miguel Gómez-Ballesteros Vanessa Andrés-Guerrero Francisco Jesús Parra Jorge Marinich Beatriz de-las-Heras Irene Teresa Molina-Martínez Blanca Vázquez-Lasa Julio San Román Rocío Herrero-Vanrell |
spellingShingle |
Miguel Gómez-Ballesteros Vanessa Andrés-Guerrero Francisco Jesús Parra Jorge Marinich Beatriz de-las-Heras Irene Teresa Molina-Martínez Blanca Vázquez-Lasa Julio San Román Rocío Herrero-Vanrell Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers Polymers nanoparticles glaucoma acetazolamide HEMA/Bayfit-MA drug delivery ophthalmology |
author_facet |
Miguel Gómez-Ballesteros Vanessa Andrés-Guerrero Francisco Jesús Parra Jorge Marinich Beatriz de-las-Heras Irene Teresa Molina-Martínez Blanca Vázquez-Lasa Julio San Román Rocío Herrero-Vanrell |
author_sort |
Miguel Gómez-Ballesteros |
title |
Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers |
title_short |
Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers |
title_full |
Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers |
title_fullStr |
Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers |
title_full_unstemmed |
Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers |
title_sort |
amphiphilic acrylic nanoparticles containing the poloxamer star bayfit® 10wf15 as ophthalmic drug carriers |
publisher |
MDPI AG |
series |
Polymers |
issn |
2073-4360 |
publishDate |
2019-07-01 |
description |
Topical application of drops containing ocular drugs is the preferred non-invasive route to treat diseases that affect the anterior segment of the eye. However, the formulation of eye drops is a major challenge for pharmacists since the access of drugs to ocular tissues is restricted by several barriers. Acetazolamide (ACZ) is a carbonic anhydrase inhibitor used orally for the treatment of ocular hypertension in glaucoma. However, large ACZ doses are needed which results in systemic side effects. Recently, we synthesized copolymers based on 2-hydroxyethyl methacrylate (HEMA) and a functionalized three-arm poloxamer star (Bayfit-MA). The new material (HEMA/Bayfit-MA) was engineered to be transformed into nanoparticles without the use of surfactants, which represents a significant step forward in developing new ophthalmic drug delivery platforms. Acetazolamide-loaded nanocarriers (ACZ-NPs) were prepared via dialysis (224 ± 19 nm, −17.2 ± 0.4 mV). The in vitro release rate of ACZ was constant over 24 h (cumulative delivery of ACZ: 83.3 ± 8.4%). Following standard specifications, ACZ-NPs were not cytotoxic in vitro in cornea, conjunctiva, and macrophages. In normotensive rabbits, ACZ-NPs generated a significant intraocular pressure reduction compared to a conventional solution of ACZ (16.4% versus 9.6%) with the same dose of the hypotensive drug (20 µg). In comparison to previously reported studies, this formulation reduced intraocular pressure with a lower dose of ACZ. In summary, HEMA:Bayfit-MA nanoparticles may be a promising system for ocular topical treatments, showing an enhanced ocular bioavailability of ACZ after a single instillation on the ocular surface. |
topic |
nanoparticles glaucoma acetazolamide HEMA/Bayfit-MA drug delivery ophthalmology |
url |
https://www.mdpi.com/2073-4360/11/7/1213 |
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