Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers
| Autor: | Julio San Román, Miguel Gómez-Ballesteros, Blanca Vázquez-Lasa, Irene T. Molina-Martínez, Beatriz de-las-Heras, Jorge Marinich, Vanessa Andrés-Guerrero, Francisco Parra, Rocío Herrero-Vanrell |
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| Přispěvatelé: | Agencia Estatal de Investigación (España), Universidad Complutense de Madrid, European Commission, Hospital Clínico San Carlos (España), Ministerio de Ciencia, Innovación y Universidades (España) |
| Rok vydání: | 2019 |
| Předmět: |
Gaucoma
Intraocular pressure Polymers and Plastics medicine.drug_class HEMA/Bayfit-MA Ocular hypertension 02 engineering and technology Pharmacology Article lcsh:QD241-441 03 medical and health sciences Tecnología farmaceútica 0302 clinical medicine lcsh:Organic chemistry Cornea medicine Carbonic anhydrase inhibitor Chemistry General Chemistry Poloxamer 021001 nanoscience & nanotechnology medicine.disease eye diseases Acetazolamide Ophthalmology medicine.anatomical_structure glaucoma Drug delivery 030221 ophthalmology & optometry Nanoparticles Oftalmología sense organs Nanocarriers 0210 nano-technology medicine.drug |
| Zdroj: | E-Prints Complutense. Archivo Institucional de la UCM instname Digital.CSIC. Repositorio Institucional del CSIC Polymers Volume 11 Issue 7 Polymers, Vol 11, Iss 7, p 1213 (2019) |
| Popis: | 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, &minus 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 µ g). 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. |
| Databáze: | OpenAIRE |
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