Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles

Ahmed F Hanafy,1,2 Ahmed M Abdalla,1 Tawheda K Guda,1 Khairy E Gabr,1,3 Paul G Royall,4 Abdulmalik Alqurshi11Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Medina, KSA; 2Research and Development Department, Al Andalous for Pharmaceutical Industries...

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Autores principales:	Hanafy AF, Abdalla AM, Guda TK, Gabr KE, Royall PG, Alqurshi A
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Nanoparticles Ocular drug delivery Chitosan Ionic gelation Prednisolone acetate Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/05d8cb1bff044308a61166b8bcea22ff
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spelling	oai:doaj.org-article:05d8cb1bff044308a61166b8bcea22ff2021-12-02T08:14:20ZOcular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles1178-2013https://doaj.org/article/05d8cb1bff044308a61166b8bcea22ff2019-05-01T00:00:00Zhttps://www.dovepress.com/ocular-anti-inflammatory-activity-of-prednisolone-acetate-loaded-chito-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ahmed F Hanafy,1,2 Ahmed M Abdalla,1 Tawheda K Guda,1 Khairy E Gabr,1,3 Paul G Royall,4 Abdulmalik Alqurshi11Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Medina, KSA; 2Research and Development Department, Al Andalous for Pharmaceutical Industries, Giza, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt; 4Institute of Pharmaceutical Science, King’s College London, London, SE1 9NH, UKBackground and purpose: Conventional topical ophthalmic aqueous solutions and suspensions are often associated with low bioavailability and high administration frequency, pulsatile dose and poor exposure to certain ocular parts. The aim of this study was to develop an ophthalmic nanoparticles loaded gel, for delivering prednisolone acetate (PA), to increase dosing accuracy, bioavailability, and accordingly, efficiency of PA in treating inflammatory ocular diseases.Methods: A novel formulation of self-assembled nanoparticles was prepared by the complexation of chitosan (CS) and, the counter-ion, sodium deoxycholate (SD), loaded with the poorly-water-soluble PA. Particle size, zeta potential, encapsulation efficiency (EE) and drug loading content (LC) of prepared nanoparticles were assessed. Moreover, the nanoparticles were characterized using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Drug release and eye anti-inflammatory potential of the prepared novel formulation was investigated.Results: Mean particle size of the nanoparticles have dropped from 976 nm ±43 (PDI 1.285) to 480 nm ±28 (PDI 1.396) when the ratio of CS-SD was decreased. The incorporation of 0.1-0.3% of polyvinyl alcohol (PVA), in the preparation stages, resulted in smaller nanoparticles: 462 nm ±19 (PDI 0.942) and 321 nm ±22 (PDI 0.454) respectively. DSC and FTIR results demonstrated the interaction between CS and SD, however, no interactions were detected between PA and CS or SD. Drug release of PA as received, in simulated tears fluid (pH 7.4), showed a twofold increase (reaching an average of 98.6% in 24 hours) when incorporated into an optimized nanoparticle gel formulation (1:5 CS-SD).Conclusion: The anti-inflammatory effect of PA nanoparticles loaded gel on female guinea pig eyes was significantly superior to that of the micronized drug loaded gel (P < 0.05).Keywords: nanoparticles, ocular drug delivery, chitosan, ionic gelation, prednisolone acetateHanafy AFAbdalla AMGuda TKGabr KERoyall PGAlqurshi ADove Medical PressarticleNanoparticlesOcular drug deliveryChitosanIonic gelationPrednisolone acetateMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 3679-3689 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Nanoparticles Ocular drug delivery Chitosan Ionic gelation Prednisolone acetate Medicine (General) R5-920
spellingShingle	Nanoparticles Ocular drug delivery Chitosan Ionic gelation Prednisolone acetate Medicine (General) R5-920 Hanafy AF Abdalla AM Guda TK Gabr KE Royall PG Alqurshi A Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
description	Ahmed F Hanafy,1,2 Ahmed M Abdalla,1 Tawheda K Guda,1 Khairy E Gabr,1,3 Paul G Royall,4 Abdulmalik Alqurshi11Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Medina, KSA; 2Research and Development Department, Al Andalous for Pharmaceutical Industries, Giza, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt; 4Institute of Pharmaceutical Science, King’s College London, London, SE1 9NH, UKBackground and purpose: Conventional topical ophthalmic aqueous solutions and suspensions are often associated with low bioavailability and high administration frequency, pulsatile dose and poor exposure to certain ocular parts. The aim of this study was to develop an ophthalmic nanoparticles loaded gel, for delivering prednisolone acetate (PA), to increase dosing accuracy, bioavailability, and accordingly, efficiency of PA in treating inflammatory ocular diseases.Methods: A novel formulation of self-assembled nanoparticles was prepared by the complexation of chitosan (CS) and, the counter-ion, sodium deoxycholate (SD), loaded with the poorly-water-soluble PA. Particle size, zeta potential, encapsulation efficiency (EE) and drug loading content (LC) of prepared nanoparticles were assessed. Moreover, the nanoparticles were characterized using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Drug release and eye anti-inflammatory potential of the prepared novel formulation was investigated.Results: Mean particle size of the nanoparticles have dropped from 976 nm ±43 (PDI 1.285) to 480 nm ±28 (PDI 1.396) when the ratio of CS-SD was decreased. The incorporation of 0.1-0.3% of polyvinyl alcohol (PVA), in the preparation stages, resulted in smaller nanoparticles: 462 nm ±19 (PDI 0.942) and 321 nm ±22 (PDI 0.454) respectively. DSC and FTIR results demonstrated the interaction between CS and SD, however, no interactions were detected between PA and CS or SD. Drug release of PA as received, in simulated tears fluid (pH 7.4), showed a twofold increase (reaching an average of 98.6% in 24 hours) when incorporated into an optimized nanoparticle gel formulation (1:5 CS-SD).Conclusion: The anti-inflammatory effect of PA nanoparticles loaded gel on female guinea pig eyes was significantly superior to that of the micronized drug loaded gel (P < 0.05).Keywords: nanoparticles, ocular drug delivery, chitosan, ionic gelation, prednisolone acetate
format	article
author	Hanafy AF Abdalla AM Guda TK Gabr KE Royall PG Alqurshi A
author_facet	Hanafy AF Abdalla AM Guda TK Gabr KE Royall PG Alqurshi A
author_sort	Hanafy AF
title	Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
title_short	Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
title_full	Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
title_fullStr	Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
title_full_unstemmed	Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
title_sort	ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/05d8cb1bff044308a61166b8bcea22ff
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Ocular anti-inflammatory activity of prednisolone acetate loaded chitosan-deoxycholate self-assembled nanoparticles

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