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Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design
Human eye is one of the most accessible organs in the body, nonetheless, its physiology and associated precorneal factors such as nasolacrimal drainage, blinking, tear film, tear turnover, and induced lacrimation has significantly decreased the residence time of any foreign substances including phar...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4932477/ https://www.ncbi.nlm.nih.gov/pubmed/27104555 http://dx.doi.org/10.3390/pharmaceutics8020014 |
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author | ElShaer, Amr Mustafa, Shelan Kasar, Mohamad Thapa, Sapana Ghatora, Baljit Alany, Raid G. |
author_facet | ElShaer, Amr Mustafa, Shelan Kasar, Mohamad Thapa, Sapana Ghatora, Baljit Alany, Raid G. |
author_sort | ElShaer, Amr |
collection | PubMed |
description | Human eye is one of the most accessible organs in the body, nonetheless, its physiology and associated precorneal factors such as nasolacrimal drainage, blinking, tear film, tear turnover, and induced lacrimation has significantly decreased the residence time of any foreign substances including pharmaceutical dosage forms. Soft contact lenses are promising delivery devices that can sustain the drug release and prolong residence time by acting as a geometric barrier to drug diffusion to tear fluid. This study investigates experimental parameters such as composition of polymer mixtures, stabilizer and the amount of active pharmaceutical ingredient on the preparation of a polymeric drug delivery system for the topical ocular administration of Prednisolone. To achieve this goal, prednisolone-loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles were prepared by single emulsion solvent evaporation method. Prednisolone was quantified using a validated high performance liquid chromatography (HPLC) method. Nanoparticle size was mostly affected by the amount of co-polymer (PLGA) used whereas drug load was mostly affected by amount of prednisolone (API) used. Longer homogenization time along with higher amount of API yielded the smallest size nanoparticles. The nanoparticles prepared had an average particle size of 347.1 ± 11.9 nm with a polydispersity index of 0.081. The nanoparticles were then incorporated in the contact lens mixture before preparing them. Clear and transparent contact lenses were successfully prepared. When the nanoparticle (NP)-loaded contact lenses were compared with control contact lenses (unloaded NP contact lenses), a decrease in hydration by 2% (31.2% ± 1.25% hydration for the 0.2 g loaded NP contact lenses) and light transmission by 8% (unloaded NP contact lenses 94.5% NP 0.2 g incorporated contact lenses 86.23%). The wettability of the contact lenses remained within the desired value (<90 °C) even upon incorporation of the NP. NP alone and NP-loaded contact lenses both displayed a slow in vitro drug release of drug over 24 h; where 42.3% and 10.8% prednisolone release were achieved, respectively. Contact lenses can be used as a medicated device to sustain ocular drug delivery and improve patient compliance; nonetheless, patients and healthcare professionals’ acceptability and perceptions of the new formulations entail further investigations. |
format | Online Article Text |
id | pubmed-4932477 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-49324772016-07-13 Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design ElShaer, Amr Mustafa, Shelan Kasar, Mohamad Thapa, Sapana Ghatora, Baljit Alany, Raid G. Pharmaceutics Article Human eye is one of the most accessible organs in the body, nonetheless, its physiology and associated precorneal factors such as nasolacrimal drainage, blinking, tear film, tear turnover, and induced lacrimation has significantly decreased the residence time of any foreign substances including pharmaceutical dosage forms. Soft contact lenses are promising delivery devices that can sustain the drug release and prolong residence time by acting as a geometric barrier to drug diffusion to tear fluid. This study investigates experimental parameters such as composition of polymer mixtures, stabilizer and the amount of active pharmaceutical ingredient on the preparation of a polymeric drug delivery system for the topical ocular administration of Prednisolone. To achieve this goal, prednisolone-loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles were prepared by single emulsion solvent evaporation method. Prednisolone was quantified using a validated high performance liquid chromatography (HPLC) method. Nanoparticle size was mostly affected by the amount of co-polymer (PLGA) used whereas drug load was mostly affected by amount of prednisolone (API) used. Longer homogenization time along with higher amount of API yielded the smallest size nanoparticles. The nanoparticles prepared had an average particle size of 347.1 ± 11.9 nm with a polydispersity index of 0.081. The nanoparticles were then incorporated in the contact lens mixture before preparing them. Clear and transparent contact lenses were successfully prepared. When the nanoparticle (NP)-loaded contact lenses were compared with control contact lenses (unloaded NP contact lenses), a decrease in hydration by 2% (31.2% ± 1.25% hydration for the 0.2 g loaded NP contact lenses) and light transmission by 8% (unloaded NP contact lenses 94.5% NP 0.2 g incorporated contact lenses 86.23%). The wettability of the contact lenses remained within the desired value (<90 °C) even upon incorporation of the NP. NP alone and NP-loaded contact lenses both displayed a slow in vitro drug release of drug over 24 h; where 42.3% and 10.8% prednisolone release were achieved, respectively. Contact lenses can be used as a medicated device to sustain ocular drug delivery and improve patient compliance; nonetheless, patients and healthcare professionals’ acceptability and perceptions of the new formulations entail further investigations. MDPI 2016-04-20 /pmc/articles/PMC4932477/ /pubmed/27104555 http://dx.doi.org/10.3390/pharmaceutics8020014 Text en © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article ElShaer, Amr Mustafa, Shelan Kasar, Mohamad Thapa, Sapana Ghatora, Baljit Alany, Raid G. Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design |
title | Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design |
title_full | Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design |
title_fullStr | Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design |
title_full_unstemmed | Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design |
title_short | Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design |
title_sort | nanoparticle-laden contact lens for controlled ocular delivery of prednisolone: formulation optimization using statistical experimental design |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4932477/ https://www.ncbi.nlm.nih.gov/pubmed/27104555 http://dx.doi.org/10.3390/pharmaceutics8020014 |
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