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Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir
Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the p...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362158/ https://www.ncbi.nlm.nih.gov/pubmed/30766442 http://dx.doi.org/10.1016/j.jsps.2018.11.011 |
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author | Alkholief, Musaed Albasit, Hammam Alhowyan, Adel Alshehri, Sultan Raish, Mohammad Abul Kalam, Mohd Alshamsan, Aws |
author_facet | Alkholief, Musaed Albasit, Hammam Alhowyan, Adel Alshehri, Sultan Raish, Mohammad Abul Kalam, Mohd Alshamsan, Aws |
author_sort | Alkholief, Musaed |
collection | PubMed |
description | Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-gp inhibitor. The optimized nanoparticles were prepared with 0.3% TPGS and had particle-size of 262.3 nm, zeta-potential of +15.14 mV. The physicochemical-characterization, ex vivo transcorneal permeation, ocular-irritation and Acyclovir ocular-availability, following topical ocular application of PLGA-NPs in rabbit eyes, were performed. The tested parameters and irritation by Draize’s test suggested the suitability and safety of PLGA-NPs for ocular use. An ultrahigh performance liquid chromatographic method was developed, validated, and applied to quantify Acyclovir in aqueous humor which was shown to be significantly higher (p < 0.05) using the developed nanoparticles as compared to Acyclovir-aqueous suspension following their single topical ocular administration. Noticeable 2.78-, 1.71- and 2.2-times increased values of AUC(0–24h), t(1/2) (h) and MRT(0–24h) were found, respectively, with the PLGA-TPGS-NPs as compared to ACY-AqS. These results demonstrate the superiority of delivering Acyclovir using a nanosystem compared to conventional methods. |
format | Online Article Text |
id | pubmed-6362158 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-63621582019-02-14 Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir Alkholief, Musaed Albasit, Hammam Alhowyan, Adel Alshehri, Sultan Raish, Mohammad Abul Kalam, Mohd Alshamsan, Aws Saudi Pharm J Article Delivering drugs via the ocular route has always been a challenge for poorly soluble drugs. The various anatomical and physiological barriers in the eye cavity hinder the residence of drugs within the corneal and precorneal regions. In this study, the nanosystem that could sufficiently deliver the poorly soluble Acyclovir topically via ocular route. Our nanosystem is composed of the biocompatible PLGA polymer stabilized with TPGS which possess a high emulsifying capacity and is also known as P-gp inhibitor. The optimized nanoparticles were prepared with 0.3% TPGS and had particle-size of 262.3 nm, zeta-potential of +15.14 mV. The physicochemical-characterization, ex vivo transcorneal permeation, ocular-irritation and Acyclovir ocular-availability, following topical ocular application of PLGA-NPs in rabbit eyes, were performed. The tested parameters and irritation by Draize’s test suggested the suitability and safety of PLGA-NPs for ocular use. An ultrahigh performance liquid chromatographic method was developed, validated, and applied to quantify Acyclovir in aqueous humor which was shown to be significantly higher (p < 0.05) using the developed nanoparticles as compared to Acyclovir-aqueous suspension following their single topical ocular administration. Noticeable 2.78-, 1.71- and 2.2-times increased values of AUC(0–24h), t(1/2) (h) and MRT(0–24h) were found, respectively, with the PLGA-TPGS-NPs as compared to ACY-AqS. These results demonstrate the superiority of delivering Acyclovir using a nanosystem compared to conventional methods. Elsevier 2019-02 2018-11-23 /pmc/articles/PMC6362158/ /pubmed/30766442 http://dx.doi.org/10.1016/j.jsps.2018.11.011 Text en © 2018 The Authors http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Article Alkholief, Musaed Albasit, Hammam Alhowyan, Adel Alshehri, Sultan Raish, Mohammad Abul Kalam, Mohd Alshamsan, Aws Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir |
title | Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir |
title_full | Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir |
title_fullStr | Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir |
title_full_unstemmed | Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir |
title_short | Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir |
title_sort | employing a plga-tpgs based nanoparticle to improve the ocular delivery of acyclovir |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362158/ https://www.ncbi.nlm.nih.gov/pubmed/30766442 http://dx.doi.org/10.1016/j.jsps.2018.11.011 |
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