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Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation
Improving the bioavailability of a drug at the ocular surface presents a profound challenge. Due to ocular physiological barriers, conventional eye drops exhibit poor bioavailability of drugs. Sustained-release nanoparticles may improve the residence time and hence increase absorption of the drug fr...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Shaheed Beheshti University of Medical Sciences
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8653660/ https://www.ncbi.nlm.nih.gov/pubmed/34904011 http://dx.doi.org/10.22037/ijpr.2021.114478.15054 |
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author | Khan, Fahim Ullah Nasir, Fazli Iqbal, Zafar Neau, Steven Khan, Ismail Hassan, Mohammad Iqbal, Muhammad Ullah, Aman Khan, Sumaira Irum Sakhi, Mirina |
author_facet | Khan, Fahim Ullah Nasir, Fazli Iqbal, Zafar Neau, Steven Khan, Ismail Hassan, Mohammad Iqbal, Muhammad Ullah, Aman Khan, Sumaira Irum Sakhi, Mirina |
author_sort | Khan, Fahim Ullah |
collection | PubMed |
description | Improving the bioavailability of a drug at the ocular surface presents a profound challenge. Due to ocular physiological barriers, conventional eye drops exhibit poor bioavailability of drugs. Sustained-release nanoparticles may improve the residence time and hence increase absorption of the drug from the corneal surface. The current study focuses on the development of a nanoparticle-based system for the ophthalmic sustained delivery of moxifloxacin, to enhance ocular retention and bioavailability of the drug. PLGA was used as the matrix-forming polymer in the nanoparticle formulation. Nanoparticles were manufactured using a double emulsion (w/o/w) solvent evaporation technique. The formulation was optimized based on physicochemical properties, including size, polydispersity index, and stability. Nanoparticles were also evaluated for in-vitro drug release and pharmacokinetic evaluation in a rabbit model. The optimized formulation exhibited a relatively high initial release rate for six hours followed by sustained release of a drug via diffusion. The in-vivo ocular tolerance studies confirmed that moxifloxacin-loaded PLGA nanoparticles were non-irritating to the eye. The pharmacokinetic studies revealed that the nanoparticles provided a high C(max), AUC, MRT, and low clearance rate when compared to commercial eye drops. It can be concluded that such PLGA nanoparticles offer the potential for improved bioavailability of moxifloxacin HCl. |
format | Online Article Text |
id | pubmed-8653660 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-86536602021-12-12 Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation Khan, Fahim Ullah Nasir, Fazli Iqbal, Zafar Neau, Steven Khan, Ismail Hassan, Mohammad Iqbal, Muhammad Ullah, Aman Khan, Sumaira Irum Sakhi, Mirina Iran J Pharm Res Original Article Improving the bioavailability of a drug at the ocular surface presents a profound challenge. Due to ocular physiological barriers, conventional eye drops exhibit poor bioavailability of drugs. Sustained-release nanoparticles may improve the residence time and hence increase absorption of the drug from the corneal surface. The current study focuses on the development of a nanoparticle-based system for the ophthalmic sustained delivery of moxifloxacin, to enhance ocular retention and bioavailability of the drug. PLGA was used as the matrix-forming polymer in the nanoparticle formulation. Nanoparticles were manufactured using a double emulsion (w/o/w) solvent evaporation technique. The formulation was optimized based on physicochemical properties, including size, polydispersity index, and stability. Nanoparticles were also evaluated for in-vitro drug release and pharmacokinetic evaluation in a rabbit model. The optimized formulation exhibited a relatively high initial release rate for six hours followed by sustained release of a drug via diffusion. The in-vivo ocular tolerance studies confirmed that moxifloxacin-loaded PLGA nanoparticles were non-irritating to the eye. The pharmacokinetic studies revealed that the nanoparticles provided a high C(max), AUC, MRT, and low clearance rate when compared to commercial eye drops. It can be concluded that such PLGA nanoparticles offer the potential for improved bioavailability of moxifloxacin HCl. Shaheed Beheshti University of Medical Sciences 2021 /pmc/articles/PMC8653660/ /pubmed/34904011 http://dx.doi.org/10.22037/ijpr.2021.114478.15054 Text en https://creativecommons.org/licenses/by/3.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/ (https://creativecommons.org/licenses/by/3.0/) ) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Article Khan, Fahim Ullah Nasir, Fazli Iqbal, Zafar Neau, Steven Khan, Ismail Hassan, Mohammad Iqbal, Muhammad Ullah, Aman Khan, Sumaira Irum Sakhi, Mirina Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation |
title | Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation |
title_full | Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation |
title_fullStr | Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation |
title_full_unstemmed | Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation |
title_short | Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation |
title_sort | improved ocular bioavailability of moxifloxacin hcl using plga nanoparticles: fabrication, characterization, in-vitro and in-vivo evaluation |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8653660/ https://www.ncbi.nlm.nih.gov/pubmed/34904011 http://dx.doi.org/10.22037/ijpr.2021.114478.15054 |
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