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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...

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Autores principales: Khan, Fahim Ullah, Nasir, Fazli, Iqbal, Zafar, Neau, Steven, Khan, Ismail, Hassan, Mohammad, Iqbal, Muhammad, Ullah, Aman, Khan, Sumaira Irum, Sakhi, Mirina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2021
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.
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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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