An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention

Introduction: Delivering drugs to ocular region is a challenging task. Eye physiological barriers lead to relatively less therapeutic and bioavailability effect by the conventional eye drops. This may be overcome by the use of in situ gel delivery system. Objective: The objective of our work was to...

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Main Authors: Himanshu Gupta, M Aqil, R K Khar, Asgar Ali, Aseem Bhatnagar, Gaurav Mittal
Format: Article
Language:English
Published: Wolters Kluwer Medknow Publications 2015-01-01
Series:Journal of Pharmacy and Bioallied Sciences
Subjects:
Online Access:http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2015;volume=7;issue=1;spage=9;epage=14;aulast=Gupta
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author Himanshu Gupta
M Aqil
R K Khar
Asgar Ali
Aseem Bhatnagar
Gaurav Mittal
author_facet Himanshu Gupta
M Aqil
R K Khar
Asgar Ali
Aseem Bhatnagar
Gaurav Mittal
author_sort Himanshu Gupta
collection DOAJ
description Introduction: Delivering drugs to ocular region is a challenging task. Eye physiological barriers lead to relatively less therapeutic and bioavailability effect by the conventional eye drops. This may be overcome by the use of in situ gel delivery system. Objective: The objective of our work was to formulate an ocular delivery system of levofloxacin, based on the concept of ion (sodium alginate) and pH (chitosan) activated in situ gelation concept. Due to its elastic properties, in situ gels resist the ocular drainage of drug leading to longer contact times with ocular surface. Materials and Methods: The formulation was evaluated for physicochemical characteristics, in vitro drug release. Ocular retention studies were carried out by Gamma scintigraphy. Time activity curve was plotted between marketed formulation and developed formulation for comparing drug drainage from the eye with time. Ocular tolerance test was performed by handheld infra-red camera. Results and Discussion: The formulations showed a first-order release pattern over 12 h. Both in vitro release studies and in vivo gamma scintigraphy precorneal retention studies indicated better therapeutic efficacy compared with standard eye drops. Conclusion: The results demonstrated that the developed in situ gel of levofloxacin is nonirritant, has prolonged action and is a better option in terms of retention, ocular bioavailability and patient compliance when compared with plain eye drops formulation.
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spelling doaj.art-9a5eb9c3f3a641aa94beb7e05ba96bb82022-12-22T02:56:00ZengWolters Kluwer Medknow PublicationsJournal of Pharmacy and Bioallied Sciences0975-74060976-48792015-01-017191410.4103/0975-7406.149810An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retentionHimanshu GuptaM AqilR K KharAsgar AliAseem BhatnagarGaurav MittalIntroduction: Delivering drugs to ocular region is a challenging task. Eye physiological barriers lead to relatively less therapeutic and bioavailability effect by the conventional eye drops. This may be overcome by the use of in situ gel delivery system. Objective: The objective of our work was to formulate an ocular delivery system of levofloxacin, based on the concept of ion (sodium alginate) and pH (chitosan) activated in situ gelation concept. Due to its elastic properties, in situ gels resist the ocular drainage of drug leading to longer contact times with ocular surface. Materials and Methods: The formulation was evaluated for physicochemical characteristics, in vitro drug release. Ocular retention studies were carried out by Gamma scintigraphy. Time activity curve was plotted between marketed formulation and developed formulation for comparing drug drainage from the eye with time. Ocular tolerance test was performed by handheld infra-red camera. Results and Discussion: The formulations showed a first-order release pattern over 12 h. Both in vitro release studies and in vivo gamma scintigraphy precorneal retention studies indicated better therapeutic efficacy compared with standard eye drops. Conclusion: The results demonstrated that the developed in situ gel of levofloxacin is nonirritant, has prolonged action and is a better option in terms of retention, ocular bioavailability and patient compliance when compared with plain eye drops formulation.http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2015;volume=7;issue=1;spage=9;epage=14;aulast=GuptaChitosangamma scintigraphyin situ gellevofloxacinocular toleranceradiolabelling
spellingShingle Himanshu Gupta
M Aqil
R K Khar
Asgar Ali
Aseem Bhatnagar
Gaurav Mittal
An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention
Journal of Pharmacy and Bioallied Sciences
Chitosan
gamma scintigraphy
in situ gel
levofloxacin
ocular tolerance
radiolabelling
title An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention
title_full An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention
title_fullStr An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention
title_full_unstemmed An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention
title_short An alternative in situ gel-formulation of levofloxacin eye drops for prolong ocular retention
title_sort alternative in situ gel formulation of levofloxacin eye drops for prolong ocular retention
topic Chitosan
gamma scintigraphy
in situ gel
levofloxacin
ocular tolerance
radiolabelling
url http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2015;volume=7;issue=1;spage=9;epage=14;aulast=Gupta
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