Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study
Rana M Gebreel,1 Noha A Edris,2 Hala M Elmofty,2 Mina I Tadros,3,4 Mohamed A El-Nabarawi,3 Doaa H Hassan1 1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Ophthalmology, Faculty of Medicin...
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Dove Medical Press
2021-02-01
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| Series: | Drug Design, Development and Therapy |
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| Online Access: | https://www.dovepress.com/development-and-characterization-of-plga-nanoparticle-laden-hydrogels--peer-reviewed-article-DDDT |
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| author | Gebreel RM Edris NA Elmofty HM Tadros MI El-Nabarawi MA Hassan DH |
| author_facet | Gebreel RM Edris NA Elmofty HM Tadros MI El-Nabarawi MA Hassan DH |
| author_sort | Gebreel RM |
| collection | DOAJ |
| description | Rana M Gebreel,1 Noha A Edris,2 Hala M Elmofty,2 Mina I Tadros,3,4 Mohamed A El-Nabarawi,3 Doaa H Hassan1 1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Ophthalmology, Faculty of Medicine, Cairo University, Cairo, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 4Department of Pharmaceutics, Faculty of Pharmacy and Drug Technology, Egyptian Chinese University, Cairo, EgyptCorrespondence: Mina I Tadros Tel +20 1223620458Fax +20 223628246Email mina.tadros@pharma.cu.edu.egAim: Norfloxacin (NFX) has low ocular bioavailability. The current work aimed to develop NFX-loaded nanoparticle (NP)-laden hydrogels to improve the ocular potential of NFX, minimize the need for frequent instillations and lower undesirable side effects.Methods: NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 21 .41 full factorial design, using two types of polylactic-co-glycolic acid (PLGA) polymer and four (drug: polymer) ratios. NPs were evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), drug entrapment efficiency percentage (EE%), drug percentage released after 30 min (Q30min) and 12 hours (Q12h), drug percentage permeated through goat corneas after 30 min (P30min) and 12 hours (P12h) and morphology. Two formulae were statistically selected and incorporated into hydroxypropyl methylcellulose (HPMC)-based hydrogels; G1 – G4. The latter systems were evaluated for appearance, clarity, pH, spreadability, rheology, drug percentages released, drug percentages permeated, antimicrobial activity against Pseudomonas aeruginosa, and histopathological changes.Results: The selected NPs (NP2 and NP6) were spherical in shape and possessed suitable PS (392.02 nm and 190.51 nm) and PDI (0.17 and 0.18), high magnitude of ZP (− 30.43 mV and − 33.62 mV), high EE% (79.24% and 91.72%), low Q30min (10.96% and 16.65%) and P30min (17.39% and 21.05%) and promising Q12h (58.23% and 71.20%) and P12h (53.31% and 65.01%), respectively. Clear, spreadable, tolerable, pseudoplastic, and thixotropic HPMC-based hydrogels were developed. They showed more prolonged drug release and drug permeation profiles. NP2- and NP6-laden hydrogels (G3 and G4 systems, respectively) had promising antibacterial activity, and reasonable histopathological safety.Conclusion: G3 and G4 are potential ocular delivery systems for NFX.Keywords: norfloxacin, nanoparticles, PLGA, ocular delivery, Pseudomonas keratitis |
| first_indexed | 2024-12-22T17:24:21Z |
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| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-22T17:24:21Z |
| publishDate | 2021-02-01 |
| publisher | Dove Medical Press |
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| series | Drug Design, Development and Therapy |
| spelling | doaj.art-79b9bb5c78104859a4475413f0f634682022-12-21T18:18:45ZengDove Medical PressDrug Design, Development and Therapy1177-88812021-02-01Volume 1539941861771Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental StudyGebreel RMEdris NAElmofty HMTadros MIEl-Nabarawi MAHassan DHRana M Gebreel,1 Noha A Edris,2 Hala M Elmofty,2 Mina I Tadros,3,4 Mohamed A El-Nabarawi,3 Doaa H Hassan1 1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Ophthalmology, Faculty of Medicine, Cairo University, Cairo, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 4Department of Pharmaceutics, Faculty of Pharmacy and Drug Technology, Egyptian Chinese University, Cairo, EgyptCorrespondence: Mina I Tadros Tel +20 1223620458Fax +20 223628246Email mina.tadros@pharma.cu.edu.egAim: Norfloxacin (NFX) has low ocular bioavailability. The current work aimed to develop NFX-loaded nanoparticle (NP)-laden hydrogels to improve the ocular potential of NFX, minimize the need for frequent instillations and lower undesirable side effects.Methods: NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 21 .41 full factorial design, using two types of polylactic-co-glycolic acid (PLGA) polymer and four (drug: polymer) ratios. NPs were evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), drug entrapment efficiency percentage (EE%), drug percentage released after 30 min (Q30min) and 12 hours (Q12h), drug percentage permeated through goat corneas after 30 min (P30min) and 12 hours (P12h) and morphology. Two formulae were statistically selected and incorporated into hydroxypropyl methylcellulose (HPMC)-based hydrogels; G1 – G4. The latter systems were evaluated for appearance, clarity, pH, spreadability, rheology, drug percentages released, drug percentages permeated, antimicrobial activity against Pseudomonas aeruginosa, and histopathological changes.Results: The selected NPs (NP2 and NP6) were spherical in shape and possessed suitable PS (392.02 nm and 190.51 nm) and PDI (0.17 and 0.18), high magnitude of ZP (− 30.43 mV and − 33.62 mV), high EE% (79.24% and 91.72%), low Q30min (10.96% and 16.65%) and P30min (17.39% and 21.05%) and promising Q12h (58.23% and 71.20%) and P12h (53.31% and 65.01%), respectively. Clear, spreadable, tolerable, pseudoplastic, and thixotropic HPMC-based hydrogels were developed. They showed more prolonged drug release and drug permeation profiles. NP2- and NP6-laden hydrogels (G3 and G4 systems, respectively) had promising antibacterial activity, and reasonable histopathological safety.Conclusion: G3 and G4 are potential ocular delivery systems for NFX.Keywords: norfloxacin, nanoparticles, PLGA, ocular delivery, Pseudomonas keratitishttps://www.dovepress.com/development-and-characterization-of-plga-nanoparticle-laden-hydrogels--peer-reviewed-article-DDDTnorfloxacinnanoparticlesplgaocular deliverypseudomonas keratitis |
| spellingShingle | Gebreel RM Edris NA Elmofty HM Tadros MI El-Nabarawi MA Hassan DH Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study Drug Design, Development and Therapy norfloxacin nanoparticles plga ocular delivery pseudomonas keratitis |
| title | Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study |
| title_full | Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study |
| title_fullStr | Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study |
| title_full_unstemmed | Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study |
| title_short | Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study |
| title_sort | development and characterization of plga nanoparticle laden hydrogels for sustained ocular delivery of norfloxacin in the treatment of pseudomonas keratitis an experimental study |
| topic | norfloxacin nanoparticles plga ocular delivery pseudomonas keratitis |
| url | https://www.dovepress.com/development-and-characterization-of-plga-nanoparticle-laden-hydrogels--peer-reviewed-article-DDDT |
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