Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes
Engy A Abdel Azim,1 Seham A Elkheshen,2,* Rania M Hathout,3,* Marwa A Fouly,4 Nada M El Hoffy1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, New Cairo, Cairo, 11835, Egypt; 2Department of Pharmaceutics and Industrial Phar...
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2022-06-01
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| Series: | International Journal of Nanomedicine |
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| Online Access: | https://www.dovepress.com/augmented-in-vitro-and-in-vivo-profiles-of-brimonidine-tartrate-using--peer-reviewed-fulltext-article-IJN |
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| author | Abdel Azim EA Elkheshen SA Hathout RM Fouly MA El Hoffy NM |
| author_facet | Abdel Azim EA Elkheshen SA Hathout RM Fouly MA El Hoffy NM |
| author_sort | Abdel Azim EA |
| collection | DOAJ |
| description | Engy A Abdel Azim,1 Seham A Elkheshen,2,* Rania M Hathout,3,* Marwa A Fouly,4 Nada M El Hoffy1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, New Cairo, Cairo, 11835, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt; 4Research Institute of Ophthalmology, Giza, Cairo, 12557, Egypt*These authors contributed equally to this workCorrespondence: Rania M Hathout, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African Union Organization Street, P.O. Box: 11566, Abbassia, Cairo, Egypt, Email r_hathout@yahoo.com; rania.hathout@pharma.asu.edu.egAbstract: Background: The low entrapment efficiency of the hydrophilic drugs such as brimonidine tartrate (BRT) in liposomes represents a challenge that requires interventions. Gelatinized core liposomes (GCLs) were fabricated to increase the drug entrapment, corneal penetration, and physical stability of the investigated molecule.Research Design and Methods: GCLs encapsulating BRT were prepared and optimized utilizing D-optimal design (DOD). The effect of plasticizer incorporation on the physicochemical characteristics and on the in vivo performance was studied. The optimized formulations were investigated for pH, rheological properties, morphological characteristics, in vitro release profiles, biological performance, safety profile. The effects of storage and gamma sterilization were also investigated.Results: The results revealed the great success of the prepared formulations to achieve high entrapment efficiency reaching 98% after a maturation period of 10 days. The addition of glycerol as plasticizer significantly minimized the particle size and shortened the maturation period to 7 days. The selected formulations were stable for 3 months after gamma sterilization. The formulations showed significant lowering of intra-ocular pressure (IOP) in glaucomatous rabbits with sustainment of the pharmacological effect for 24 hours compared to drug solution.Conclusions: Enhanced in vitro and in vivo profiles of brimonidine tartrate loaded gelatinized-core-liposomes were obtained.Keywords: gelatin, brimonidine tartrate, D-optimal design, glaucoma, gelatinized core liposomes, ocular drug delivery, plasticizer, intra-ocular pressure, BRT, IOP, DOD |
| first_indexed | 2024-04-13T12:04:09Z |
| format | Article |
| id | doaj.art-a5e9371828ee4de3956ef94d44eadde8 |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-04-13T12:04:09Z |
| publishDate | 2022-06-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-a5e9371828ee4de3956ef94d44eadde82022-12-22T02:47:42ZengDove Medical PressInternational Journal of Nanomedicine1178-20132022-06-01Volume 172753277676169Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core LiposomesAbdel Azim EAElkheshen SAHathout RMFouly MAEl Hoffy NMEngy A Abdel Azim,1 Seham A Elkheshen,2,* Rania M Hathout,3,* Marwa A Fouly,4 Nada M El Hoffy1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, New Cairo, Cairo, 11835, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt; 4Research Institute of Ophthalmology, Giza, Cairo, 12557, Egypt*These authors contributed equally to this workCorrespondence: Rania M Hathout, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African Union Organization Street, P.O. Box: 11566, Abbassia, Cairo, Egypt, Email r_hathout@yahoo.com; rania.hathout@pharma.asu.edu.egAbstract: Background: The low entrapment efficiency of the hydrophilic drugs such as brimonidine tartrate (BRT) in liposomes represents a challenge that requires interventions. Gelatinized core liposomes (GCLs) were fabricated to increase the drug entrapment, corneal penetration, and physical stability of the investigated molecule.Research Design and Methods: GCLs encapsulating BRT were prepared and optimized utilizing D-optimal design (DOD). The effect of plasticizer incorporation on the physicochemical characteristics and on the in vivo performance was studied. The optimized formulations were investigated for pH, rheological properties, morphological characteristics, in vitro release profiles, biological performance, safety profile. The effects of storage and gamma sterilization were also investigated.Results: The results revealed the great success of the prepared formulations to achieve high entrapment efficiency reaching 98% after a maturation period of 10 days. The addition of glycerol as plasticizer significantly minimized the particle size and shortened the maturation period to 7 days. The selected formulations were stable for 3 months after gamma sterilization. The formulations showed significant lowering of intra-ocular pressure (IOP) in glaucomatous rabbits with sustainment of the pharmacological effect for 24 hours compared to drug solution.Conclusions: Enhanced in vitro and in vivo profiles of brimonidine tartrate loaded gelatinized-core-liposomes were obtained.Keywords: gelatin, brimonidine tartrate, D-optimal design, glaucoma, gelatinized core liposomes, ocular drug delivery, plasticizer, intra-ocular pressure, BRT, IOP, DODhttps://www.dovepress.com/augmented-in-vitro-and-in-vivo-profiles-of-brimonidine-tartrate-using--peer-reviewed-fulltext-article-IJNgelatinbrimonidine tartrated-optimal designglaucomagelatinized core liposomesocular drug deliveryplasticizerintra-ocular pressure |
| spellingShingle | Abdel Azim EA Elkheshen SA Hathout RM Fouly MA El Hoffy NM Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes International Journal of Nanomedicine gelatin brimonidine tartrate d-optimal design glaucoma gelatinized core liposomes ocular drug delivery plasticizer intra-ocular pressure |
| title | Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes |
| title_full | Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes |
| title_fullStr | Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes |
| title_full_unstemmed | Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes |
| title_short | Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes |
| title_sort | augmented in vitro and in vivo profiles of brimonidine tartrate using gelatinized core liposomes |
| topic | gelatin brimonidine tartrate d-optimal design glaucoma gelatinized core liposomes ocular drug delivery plasticizer intra-ocular pressure |
| url | https://www.dovepress.com/augmented-in-vitro-and-in-vivo-profiles-of-brimonidine-tartrate-using--peer-reviewed-fulltext-article-IJN |
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