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1 General aspects (0)   1.1 Epidemiology (15)   1.2 Population genetics (0)   1.3 Pathogenesis (0)   1.4 Quality of life (19)   1.5 Glaucomas as cause of blindness (12)   1.6 Prevention and screening (11) 2 Anatomical structures in glaucoma (0)   2.1 Conjunctiva (11)   2.2 Cornea (16)   2.3 Sclera (8)   2.4 Anterior chamber angle (2)   2.5 Meshwork (0)     2.5.1 Trabecular meshwork (6)     2.5.2 Schlemms canal (3)     2.5.3 Scleral outlet channels (2)   2.6 Aqueous humor dynamics (0)     2.6.1 Production (0)     2.6.2 Outflow (0)       2.6.2.1 Trabecular meshwork (3)       2.6.2.2 Uveoscleral (0)     2.6.3 Compostion (1)   2.7 Episcleral veins and venous pressure (0)   2.8 Iris (5)   2.9 Ciliary body (3)   2.10 Lens (0)   2.11 Vitreous body (1)   2.12 Choroid, peripapillary choroid, peripapillary atrophy (9)   2.13 Retina and retinal nerve fibre layer (25)   2.14 Optic disc (26)   2.15 Optic nerve (3)   2.16 Chiasma and retrochiasmal central nervous system (6)   2.17 Stem cells (5)   2.20 Other (1) 3 Laboratory methods (0)   3.1 Microscopy (2)   3.2 Electron microscopy (0)   3.3 Immunohistochemistry (0)   3.4 Molecular genetics (0)     3.4.1 Linkage studies (0)     3.4.2 Gene studies (22)   3.5 Molecular biology incl. 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Miscellaneous (34)

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Abstract #79181 Published in IGR 20-1

Formulation and Characterization of Carvedilol Leciplex for Glaucoma Treatment: In-Vitro, Ex-Vivo and In-Vivo Study

Hassan DH; Abdelmonem R; Abdellatif MM
Pharmaceutics 2018; 10:

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This study evaluated the efficacy of cationic nanoparticle (leciplex) to deliver carvedilol to ocular surface for glaucoma treatment as recent studies pointed out the effect of topical carvedilol on intraocular pressure, therefore carvedilol loaded leciplex formulae were prepared using soy phosphatidyl choline (SPC) and cationic surfactant (CTAB/DDAB) and characterized for morphology, entrapment efficiency, particle size, zeta potential and ex-vivo corneal permeation. Then the selected formula was evaluated via in-vivo studies in comparison with carvedilol solution. Leciplex nanoparticles appeared spherical in shape with entrapment efficiency exceeded 95% in all formulae. Leciplex formula composed of SPC and DDAB in (1:1) molar ratio showed the smallest particle size (16.04 ± 1.2 nm), highest zeta potential value (53.9 ± 0.91 mv) and highest apparent corneal permeability coefficient (0.1157 cm/h). Carvedilol leciplex reduced intraocular pressure (IOP) to normal range in ocular hypertensive rabbits after 30 min and duration of action lasted for 24 h, while carvedilol solution reduced IOP to normal value after 60 min and duration of action lasted for 6 h. Furthermore, histological examination of eyeballs of rabbits treated with carvedilol leciplex showed improvement of retinal atrophy of glaucomatous eyes. This study concluded that leciplex improve transcorneal permeation and bioavailability of carvedilol.

Department of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Misr University for Science and Technology (MUST), Giza 12566, Egypt. doaa.hassan@must.edu.eg.

Full article

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Classification:

11.16 Vehicles, delivery systems, pharmacokinetics, formulation (Part of: 11 Medical treatment)
11.3.4 Betablocker (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)

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