Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma
Glaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer from rela...
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| Format: | Article |
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MDPI AG
2023-07-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/16/7/1001 |
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| author | Sandeep Divate Satyanarayana Amr Selim Abu Lila Afrasim Moin Ehssan H. Moglad El-Sayed Khafagy Hadil Faris Alotaibi Ahmad J. Obaidullah Rompicherla Narayana Charyulu |
| author_facet | Sandeep Divate Satyanarayana Amr Selim Abu Lila Afrasim Moin Ehssan H. Moglad El-Sayed Khafagy Hadil Faris Alotaibi Ahmad J. Obaidullah Rompicherla Narayana Charyulu |
| author_sort | Sandeep Divate Satyanarayana |
| collection | DOAJ |
| description | Glaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer from relatively low ocular bioavailability. The objective of this study was to fabricate and optimize solid lipid nanoparticles (SLNs) containing Bimatoprost for ocular administration for the management of glaucoma. Bimatoprost-loaded SLNs were fabricated by solvent evaporation/ultrasonication technique. Glyceryl Monostearate (GMS) was adopted as solid lipid and poloxamer 407 as surfactant. Optimization of SLNs was conducted by central composite design. The optimized formulation was assessed for average particle size, entrapment efficiency (%), zeta potential, surface morphology, drug release study, sterility test, isotonicity test, Hen’s egg test-chorioallantoic membrane (HET-CAM) test and histopathology studies. The optimized Bimatoprost-loaded SLNs formulation had an average size of 183.3 ± 13.3 nm, zeta potential of −9.96 ± 1.2 mV, and encapsulation efficiency percentage of 71.8 ± 1.1%. Transmission electron microscopy (TEM) study revealed the nearly smooth surface of formulated particles with a nano-scale size range. In addition, SLNs significantly sustained Bimatoprost release for up to 12 h, compared to free drug (<i>p</i> < 005). Most importantly, HET-CAM test nullified the irritancy of the formulation was verified its tolerability upon ocular use, as manifested by a significant reduction in mean irritation score, compared to positive control (1% sodium dodecyl sulfate; <i>p</i> < 0.001). Histopathology study inferred the absence of any signs of cornea tissue damage upon treatment with Bimatoprost optimized formulation. Collectively, it was concluded that SLNs might represent a viable vehicle for enhancing the corneal permeation and ocular bioavailability of Bimatoprost for the management of glaucoma. |
| first_indexed | 2024-03-11T00:44:46Z |
| format | Article |
| id | doaj.art-563cc78cb5fb42e1ac609de631801ad3 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-11T00:44:46Z |
| publishDate | 2023-07-01 |
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| series | Pharmaceuticals |
| spelling | doaj.art-563cc78cb5fb42e1ac609de631801ad32023-11-18T20:52:59ZengMDPI AGPharmaceuticals1424-82472023-07-01167100110.3390/ph16071001Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of GlaucomaSandeep Divate Satyanarayana0Amr Selim Abu Lila1Afrasim Moin2Ehssan H. Moglad3El-Sayed Khafagy4Hadil Faris Alotaibi5Ahmad J. Obaidullah6Rompicherla Narayana Charyulu7Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangalore 575018, IndiaDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig 44519, EgyptDepartment of Pharmaceutics, College of Pharmacy, University of Hail, Hail 81442, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint Abdul Rahman University, Riyadh 11671, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangalore 575018, IndiaGlaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer from relatively low ocular bioavailability. The objective of this study was to fabricate and optimize solid lipid nanoparticles (SLNs) containing Bimatoprost for ocular administration for the management of glaucoma. Bimatoprost-loaded SLNs were fabricated by solvent evaporation/ultrasonication technique. Glyceryl Monostearate (GMS) was adopted as solid lipid and poloxamer 407 as surfactant. Optimization of SLNs was conducted by central composite design. The optimized formulation was assessed for average particle size, entrapment efficiency (%), zeta potential, surface morphology, drug release study, sterility test, isotonicity test, Hen’s egg test-chorioallantoic membrane (HET-CAM) test and histopathology studies. The optimized Bimatoprost-loaded SLNs formulation had an average size of 183.3 ± 13.3 nm, zeta potential of −9.96 ± 1.2 mV, and encapsulation efficiency percentage of 71.8 ± 1.1%. Transmission electron microscopy (TEM) study revealed the nearly smooth surface of formulated particles with a nano-scale size range. In addition, SLNs significantly sustained Bimatoprost release for up to 12 h, compared to free drug (<i>p</i> < 005). Most importantly, HET-CAM test nullified the irritancy of the formulation was verified its tolerability upon ocular use, as manifested by a significant reduction in mean irritation score, compared to positive control (1% sodium dodecyl sulfate; <i>p</i> < 0.001). Histopathology study inferred the absence of any signs of cornea tissue damage upon treatment with Bimatoprost optimized formulation. Collectively, it was concluded that SLNs might represent a viable vehicle for enhancing the corneal permeation and ocular bioavailability of Bimatoprost for the management of glaucoma.https://www.mdpi.com/1424-8247/16/7/1001bimatoprostcentral composite designglaucomaHET-CAM testsolid lipid nanoparticles (SLNs) |
| spellingShingle | Sandeep Divate Satyanarayana Amr Selim Abu Lila Afrasim Moin Ehssan H. Moglad El-Sayed Khafagy Hadil Faris Alotaibi Ahmad J. Obaidullah Rompicherla Narayana Charyulu Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma Pharmaceuticals bimatoprost central composite design glaucoma HET-CAM test solid lipid nanoparticles (SLNs) |
| title | Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma |
| title_full | Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma |
| title_fullStr | Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma |
| title_full_unstemmed | Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma |
| title_short | Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma |
| title_sort | ocular delivery of bimatoprost loaded solid lipid nanoparticles for effective management of glaucoma |
| topic | bimatoprost central composite design glaucoma HET-CAM test solid lipid nanoparticles (SLNs) |
| url | https://www.mdpi.com/1424-8247/16/7/1001 |
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