Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity
The present research work was designed to prepare Azithromycin (AM)-loaded nano lipid carriers (NLs) for ocular delivery. NLs were prepared by the emulsification–homogenization method and further optimized by the Box Behnken design. AM-NLs were optimized using the independent constraints of homogeni...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-04-01
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| Series: | Gels |
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| Online Access: | https://www.mdpi.com/2310-2861/8/5/255 |
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| author | Sadaf Jamal Gilani May Nasser bin Jumah Ameeduzzafar Zafar Syed Sarim Imam Mohd Yasir Mohammad Khalid Sultan Alshehri Mohammed M. Ghuneim Fatima M. Albohairy |
| author_facet | Sadaf Jamal Gilani May Nasser bin Jumah Ameeduzzafar Zafar Syed Sarim Imam Mohd Yasir Mohammad Khalid Sultan Alshehri Mohammed M. Ghuneim Fatima M. Albohairy |
| author_sort | Sadaf Jamal Gilani |
| collection | DOAJ |
| description | The present research work was designed to prepare Azithromycin (AM)-loaded nano lipid carriers (NLs) for ocular delivery. NLs were prepared by the emulsification–homogenization method and further optimized by the Box Behnken design. AM-NLs were optimized using the independent constraints of homogenization speed (A), surfactant concentration (B), and lipid concentration (C) to obtain optimal NLs (AM-NLop). The selected AM-NLop was further converted into a sol-gel system using a mucoadhesive polymer blend of sodium alginate and hydroxyl propyl methyl cellulose (AM-NLopIG). The sol-gel system was further characterized for drug release, permeation, hydration, irritation, histopathology, and antibacterial activity. The prepared NLs showed nano-metric size particles (154.7 ± 7.3 to 352.2 ± 15.8 nm) with high encapsulation efficiency (48.8 ± 1.1 to 80.9 ± 2.9%). AM-NLopIG showed a more prolonged drug release (98.6 ± 4.6% in 24 h) than the eye drop (99.4 ± 5.3% in 3 h). The ex vivo permeation result depicted AM-NLopIG, AM-IG, and eye drop. AM-NLopIG exhibited significant higher AM permeation (60.7 ± 4.1%) than AM-IG (33.46 ± 3.04%) and eye drop (23.3 ± 3.7%). The corneal hydration was found to be 76.45%, which is within the standard limit. The histopathology and HET-CAM results revealed that the prepared formulation is safe for ocular use. The antibacterial study revealed enhanced activity from the AM-NLopIG. |
| first_indexed | 2024-03-10T03:51:40Z |
| format | Article |
| id | doaj.art-d93ec90a58144537b1882a50a301fbf6 |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-10T03:51:40Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Gels |
| spelling | doaj.art-d93ec90a58144537b1882a50a301fbf62023-11-23T11:04:38ZengMDPI AGGels2310-28612022-04-018525510.3390/gels8050255Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial ActivitySadaf Jamal Gilani0May Nasser bin Jumah1Ameeduzzafar Zafar2Syed Sarim Imam3Mohd Yasir4Mohammad Khalid5Sultan Alshehri6Mohammed M. Ghuneim7Fatima M. Albohairy8Department of Basic Health Sciences, Preparatory Year, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi ArabiaBiology Department, College of Science, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmacy, College of Health Science, Arsi University, Asella 396, EthiopiaDepartment of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Ad Diriyah 13713, Saudi ArabiaElectron Microscope Research Unit, Health Sciences Research Center, Princes Nourah bint Abdulrahman University, Riyadh 11671, Saudi ArabiaThe present research work was designed to prepare Azithromycin (AM)-loaded nano lipid carriers (NLs) for ocular delivery. NLs were prepared by the emulsification–homogenization method and further optimized by the Box Behnken design. AM-NLs were optimized using the independent constraints of homogenization speed (A), surfactant concentration (B), and lipid concentration (C) to obtain optimal NLs (AM-NLop). The selected AM-NLop was further converted into a sol-gel system using a mucoadhesive polymer blend of sodium alginate and hydroxyl propyl methyl cellulose (AM-NLopIG). The sol-gel system was further characterized for drug release, permeation, hydration, irritation, histopathology, and antibacterial activity. The prepared NLs showed nano-metric size particles (154.7 ± 7.3 to 352.2 ± 15.8 nm) with high encapsulation efficiency (48.8 ± 1.1 to 80.9 ± 2.9%). AM-NLopIG showed a more prolonged drug release (98.6 ± 4.6% in 24 h) than the eye drop (99.4 ± 5.3% in 3 h). The ex vivo permeation result depicted AM-NLopIG, AM-IG, and eye drop. AM-NLopIG exhibited significant higher AM permeation (60.7 ± 4.1%) than AM-IG (33.46 ± 3.04%) and eye drop (23.3 ± 3.7%). The corneal hydration was found to be 76.45%, which is within the standard limit. The histopathology and HET-CAM results revealed that the prepared formulation is safe for ocular use. The antibacterial study revealed enhanced activity from the AM-NLopIG.https://www.mdpi.com/2310-2861/8/5/255NLsin situ gelocular deliveryazithromycinantibacterialHET CAM |
| spellingShingle | Sadaf Jamal Gilani May Nasser bin Jumah Ameeduzzafar Zafar Syed Sarim Imam Mohd Yasir Mohammad Khalid Sultan Alshehri Mohammed M. Ghuneim Fatima M. Albohairy Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity Gels NLs in situ gel ocular delivery azithromycin antibacterial HET CAM |
| title | Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity |
| title_full | Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity |
| title_fullStr | Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity |
| title_full_unstemmed | Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity |
| title_short | Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity |
| title_sort | formulation and evaluation of nano lipid carrier based ocular gel system optimization to antibacterial activity |
| topic | NLs in situ gel ocular delivery azithromycin antibacterial HET CAM |
| url | https://www.mdpi.com/2310-2861/8/5/255 |
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