Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone
This study aimed to develop and evaluate thermoresponsive in situ microgels for the local ocular delivery of prednisolone (PRD) (PRD microgels) to improve drug bioavailability and prolong ocular drug residence time. Lipid nanosystems of PRD microemulsions (PRD-MEs) were prepared and evaluated at a d...
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MDPI AG
2022-09-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/9/1975 |
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| author | Rania Hamed Amani D. Abu Kwiak Yasmeen Al-Adhami Alaa M. Hammad Rana Obaidat Osama H. Abusara Rana Abu Huwaij |
| author_facet | Rania Hamed Amani D. Abu Kwiak Yasmeen Al-Adhami Alaa M. Hammad Rana Obaidat Osama H. Abusara Rana Abu Huwaij |
| author_sort | Rania Hamed |
| collection | DOAJ |
| description | This study aimed to develop and evaluate thermoresponsive in situ microgels for the local ocular delivery of prednisolone (PRD) (PRD microgels) to improve drug bioavailability and prolong ocular drug residence time. Lipid nanosystems of PRD microemulsions (PRD-MEs) were prepared and evaluated at a drug concentration of 0.25–0.75%. PRD microgels were prepared by incorporating PRD-MEs into 10 and 12% Pluronic<sup>®</sup> F127 (F127) or combinations of 12% F127 and 1–10% Kolliphor<sup>®</sup>P188 (F68). PRD microgels were characterized for physicochemical, rheological, and mucoadhesive properties, eye irritation, and stability. Results showed that PRD-MEs were clear, miscible, thermodynamically stable, and spherical with droplet size (16.4 ± 2.2 nm), polydispersity index (0.24 ± 0.01), and zeta potential (−21.03 ± 1.24 mV). The PRD microgels were clear with pH (5.37–5.81), surface tension (30.96–38.90 mN/m), size, and zeta potential of mixed polymeric micelles (20.1–23.9 nm and −1.34 to −10.25 mV, respectively), phase transition temperature (25.3–36 °C), and gelation time (1.44–2.47 min). The FTIR spectra revealed chemical compatibility between PRD and microgel components. PRD microgels showed pseudoplastic flow, viscoelastic and mucoadhesive properties, absence of eye irritation, and drug content (99.3 to 106.3%) with a sustained drug release for 16–24 h. Microgels were physicochemically and rheologically stable for three to six months. Therefore, PRD microgels possess potential vehicles for local ocular delivery. |
| first_indexed | 2024-03-09T22:49:33Z |
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| id | doaj.art-988919e5082847b7b25253fc0457626d |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T22:49:33Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
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| series | Pharmaceutics |
| spelling | doaj.art-988919e5082847b7b25253fc0457626d2023-11-23T18:24:02ZengMDPI AGPharmaceutics1999-49232022-09-01149197510.3390/pharmaceutics14091975Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of PrednisoloneRania Hamed0Amani D. Abu Kwiak1Yasmeen Al-Adhami2Alaa M. Hammad3Rana Obaidat4Osama H. Abusara5Rana Abu Huwaij6Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanDepartment of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanDepartment of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanDepartment of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid 22110, JordanDepartment of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, JordanPharmacological and Diagnostic Research Center, Faculty of Pharmacy, Al-Ahliyya Amman University, Al-Salt 19328, JordanThis study aimed to develop and evaluate thermoresponsive in situ microgels for the local ocular delivery of prednisolone (PRD) (PRD microgels) to improve drug bioavailability and prolong ocular drug residence time. Lipid nanosystems of PRD microemulsions (PRD-MEs) were prepared and evaluated at a drug concentration of 0.25–0.75%. PRD microgels were prepared by incorporating PRD-MEs into 10 and 12% Pluronic<sup>®</sup> F127 (F127) or combinations of 12% F127 and 1–10% Kolliphor<sup>®</sup>P188 (F68). PRD microgels were characterized for physicochemical, rheological, and mucoadhesive properties, eye irritation, and stability. Results showed that PRD-MEs were clear, miscible, thermodynamically stable, and spherical with droplet size (16.4 ± 2.2 nm), polydispersity index (0.24 ± 0.01), and zeta potential (−21.03 ± 1.24 mV). The PRD microgels were clear with pH (5.37–5.81), surface tension (30.96–38.90 mN/m), size, and zeta potential of mixed polymeric micelles (20.1–23.9 nm and −1.34 to −10.25 mV, respectively), phase transition temperature (25.3–36 °C), and gelation time (1.44–2.47 min). The FTIR spectra revealed chemical compatibility between PRD and microgel components. PRD microgels showed pseudoplastic flow, viscoelastic and mucoadhesive properties, absence of eye irritation, and drug content (99.3 to 106.3%) with a sustained drug release for 16–24 h. Microgels were physicochemically and rheologically stable for three to six months. Therefore, PRD microgels possess potential vehicles for local ocular delivery.https://www.mdpi.com/1999-4923/14/9/1975Pluronic<sup>®</sup> F127kolliphor<sup>®</sup> P188 (F68)prednisolonein situ thermoresponsive microgelrheological propertiesmucoadhesion |
| spellingShingle | Rania Hamed Amani D. Abu Kwiak Yasmeen Al-Adhami Alaa M. Hammad Rana Obaidat Osama H. Abusara Rana Abu Huwaij Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone Pharmaceutics Pluronic<sup>®</sup> F127 kolliphor<sup>®</sup> P188 (F68) prednisolone in situ thermoresponsive microgel rheological properties mucoadhesion |
| title | Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone |
| title_full | Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone |
| title_fullStr | Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone |
| title_full_unstemmed | Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone |
| title_short | Microemulsions as Lipid Nanosystems Loaded into Thermoresponsive In Situ Microgels for Local Ocular Delivery of Prednisolone |
| title_sort | microemulsions as lipid nanosystems loaded into thermoresponsive in situ microgels for local ocular delivery of prednisolone |
| topic | Pluronic<sup>®</sup> F127 kolliphor<sup>®</sup> P188 (F68) prednisolone in situ thermoresponsive microgel rheological properties mucoadhesion |
| url | https://www.mdpi.com/1999-4923/14/9/1975 |
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