Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis
Periodontitis is an inflammatory disorder associated with dysbiosis and characterized by microbiologically related, host-mediated inflammation that leads to the damage of periodontal tissues including gingiva, connective tissues, and alveolar bone. The aim of this study was to develop an in situ gel...
| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-07-01
|
| Series: | Gels |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2310-2861/9/7/577 |
| _version_ | 1797589197163331584 |
|---|---|
| author | Poornima K. Gopalakrishna Rajamma Abburu Jayaramu Sateesha Shivally Boregowda Shruthi Eshwar Nikhil V. Suresh Amr Selim Abu Lila Afrasim Moin Hadil Faris Alotaibi Ahmad J. Obaidullah El-Sayed Khafagy |
| author_facet | Poornima K. Gopalakrishna Rajamma Abburu Jayaramu Sateesha Shivally Boregowda Shruthi Eshwar Nikhil V. Suresh Amr Selim Abu Lila Afrasim Moin Hadil Faris Alotaibi Ahmad J. Obaidullah El-Sayed Khafagy |
| author_sort | Poornima K. Gopalakrishna |
| collection | DOAJ |
| description | Periodontitis is an inflammatory disorder associated with dysbiosis and characterized by microbiologically related, host-mediated inflammation that leads to the damage of periodontal tissues including gingiva, connective tissues, and alveolar bone. The aim of this study was to develop an in situ gel consisting of piperine. Eight in situ gel formulations were designed by varying the concentration of deacylated gellan gum cross-linked with sodium tripolyphosphate, and poloxamer-407. The prepared gels were evaluated for gelation temperature, gelation time, viscosity, piperine-loading efficiency, and piperine release. Finally, the optimized formula was evaluated for anti-inflammatory effectiveness among human patients during a 14-day follow-up. The optimized in situ gel formulation exhibited a gelation temperature of 35 ± 1 °C, gelling of 36 ± 1 s, excellent syringeability, and piperine loading of 95.3 ± 2.3%. This formulation efficiently sustained in vitro drug release for up to 72 h. In vivo studies revealed an efficient sol-to-gel transformation of optimized in situ gel formulation at physiological conditions, permitting an efficient residence time of the formulation within a periodontitis pocket. Most importantly, a clinical study revealed that treatment with the optimized formulation elicited a significant reduction in the mean plaque score (<i>p</i> = 0.001), gingival index (<i>p</i> = 0.003), and pocket depth (<i>p</i> = 0.002), and exerted a potent anti-inflammatory potential, compared to the control group. Collectively, piperine-loaded in situ gel might represent a viable therapeutic approach for the management of gingival and periodontal diseases. |
| first_indexed | 2024-03-11T01:03:05Z |
| format | Article |
| id | doaj.art-c45ed8def70640ed84d0eb3d80df77c0 |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-11T01:03:05Z |
| publishDate | 2023-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Gels |
| spelling | doaj.art-c45ed8def70640ed84d0eb3d80df77c02023-11-18T19:28:12ZengMDPI AGGels2310-28612023-07-019757710.3390/gels9070577Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against PeriodontitisPoornima K. Gopalakrishna0Rajamma Abburu Jayaramu1Sateesha Shivally Boregowda2Shruthi Eshwar3Nikhil V. Suresh4Amr Selim Abu Lila5Afrasim Moin6Hadil Faris Alotaibi7Ahmad J. Obaidullah8El-Sayed Khafagy9Department of Pharmaceutics, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, IndiaDepartment of Pharmacognosy, KLE College of Pharmacy, Bengaluru 560010, IndiaDepartment of Pharmaceutics, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, IndiaKLE Society’s Institute of Dental Sciences, Bengaluru 560022, IndiaKLE Society’s Institute of Dental Sciences, Bengaluru 560022, 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 Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint AbdulRahman University, Riyadh 11671, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi ArabiaPeriodontitis is an inflammatory disorder associated with dysbiosis and characterized by microbiologically related, host-mediated inflammation that leads to the damage of periodontal tissues including gingiva, connective tissues, and alveolar bone. The aim of this study was to develop an in situ gel consisting of piperine. Eight in situ gel formulations were designed by varying the concentration of deacylated gellan gum cross-linked with sodium tripolyphosphate, and poloxamer-407. The prepared gels were evaluated for gelation temperature, gelation time, viscosity, piperine-loading efficiency, and piperine release. Finally, the optimized formula was evaluated for anti-inflammatory effectiveness among human patients during a 14-day follow-up. The optimized in situ gel formulation exhibited a gelation temperature of 35 ± 1 °C, gelling of 36 ± 1 s, excellent syringeability, and piperine loading of 95.3 ± 2.3%. This formulation efficiently sustained in vitro drug release for up to 72 h. In vivo studies revealed an efficient sol-to-gel transformation of optimized in situ gel formulation at physiological conditions, permitting an efficient residence time of the formulation within a periodontitis pocket. Most importantly, a clinical study revealed that treatment with the optimized formulation elicited a significant reduction in the mean plaque score (<i>p</i> = 0.001), gingival index (<i>p</i> = 0.003), and pocket depth (<i>p</i> = 0.002), and exerted a potent anti-inflammatory potential, compared to the control group. Collectively, piperine-loaded in situ gel might represent a viable therapeutic approach for the management of gingival and periodontal diseases.https://www.mdpi.com/2310-2861/9/7/577anti-inflammatoryanti-plaquein situ gelperiodontitispiperine |
| spellingShingle | Poornima K. Gopalakrishna Rajamma Abburu Jayaramu Sateesha Shivally Boregowda Shruthi Eshwar Nikhil V. Suresh Amr Selim Abu Lila Afrasim Moin Hadil Faris Alotaibi Ahmad J. Obaidullah El-Sayed Khafagy Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis Gels anti-inflammatory anti-plaque in situ gel periodontitis piperine |
| title | Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis |
| title_full | Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis |
| title_fullStr | Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis |
| title_full_unstemmed | Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis |
| title_short | Piperine-Loaded In Situ Gel: Formulation, In Vitro Characterization, and Clinical Evaluation against Periodontitis |
| title_sort | piperine loaded in situ gel formulation in vitro characterization and clinical evaluation against periodontitis |
| topic | anti-inflammatory anti-plaque in situ gel periodontitis piperine |
| url | https://www.mdpi.com/2310-2861/9/7/577 |
| work_keys_str_mv | AT poornimakgopalakrishna piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT rajammaabburujayaramu piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT sateeshashivallyboregowda piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT shruthieshwar piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT nikhilvsuresh piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT amrselimabulila piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT afrasimmoin piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT hadilfarisalotaibi piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT ahmadjobaidullah piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis AT elsayedkhafagy piperineloadedinsitugelformulationinvitrocharacterizationandclinicalevaluationagainstperiodontitis |