Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin
In oral administration systems, mucoadhesive polymers are crucial for drug localization and target-specific activities. The current work focuses on the application of thiolated xanthan gum (TXG) to develop and characterize a novel mucoadhesive nanocrystal (NC) system of simvastatin (SIM). Preparatio...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/23/5184 |
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| author | Rana B. Bakhaidar Nimbagal Raghavendra Naveen Pratap Basim Samar S. Murshid Mallesh Kurakula Abdulmohsin J. Alamoudi Deena M. Bukhary Abdulmajeed M. Jali Mohammed A. Majrashi Sameer Alshehri Mohammed Alissa Rayan A. Ahmed |
| author_facet | Rana B. Bakhaidar Nimbagal Raghavendra Naveen Pratap Basim Samar S. Murshid Mallesh Kurakula Abdulmohsin J. Alamoudi Deena M. Bukhary Abdulmajeed M. Jali Mohammed A. Majrashi Sameer Alshehri Mohammed Alissa Rayan A. Ahmed |
| author_sort | Rana B. Bakhaidar |
| collection | DOAJ |
| description | In oral administration systems, mucoadhesive polymers are crucial for drug localization and target-specific activities. The current work focuses on the application of thiolated xanthan gum (TXG) to develop and characterize a novel mucoadhesive nanocrystal (NC) system of simvastatin (SIM). Preparation of SIM-NC was optimized using response surface methodology (RSM) coupled with statistical applications. The concentration of Pluronic F-127 and vacuum pressure were optimized by central composite design. Based on this desirable approach, the prerequisites of the optimum formulation can be achieved by a formulation having 92.568 mg of F-127 and 77.85 mbar vacuum pressure to result in EE of 88.8747% and PS of 0.137.835 nm. An optimized formulation was prepared with the above conditions along with xanthan gum (XG) and TXG and various parameters were evaluated. A formulation containing TXG showed 98.25% of SIM at the end of 96 h. Regarding the mucoadhesion potential evaluated by measuring zeta potential, TXG-SIM-NC shoed the maximum zeta potential of 16,455.8 ± 869 mV at the end of 6 h. The cell viability percentage of TXG-SIM-NC (52.54 ± 3.4% with concentration of 50 µg/mL) was less than the plain SIM, with XG-SIM-NC showing the highest cytotoxicity on HSC-3 cells. In vivo pharmacokinetic studies confirm the enhanced bioavailability of formulated mucoadhesive systems of SIM-NC, with TXG-SIM-NC exhibiting the maximum. |
| first_indexed | 2024-03-09T17:34:32Z |
| format | Article |
| id | doaj.art-22f1a4522b0943b387742501af802ae0 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T17:34:32Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-22f1a4522b0943b387742501af802ae02023-11-24T11:59:48ZengMDPI AGPolymers2073-43602022-11-011423518410.3390/polym14235184Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of SimvastatinRana B. Bakhaidar0Nimbagal Raghavendra Naveen1Pratap Basim2Samar S. Murshid3Mallesh Kurakula4Abdulmohsin J. Alamoudi5Deena M. Bukhary6Abdulmajeed M. Jali7Mohammed A. Majrashi8Sameer Alshehri9Mohammed Alissa10Rayan A. Ahmed11Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaSri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B. G. Nagar, Karnataka 571448, IndiaThermo Fisher Scientific, Cincinnati, OH 45237, USADepartment of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaThermo Fisher Scientific, Bend, OR 97701, USADepartment of Pharmacology and Toxicology, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, Makkah 24381, Saudi ArabiaDepartment of Pharmacology and Toxicology, College of Pharmacy, Jazan University, Jazan 45142, Saudi ArabiaDepartment of Pharmacology, College of Medicine, University of Jeddah, Jeddah 23890, Saudi ArabiaDepartment of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Taif University, Taif 21944, Saudi ArabiaDepartment of Medical Laboratory Sciences, College of Applied Medical Sciences, Prince Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmacology and Toxicology, College of Pharmacy, Jazan University, Jazan 45142, Saudi ArabiaIn oral administration systems, mucoadhesive polymers are crucial for drug localization and target-specific activities. The current work focuses on the application of thiolated xanthan gum (TXG) to develop and characterize a novel mucoadhesive nanocrystal (NC) system of simvastatin (SIM). Preparation of SIM-NC was optimized using response surface methodology (RSM) coupled with statistical applications. The concentration of Pluronic F-127 and vacuum pressure were optimized by central composite design. Based on this desirable approach, the prerequisites of the optimum formulation can be achieved by a formulation having 92.568 mg of F-127 and 77.85 mbar vacuum pressure to result in EE of 88.8747% and PS of 0.137.835 nm. An optimized formulation was prepared with the above conditions along with xanthan gum (XG) and TXG and various parameters were evaluated. A formulation containing TXG showed 98.25% of SIM at the end of 96 h. Regarding the mucoadhesion potential evaluated by measuring zeta potential, TXG-SIM-NC shoed the maximum zeta potential of 16,455.8 ± 869 mV at the end of 6 h. The cell viability percentage of TXG-SIM-NC (52.54 ± 3.4% with concentration of 50 µg/mL) was less than the plain SIM, with XG-SIM-NC showing the highest cytotoxicity on HSC-3 cells. In vivo pharmacokinetic studies confirm the enhanced bioavailability of formulated mucoadhesive systems of SIM-NC, with TXG-SIM-NC exhibiting the maximum.https://www.mdpi.com/2073-4360/14/23/5184health caresimvastatinxanthan gumthiolationmucoadhesionresponse surface methodology |
| spellingShingle | Rana B. Bakhaidar Nimbagal Raghavendra Naveen Pratap Basim Samar S. Murshid Mallesh Kurakula Abdulmohsin J. Alamoudi Deena M. Bukhary Abdulmajeed M. Jali Mohammed A. Majrashi Sameer Alshehri Mohammed Alissa Rayan A. Ahmed Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin Polymers health care simvastatin xanthan gum thiolation mucoadhesion response surface methodology |
| title | Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin |
| title_full | Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin |
| title_fullStr | Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin |
| title_full_unstemmed | Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin |
| title_short | Response Surface Methodology (RSM) Powered Formulation Development, Optimization and Evaluation of Thiolated Based Mucoadhesive Nanocrystals for Local Delivery of Simvastatin |
| title_sort | response surface methodology rsm powered formulation development optimization and evaluation of thiolated based mucoadhesive nanocrystals for local delivery of simvastatin |
| topic | health care simvastatin xanthan gum thiolation mucoadhesion response surface methodology |
| url | https://www.mdpi.com/2073-4360/14/23/5184 |
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