Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach
Currently, gastro-retentive dosage forms achieved a remarkable position among the oral drug delivery systems. This is a broadly used technique to hold the drug delivery systems for a long duration in the gastro intestine (GI) region, slow drug delivery, and overcome other challenges related to typic...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-08-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/8/981 |
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| author | Shaima Alaithan Nimbagal Raghavendra Naveen Prakash S. Goudanavar Penmetsa Durga Bhavani Beveenahalli Ramesh Naga Prashant Koppuravuri Santosh Fattepur Nagaraja Sreeharsha Anroop B. Nair Bandar E. Aldhubiab Pottathil Shinu Rashed M. Almuqbil |
| author_facet | Shaima Alaithan Nimbagal Raghavendra Naveen Prakash S. Goudanavar Penmetsa Durga Bhavani Beveenahalli Ramesh Naga Prashant Koppuravuri Santosh Fattepur Nagaraja Sreeharsha Anroop B. Nair Bandar E. Aldhubiab Pottathil Shinu Rashed M. Almuqbil |
| author_sort | Shaima Alaithan |
| collection | DOAJ |
| description | Currently, gastro-retentive dosage forms achieved a remarkable position among the oral drug delivery systems. This is a broadly used technique to hold the drug delivery systems for a long duration in the gastro intestine (GI) region, slow drug delivery, and overcome other challenges related to typical oral delivery such as low bioavailability. The current work aimed to formulate and characterize a new expandable gastro-retentive system through Itopride Hydrochloride (IH)’s unfolding process for controlled release. The IH-loaded unfolding film formulation was optimized using the Box-Behnken design for folding endurance and length of tested layer (LTL). Initially, the formulation was made using several anti-adhesive additives to promote the unfolding mechanism. Citric acid and sodium bicarbonate were selected as anti-adhesives based on these results. The enfolded film in a capsule shell was shown to unroll in the stomach fluids and render drug delivery up to 12 h in acidic conditions. A fabricated system should have dimensions more than the size of the relaxed pyloric sphincter, and as required, >20 mm LTL was identified. This further confirms that the residence period in the stomach is irrelevant to the fed or fasted condition. Based on desirability criteria, the formulation containing 143.83, 0.7982, and 14.6096 Eudragit L100, PEG, and sodium bicarbonate are selected as optimized formulations (O-IH-UF). The optimized formulation was further analyzed for various parameters such as tensile strength, mechanical strength, unfolding nature, degradability, and in vitro release studies. The pharmacokinetic study revealed greater AUC (area under the curve) and long half-life with the designed O-IH-UF formulation, confirming that the unfolding film type can be a favorable drug system for enhancing the bioavailability of low soluble drugs. The results showed that unfolding types of gastro retentive systems could potentiate the drugs with stability issues in an alkaline medium or those with absorption in acidic conditions. |
| first_indexed | 2024-03-09T09:50:32Z |
| format | Article |
| id | doaj.art-03a5343ea6dd4edbb5a197aebfa5237d |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T09:50:32Z |
| publishDate | 2022-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-03a5343ea6dd4edbb5a197aebfa5237d2023-12-02T00:08:58ZengMDPI AGPharmaceuticals1424-82472022-08-0115898110.3390/ph15080981Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive ApproachShaima Alaithan0Nimbagal Raghavendra Naveen1Prakash S. Goudanavar2Penmetsa Durga Bhavani3Beveenahalli Ramesh4Naga Prashant Koppuravuri5Santosh Fattepur6Nagaraja Sreeharsha7Anroop B. Nair8Bandar E. Aldhubiab9Pottathil Shinu10Rashed M. Almuqbil11Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaSri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagar 571448, Karnataka, IndiaSri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagar 571448, Karnataka, IndiaDepartment of Pharmaceutics, Vishnu Institute of Pharmaceutical Education and Research, Narsapur Medak 502313, Telangana, IndiaSri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagar 571448, Karnataka, IndiaSri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G. Nagar 571448, Karnataka, IndiaSchool of Pharmacy, Management and Science University, Seksyen 13, Shah Alam 40100, MalaysiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaCurrently, gastro-retentive dosage forms achieved a remarkable position among the oral drug delivery systems. This is a broadly used technique to hold the drug delivery systems for a long duration in the gastro intestine (GI) region, slow drug delivery, and overcome other challenges related to typical oral delivery such as low bioavailability. The current work aimed to formulate and characterize a new expandable gastro-retentive system through Itopride Hydrochloride (IH)’s unfolding process for controlled release. The IH-loaded unfolding film formulation was optimized using the Box-Behnken design for folding endurance and length of tested layer (LTL). Initially, the formulation was made using several anti-adhesive additives to promote the unfolding mechanism. Citric acid and sodium bicarbonate were selected as anti-adhesives based on these results. The enfolded film in a capsule shell was shown to unroll in the stomach fluids and render drug delivery up to 12 h in acidic conditions. A fabricated system should have dimensions more than the size of the relaxed pyloric sphincter, and as required, >20 mm LTL was identified. This further confirms that the residence period in the stomach is irrelevant to the fed or fasted condition. Based on desirability criteria, the formulation containing 143.83, 0.7982, and 14.6096 Eudragit L100, PEG, and sodium bicarbonate are selected as optimized formulations (O-IH-UF). The optimized formulation was further analyzed for various parameters such as tensile strength, mechanical strength, unfolding nature, degradability, and in vitro release studies. The pharmacokinetic study revealed greater AUC (area under the curve) and long half-life with the designed O-IH-UF formulation, confirming that the unfolding film type can be a favorable drug system for enhancing the bioavailability of low soluble drugs. The results showed that unfolding types of gastro retentive systems could potentiate the drugs with stability issues in an alkaline medium or those with absorption in acidic conditions.https://www.mdpi.com/1424-8247/15/8/981itopride hydrochloridegastro retentive systemsunfolding filmBox-Behnken designoptimization |
| spellingShingle | Shaima Alaithan Nimbagal Raghavendra Naveen Prakash S. Goudanavar Penmetsa Durga Bhavani Beveenahalli Ramesh Naga Prashant Koppuravuri Santosh Fattepur Nagaraja Sreeharsha Anroop B. Nair Bandar E. Aldhubiab Pottathil Shinu Rashed M. Almuqbil Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach Pharmaceuticals itopride hydrochloride gastro retentive systems unfolding film Box-Behnken design optimization |
| title | Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach |
| title_full | Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach |
| title_fullStr | Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach |
| title_full_unstemmed | Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach |
| title_short | Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach |
| title_sort | development of novel unfolding film system of itopride hydrochloride using box behnken design a gastro retentive approach |
| topic | itopride hydrochloride gastro retentive systems unfolding film Box-Behnken design optimization |
| url | https://www.mdpi.com/1424-8247/15/8/981 |
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