The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems
<b>Objectives</b>: A novel two-step flow-through in vitro lipolysis model was developed for the evaluation of drug release from a self-microemulsifying drug delivery system (SMEDDS). <b>Methods</b>: Firstly, the SMEDDS was dispersed in an acidic medium. Subsequently, the pH w...
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2025-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/17/5/545 |
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| author | Katarina Rede Mirjana Gašperlin Marija Bogataj Katarina Bolko Seljak |
| author_facet | Katarina Rede Mirjana Gašperlin Marija Bogataj Katarina Bolko Seljak |
| author_sort | Katarina Rede |
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| description | <b>Objectives</b>: A novel two-step flow-through in vitro lipolysis model was developed for the evaluation of drug release from a self-microemulsifying drug delivery system (SMEDDS). <b>Methods</b>: Firstly, the SMEDDS was dispersed in an acidic medium. Subsequently, the pH was increased, and a lipolytic reaction was immediately initiated, accompanied by medium flow onset. The latter enabled increase of the initial low pH of the medium, improving the physiological relevance of the method by simulating dosage form retainment in the stomach and transfer to the duodenum, which is very important for a weakly basic active pharmaceutical ingredient (API) incorporated in an SMEDDS. <b>Results</b>: Conversely to the traditional pH-stat in vitro lipolysis, the developed method is not established on titration, as the reaction vessel pH is regulated by a medium flow and buffer capacity. Individual parameters, such as pancreatin activity, buffer capacity, and medium shift, were researched using traditional pH-stat in vitro lipolysis prior to their implementation in the flow-through setup. <b>Conclusions</b>: The concentration of the solubilized model API, carvedilol, was increased as pancreatin activity decreased and as buffer capacity increased. The ratios between release profiles obtained under different conditions utilizing the pH-stat and novel two-step flow-through in vitro lipolysis were comparable; however, the differences were more pronounced in the flow-through method. |
| format | Article |
| id | doaj-art-adab5c36c9dd4772b33cf204897e8042 |
| institution | OA Journals |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-04-01 |
| publisher | MDPI AG |
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| series | Pharmaceutics |
| spelling | doaj-art-adab5c36c9dd4772b33cf204897e80422025-08-20T01:56:38ZengMDPI AGPharmaceutics1999-49232025-04-0117554510.3390/pharmaceutics17050545The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery SystemsKatarina Rede0Mirjana Gašperlin1Marija Bogataj2Katarina Bolko Seljak3Faculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, SloveniaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, SloveniaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, SloveniaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia<b>Objectives</b>: A novel two-step flow-through in vitro lipolysis model was developed for the evaluation of drug release from a self-microemulsifying drug delivery system (SMEDDS). <b>Methods</b>: Firstly, the SMEDDS was dispersed in an acidic medium. Subsequently, the pH was increased, and a lipolytic reaction was immediately initiated, accompanied by medium flow onset. The latter enabled increase of the initial low pH of the medium, improving the physiological relevance of the method by simulating dosage form retainment in the stomach and transfer to the duodenum, which is very important for a weakly basic active pharmaceutical ingredient (API) incorporated in an SMEDDS. <b>Results</b>: Conversely to the traditional pH-stat in vitro lipolysis, the developed method is not established on titration, as the reaction vessel pH is regulated by a medium flow and buffer capacity. Individual parameters, such as pancreatin activity, buffer capacity, and medium shift, were researched using traditional pH-stat in vitro lipolysis prior to their implementation in the flow-through setup. <b>Conclusions</b>: The concentration of the solubilized model API, carvedilol, was increased as pancreatin activity decreased and as buffer capacity increased. The ratios between release profiles obtained under different conditions utilizing the pH-stat and novel two-step flow-through in vitro lipolysis were comparable; however, the differences were more pronounced in the flow-through method.https://www.mdpi.com/1999-4923/17/5/545in vitro lipolysisflow-through dissolution systemdrug releaseself-microemulsifying drug delivery systems |
| spellingShingle | Katarina Rede Mirjana Gašperlin Marija Bogataj Katarina Bolko Seljak The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems Pharmaceutics in vitro lipolysis flow-through dissolution system drug release self-microemulsifying drug delivery systems |
| title | The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems |
| title_full | The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems |
| title_fullStr | The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems |
| title_full_unstemmed | The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems |
| title_short | The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems |
| title_sort | advancement of in vitro lipolysis two step flow through method for the evaluation of lipid based drug delivery systems |
| topic | in vitro lipolysis flow-through dissolution system drug release self-microemulsifying drug delivery systems |
| url | https://www.mdpi.com/1999-4923/17/5/545 |
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