Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model
The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/5/627 |
| _version_ | 1797535954511069184 |
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| author | Ahmad A. Shahba Ahmad Y. Tashish Fars K. Alanazi Mohsin Kazi |
| author_facet | Ahmad A. Shahba Ahmad Y. Tashish Fars K. Alanazi Mohsin Kazi |
| author_sort | Ahmad A. Shahba |
| collection | DOAJ |
| description | The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin<sup>®</sup> US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release. |
| first_indexed | 2024-03-10T11:52:41Z |
| format | Article |
| id | doaj.art-08cf3d8047364d3b9c44bfadac9eac70 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T11:52:41Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-08cf3d8047364d3b9c44bfadac9eac702023-11-21T17:32:53ZengMDPI AGPharmaceutics1999-49232021-04-0113562710.3390/pharmaceutics13050627Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution ModelAhmad A. Shahba0Ahmad Y. Tashish1Fars K. Alanazi2Mohsin Kazi3Kayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaKayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaKayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaThe study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin<sup>®</sup> US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release.https://www.mdpi.com/1999-4923/13/5/627self-nanoemulsifying drug delivery systems (SNEDDS)solid dispersionpoorly-water soluble drugshypochlorhydria/achlorhydriasolidificationelevated gastric pH |
| spellingShingle | Ahmad A. Shahba Ahmad Y. Tashish Fars K. Alanazi Mohsin Kazi Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model Pharmaceutics self-nanoemulsifying drug delivery systems (SNEDDS) solid dispersion poorly-water soluble drugs hypochlorhydria/achlorhydria solidification elevated gastric pH |
| title | Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model |
| title_full | Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model |
| title_fullStr | Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model |
| title_full_unstemmed | Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model |
| title_short | Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model |
| title_sort | combined self nanoemulsifying and solid dispersion systems showed enhanced cinnarizine release in hypochlorhydria achlorhydria dissolution model |
| topic | self-nanoemulsifying drug delivery systems (SNEDDS) solid dispersion poorly-water soluble drugs hypochlorhydria/achlorhydria solidification elevated gastric pH |
| url | https://www.mdpi.com/1999-4923/13/5/627 |
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