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Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery.
- Source :
-
Pharmaceuticals (14248247) . Mar2022, Vol. 15 Issue 3, p311. 17p. - Publication Year :
- 2022
-
Abstract
- The present work aimed to develop a chronotherapeutic system of valsartan (VS) using nanocrystal formulation to improve dissolution. VS nanocrystals (VS-NC) were fabricated using modified anti-solvent precipitation by employing a Box–Behnken design to optimize various process variables. Based on the desirability approach, a formulation containing 2.5% poloxamer, a freezing temperature of −25 °C, and 24 h of freeze-drying time can fulfill the optimized formulation's requirements to result in a particle size of 219.68 nm, 0.201 polydispersity index, and zeta potential of −38.26 mV. Optimized VS-NC formulation was compressed (VNM) and coated subsequently with ethyl cellulose and HPMC E 5. At the same time, fast dissolving tablets of VS were designed, and the best formulation was loaded with VNM into a capsule size 1 (average fill weight—400–500 mg, lock length—19.30 mm, external diameter: Cap—6.91 mm; Body—6.63 mm). The final tab in cap (tablet-in-capsule) system was studied for in vitro dissolution profile to confirm the chronotherapeutic release of VS. As required, a bi-pulse release of VS was identified with a lag time of 5 h. The accelerated stability studies confirmed no significant changes in the dissolution profiles of the tab in cap system (f2 similarity profile: >90). To conclude, the tab in cap system was successfully developed to induce a dual pulsatile release, which will ensure bedtime dosing with release after a lag-time to match with early morning circadian spikes. [ABSTRACT FROM AUTHOR]
- Subjects :
- *ETHYLCELLULOSE
*ZETA potential
*NANOCAPSULES
*NANOCRYSTALS
*FREEZE-drying
*VALSARTAN
Subjects
Details
- Language :
- English
- ISSN :
- 14248247
- Volume :
- 15
- Issue :
- 3
- Database :
- Academic Search Index
- Journal :
- Pharmaceuticals (14248247)
- Publication Type :
- Academic Journal
- Accession number :
- 156072694
- Full Text :
- https://doi.org/10.3390/ph15030311