Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery
In: Pharmaceuticals, Vol 15, Iss 311, p 311 (2022, Jg. 15 (2022), Heft 311, p 311
Online
academicJournal
Zugriff:
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 ( f 2 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.
Titel: |
Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery
|
---|---|
Autor/in / Beteiligte Person: | Sreeharsha, Nagaraja ; Nimbagal Raghavendra Naveen ; Anitha, Posina ; Goudanavar, Prakash S. ; Ramkanth, Sundarapandian ; Fattepur, Santosh ; Telsang, Mallikarjun ; Habeebuddin, Mohammed ; Md. Khalid Answer |
Link: | |
Zeitschrift: | Pharmaceuticals, Vol 15, Iss 311, p 311 (2022, Jg. 15 (2022), Heft 311, p 311 |
Veröffentlichung: | MDPI AG, 2022 |
Medientyp: | academicJournal |
ISSN: | 1424-8247 (print) |
DOI: | 10.3390/ph15030311 |
Schlagwort: |
|
Sonstiges: |
|