Literature DB >> 28236269

The Development of Self-nanoemulsifying Liquisolid Tablets to Improve the Dissolution of Simvastatin.

Shaimaa Elkadi1, Samar Elsamaligy2, Saleh Al-Suwayeh3, Hanaa Mahmoud3.   

Abstract

The aim of this work was to develop self-nanoemulsifying liquisolid tablets (SNELT) to enhance the dissolution profile of poorly water-soluble simvastatin. SNELT present a unique technique of incorporating self-nanoemulsifying drug delivery systems (SNEDDS) into tablets. Optimized SNEDDS containing different oils, Cremophor® RH 40 (surfactant) and Transcutol® HP (co-surfactant), at different ratios, were used as liquid vehicles and loaded on carrier material, microcrystalline cellulose (MCC), and coating material, Cab-o-sil® H-5 (nanosize colloidal silicon dioxide) powders at different loading factors (L f ) and fixed excipient ratio (R = 20). The effect of using different carrier materials, granulated mannitol, crystalline mannitol, and maltodextrin with MCC at different ratios, and different coating materials, Aeroperl® 300 (granulated silicon dioxide) at different excipient ratios (R), was also emphasized. Liquisolid powders with acceptable flowability, compressibility, and tablet weight were compressed into tablets. Results revealed that powders with L f  = 0.2 possessed the most preferable properties to be tableted. SNELT with MCC and Cab-o-sil® H-5 were able to generate nanoemulsions and to enhance the cumulative percent of drug dissolved at 60 min significantly to reach up to 90%. Furthermore, using carrier material (granulated mannitol/MCC at ratio 3:1) enabled SNELT to disperse into nanoemulsion (Z-average = 25.7 nm) and improved the dissolution profile significantly to reach 99% at 60 min. Cab-o-sil® H-5 proved to be a better coating material compared to Aeroperl® 300. In conclusion, developed SNELT were promising in enhancing in vitro dissolution of simvastatin and excipients highly affect SNELT's performance.

Entities:  

Keywords:  BCS class II drug; Cab-o-sil® H-5; granulated mannitol; self-nanoemulsifying liquisolid tablets; simvastatin

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Year:  2017        PMID: 28236269     DOI: 10.1208/s12249-017-0743-z

Source DB:  PubMed          Journal:  AAPS PharmSciTech        ISSN: 1530-9932            Impact factor:   3.246


  3 in total

1.  Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs.

Authors:  Hey-Won Shin; Joo-Eun Kim; Young-Joon Park
Journal:  Pharmaceutics       Date:  2021-01-06       Impact factor: 6.321

2.  Effects of simvastatin-loaded PLGA microspheres on treatment of rats with intervertebral disk degeneration and on 6-K-PGF1α and HIF-1α.

Authors:  Kai Zhu; Futing Zhao; Yanhua Yang; Weidong Mu
Journal:  Exp Ther Med       Date:  2019-12-02       Impact factor: 2.447

3.  Formation of Self-Assembled Liquid Crystalline Nanoparticles and Absorption Enhancement of Ω-3s by Phospholipids and Oleic Acids.

Authors:  Sang-Won Jeon; Han-Sol Jin; Young-Joon Park
Journal:  Pharmaceutics       Date:  2021-12-28       Impact factor: 6.321

  3 in total

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