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Pharmaceutics 2018, 10(3), 155; https://doi.org/10.3390/pharmaceutics10030155

Amorphous Nanoparticulate Formulation of Sirolimus and Its Tablets

State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, China
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Received: 14 August 2018 / Revised: 28 August 2018 / Accepted: 29 August 2018 / Published: 11 September 2018
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Abstract

Nanocrystallization and amorphization have proven to be two effective strategies to improve the bioavailability of water-insoluble drugs. The purpose of our work was to develop a nano-formulated tablet of sirolimus (SRL) for enhanced dissolution. Amorphous SRL nanocomposites were prepared using anti-solvent precipitation via a high-gravity rotating packed bed. Various factors that affect particle size and size distribution, such as excipients, rotating speed, antisolvent/solvent flow rate, were investigated. Structure, stability and in vitro dissolution of the as-prepared SRL were evaluated. Furthermore, the nanoparticulated SRL tablet formula was screened to control drug release. Importantly, SRL tablets exhibit different dissolution profile by adjusting HPMC (hydroxypropyl methyl cellulose) content, which makes them more suitable for various formulation developments. View Full-Text
Keywords: amorphous sirolimus nanoparticles; antisolvent precipitation; high gravity rotating packed bed; dissolution rate; tablet formula amorphous sirolimus nanoparticles; antisolvent precipitation; high gravity rotating packed bed; dissolution rate; tablet formula
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Shen, Y.; Li, X.; Le, Y. Amorphous Nanoparticulate Formulation of Sirolimus and Its Tablets. Pharmaceutics 2018, 10, 155.

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