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    Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion

    Year: 2021

    Journal: Pharmaceutics, Volume 13, JUL

    Authors: Li, Meng; Furey, Casey; Skros, Jeffrey; Xu, Olivia; Rahman, Mahbubur; Azad, Mohammad; Dave, Rajesh; Bilgili, Ecevit

    Organizations: U.S. National Science Foundation Engineering Research Center for Structured Organic Particulate Systems (NSF) [EEC-0540855]

    Keywords: nanocomposites; amorphous solid dispersion; wet media milling; nanoextrusion; wettability; dissolution

    We aimed to examine the impact of milling of extrudates prepared via nanoextrusion and the resulting matrix surface area of the particles on griseofulvin (GF, a model poorly soluble drug) release during in vitro dissolution. Wet-milled GF nanosuspensions containing a polymer (Sol: Soluplus(R), Kol: Kolliphor(R) P407, or HPC: Hydroxypropyl cellulose) and sodium dodecyl sulfate were mixed with additional polymer and dried in an extruder. The extrudates with 2% and 10% GF loading were milled-sieved into three size fractions. XRPD-SEM results show that nanoextrusion produced GF nanocomposites with Kol/HPC and an amorphous solid dispersion (ASD) with Sol. For 8.9 mg GF dose (non-supersaturating condition), the dissolution rate parameter was higher for extrudates with higher external specific surface area and those with 10% drug loading. It exhibited a monotonic increase with surface area of the ASD, whereas its increase tended to saturate above similar to 30 x 10(-3) m(2)/cm(3) for the nanocomposites. In general, the nanocomposites released GF faster than the ASD due to greater wettability and faster erosion imparted by Kol/HPC than by Sol. For 100 mg GF dose, the ASD outperformed the nanocomposites due to supersaturation and only 10% GF ASD with 190 x 10(-3) m(2)/cm(3) surface area achieved immediate release (80% release within 30 min). Hence, this study suggests that ASD extrudates entail fine milling yielding > similar to 200 x 10(-3) m(2)/cm(3) for rapid drug release, whereas only a coarse milling yielding similar to 30 x 10(-3) m(2)/cm(3) may enable nanocomposites to release low-dose drugs rapidly.
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