"Impact of matrix surface area on griseofulvin release from extrudates " by Meng Li, Casey Furey et al.
 

Impact of matrix surface area on griseofulvin release from extrudates prepared via nanoextrusion

Document Type

Article

Publication Date

7-1-2021

Abstract

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®, Kol: Kolliphor® 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 ~30 × 10−3 m2 /cm3 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 × 10−3 m2 /cm3 surface area achieved immediate release (80% release within 30 min). Hence, this study suggests that ASD extrudates entail fine milling yielding > ~200 × 10−3 m2 /cm3 for rapid drug release, whereas only a coarse milling yielding ~30 × 10−3 m2 /cm3 may enable nanocomposites to release low-dose drugs rapidly.

Identifier

85110828644 (Scopus)

Publication Title

Pharmaceutics

External Full Text Location

https://doi.org/10.3390/pharmaceutics13071036

e-ISSN

19994923

Issue

7

Volume

13

Grant

EEC-0540855

Fund Ref

National Science Foundation

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