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

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.

SUBMITTER: Li M

PROVIDER: S-EPMC8308970 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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

Li Meng M Furey Casey C Skros Jeffrey J Xu Olivia O Rahman Mahbubur M Azad Mohammad M Dave Rajesh R Bilgili Ecevit E

Pharmaceutics 20210707 7

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<sup>®</sup>, Kol: Kolliphor<sup>®</sup> 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 ...[more]

PMID: 34371728

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Dataset Information

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

Publications

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

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