Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion
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>...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/7/1036 |
| _version_ | 1797526326317416448 |
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| author | Meng Li Casey Furey Jeffrey Skros Olivia Xu Mahbubur Rahman Mohammad Azad Rajesh Dave Ecevit Bilgili |
| author_facet | Meng Li Casey Furey Jeffrey Skros Olivia Xu Mahbubur Rahman Mohammad Azad Rajesh Dave Ecevit Bilgili |
| author_sort | Meng Li |
| collection | DOAJ |
| description | 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 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<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> 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<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> surface area achieved immediate release (80% release within 30 min). Hence, this study suggests that ASD extrudates entail fine milling yielding > ~200 × 10<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> for rapid drug release, whereas only a coarse milling yielding ~30 × 10<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> may enable nanocomposites to release low-dose drugs rapidly. |
| first_indexed | 2024-03-10T09:28:24Z |
| format | Article |
| id | doaj.art-85e6b4e458c74cf2aea72ade69cefd05 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T09:28:24Z |
| publishDate | 2021-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-85e6b4e458c74cf2aea72ade69cefd052023-11-22T04:41:02ZengMDPI AGPharmaceutics1999-49232021-07-01137103610.3390/pharmaceutics13071036Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via NanoextrusionMeng Li0Casey Furey1Jeffrey Skros2Olivia Xu3Mahbubur Rahman4Mohammad Azad5Rajesh Dave6Ecevit Bilgili7Otto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USAOtto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USAOtto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USAOtto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USAOtto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USADepartment of Chemical, Biological and Bioengineering, North Carolina A&T State University, Greensboro, NC 27411, USAOtto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USAOtto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USAWe 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 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<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> 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<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> surface area achieved immediate release (80% release within 30 min). Hence, this study suggests that ASD extrudates entail fine milling yielding > ~200 × 10<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> for rapid drug release, whereas only a coarse milling yielding ~30 × 10<sup>−3</sup> m<sup>2</sup>/cm<sup>3</sup> may enable nanocomposites to release low-dose drugs rapidly.https://www.mdpi.com/1999-4923/13/7/1036nanocompositesamorphous solid dispersionwet media millingnanoextrusionwettabilitydissolution |
| spellingShingle | Meng Li Casey Furey Jeffrey Skros Olivia Xu Mahbubur Rahman Mohammad Azad Rajesh Dave Ecevit Bilgili Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion Pharmaceutics nanocomposites amorphous solid dispersion wet media milling nanoextrusion wettability dissolution |
| title | Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion |
| title_full | Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion |
| title_fullStr | Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion |
| title_full_unstemmed | Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion |
| title_short | Impact of Matrix Surface Area on Griseofulvin Release from Extrudates Prepared via Nanoextrusion |
| title_sort | impact of matrix surface area on griseofulvin release from extrudates prepared via nanoextrusion |
| topic | nanocomposites amorphous solid dispersion wet media milling nanoextrusion wettability dissolution |
| url | https://www.mdpi.com/1999-4923/13/7/1036 |
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