Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate
The aim of this work is to present an approach to enhance the dissolution of progestin medication, megestrol acetate (also known as MEGACE), for improving the dissolution rate and kinetic solubility by incorporating nano graphene oxide (nGO). An antisolvent precipitation process was investigated for...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-03-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/7/1972 |
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| author | Mohammad Saiful Islam Faradae Renner Kimberly Foster Martin S. Oderinde Kevin Stefanski Somenath Mitra |
| author_facet | Mohammad Saiful Islam Faradae Renner Kimberly Foster Martin S. Oderinde Kevin Stefanski Somenath Mitra |
| author_sort | Mohammad Saiful Islam |
| collection | DOAJ |
| description | The aim of this work is to present an approach to enhance the dissolution of progestin medication, megestrol acetate (also known as MEGACE), for improving the dissolution rate and kinetic solubility by incorporating nano graphene oxide (nGO). An antisolvent precipitation process was investigated for nGO-drug composite preparation, where prepared composites showed crystalline properties that were similar to the pure drug but enhanced aqueous dispersibility and colloidal stability. To validate the efficient release profile of composite, in vitro dissolution testing was carried out using United States Pharmacopeia, USP-42 paddle method, with gastric pH (1.4) and intestinal pH (6.5) solutions to mimic in vivo conditions. Pure MA is practically insoluble (2 µg/mL at 37 °C). With the incorporation of nGO, it was possible to dissolve nearly 100% in the assay. With the incorporation of 1.0% of nGO, the time required to dissolve 50% and 80% of drug, namely T<sub>50</sub> and T<sub>80</sub>, decreased from 138.0 min to 27.0 min, and the drug did not dissolve for 97.0 min in gastric media, respectively. Additionally, studies done in intestinal media have revealed T<sub>50</sub> did not dissolve for 92.0 min. This work shows promise in incorporating functionalized nanoparticles into the crystal lattice of poorly soluble drugs to improve dissolution rate. |
| first_indexed | 2024-03-10T12:44:28Z |
| format | Article |
| id | doaj.art-5e9ee8d14c414b3da02e3a75c5bf9eb9 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T12:44:28Z |
| publishDate | 2021-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-5e9ee8d14c414b3da02e3a75c5bf9eb92023-11-21T13:37:28ZengMDPI AGMolecules1420-30492021-03-01267197210.3390/molecules26071972Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol AcetateMohammad Saiful Islam0Faradae Renner1Kimberly Foster2Martin S. Oderinde3Kevin Stefanski4Somenath Mitra5Department of Chemistry and Environmental Science, New Jersey Institute of Technology, Newark, NJ 07102, USADepartment of Chemistry and Environmental Science, New Jersey Institute of Technology, Newark, NJ 07102, USABristol Myers Squibb Research and Early Development, Princeton, NJ 08543, USABristol Myers Squibb Research and Early Development, Princeton, NJ 08543, USABristol Myers Squibb Research and Early Development, Princeton, NJ 08543, USADepartment of Chemistry and Environmental Science, New Jersey Institute of Technology, Newark, NJ 07102, USAThe aim of this work is to present an approach to enhance the dissolution of progestin medication, megestrol acetate (also known as MEGACE), for improving the dissolution rate and kinetic solubility by incorporating nano graphene oxide (nGO). An antisolvent precipitation process was investigated for nGO-drug composite preparation, where prepared composites showed crystalline properties that were similar to the pure drug but enhanced aqueous dispersibility and colloidal stability. To validate the efficient release profile of composite, in vitro dissolution testing was carried out using United States Pharmacopeia, USP-42 paddle method, with gastric pH (1.4) and intestinal pH (6.5) solutions to mimic in vivo conditions. Pure MA is practically insoluble (2 µg/mL at 37 °C). With the incorporation of nGO, it was possible to dissolve nearly 100% in the assay. With the incorporation of 1.0% of nGO, the time required to dissolve 50% and 80% of drug, namely T<sub>50</sub> and T<sub>80</sub>, decreased from 138.0 min to 27.0 min, and the drug did not dissolve for 97.0 min in gastric media, respectively. Additionally, studies done in intestinal media have revealed T<sub>50</sub> did not dissolve for 92.0 min. This work shows promise in incorporating functionalized nanoparticles into the crystal lattice of poorly soluble drugs to improve dissolution rate.https://www.mdpi.com/1420-3049/26/7/1972enhanced dissolutionnano graphene oxideoral medicationpaddle methodgastrointestinal pHmegestrol acetate |
| spellingShingle | Mohammad Saiful Islam Faradae Renner Kimberly Foster Martin S. Oderinde Kevin Stefanski Somenath Mitra Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate Molecules enhanced dissolution nano graphene oxide oral medication paddle method gastrointestinal pH megestrol acetate |
| title | Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate |
| title_full | Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate |
| title_fullStr | Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate |
| title_full_unstemmed | Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate |
| title_short | Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate |
| title_sort | hydrophilic and functionalized nanographene oxide incorporated faster dissolving megestrol acetate |
| topic | enhanced dissolution nano graphene oxide oral medication paddle method gastrointestinal pH megestrol acetate |
| url | https://www.mdpi.com/1420-3049/26/7/1972 |
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