Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in dev...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-10-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/11/1777 |
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| author | You Zhuan Lee Eng Kwong Seow Sheau Chin Lim Kah Hay Yuen Nurzalina Abdul Karim Khan |
| author_facet | You Zhuan Lee Eng Kwong Seow Sheau Chin Lim Kah Hay Yuen Nurzalina Abdul Karim Khan |
| author_sort | You Zhuan Lee |
| collection | DOAJ |
| description | Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in developing s-SEDDS are solid in nature, with a high amount of surfactants added. The aim of this study was to develop an s-SEDDS using a tocotrienol-rich fraction (TRF) as the model liquid active substance via a simple adsorption method. The solid formulation was developed using magnesium aluminosilicate as the carrier with 70% TRF and 30% surfactants (poloxamer and Labrasol<sup>®</sup>). The formulation showed good self-emulsification efficiency with stable emulsion formed, excellent powder flowability, and small emulsion droplet size of 210–277 nm. The s-SEDDS with combined surfactants (poloxamer and Labrasol<sup>®</sup>) showed a faster absorption rate compared to preparations with only a single surfactant and enhanced oral bioavailability (3.4–3.8 times higher) compared to the non-self-emulsifying oily preparation when administered at a fasted state in rats. In conclusion, an s-SEDDS containing a high amount of TRF was successfully developed. It may serve as a useful alternative to a liquid product with enhanced oral bioavailability and the added advantage of being a solid dosage form. |
| first_indexed | 2024-03-10T05:08:50Z |
| format | Article |
| id | doaj.art-4bc8443fe1ca49f6b03c5e464861f2bd |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T05:08:50Z |
| publishDate | 2021-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4bc8443fe1ca49f6b03c5e464861f2bd2023-11-23T00:57:27ZengMDPI AGPharmaceutics1999-49232021-10-011311177710.3390/pharmaceutics13111777Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active SubstanceYou Zhuan Lee0Eng Kwong Seow1Sheau Chin Lim2Kah Hay Yuen3Nurzalina Abdul Karim Khan4School of Pharmaceutical Sciences, Universiti Sains Malaysia, George Town 11800, Penang, MalaysiaSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, George Town 11800, Penang, MalaysiaSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, George Town 11800, Penang, MalaysiaSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, George Town 11800, Penang, MalaysiaSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, George Town 11800, Penang, MalaysiaSelf-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in developing s-SEDDS are solid in nature, with a high amount of surfactants added. The aim of this study was to develop an s-SEDDS using a tocotrienol-rich fraction (TRF) as the model liquid active substance via a simple adsorption method. The solid formulation was developed using magnesium aluminosilicate as the carrier with 70% TRF and 30% surfactants (poloxamer and Labrasol<sup>®</sup>). The formulation showed good self-emulsification efficiency with stable emulsion formed, excellent powder flowability, and small emulsion droplet size of 210–277 nm. The s-SEDDS with combined surfactants (poloxamer and Labrasol<sup>®</sup>) showed a faster absorption rate compared to preparations with only a single surfactant and enhanced oral bioavailability (3.4–3.8 times higher) compared to the non-self-emulsifying oily preparation when administered at a fasted state in rats. In conclusion, an s-SEDDS containing a high amount of TRF was successfully developed. It may serve as a useful alternative to a liquid product with enhanced oral bioavailability and the added advantage of being a solid dosage form.https://www.mdpi.com/1999-4923/13/11/1777self-emulsifying drug delivery systempoorly water-soluble drugssolid dosage formsin vivo oral bioavailabilitypharmacokinetictocotrienols |
| spellingShingle | You Zhuan Lee Eng Kwong Seow Sheau Chin Lim Kah Hay Yuen Nurzalina Abdul Karim Khan Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance Pharmaceutics self-emulsifying drug delivery system poorly water-soluble drugs solid dosage forms in vivo oral bioavailability pharmacokinetic tocotrienols |
| title | Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance |
| title_full | Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance |
| title_fullStr | Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance |
| title_full_unstemmed | Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance |
| title_short | Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance |
| title_sort | formulation and in vivo evaluation of a solid self emulsifying drug delivery system using oily liquid tocotrienols as model active substance |
| topic | self-emulsifying drug delivery system poorly water-soluble drugs solid dosage forms in vivo oral bioavailability pharmacokinetic tocotrienols |
| url | https://www.mdpi.com/1999-4923/13/11/1777 |
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