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Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation.

Cai S, Shi CH, Zhang X, Tang X, Suo H, Yang L, Zhao Y - Int J Nanomedicine (2014)

Bottom Line: The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension.Improved solubility and lymphatic transport may contribute to this enhanced bioavailability.Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, The First Affiliated Hospital of China Medical University, People's Republic of China.

ABSTRACT
The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD). Optimized SMEDDS formulations for 25-OCH3-PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OCH3-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH3-PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route.

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Related in: MedlinePlus

Transmission electron micrograph of 25-OCH3-PPD-loaded self-microemulsifying drug-delivery system.
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f3-ijn-9-913: Transmission electron micrograph of 25-OCH3-PPD-loaded self-microemulsifying drug-delivery system.

Mentions: The 25-OCH3-PPD-loaded SMEDDS became a microemulsion when diluted with distilled water (1:200, w/w). A transmission electron microscopy image is shown in Figure 3. The nanoemulsion droplets were observed to be spherical.


Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation.

Cai S, Shi CH, Zhang X, Tang X, Suo H, Yang L, Zhao Y - Int J Nanomedicine (2014)

Transmission electron micrograph of 25-OCH3-PPD-loaded self-microemulsifying drug-delivery system.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3928458&req=5

f3-ijn-9-913: Transmission electron micrograph of 25-OCH3-PPD-loaded self-microemulsifying drug-delivery system.
Mentions: The 25-OCH3-PPD-loaded SMEDDS became a microemulsion when diluted with distilled water (1:200, w/w). A transmission electron microscopy image is shown in Figure 3. The nanoemulsion droplets were observed to be spherical.

Bottom Line: The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension.Improved solubility and lymphatic transport may contribute to this enhanced bioavailability.Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, The First Affiliated Hospital of China Medical University, People's Republic of China.

ABSTRACT
The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD). Optimized SMEDDS formulations for 25-OCH3-PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OCH3-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH3-PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route.

Show MeSH
Related in: MedlinePlus