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Formulation of 20(S)-protopanaxadiol nanocrystals to improve oral bioavailability and brain delivery
Chen C.2; Wang L.1; Cao F.1; Miao X.2; Chen T.2; Chang Q.1; Zheng Y.2
2016-01-30
Source PublicationInternational Journal of Pharmaceutics
ISSN18733476 03785173
Volume497Issue:1-2Pages:239-247
Abstract

The aim of this study was to fabricate 20(S)-protopanaxadiol (PPD) nanocrystals to improve PPD's oral bioavailability and brain delivery. PPD nanocrystals were fabricated using an anti-solvent precipitation approach where d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) was optimized as the stabilizer. The fabricated nanocrystals were nearly spherical with a particle size and drug loading of 90.44 ± 1.45 nm and 76.92%, respectively. They are in the crystalline state and stable at 4 °C for at least 1 month. More than 90% of the PPD could be rapidly released from the nanocrystals, which was much faster than the physical mixture and PPD powder. PPD nanocrystals demonstrated comparable permeability to solution at 2.52 ± 0.44 × 10 cm/s on MDCK monolayers. After oral administration of PPD nanocrystals to rats, PPD was absorbed quickly into the plasma and brain with significantly higher C and AUC compared to those of the physical mixture. However, no brain targeting was observed, as the ratios of the plasma AUC to brain AUC for the two groups were similar. In summary, PPD nanocrystals are a potential oral delivery system to improve PPD's poor bioavailability and its delivery into the brain for neurodegenerative disease and intracranial tumor therapies in the future.

Keyword20(s)-protopanaxadiol Bioavailability Brain Delivery D-α-tocopheryl Polyethylene Glycol 1000 Succinate Nanocrystals
DOI10.1016/j.ijpharm.2015.12.014
URLView the original
Indexed BySCI
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000367385600025
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Cited Times [WOS]:17   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Chinese Academy of Medical Sciences
2.Universidade de Macau
Recommended Citation
GB/T 7714
Chen C.,Wang L.,Cao F.,et al. Formulation of 20(S)-protopanaxadiol nanocrystals to improve oral bioavailability and brain delivery[J]. International Journal of Pharmaceutics,2016,497(1-2):239-247.
APA Chen C..,Wang L..,Cao F..,Miao X..,Chen T..,...&Zheng Y..(2016).Formulation of 20(S)-protopanaxadiol nanocrystals to improve oral bioavailability and brain delivery.International Journal of Pharmaceutics,497(1-2),239-247.
MLA Chen C.,et al."Formulation of 20(S)-protopanaxadiol nanocrystals to improve oral bioavailability and brain delivery".International Journal of Pharmaceutics 497.1-2(2016):239-247.
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