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Development and characterisation of ursolic acid nanocrystals without stabiliser having improved dissolution rate and in vitro anticancer activity
Song Ju.1,2; Wang Y.1,2; Song Y.1,2; Chan H.1,2; Bi C.1,2; Yang X.1,2; Yan R.1,2; Wang Y.1,2; Zheng Y.1,2
2014
Source PublicationAAPS PharmSciTech
ISSN15309932
Volume15Issue:1Pages:11
Abstract

Ursolic acid (UA), which is a natural pentacyclic triterpenoid, has the potential to be developed as an anticancer drug, whereas its poor aqueous solubility and dissolution rate limit its clinical application. The aim of the present study was to develop UA nanocrystals to enhance its aqueous dispersibility, dissolution rate and anticancer activity. Following the investigation on the effects of stabiliser, the ratio of organic phase to aqueous solution and drug concentration, the UA nanocrystals without stabiliser were successfully prepared by anti-solvent precipitation approach. The nanocrystals maintained similar crystallinity with particle size, polydispersion index and zeta potential values of 188.0 ± 4.4 nm, 0.154 ± 0.022, and -25.0 ± 5.9 mV, respectively. Compared with the raw material, the UA nanocrystals showed good aqueous dispensability and a higher dissolution rate, and they could be completely dissolved in 0.5% SDS solution within 120 min. Moreover, the suspension of UA nanocrystals was physically stable after storage at 4 C for 7 weeks. By inducing G2/M phase cell cycle arrest, the UA nanocrystals significantly induced stronger cell growth inhibition activity against MCF-7 cells compared with free drug in vitro, although the uptake of free UA was approximately twice higher than that of the UA nanocrystals. The UA nanocrystals may be used as a potential delivery formulation for intravenous injection with enhanced dissolution velocity and anticancer activity. © 2013 American Association of Pharmaceutical Scientists.

KeywordAnticancer Dissolution Mcf-7 Nanocrystals Ursolic Acid
DOI10.1208/s12249-013-0028-0
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000334053200002
The Source to ArticleScopus
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Cited Times [WOS]:23   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, 2/F, Room 204A, Block 3, Av. Padre Tomás Pereira, S.J. Taipa, Macao,, SAR China
2.School of Chemistry and Pharmaceutical Engineering, Shandong Polytechnic University, Jinan, 250353 China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Song Ju.,Wang Y.,Song Y.,et al. Development and characterisation of ursolic acid nanocrystals without stabiliser having improved dissolution rate and in vitro anticancer activity[J]. AAPS PharmSciTech,2014,15(1):11.
APA Song Ju..,Wang Y..,Song Y..,Chan H..,Bi C..,...&Zheng Y..(2014).Development and characterisation of ursolic acid nanocrystals without stabiliser having improved dissolution rate and in vitro anticancer activity.AAPS PharmSciTech,15(1),11.
MLA Song Ju.,et al."Development and characterisation of ursolic acid nanocrystals without stabiliser having improved dissolution rate and in vitro anticancer activity".AAPS PharmSciTech 15.1(2014):11.
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