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Title: Formulation, biological and pharmacokinetic studies of sucrose ester-stabilized nanosuspensions of oleanolic acid
Authors: Li, W.
Das, S.
Ng, K.-Y. 
Heng, P.W.S. 
Keywords: bioavailability
dissolution rate
hydrophobic drug
oleanolic acid
saturation solubility
sucrose ester
surfactant stabilized nanosuspensions
Issue Date: Aug-2011
Citation: Li, W., Das, S., Ng, K.-Y., Heng, P.W.S. (2011-08). Formulation, biological and pharmacokinetic studies of sucrose ester-stabilized nanosuspensions of oleanolic acid. Pharmaceutical Research 28 (8) : 2020-2033. ScholarBank@NUS Repository.
Abstract: Purpose: The aim of this study was to develop sucrose ester (SE)-stabilized oleanolic acid (OA) nanosuspensions (NS) for enhanced delivery. Methods: SEOA NS were prepared via O/W emulsion and organic solvent evaporation methods. The particles' size and polydispersity index were measured by nanosizer. Their percent encapsulation efficiency, saturation solubility and in vitro dissolution rate were obtained via HPLC. The in vitro bioefficacy was analyzed by MTT measurements in A549 human non-small-cell lung cancer cell line. The cellular uptake of OA and in vivo pharmacokinetics profile were determined using LC-ESI-MS/MS. Results: Spherical SEOA NS particles (~100 nm in diameter) were produced and found to be physicochemically stable over a month at 4°C. In particular, SEOA 4121 NS (SEL: SEP at 4:1 w/w; SE: OA at 2:1 w/w) produced the greatest increase in saturation solubility (1.89 mg/mL vs. 3.43 μg/mL), dissolution rate, cytotoxicity and bioavailability. Preliminary studies indicated that cellular uptake of SEOA NS by A549 cells was temperature-, concentration- and time-dependent. Conclusion: Preparing OA as SE-stabilized NS particles provides a novel method to enhance saturation solubility, in vitro dissolution rate, bioefficacy and in vivo bioavailability of free OA and/or other potentially useful hydrophobic drugs. © 2011 Springer Science+Business Media, LLC.
Source Title: Pharmaceutical Research
ISSN: 07248741
DOI: 10.1007/s11095-011-0428-3
Appears in Collections:Staff Publications

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