Formulation and Characterization of Novel Dry Suspension and Dry Emulsion of 20(S)-Protopanaxadiol

AAPS PharmSciTech
Liying ZhangTong Zhang

Abstract

To improve the absorption of poorly water-soluble 20(S)-protopanaxadiol (20(S)-PPD), novel 20(S)-PPD-loaded redispersible dry suspension and dry emulsion were developed in this study. 20(S)-PPD dry suspension (PPD-DS) was prepared by enabling drug fully dispersed with suspending agent Avicel CL611 and solubilizer Poloxamer 188. 20(S)-PPD dry emulsion (PPD-DE) was prepared by employing oleic acid as oil phase, Cremophor RH-40 as surfactant, and n-butyl alcohol as co-surfactant. Both PPD-DS and PPD-DE were evaluated for their physicochemical characterization after being dispersed in distilled water. The in vivo pharmacokinetics was evaluated by UPLC-MS/MS. The droplet size of PPD-DS and PPD-DE was in the scope of 1446-1653 nm and 652.8-784.5 nm. The sedimentation volume ratios of PPD-DS and PPD-DE were both at value of 1. The zeta potential of PPD-DS and PPD-DE were from - 53.7 to - 70.4 mV and - 27.5 to - 34.5 mV, respectively, which indicated stable systems. PPD-DS and PPD-DE both achieved dramatically enhanced aqueous solubility and higher perfusion of 20(S)-PPD in rats' intestine. Although statistically, no oral bioavailability enhancements of 20(S)-PPD were achieved in PPD-DE and PPD-DS, there were some improvements in the p...Continue Reading

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Methods Mentioned

BETA
light scattering

Software Mentioned

DE
Origin
DAS
SPSS
PPD

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