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Formulation optimization and bioavailability after oral and nasal administration in rabbits of puerarin-loaded microemulsion.

Journal of pharmaceutical sciences (2010-09-24)
Aihua Yu, Haigang Wang, Jiali Wang, Fengliang Cao, Yan Gao, Jing Cui, Guangxi Zhai
ABSTRACT

The main objective of the study was to investigate the efficacy of microemulsion (ME) to facilitate bioavailability of puerarin (PUE) after oral and nasal administration. The pseudo-ternary phase diagrams were constructed to screen the ME components and optimize the ME formulation. The optimized formulation for bioavailability assessment consisted of 20% Tween 80, 20% glycerin, and 1.6% ethyl oleate. The solubility (27.8 mg/mL) of PUE in ME was significantly improved compared to that (4.58 mg/mL) of crude PUE in water. The ME droplets were spherical with a mean particle diameter of 23.4 nm. After nasal (5 mg/kg) and oral (20 mg/kg) administration of a single dose of PUE as ME to fasted rabbits, the absolute bioavailability was 34.58% and 13.54%, respectively. It showed a shorter T(max) (0.75 h) for nasal administration than that (1.0 h) for oral administration of PUE-loaded ME. The C(max) of PUE-loaded ME was 0.55 μg/mL after nasal administration and 0.64 μg/mL after oral administration, respectively. The results showed that nasal administration might be a promising route to enhance the absorption of PUE in the form of ME.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Ethyl oleate, 98%
Sigma-Aldrich
Ethyl oleate, tested according to Ph. Eur.
Sigma-Aldrich
Ethyl oleate, natural, ≥85%
Sigma-Aldrich
Ethyl oleate, technical grade, 70%

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