Enhancement of epimedium fried with suet oil based on in vivo formation of self-assembled flavonoid compound nanomicelles.

Li Cui,Xiao-Bin Tan,Xiao-Bin Jia,Xin Jin,Ying-Jie Wei,Zhen-Hai Zhang,E Sun

doi:10.3390/molecules171112984

Abstract

The purpose of this work was to research the enhancement of Epimedium fried with suet oil based on the in vivo formation self-assembled flavonoid nanomicelles. Taking icariin as the representative, under the action of suet oil, self-assembled nanomicelles were prepared under simulated gastrointestinal tract conditions and were characterized by dynamic light scattering and transmission electron microscopy (TEM). The experiments with icariin self-assembled nanomicelles without suet oil were done according to the above. The influence of suet oil on the transportation of icariin across Caco-2 cell monolayers and the absorption in rat intestine of self-assembled nanomicelles were evaluated. The particle size of icariin self-assembled nanomicelles with suet oil was smaller than without suet oil. The nanomicelles seemed to be monodisperse spherical particle with smooth surfaces. The icariin entrapment efficiency of self-assembled nanomicelles with suet oil was increased from 43.1% to 89.7%. In Caco-2 cell monolayers, the absorptive permeability, secretory permeability and efflux ratio of icariin self-assembled nanomicelles with suet oil was 1.26 × 10−6 cm/s, 5.91 × 10−6 cm/s and 4.69, respectively, while that of icariin self-assembled nanomicelles without suet oil was 0.62 × 10−6 cm/s, 3.00 × 10−6 cm/s, and 4.84, respectively. In rat intestinal perfusion experiments, the permeability coefficient of icariin self-assembled nanomicelles with suet oil in duodenum was higher than the value of icariin self-assembled nanomicelles without suet oil (p < 0.05). With the action of suet oil, icariin self-assembled nanomicelles were more stable and the entrapment efficiency was higher than that without suet oil, which could increase the solubility of icariin and improve its intestinal absorption. Therefore, suet oil plays a role in its enhancement.

Highlights

Herba Epimedii, the dried aerial parts of Epimedium brevicornu Maxim, Epimedium sagittatumMaxim, Epimedium pubescens Maxim and Epimedium koreanum Nakai, have been traditionally used as tonic, aphrodisiac and antirheumatic medical herbs for cardiovascular, bone loss and impotence diseases in East Asian countries for many years
Our experiments found that suet oil can work with DOC to prepare mixed micelles, as the carrier of icariin under simulated gastrointestinal tract conditions
We could conclude that the suet oil used in the fabrication process is an important factor to influence the particle size, size distribution and the drug encapsulation efficiency in the self-assembled nanomicelles

Summary

Introduction

Herba Epimedii, the dried aerial parts of Epimedium brevicornu Maxim, Epimedium sagittatumMaxim, Epimedium pubescens Maxim and Epimedium koreanum Nakai, have been traditionally used as tonic, aphrodisiac and antirheumatic medical herbs for cardiovascular, bone loss and impotence diseases in East Asian countries for many years. Herba Epimedii, the dried aerial parts of Epimedium brevicornu Maxim, Epimedium sagittatum. The major active constituents of Epimedii are flavonoids, of which more than 141 flavonoid compounds, including flavonols, flavones, chalcones, flavanones, and flavonol glycosides, have been isolated [1,2]. Herba Epimedii, has numerous pharmacological and biological activities, including prevention of osteoporosis, erectile impotence, and anti-cancer and anti-depression properties [3−5]. Epimedium fried with suet oil was usually used, which could enhance the kidney invigorating and “Yang” strengthening roles of Epimedium [6]. The role the “heat” factor during processing has been clarified before: heating causes Epimedium to produce more absorbable bioactive flavonoids [7]. The mechanism of action of how suet oil increases the effects has not been elucidated

Objectives

Methods

Results

Conclusion