Bioavailability And Anti-oxidative Stress Activity Of Orally Administered Ouerarin Suspension In Silkworm Pupa Oil

Puerarin is a component extracted from a Chinese medical herb Pueraria lobata and it hasextensive biological activity and pharmacologic activities. It is necessary to explore the methodwhich can improve the oral bioavailability of puerarin because of its low oral bioavailability. Inthis study, we investigated the oral bioavailability and the anti-oxidative stress activity of thesuspension of puerarin mixed with silkworm pupa oil, seeking to provide new method for theimprovement of the oral dosage form of puerarin.In this study, a method to determine the concentration of puerarin in serum was establishedusing high-performance liquid chromatography (HPLC) technique and the methodologyvalidation was conducted. Then the components of silkworm pupa oil and its effect on theabsorption of orally administered puerarin into blood were a nalyzed. Our results showed thatoleic acid, α-Linolenic acid and palmitic acid comprised the majority of the fatty acids indomestic silkworm pupa oil, in which α-Linolenic acid accounts for31.42%. Silkworm pupa oilcould enhance the absorption of orally administered puerarin into blood comparing with othercontrol reagents. Next, the oral bioavailability of puerarin suspension in silkworm pupa oil wasanalyzed. The puerarin suspension in0.5%carboxymethyl cellulose (CMC) was used as thereference reagent and puerarin suspension in silkworm pupa oil was used as the subject reagent.The dosages of them were200mg (puerarin)/kg. Blood samples of mice were collected fromorbital at different time points and the serum concentration of puerarin was analyzed by HPLC.Compared with the reference group, the relative bioavailability of puerarin suspension insilkworm pupa oil was391%, indicating the bioavailability-improving effect of silkworm pupaoil on orally administered puerarin. At last, the anti-hypoxia effect of puerarin suspension insilkworm pupa oil was explored. Our results revealed that puerarin suspension in silkworm pupaoil could increase the anti-hypoxia capability of mice and the survival ability of NaNO2-poisonedmice. Puerarin suspension in silkworm pupa oil has better effect on improving the anti-hypoxiacapability of mice when compared with the reference. Moreover, the anti-oxidative stress activityof puerarin suspension in silkworm pupa oil was analyzed. Using the constructedalcohol-induced oxidative stress model, we found that puerarin suspension in silkworm pupa oilcould decrease the liver index the concentration of MDA, protein carbonyl, cytokines il-6andTNF-α, and it also could increase the content of anti-oxidants and the activity of anti-oxidativeenzymes in mice treated with puerarin suspension in silkworm pupa oil when compared withthose treated with puerarin suspension in0.5%CMC. In summary, puerar in suspension insilkworm pupa oil could improve activities. It is necessary to explore the method the oral bioavailability, decrease the level of oxidative stress and better therapeutic effect, providing thebasis for clinical trials.