Puerarin Derivatives The 4ac Nanoparticles And The In Vitro And In Vivo Evaluation

Pueraria lobata(Willd.) Ohwi., a traditional Chinese medicinal herb, was first described in the Chinese material medica, Shen Nong Ben Cao Jing and has been used for the treatment of hypertension, senile ischemic cerebrovasular disease and angina pectoris for a long time. Four magor isoflavones were identified in the Pueraria lobata extract and quantified-namely, puerarin, daidzin, genistin and daidzein. pharmacology and clinical applications have shown that puerarin is the most major and abundant active ingredients. In years, Researches indicated that apart from treating of cerebrovascular and cardiovascular diseases, puerarin also has neuroprotective effects and can be used for protection of learning and memory and suppression of alcohol drinking. However, in spite of the great therapeutic interest of this drug, due to its low oral bioavailability, 5—6% only in rats and rabbit, puerarin is administered intravenously as its primary form of clinical application. Howerver, propylene glycol of high concentration is added in formulation of puerarin injection, resulting in much a few side effects. Oral form is convenient and thus preferred by the patients ,which can greatly improve the quality of life of the patients.Various techniques and methods for enhancement of oral bioavailability are proposed to improve patient compliance. For this reason, 4ac was selected from the series of derivatives of puerarin developed in our laboratory. Its oral bioavailability is markedly increased comparing with puerarin, but which still can not match clinical require. In order to overcome the difficulties as described above, improve the therapeutic efficacy and decrease its side effects, Alternative dosage forms have been suggested including incorporation of the drug into particulate carriers. Polymeric nanoparticles (NP),defined as solid particles with assize in the range of 10-1000nm, allow encapsulation of the drugs inside polymeric matrix. Nanoparticle have been proven to be an efficient approach to achieve better pharmacokinetic profiles and to increase the oral bioavailability. Most evidence suggests that the favoured site for uptake is the PP lympho-epitelial M cell. It was recently reported that particles in the...