Study on Preparation of CyA-Eudragit S100-Nanoparticles and Its Characteristics in Vivo and in Vitro

YNG Zhi-qing;PN Ping;XU Jie;ZHNG Xue-nong;CHEN Y-gen;ZHNG Jin-kng;WEI Mio

Chinese Pharmaceutical Journal ›› 2008, Vol. 43 ›› Issue (23) : 1798-1803.

Chinese Pharmaceutical Journal ›› 2008, Vol. 43 ›› Issue (23) : 1798-1803.
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Study on Preparation of CyA-Eudragit S100-Nanoparticles and Its Characteristics in Vivo and in Vitro

  • YANG Zhi-qiang，PAN Ping，XU Jie，ZHANG Xue-nong*，CHEN Ya-gen，ZHANG Jian-kang，WEI Miao
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Abstract

OBJECTIVE To study the preparation and pharmaceutical characteristics of cyclosporine A-Eudragit S100-nanoparticles(CyA-NP) in vitro and in vivo by using Neoral as reference preparation.METHODS CyA-NP were prepared with quasi-emulsion solvent diffusion technique and freeze-drying technique.Dynamic dialyse method was used to study the release dynamics of the three kinds of nanoparticles in vitro.The bioavailability of CyA-NP and freeze-drying nanoparticles was determined by HPLC and its pharmacokinetics parameters were calculated by 3P97 program.RESULTS The particle sizes of CyA-NP and Fd-CyA-NP were(44.8±3.2) and(55.7±3.6) nm.The encapsulation efficiency of CyA was 90%.The drug-loaded nanoparicles were spherical observed by the transmission electric microscope.The release study in vitro showed evidently pH-sensitive when the medium pH were over 6.0.The relative bioavailability of CyA-NP and Fd-CyA-NP were 162.1% and 130.1% compared with Neoral.CONCLUSION pH-sensitive Eudragit S100 was a potential carrier material in developing a high performance CyA nanometer system with low toxicity.

Key words

cyclosporine A / pH-sensitive nanoparticle / freeze-drying powder / relative bioavailability

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YNG Zhi-qing;PN Ping;XU Jie;ZHNG Xue-nong;CHEN Y-gen;ZHNG Jin-kng;WEI Mio. Study on Preparation of CyA-Eudragit S100-Nanoparticles and Its Characteristics in Vivo and in Vitro[J]. Chinese Pharmaceutical Journal, 2008, 43(23): 1798-1803

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