Study on liver targeting and hepatocytes permeable valaciclovir polybutylcyanoacrylate nanoparticles

doi:10.3748/wjg.v5.i4.330

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Aug 15, 1999 (publication date) through Apr 19, 2024

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World Journal of Gastroenterology

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1007-9327

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

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World J Gastroenterol. Aug 15, 1999; 5(4): 330-333
Published online Aug 15, 1999. doi: 10.3748/wjg.v5.i4.330

Study on liver targeting and hepatocytes permeable valaciclovir polybutylcyanoacrylate nanoparticles

Zhi-Rong Zhang, Qin He

Zhi-Rong Zhang, Qin He, School of Pharmacy, West China University of Medical Sciences, Chengdu 610041, Sichuan Province, China

Author contributions: All authors contributed equally to the work.

Supported by the National Natural Science Foundation of China, NO. 39470831

Correspondence to: Dr. Zhi-Rong Zhang, School of Pharmacy, West China University of Medical Sciences, Chengdu 610041, China

Telephone: +86-28-5501566, Fax: +86-28-5583252

Received: March 10, 1999
Revised: July 3, 1999
Accepted: July 19, 1999
Published online: August 15, 1999

Abstract

AIM: To prepare valaciclovir polybutylcyan-oacrylate nanopa rticles (VACV-PBCA-NP) with liver targeting and hepatocyte permeable characteristics.

METHODS: Emulsion polymerization method was employed to prepare VACV-PBCA-NP. The formula and preparation conditions were optimized by using the uniform design. The organ distribution of the intravenously injected VACV-P BCA-NP and VACV in animal was determined using HPLC. The hepatocytes permeability of VACV-PBCA-NP was demonstrated by cell uptake experiment in vitro.

RESULTS: The drug loading and the drug embedding ratio of VACV-PBCA-NP were 11.20% and 84.85% respectively, with an average diameter of 104.77 nm ± 11.78 nm. The releasing characteristics in vitro fitted the two-phase kinetics. 74.49% of the drug was found to localize in the liver 15 min after the administration of VACV-PBCA-NP in the mice. Compared with VACV, VACV-PBCA-NP showed distinct characteristic of sustained-release in vivo and the drug entering hepatocytes were also greatly increased.

CONCLUSION: VACV-PBCA-NP has the characteristic of liver targeting and can increase the permeability of VACV to hepatocytes.

Keywords: valaciclovir, polybutylcyan-oacrylate nanoparticles, liver targeting, hepatocytes permeability