Abstract

Tetrandrine is an alkaloid extracted from the roots of Stephania tetrandra S. Moore. It is employed in China to treat silicosis; its site of activities being within the lungs. Chronic treatment with tetrandrine is limited by unacceptable toxicity to the liver. Entrapment of tetrandrine within albumin microspheres with a view to promoting deposition within the lung may result in an improved therapeutic modality. Accordingly, the preparation of tetrandrine-entrapped albumin microspheres (MS) was optimised using central composite design. The influence of albumin concentration, drug concentration and pH of albumin solution on MS particle size and drug entrapment was investigated. An optimum preparation was established, which produced albumin MS with mean diameter 11.65 ± 0.31 μm ( n = 3) and 113 ± 12.5 μg entrapped tetrandrine per mg MS ( n = 3). Such MS could have the potential for targeting tetrandrine to the lung.

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