Abstract
Tetrandrine is a bisbenzylisoquinoline alkaloid extracted from the roots of Stephania tetrandra S. Moore. It has been used in China as a treatment of silicosis which is an occupational disease caused by the inhalation of silica particles. Tetrandrine is reported to be metabolised slowly, accumulate in the liver and induce hepatic damage. Hence, the aim of the present study is to deliver and retain tetrandrine in the lung so as to promote any antisilicotic effects but to minimise its side effects to other organs. Albumin microspheres (MS) may provide a suitable carrier for airway delivery because of their biocompatibility and biodegradability. The albumin MS were prepared with micronised tetrandrine by high speed homogenisation and heat denaturation. Factorial design was used to optimise the preparative process. The particle size was measured by laser light scattering and drug entrapment determined by HPLC. Albumin MS with mean diameter 4.41 ± 0.45 μm ( n = 6) and drug entrapment 120.2 ± 26.2 μg drug per mg MS ( n = 6) were prepared. The tetrandrine recovered from the lower stage of a twin-stage impinger operated under Pharmacopoeial conditions was 13.83 ± 2.58% ( n = 6). The results showed that albumin MS may have the potential to deliver tetrandrine to the lung via airways.
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