Study of pharmacokinetics and tissue distribution of liposomal brucine for dermal administration

研究脂质体番木鳖碱经皮给药后的药代动力学和组织分布

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Abstract

OBJECTIVE: To evaluate the pharmacokinetics and tissue distribution of liposomal brucine (LB) for dermal application. METHODS: Pharmacokinetics and tissue distribution were studied by in vivo animal testing. High performance liquid chromatography (HPLC) was used to detect the concentration of brucine in rats' skin, plasma and various tissues. RESULTS: After dermal administration, LB was absorbed rapidly in the skin and could be detected after 0.5 hours. After 36 hours, levels were too low to be detected. In plasma, levels were also too low to be detected after 36 hours. The concentration of LB reached 50% of the maximum in all tissues except the brain, peaking after 1.5 hours but still detectable after 12 hours. CONCLUSION: The concentration of LB was high in skin at the application site. LB was quickly absorbed into tissues through the blood circulation and widely distributed throughout the whole body. There was no obvious toxicity and LB did not readily accumulate in tissues and organs. It showed local potency but low overall systemic toxicity.

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