Khairy L, Isom G E, Kildsig D O
Res Commun Chem Pathol Pharmacol. 1983 Oct;42(1):153-6.
An N-acetyl-l-cysteine (NAC)-liposome drug delivery system was assessed for its ability to reverse acetaminophen toxicity. Positively charged NAC-liposomes, as compared to neutral and negatively charged preparations, were highly effective in reversing acetaminophen-induced lethality in mice. The positively charged liposome preparation, when administered at a dose equivalent to 50 mg/kg NAC, increased the LD50 of acetaminophen from 840 to 1507 mg/kg; free NAC (50 mg/kg) did not significantly alter the LD50 (829 mg/kg). At this dose, only the liposome entrapped NAC protects against acetaminophen-induced lethality suggesting that positively charged liposomes enhance the delivery of NAC to hepatic parenchymal cells, the site of acetaminophen-induced necrosis.
评估了N-乙酰-L-半胱氨酸（NAC）脂质体药物递送系统逆转对乙酰氨基酚毒性的能力。与中性和带负电荷的制剂相比，带正电荷的NAC脂质体在逆转对乙酰氨基酚诱导的小鼠致死性方面非常有效。当以相当于50 mg/kg NAC的剂量给药时，带正电荷的脂质体制剂将对乙酰氨基酚的半数致死量（LD50）从840 mg/kg提高到1507 mg/kg；游离NAC（50 mg/kg）并未显著改变LD50（829 mg/kg）。在此剂量下，只有脂质体包裹的NAC能防止对乙酰氨基酚诱导的致死性，这表明带正电荷的脂质体增强了NAC向肝实质细胞的递送，而肝实质细胞是对乙酰氨基酚诱导坏死的部位。
