Liposomal aerosols for delivery of chemotherapeutic retinoids to the lungs

Abstract

To optimize the delivery of all-trans retinoic acid to lung tissue, the potential of vehiculating this drug in liposomes and delivering it via aerosol was determined. Liposomes provide a means to prevent local irritation of lung tissue, reduce pulmonary toxicity, prolong therapeutic levels, and generate high drug concentrations at the tumor sites. Therefore, the delivery of ATRA to the lung tissue in mice was accomplished by nebulization of L-ATRA. The liposomes in the aerosol were uniform, stable, and retained the drug well. The drug was effectively delivered at high concentrations to the lungs of mice and was retained at least up to 96 h after a single exposure to L-ATRA aerosols. The aerosol-delivered ATRA was biologically active as demonstrated by its ability to induce the expression of tissue-type transglutaminase. Aerosol delivery of L-ATRA offers an effective way to deliver high levels of ATRA to the lung without apparent pulmonary toxic effects.

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