Liposome Dependent Delivery of N-(Phosphonacetyl)-L-Aspartic Acid to Cellsin Vitro

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Abstract
N-(phosphonacetyl)-L-aspartic acid (PALA) exhibits a considerable increase in its in vitro growth inhibitory potency when it is incorporated into liposomes. Encapsulation in negatively charged liposomes increases the growth inhibitory potency of PALA by up to 360 times. For CV1-P and L929 cells, encapsulation in liposomes prepared from neutral phospholipids does not increase the potency of PALA. the potency of encapsulated PALA is not dependent on the size of liposomes, being equally effective in all liposomes between 0.1 and 1 µm in diameter. the potency of PALA is greatest when it is incorporated into liposomes prepared from high phase transition temperature lipids. Exposure of cells to 7.5 mM ammonium chloride substantially inhibits the effects of both free and encapsulated PALA. the potency of free PALA is more sensitive to changes in exposure length than is the potency of encapsulated PALA. Consequently the difference in potency between free and encapsulated PALA is greatest when exposure length is short (1-2 hr). the considerable potency of encapsulated PALA makes this drug a possible treatment for tumors and ocular cicatricial diseases.

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