Pinocytic uptake and intracellular degradation of N-(2-hydroxypropyl)methacrylamide copolymers. A potential drug delivery system.
Synthetic 125I-labelled N-(2-hydroxypropyl)methacrylamide copolymers containing four different, potentially degradable peptidyl side chains were incubated with rat visceral yolk sacs cultured in vitro. All copolymers were captured by fluid-phase pinocytosis and three of the side chains were susceptible to lysosomal hydrolysis, resulting in release of [125I]iodotyrosine back into the culture medium. Uptake and degradation was completely inhibited by 2,4-dinitrophenol. The thiol-proteinase inhibitor leupeptin did not affect the rate of pinocytosis, but caused different degrees of inhibition of hydrolysis depending on side chain composition.
D019297:2,4-Dinitrophenol; D000178:Acrylamides / Q000378:metabolism*; D000818:Animals; D046508:Culture Techniques; D004140:Dinitrophenols / Q000494:pharmacology; D004304:Dosage Forms; D005260:Female; D006868:Hydrolysis; D007976:Leupeptins / Q000494:pharmacology; D008247:Lysosomes / Q000378:metabolism*; D009842:Oligopeptides / Q000378:metabolism*; D010873:Pinocytosis; D051381:Rats; D013329:Structure-Activity Relationship; D015017:Yolk Sac / Q000378:metabolism*
D000178:Acrylamides; D004140:Dinitrophenols; D004304:Dosage Forms; D007976:Leupeptins; D009842:Oligopeptides; D019297:2,4-Dinitrophenol; C032976:N-(2-hydroxypropyl)methacrylamide