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TEMPERATURE-SENSITIVE RELEASES FROM LIPOSOMES CONTAINING HYDROPHOBICALLY MODIFIED POLY (N-ISOPROPYLACRYLAMIDE)
Korean Journal of Chemical Engineering, January 1999, 16(1), 28-33(6), 10.1007/BF02699001
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Abstract
Novel temperature-sensitive liposomes containing hydrophobically modified poly(N-isopropylacylamide) (HPNIPAM) and their release behaviors were investigated using calcein as a fluorescence probe. Above the lower critical solution temperature (LCST) of the polymer (e.g., 40℃), the degree of calcein release in 280 sec from reverse-phase evaporation vesicles (REVs) of egg phosphatidylcholine (egg PC) was 43% while egg PC MLVs was 16%. Such a large difference of release may be attributed to the lamellarity of liposomes. The incorporation of dioleoyl-phosphatidylethanolamine (DOPE) into the PC bilayer enhanced the release by 10-13% at 40 ℃, probably due to the increased instability of mixture bilayers. Meanwhile, a temperature-sensitive device of DOPE liposomes was prepared by using HPNIPAM as a stabilizer. The optimal ratio of HPNIPAM to lipid to stabilize the bilayer was 0.1. Above the LCST (e.g., 40℃), the release percentage was about 80 % of the entrapped calcein. DOPE liposomes were the most temperature-sensitive among liposomes tested. This is probably because DOPE liposomes disintegrate into a non-liposomal phase, such as hexagonal (HII), by a thermal contraction of HPNIPAM.
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References
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Kono K, Hayashi H, Takagishi T, J. Control. Release, 30, 69 (1994)
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Park JH, Lee EO, Kim JD, J. Korean Pharm. Sci., 22, 115 (1992)
Perez-Solar R, Priebe W, Cancer Res., 50, 4260 (1990)
Ringsdorf H, Venzmer J, Winnik FM, Macromolecules, 24, 1678 (1991)
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Yatvin MB, Weinstein JN, Dennis WH, Blumenthal R, Science, 202, 1290 (1978)
