TEMPERATURE-SENSITIVE RELEASES FROM LIPOSOMES CONTAINING HYDROPHOBICALLY MODIFIED POLY (N-ISOPROPYLACRYLAMIDE)

Kim JC; Kim MS; Kim JD

Korean Journal of Chemical Engineering, Vol.16, No.1, 28-33, January, 1999

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 (H_II), by a thermal contraction of HPNIPAM.

Keywords:Liposomes;Poly(N-isopropylacrylamide);Temperature-Sensitivity;Dioleoylphosphatidylethanolamine;Reverse-Phase Evaporation Vesicles

[References]

Bae YH, Okano T, Kim SW, Pharm. Res., 8, 624 (1991)
Bangham AD, "Liposomes: from Physical Structure to Therapeutic Applications," ed., Knight, C.G., Elsevier/North-Holland, 1 (1981)
Chen H, Torchilin V, Langer R, Pharm. Res., 13, 1378 (1996)
Choe T, Ku J, Jung S, Yang J, Kim J, Korean J. Chem. Eng., 13(4), 393 (1996)
Choi MJ, Han HS, Kim H, J. Biochem., 112, 694 (1992)
Chun SW, Kim JD, J. Control. Release, 38, 39 (1996)
Crommelin DJA, Grit M, Talsma H, Zuidam NJ, Drug Development Ind. Pharmacy, 20, 547 (1994)
Cudd A, Noonan CA, Tossi PF, Melnick JL, Nicolau L, J. AIDS, 3, 109 (1990)
Gao X, Huang L, Biochemistry, 35, 1027 (1996)
Gruner SM, Cullis PR, Hope MJ, Tilcock CPS, Annu. Rev. Biophys. Chem., 14, 211 (1985)
Heskins M, Guillet JE, J. Macromol. Sci.-Chem., A2, 1441 (1968)
Ho RJY, Rouse BT, Huang L, Biochemistry, 25, 5500 (1986)
Huang A, Tsao YS, Kennel SJ, Huang L, Biochim. Biophys. Acta, 716, 140 (1983)
Juliano, Stamp D, Nature, 261, 235 (1972)
Kim JC, Bae SK, Kim JD, J. Biochemistry, 121, 15 (1997)
Kim JC, Lee EO, Kim JY, Bae SK, Choi TB, Kim JD, Pharm. Develop. Technol., 2, 275 (1997)
Kim JG, Kim JD, HWAHAK KONGHAK, 26(2), 171 (1988)
Kono K, Hayashi H, Takagishi T, J. Control. Release, 30, 69 (1994)
Lee EO, Kim JD, J. Biochem., 117, 54 (1995)
Lee EO, Kim JG, Kim JD, J. Biochem., 112, 671 (1992)
Maeda M, Kumano A, Tirrell DA, J. Am. Chem. Soc., 110, 7455 (1988)
New RRC, Black CDV, Parker RJ, Puri A, Scherphof GL, "Liposomes: a Practical Approach," New, R.R.C. ed., Oxford University Press, New York, 221 (1990)
New RRC, "Liposomes: a Practical Approach," New, R.R.C. ed., 1-32 Oxford University Press, New York (1990)
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)
Szoka F, Papahadjopoulos D, Proc. Natl. Acad. Sci., 75, 4194 (1978)
Tarashi TF, van der Steen TM, DeKruijff B, Tellier C, Verkleij AJ, Biochemistry, 21, 5756 (1982)
Yatvin MB, Weinstein JN, Dennis WH, Blumenthal R, Science, 202, 1290 (1978)

[Referenced By]

[1] Bae YH, Okano T, Kim SW, Pharm. Res., 8, 624 (1991)

[2] Bangham AD, "Liposomes: from Physical Structure to Therapeutic Applications," ed., Knight, C.G., Elsevier/North-Holland, 1 (1981)

[3] Chen H, Torchilin V, Langer R, Pharm. Res., 13, 1378 (1996)

[4] Choe T, Ku J, Jung S, Yang J, Kim J, Korean J. Chem. Eng., 13(4), 393 (1996)

[5] Choi MJ, Han HS, Kim H, J. Biochem., 112, 694 (1992)

[6] Chun SW, Kim JD, J. Control. Release, 38, 39 (1996)

[7] Crommelin DJA, Grit M, Talsma H, Zuidam NJ, Drug Development Ind. Pharmacy, 20, 547 (1994)

[8] Cudd A, Noonan CA, Tossi PF, Melnick JL, Nicolau L, J. AIDS, 3, 109 (1990)

[9] Gao X, Huang L, Biochemistry, 35, 1027 (1996)

[10] Gruner SM, Cullis PR, Hope MJ, Tilcock CPS, Annu. Rev. Biophys. Chem., 14, 211 (1985)

[11] Heskins M, Guillet JE, J. Macromol. Sci.-Chem., A2, 1441 (1968)

[12] Ho RJY, Rouse BT, Huang L, Biochemistry, 25, 5500 (1986)

[13] Huang A, Tsao YS, Kennel SJ, Huang L, Biochim. Biophys. Acta, 716, 140 (1983)

[14] Juliano, Stamp D, Nature, 261, 235 (1972)

[15] Kim JC, Bae SK, Kim JD, J. Biochemistry, 121, 15 (1997)

[16] Kim JC, Lee EO, Kim JY, Bae SK, Choi TB, Kim JD, Pharm. Develop. Technol., 2, 275 (1997)

[17] Kim JG, Kim JD, HWAHAK KONGHAK, 26(2), 171 (1988)

[18] Kono K, Hayashi H, Takagishi T, J. Control. Release, 30, 69 (1994)

[19] Lee EO, Kim JD, J. Biochem., 117, 54 (1995)

[20] Lee EO, Kim JG, Kim JD, J. Biochem., 112, 671 (1992)

[21] Maeda M, Kumano A, Tirrell DA, J. Am. Chem. Soc., 110, 7455 (1988)

[22] New RRC, Black CDV, Parker RJ, Puri A, Scherphof GL, "Liposomes: a Practical Approach," New, R.R.C. ed., Oxford University Press, New York, 221 (1990)

[23] New RRC, "Liposomes: a Practical Approach," New, R.R.C. ed., 1-32 Oxford University Press, New York (1990)

[24] Park JH, Lee EO, Kim JD, J. Korean Pharm. Sci., 22, 115 (1992)

[25] Perez-Solar R, Priebe W, Cancer Res., 50, 4260 (1990)

[26] Ringsdorf H, Venzmer J, Winnik FM, Macromolecules, 24, 1678 (1991)

[27] Szoka F, Papahadjopoulos D, Proc. Natl. Acad. Sci., 75, 4194 (1978)

[28] Tarashi TF, van der Steen TM, DeKruijff B, Tellier C, Verkleij AJ, Biochemistry, 21, 5756 (1982)

[29] Yatvin MB, Weinstein JN, Dennis WH, Blumenthal R, Science, 202, 1290 (1978)