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Hemolytic and antifungal activity of liposome-entrapped amphotericin B prepared by the precipitation method.
Pharm Dev Technol. 1997 Aug; 2(3):275-84.PD

Abstract

A new method of preparing liposomes containing amphotericin B (AmB) was developed with the purpose of reducing the toxicity of AmB without causing a loss in its antifungal activity. The procedure involved the precipitation of AmB and egg phosphatidylcholine (PC) in phosphate buffered saline (PBS, pH 7.4) or tris buffered saline (TBS, pH 7.4) by evaporating methanol and chloroform, which had been previously mixed in the buffer solution, at 4 degrees C and 600 mm Hg. The in vitro toxicity of the precipitated liposomes containing 3, 6, 9, 12, and 15 wt% AmB was compared with that of the film-swollen liposomes containing the equivalent contents of the drug. The hemolytic ability of the precipitated liposomes at 37 degrees C was 50.3% at maximum of the film-swollen liposomes at a dose of 30 micrograms AmB/ml, as measured after 17-hr incubation. The significant reduction in the hemolysis effect may in fact be attributed to the reduced rate of drug release from the precipitated liposomes. The precipitated liposomes were multilayered and aggregates of AmB were embedded in the bilayers. These aggregates of AmB would be responsible for an intensive positive peak around 330 nm and reduced toxicity. Despite the decrease in toxicity, the activity of the precipitated liposomes against Candida albicans remained almost equipotent to that of the film-swollen liposomes. Therefore, liposomes prepared by the precipitation method are less toxic but equally as active.

Authors+Show Affiliations

Department of Chemical Engineering, Korea Advanced Institute of Science and Technology, Yusong-Gu, Taejon, Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

9552455

Citation

Kim, J C., et al. "Hemolytic and Antifungal Activity of Liposome-entrapped Amphotericin B Prepared By the Precipitation Method." Pharmaceutical Development and Technology, vol. 2, no. 3, 1997, pp. 275-84.
Kim JC, Lee EO, Kim JY, et al. Hemolytic and antifungal activity of liposome-entrapped amphotericin B prepared by the precipitation method. Pharm Dev Technol. 1997;2(3):275-84.
Kim, J. C., Lee, E. O., Kim, J. Y., Bae, S. K., Choi, T. B., & Kim, J. D. (1997). Hemolytic and antifungal activity of liposome-entrapped amphotericin B prepared by the precipitation method. Pharmaceutical Development and Technology, 2(3), 275-84.
Kim JC, et al. Hemolytic and Antifungal Activity of Liposome-entrapped Amphotericin B Prepared By the Precipitation Method. Pharm Dev Technol. 1997;2(3):275-84. PubMed PMID: 9552455.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hemolytic and antifungal activity of liposome-entrapped amphotericin B prepared by the precipitation method. AU - Kim,J C, AU - Lee,E O, AU - Kim,J Y, AU - Bae,S K, AU - Choi,T B, AU - Kim,J D, PY - 1997/8/1/pubmed PY - 1998/4/29/medline PY - 1997/8/1/entrez SP - 275 EP - 84 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 2 IS - 3 N2 - A new method of preparing liposomes containing amphotericin B (AmB) was developed with the purpose of reducing the toxicity of AmB without causing a loss in its antifungal activity. The procedure involved the precipitation of AmB and egg phosphatidylcholine (PC) in phosphate buffered saline (PBS, pH 7.4) or tris buffered saline (TBS, pH 7.4) by evaporating methanol and chloroform, which had been previously mixed in the buffer solution, at 4 degrees C and 600 mm Hg. The in vitro toxicity of the precipitated liposomes containing 3, 6, 9, 12, and 15 wt% AmB was compared with that of the film-swollen liposomes containing the equivalent contents of the drug. The hemolytic ability of the precipitated liposomes at 37 degrees C was 50.3% at maximum of the film-swollen liposomes at a dose of 30 micrograms AmB/ml, as measured after 17-hr incubation. The significant reduction in the hemolysis effect may in fact be attributed to the reduced rate of drug release from the precipitated liposomes. The precipitated liposomes were multilayered and aggregates of AmB were embedded in the bilayers. These aggregates of AmB would be responsible for an intensive positive peak around 330 nm and reduced toxicity. Despite the decrease in toxicity, the activity of the precipitated liposomes against Candida albicans remained almost equipotent to that of the film-swollen liposomes. Therefore, liposomes prepared by the precipitation method are less toxic but equally as active. SN - 1083-7450 UR - https://www.unboundmedicine.com/medline/citation/9552455/Hemolytic_and_antifungal_activity_of_liposome_entrapped_amphotericin_B_prepared_by_the_precipitation_method_ L2 - https://www.tandfonline.com/doi/full/10.3109/10837459709031447 DB - PRIME DP - Unbound Medicine ER -