Large unilamellar vesicles (LUV) and method of preparing same

阅读量:

35

申请(专利)号:

US19760701190

申请日期:

1976-06-30

公开/公告号:

US4078052A

公开/公告日期:

1978-03-07

申请(专利权)人:

THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY OF HEALTH, EDUCATION AND WELFARE

发明人:

PD Papahadjopoulos

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被引量:

242

摘要:

A process and resulting product for producing large unilamellar phosphatidylserine vesicles (LUV) in the diameter of about 2, 000-12,000 A which may additionally encapsulate a drug. The large vesicles are prepared from an initial phosphatidylserine aqueous solution which is subjected to ultrasound or sonicated which produces small unilamellar vesicles (SUV) in the diameter range of 200-500 A. After the addition of calcium ion (Ca.sup.2+) in the molar concentration of about 1- 10 mM (threshold 1-2 mM) and incubating for 30-60 minutes at room temperature above 10° C and preferably 37° C, intermediate cochleate lipid cylinders form. Finally, addition of a calcium chelating agent such as EDTA or EGTA to these cochleate cylinders produces by fusion the desired large closed spherical unilamellar vesicles (LUV). The intermediate cochleate form appears specific to the phospholipid serine utilized and to the calcium ion (Ca.sup.2+) incubating agent. Specific examples of drugs encapsulated in the phosphatidylserine LUV vesicles are Actinomycin D, cyclic 3'5'-adenosine monophosphate, Poly I Poly C, RNA, DNA, and arabinose cytocine and its phosphorylated analogs.

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