Novel method for producing lipoplex for topical administration and antitumor agent using such lipoplex
AssigneeDelta-Fly Pharma, Inc.
InventorsTatsuhiro ISHIDA, Kiyoshi ESHIMA, Masakazu FUKUSHIMA
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Abstract
An object of this invention is to provide a novel delivery means that enables efficient delivery of an active ingredient to a target cell. Such objective is attained by a lipoplex comprising dioleylphosphatidylethanolamine (DOPE), phosphatidylcholine, a cationic lipid, and an RNAi molecule and an industrial method for producing the same.
Claims15
A method for producing a lipoplex comprising dioleylphosphatidylethanolamine (DOPE), phosphatidylcholine, a cationic lipid, and RNAi molecules, comprising steps of:
- (a) dissolving in alcohol
- dioleylphosphatidylethanolamine (DOPE),
- phosphatidylcholine, wherein the phosphatidylcholine is 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), palmitoyl-oeoyl phosphatidylcholine (POPC), or 1,2-dieicosenoyl-sn-glycero-3-phosphocholine (DEPC), and
- a cationic lipid, wherein the cationic lipid is O,O′-ditetradecanoyl-N-(α-trimethylammonioacetyl)diethanolamine chloride (DC-6-14);
- (b) adding the alcohol solution obtained in (a) dropwise to a solution of RNAi molecules with agitation;
- and
- (c) lyophilizing the solution obtained in (b).
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A pharmaceutical composition used for topical administration aimed at treatment of peritoneal metastasis of gastric cancer, ovarian cancer, and pancreatic cancer, which comprises:
- a lipid mixture consisting of dioleylphosphatidylethanolamine (DOPE), phosphatidylcholine, wherein the phosphatidylcholine is 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), palmitoyl-oeoyl phosphatidylcholine (POPC), or 1,2-dieicosenoyl-sn-glycero-3-phosphocholine (DEPC), and a cationic lipid, wherein the cationic lipid is O,O′-ditetradecanoyl-N-(α-trimethylammonioacetyl)diethanolamine chloride (DC-6-14);
- and
- short hairpin RNA (shRNA) capable of inhibiting thymidylate synthase expression via RNAi (TS-shRNA).
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Dependencies are inferred from the claim text.