Dual loaded liposomal pharmaceutical formulations

一种脂质体、药物的技术，应用在脂质体输送、药物组合、药物输送等方向，能够解决产品异质性、低可重复性等问题，达到降低毒性、减轻不期望的副作用的效果

Inactive Publication Date: 2018-01-02
CUREPORT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although there are some approved liposomal drug formulations, the field still presents the unique challenges and unpredictability of each different API and the limitations of currently available methods of preparing liposomal formulations, which face challenges related to scalability, Challenges associated with low repeatability and product heterogeneity

Method used

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  • Dual loaded liposomal pharmaceutical formulations
  • Dual loaded liposomal pharmaceutical formulations
  • Dual loaded liposomal pharmaceutical formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0139] Embodiment 1: Preparation of liposome formulation CPT307C

[0140] CPT307 contains the unsaturated lipids 1,2-dioleoyl-sn-glycero-3-phosphatidylcholine (DOPC), cholesterol and 1,2-distearoyl-sn-glycero-3-phosphatidylethanolamine-N -[methoxy9 polyethylene glycol)-2000] (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy9polyethyleneglycol)-2000]) (mPEG2000-DSPE). Unsaturated lipids were found to have a greater ability to encapsulate docetaxel compared to saturated lipids. The liposomal formulation CPT307B was prepared by dissolving 2100 mg DOPC, 280 mg cholesterol, 700 mg mPEG2000-DSPE and 175 mg docetaxel (DOCE) in 70 mL absolute ethanol. The composition (mol%) of the CPT307B lipid solution is shown in Table 1. In addition, three aqueous solutions of 250 mM ammonium sulfate (pH 6.5) were used. Twenty milliliters of each of the above four solutions were loaded into a 20 mL syringe. Each syringe is connected by tubing to the inlet of a five-port manifold. Thr...

Embodiment 2

[0145] Embodiment 2: Preparation of liposome formulation CPT308C

[0146] Different from CPT307C in Example 1, CPT308C contains polyunsaturated lipid L-α-phosphatidylcholine (soybean PC), which has a higher ability to encapsulate DOCE. Two milliliters of lipid / DOCE solution was prepared by dissolving 30 mg of soy PC, 10 mg of cholesterol, 10 mg of mPEG2000-DSPE and 6 mg of DOCE in absolute ethanol. The composition (mol %) of the lipid solution of the liposome formulation CPT308C is shown in Table 2. In addition, three 250 mM ammonium sulfate aqueous solutions (pH 6.5) were used. Two milliliters of each of the above four solutions were loaded into a 20 mL syringe. Each syringe is connected by tubing to the inlet of a five-port manifold. Through the tubing, the solution in the syringe is pumped by the syringe pump into the mixing chamber of the manifold. The liposome solution is expelled through the outlet and collected in a glass vial. The buffer was changed to histidine / s...

Embodiment 3

[0151] Embodiment 3: Preparation of liposome formulation CPT309C

[0152] Compared to CPT308C in Example 2, CPT309C contained a higher molar ratio of polyunsaturated lipid soybean PC, and thus showed a higher ability to encapsulate DEOCE. Two milliliters of lipid / DOCE solution was prepared by dissolving 30 mg of L-α-phosphatidylcholine (soybean PC), 4 mg of cholesterol, 10 mg of mPEG2000-DSPE and 6 mg of DOCE in absolute ethanol. The composition (mol %) of liposome preparation CPT309C lipid solution is shown in Table 3. In addition, three aqueous solutions of 250 mM ammonium sulfate (pH 6.5) were used. Two milliliters of each of the above four solutions were loaded into a 20 mL syringe. Each syringe is connected by tubing to the inlet of a five-port manifold. Through the tubing, the solution in the syringe is pumped by the syringe pump into the mixing chamber of the manifold. The liposome solution is expelled through the outlet and collected in a glass vial. The buffer wa...

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Abstract

A pharmaceutical composition can include a plurality of liposomes comprising docetaxel and doxorubicin. In various embodiments, a liposome can include (i) an active pharmaceutical ingredient (API) comprising docetaxel and doxorubicin; (ii) a lipid layer comprising an unsaturated phospholipid, a cholesterol, a cationic lipid, and preferably a pegylated phospholipid; and (iii) an aqueous interior, wherein the docetaxel is in the lipid layer and the doxorubicin is crystallized in the aqueous interior. The liposomes can be used to treat a subject, for example, a human subject having cancer. The cancer can be, for example, a lung cancer, preferably non-small cell lung cancer (NSCLC), colon cancer, breast cancer, or liver cancer.

Description

technical field [0001] The present invention relates generally to liposomal pharmaceutical formulations, and in various embodiments more particularly to liposomal pharmaceuticals comprising an active pharmaceutical ingredient having two components (e.g., a combination of docetaxel and doxorubicin) preparation. Background technique [0002] Liposome technology has been used for drug delivery in clinical therapy and scientific research. To date, several liposomal pharmaceutical formulations have been approved by the US Food and Drug Administration (FDA), and many new liposomal formulations are undergoing clinical trials. However, the field of liposomal formulations is still evolving, and each active pharmaceutical ingredient ("API") presents unique challenges. [0003] One area where liposomal formulations may be applicable is cancer APIs. For example, liposomal formulations of doxorubicin are currently available under the trade name with get. Doxorubicin is a pegylat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K9/127A61K49/18
CPCA61K9/0019A61K9/127A61K9/1271A61K9/1272A61K9/1278A61K31/337A61K31/704A61P35/00A61P35/02A61P43/00A61K2300/00
Inventor D-M.朱G.陈
Owner CUREPORT
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