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Method for producing solid-lipid composite drug particles

a technology of solid-lipid composite drug particles and lipid-based drug particles, which is applied in the direction of drug compositions, solvent extraction, separation processes, etc., can solve the problems of limited use of drug-containing emulsions, limited liposome-based drug delivery systems, and limited biodegradable polymer nanoparticles, etc., and achieve low temperature processing and high drug loading

Inactive Publication Date: 2006-01-12
FERRO CORP
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Benefits of technology

[0008] The present invention provides an apparatus and a method of producing solid composite lipid / drug nanoparticles for controlled drug delivery that offers several advantages over conventional processing techniques, including the consistent production of solid composite lipid / drug particles having an average diameter below 100 nm, high drug loading and low temperature processing. The method of the invention is sometimes referred to herein by the acronym PSFEE, which stands for Particles from Supercritical Fluid Extraction of Emulsions (“PSFEE”), and involves the steps of: (1) dissolving a lipid and a drug in a suitable organic solvent to form a solution; (2) emulsifying the solution in a liquid to form an emulsion having a discontinuous phase of micelles comprising the organic solvent, the drug and the lipid, and a continuous phase comprising the liquid; and (3) contacting the emulsion with a supercritical fluid under conditions suitable to keep the supercritical fluid in a supercritical state, whereby the supercritical fluid extracts the organic solvent from the micelles, causing them to precipitate as organic-solvent free solid composite lipid / drug nanoparticles suspended or dispersed in the liquid.

Problems solved by technology

The use of drug-containing emulsions, for example, is limited by the physical stability of the drug-containing emulsions, and also by the low dissolution of most drugs in the triglycerides used to form the emulsions.
Liposome based drug delivery systems are limited by the non-availability of inexpensive pharmaceutical liposomes, and also by the low solubility of most drugs in the liposome membrane.
Biodegradable polymer nanoparticles are limited by the cytotoxicity of certain polymers in the human body.
There are some inherent limitations on the conventional methods of forming solid composite lipid / drug particles.
The high-pressure homogenization process, for example, is limited by the solubility of the drug in the molten lipid, and cannot be used to effectively produce solid composite lipid / drug particles having an average particle diameter of less than 100 nm.
The average particle size of solid composite lipid / drug particles produced via the microemulsion process tends to be quite small, but the dispersion obtained using this process is extremely dilute and is thus not suitable for drug delivery applications.
Scale up of the process is also problematic.

Method used

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[0059] Preparation of Emulsions

[0060] Four organic solutions (Examples 1-4, respectively) were prepared by dissolving 5 percent of a lipid (GLUCIRE 50 / 13) and the amounts shown in Table 1 of either Indomethacin or Ketoprofen in chloroform (all amounts are specified as weight percents relative to the weight of the organic solvent). The resulting organic solutions were then dispersed in an aqueous 0.13% w / w of sodium glychocholate solution in the amounts shown in Table 1 in parts by weight relative to water to form coarse oil-in-water (O / W) emulsions. The resulting emulsions were then homogenized using a homogenizer commercially available from Microfluidics, Inc. (Newton, Mass.) at 16,000 p.s.i. in 3 passes.

TABLE 1Weight % ofWeight % of OrganicExampleDrugDrug in SolventSolution in Water1Indomethacin15102Indomethacin10303Indomethacin15304Ketoprofen1530

[0061] Precipitation of Nanoparticles

[0062] An apparatus such as shown in FIG. 1 was used to precipitate solid composite lipid / drug ...

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Abstract

A method of producing solid composite lipid / drug nanoparticles that includes the steps of: (1) dissolving a lipid and a drug in a suitable organic solvent to form a solution; (2) emulsifying the solution in a liquid to form an emulsion having a discontinuous phase of micelles comprising the organic solvent, the drug and the lipid, and a continuous phase comprising the liquid; and (3) contacting the emulsion with a supercritical fluid under conditions suitable to keep the supercritical fluid in a supercritical state, whereby the supercritical fluid extracts the organic solvent from the micelles, causing them to precipitate as organic-solvent free solid composite lipid / drug nanoparticles suspended or dispersed in the liquid.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] The present application is a continuation-in-part of application Ser. No. 10 / 434,426, filed May 8, 2003.BACKGROUND OF THE INVENTION [0002] 1. Field of Invention [0003] The present invention relates generally to an apparatus and a method of producing solid-lipid composite drug particles. [0004] 2. Description of Related Art [0005] In recent years, solid composite lipid / drug particles have been used for oral, pulmonary and parenteral drug delivery as an alternative to traditional drug delivery systems such as emulsions, liposomes and biodegradable polymer nanoparticles. Solid lipid / drug composite particles provide the advantages of traditional drug delivery systems, such as improved dissolution and controlled release, but avoid some of the disadvantages of traditional drug delivery systems. The use of drug-containing emulsions, for example, is limited by the physical stability of the drug-containing emulsions, and also by the low dissolut...

Claims

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Application Information

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IPC IPC(8): A61K9/14
CPCA61K9/167A61K9/5123B01D11/0411B01D11/0407B01J13/02B01D11/0403B01D11/0484A61P43/00
Inventor SHEKUNOV, BORIS Y.CHATTOPADHYAY, PRATIBHASHHUFF, ROBERT W.
Owner FERRO CORP
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