Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Biocides; animal or insect repellents or attractants
Patent
1996-07-08
1999-01-12
Levy, Neil S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Biocides; animal or insect repellents or attractants
424406, 424450, 424489, 424490, 424498, 424502, 514938, A01N 2500
Patent
active
058583823
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to pharmaceutical compositions and a method for drug targeting. More specifically said invention relates to pharmaceutical compositions containing an oil/water emulsion wherein a drug is dissolved or solubilized or dispersed inside the oil droplets and wherein said emulsion droplets are coated with adsorbed native and modified antibodies. The invention relates also to a process for the preparation of said pharmaceutical compositions and to a method for drug targeting toward specific molecules or sites in the body, comprising administration to a host an effective amount of above mentioned pharmaceutical compositions.
Emulsion droplets are coated with adsorbed native and/or modified antibodies which are capable of interacting with specific molecules or antigenic determinants. Therefore, the droplets will be directed towards specific molecules or sites in the body. When a drug is dissolved, dispersed or solubilized inside the oil droplet, a novel drug targeting system is obtained.
BACKGROUND OF THE INVENTION
The present invention relates to drug targeting by small emulsion droplets, using biologically active targeting molecules. The advantages of being able to direct the drug to the tissue or cells where it is required, and to minimize the amount delivered to inappropriate sites has implications for many clinical situations, such as cancer chemotherapy, inflammations and viral infections (Davis S. S et al. Drug Exptl. Clin. Res. 9, 632, 1985).
In the past, several attempts to achieve drug targeting were reported, by using polyclonal and monoclonal antibodies. These attempts include: polymer molecule such as dextran. particles, by covalent linkage by direct adsorption or by adsorption via protein A. modification of the antibody.
The above suggested method to achieve drug targeting have many disadvantages: binding process for each drug to be tested. attachment. solid particle.
The present invention will provide a novel drug targeting method, which would overcome most of the above disadvantages, by the use of emulsions and micro emulsions.
BRIEF DESCRIPTION OF THE INVENTION
The present invention relates to pharmaceutical compositions containing an oil/water emulsion wherein a drug is dissolved or dispersed or solubilized inside the oil droplets and wherein said emulsion droplets are coated with adsorbed native and/or modified antibodies.
The present invention further relates to a process for the preparation of said pharmaceutical compositions comprising: hydrophobic groups to the antibodies;
The present invention also relates to a method for drug targeting towards specific molecules or sites in the body (such as antigenic determinants), comprising administration to a host of an effective amount of pharmaceutical composition according to claim 1.
DESCRIPTION OF THE INVENTION
The invention is based on a simple process, which may be applied to various types of drugs.
As described in FIG. 1, the final composition contains oil emulsion droplets onto which native or chemically modified antibodies are adsorbed. A hydrophobic drug is dissolved or solubilized inside the oil droplet, and there-fore, the drug may be targeted to specific sites by the antibodies. The following principle steps are required for obtaining the final composition: This step will lead to formation of a "surface-active-antibody". established. The oil phase initially contains the desired drugs. period of time. The resulting composition is demonstrated in FIG. 1.
This process is very simple and may be applied rapidly to various types of drugs, antibodies, and emulsions. The main advantages of the proposed method are: may be adopted by the final user, provided the drug has a suitable solubility in the emulsion droplets, or may be dispersed or solubilized in the oil phase. emulsion to meet the requirement of drug solubility or dispersion. original drug is maintained through the whole process. oil droplets upon storage. has become a "surface-active-antibody" with improved adsorption capability; more protein molecule
REFERENCES:
patent: 4634681 (1987-01-01), Giaever et al.
patent: 5576016 (1996-11-01), Amselem et al.
Davis et al, Drugs Exptl. Clin. Res., XI(9), pp. 633-640 (1985).
Database WPI, Week 8807, Derwent Pub. Ltd. AN 88-045802 & JP-A-63-002923.
Database WPI, Week 8848, Derwent Pub. Ltd. AN 88-341492 & JP-A-63-253021.
Journal of Biological Chemistry, vol. 225, No. 17, Sep. 10, 1980, Huang et al., "Monoclonal Antibody Covalently Coupled . . . ".
Linevitz Moshe
Magdassi Shlomo
Rones Zichria Zakay
Shanberg Oren
Levy Neil S.
Yissum Research Development Company of The Hebrew University of
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