Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1990-01-26
1992-09-29
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
424408, 424409, 424450, 424489, 424490, 424491, 424492, 424493, 424494, 424495, 424499, 424502, 42721331, 42840224, A61K 3722, A61K 914, A61K 916, A61K 950
Patent
active
051512645
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a new particulate carrier useable in particular for the transport of molecules having biological activity.
Amongst the processes used to cause a compound (active principle) to penetrate into and react in the interior of a biological or biochemical system it is sometimes valuable to use a particulate carrier in which the active product is encapsulated.
This is the case in particular: body or in the biological or biochemical systems. The carrier then enables the compound to be protected and ensures that it has a constant diffusion. presented in a certain manner. This is the case for anticancer products and antigens. The carrier can then ensure the presentation and the targeting towards the chosen target. membranes: intestine, ENT system, vagina or the skin. The carrier then serves as a coating to facilitate the passage through the barrier.
A particulate carrier of this type must satisfy a certain number of demands relating in particular: to its useful load, its stability, its biometabolization and its possibilities for diffusion of the active principles. In order to be of value it must, in addition, by virtue of its properties, tend to resemble as far as possible natural systems for the transport of molecules in the body or systems encountered in natural media, this being a requirement in order not to disturb the physiological balance and in order to be able to benefit, if appropriate, from the advantages linked to natural vital processes.
Amongst the natural transport systems which the carriers can tend to imitate, the most interesting for study are the lipoproteins.
All of the lipoproteins have the same type of structural organization with an internal lipid core surrounded by phospholipids. An apolipoprotein is furthermore anchored in the phospholipid layer and ensures guiding of the lipoprotein. There are various types of lipoproteins which differ in respect of their size, the nature of the transported lipids and the structure of the apolipoprotein. The chylomicrons, for example, are relatively large lipoproteins (1 .mu.m) and have the role of transporting the fats arising from digestion. The low density lipoproteins or LDL are much smaller (20-25 nm) and have the role of transporting cholesterol. The small size of the LDL enables them to diffuse within tissues.
The synthetic carrier closest to these natural carriers is a liposome, which consists of a phospholipid bilayer surrounding an aqueous vacuole. The liposomes have been the subject of numerous studies to develop their use as carriers for active principles.
However, they have a number of disadvantages which have prevented their use in the pharmaceutical industry. These are, in particular, their fragility, heterogeneity, their low transport capacity and the difficulties posed by their production on an industrial scale.
It is therefore desirable to have available a carrier which is structurally close to the natural carriers but does not have the drawbacks encountered with liposomes.
The invention in question relates to particulate carriers of a phospholipid/glycolipid/polysaccharide nature, which are also termed Bio Vecteurs Supra Moleculaires (BVSM) [Supramolecular Biocarriers], which permit the transport of molecules of natural, synthetic, semisynthetic or recombinant origin in various biological and biochemical systems: eukaryotes or prokaryotes, for enzymatic, chemical or immunological reactions or diagnostic tests or for fermentations.
Although particulate systems for the transport of active substances have already been described, none of these has the particular multilayer structure of the particulate carriers according to the invention which enables entities of defined size to be obtained which are adjustable and very stable and can be lyophilized, sterilized and completely metabolized and have a structure and surface which are very similar to those of natural carriers
More particularly, the present invention relates to a particulate carrier characterized in that it comprises: polymer, polysaccharide for example
REFERENCES:
French Search Report and Annex, Application No. 88 07110.
International Search Report and Annex, Application No. FR 8900229.
Bec Jean-Louis
Cohen Edith
Nguyen Frederique
Peyrot Marianne
Samain Daniel
Azpuru C.
Centre National de la Recherche Scientifique
Page Thurman K.
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