The Royal Veterinary College

Tecrea Limited

Kantaraja Chindera

Liam Good

Valentina Gburcik

A method for promoting entry of an agent (introduced agent) into a cell, the method comprising the step of complexing the introduced agent in the presence of an entry-promoting agent and then exposing to cells, wherein the entry-promoting agent comprises a linear and/or branched or cyclic polymonoguanide/polyguanidine, polybiguanide, analogue or derivative thereof according to the following Formula 1a & b. The method also provides a means for formation of nanoparticles formed between the entry promoting agent and the introduced agent. wherein: 'n', refers to number of repeating units in the polymer, and n can vary from 2 to 1000, for example from 2 or 5 to 10, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200, 250, 300, 350, 400, 450, 500, 600, 700, 800 or 900; Gand Gindependently represent a cationic group comprising biguanide or guanidine, wherein L, and Lare directly joined to a Nitrogen atom of the guanide; Land Lare linking groups between the Gand Gcationic groups in the polymer and independently represent an aliphatic group containing C-Ccarbon atoms, for example an alkyl group such as methylene, ethylene, propylene, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C-C, -C, -C, -C-, -C, -C, -Cor -C, alkyl; or a C-C(for example C, C, C, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C, -C, -C, -C, -C, -C, -C, -Cor -C), cycloaliphatic, heterocyclic, aromatic, aryl, alkylaryl, arylalkyl, or oxyalkylene radical; or a polyalkylene radical optionally interrupted by one or more, preferably one, oxygen, nitrogen or sulphur atoms, functional groups or saturated or unsaturated cyclic moiety: N and Gare optional end groups; X can be either present or absent; L, Land X are linking groups between the Gand Gcationic groups in the polymer and independently represent an aliphatic group containing C-Ccarbon atoms, for example an alkyl group such as methylene, ethylene, propylene, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C, -C, -C, -C, -C, -C, -C, -Cor -C, alkyl; or Land Land X can independently be C-C(for example C, C, C, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C, -C, -C, -C, -C, -C, -C, -Cor -C), cycloaliphatic, heterocyclic, aromatic, aryl, alkylaryl, arylalkyl, oxyalkylene radicals; or a polyalkylene radical optionally interrupted by one or more, preferably one, oxygen, nitrogen or sulphur atoms, functional groups as well as saturated or unsaturated cyclic moiety; “G” and “G” are cationic moieties and can be same or different, and at least one of them is a biguanidine moiety or carbamoylguanidine, and the other moiety may be biguanidine or carbamoylguanidine or amine; and cationic moieties Gand Gdo not contain single guanidine groups. The entry-promoting agent may comprise homogeneous or heterogeneous mixture of one or more of agents arising from formulae 1 a and b, for example polyhexamethylene biguanide (PHMB), polyhexamethylene monoguanide (PHMG), polyethylene biguanide (PEB), polytetramethylene biguanide (PTMB), polyethylene hexamethylene biguanide (PEHMB), polymethylene biguanides (PMB), poly(allylbiguanidnio-co-allylamine), poly(N-vinylbiguanide), polyallybiguanide.

Methods for promoting entry of an agent into a cell

A method for promoting entry of an agent (introduced agent) into a cell, the method comprising the step of complexing the introduced agent in the presence of an entry-promoting agent and then exposing to cells, wherein the entry-promoting agent comprises a linear and/or branched or cyclic polymonoguanide/polyguanidine, polybiguanide, analogue or derivative thereof according to the following Formula 1a & b. The method also provides a means for formation of nanoparticles formed between the entry promoting agent and the introduced agent. wherein: 'n', refers to number of repeating units in the polymer, and n can vary from 2 to 1000, for example from 2 or 5 to 10, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200, 250, 300, 350, 400, 450, 500, 600, 700, 800 or 900; Gand Gindependently represent a cationic group comprising biguanide or guanidine, wherein L, and Lare directly joined to a Nitrogen atom of the guanide; Land Lare linking groups between the Gand Gcationic groups in the polymer and independently represent an aliphatic group containing C-Ccarbon atoms, for example an alkyl group such as methylene, ethylene, propylene, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C-C, -C, -C0, -C-, -C, -C, -Cor -C, alkyl; or a C-C(for example C, C, C, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C, - C, -C, -C, -C, -C0, -C, -Co or -C), cycloaliphatic, heterocyclic, aromatic, aryl, alkylaryl, arylalkyl, or oxyalkylene radical; or a polyalkylene radical optionally interrupted by one or more, preferably one, oxygen, nitrogen or sulphur atoms, functional groups or saturated or unsaturated cyclic moiety; N and Gare optional end groups; X can be either present or absent; L, Land X are linking groups between the Gand Gcationic groups in the polymer and independently represent an aliphatic group containing C-Ccarbon atoms, for example an alkyl group such as methylene, ethylene, propylene, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C, -C, -C, -C, -C, -C, -C, -Cor -C, alkyl; or Land Land X can independently be C-C(for example C, C, C, C, C, C, C, C, Cor C; C-C, -C, -C, -C, -C-C, -C, -C, -C, -C, -C, -C, -Cor -C), cycloaliphatic, heterocyclic, aromatic, aryl, alkylaryl, arylalkyl, oxyalkylene radicals; or a polyalkylene radical optionally interrupted by one or more, preferably one, oxygen, nitrogen or sulphur atoms, functional groups as well as saturated or unsaturated cyclic moiety; 'G' and &#x201c;G&#x201d; are cationic moieties and can be same or different, and at least one of them is a biguanidine moiety or carbamoylguanidine, and the other moiety may be biguanidine or carbamoylguanidine or amine; and cationic moieties Gand Gdo not contain single guanidine groups. The entry-promoting agent may comprise homogeneous or heterogeneous mixture of one or more of agents arising from formula 1 a and b, for example polyhexamethylene biguanide (PHMB), polyhexamethylene monoguanide (PHMG), polyethylene biguanide (PEB), polytetramethylene biguanide (PTMB), polyethylene hexamethylene biguanide (PEHMB), polymethylene biguanides (PMB), poly(allylbiguanidnio-co-allylamine), poly(N-vinylbiguanide), polyallybiguanide. 

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London, United Kingdom

Kantaraja Chindera