Bioactive and/or targeted dendrimer conjugates

A composition comprising a dendritic polymer complexed with at least one unit of biological response modifier, selected from the group consisting of an interleukin, interferon, tumor necrosis factor, and granulocyte colony stimulating factor.

A composition comprising a dendritic polymer complexed with at least one unit of biological response modifier, wherein said biological response modifier is genetic material.

A process for preparing a conjugate of dendritic polymer and biological response modifier, selected from the group consisting of an interleukin, interferon, tumor necrosis factor, and granulocyte colony stimulating factor, comprising reacting the dendritic polymer with the biological response modifier in a suitable solvent at a temperature which facilitates the association of the biological response modifier and the dendritic polymer.

A process for preparing a conjugate of dendritic polymer and biological response modifier, wherein said biological response modifier comprises genetic material and said dendritic polymer has a predominantly cationic surface character, comprising reacting the dendritic polymer with the biological response modifier in a suitable solvent at a temperature which facilitates the association of the biological response modifier and the dendritic polymer, said process comprising electrostatically attaching said genetic material to said dendritic polymer to create said conjugate.

A process for preparing a complex of dendritic polymer and genetic material comprising:

• reacting said dendritic polymer with said genetic material in a suitable solvent at a temperature which facilitates the complexing of said genetic material with said dendritic polymer, said process
• comprising placing said complex in a solution with DEAE-dextran or glycerol.

A process for forming a dendritic polymer-genetic material complex comprising:

• complexing genetic material with a first dendritic polymer by reacting the polymer with the genetic material in a suitable solvent at a temperature which facilitates association of the genetic material with the polymer;
• and
• placing said complex in a solution containing a second dendritic polymer, said second dendritic polymer being larger than said first dendritic polymer.

A process for forming a genetic material:dendritic polymer complex comprising:

• mixing, in water, sufficient genetic material to yield a final concentration from about 1 to about 10 .mu.g per mL, with sufficient dendritic polymer, having positive surface functionality, to yield a genetic material:dendritic polymer charge ratio from about 3:1 to about 1:10,000;
• said mixing being done at a pH from about 5 to about 10 and at a temperature from about 20.degree. to about 40.degree. C.

A process for forming a concentrated genetic material:dendritic polymer complex which can be diluted for use comprising:

• mixing, in water, sufficient genetic material to yield a concentration from about 1 to about 10 .mu.g per 20 .mu.L, with sufficient dendritic polymer, having positive surface functionality, to yield a genetic material:dendritic polymer charge ratio from about 4:1 to about 1:10,000;
• said mixing being done at a pH from about 5 to about 10 and at a temperature from about 20.degree. to about 40.degree. C.

The process of claim 123 wherein said dendritic polymer comprises relatively small dendrimer particles having a diameter of about 22 to about 50 .ANG. at their smallest dimension;

• said process further including adding dendritic polymers whose particles have diameters from about 50 to about 110 .ANG. at their smallest dimension, after said complex is formed.

A method of effecting cell transfection and bioavailability of genetic material comprising providing a complex of a dendritic polymer and genetic material, and making said complex available to cells to be transfected.

A method for transporting genetic material through a cellular membrane and into a cellular nucleus comprising:

• complexing said genetic material with dendritic polymer;
• followed by making said complex available to cells to be transfected.

A method for protecting genetic material from digestion during transit to and transfection into a cell comprising:

• complexing said genetic material with dendritic polymer prior to exposing the said genetic material to digestive enzymes.

A method for stabilizing and compacting genetic material comprising:

• complexing said genetic material with dendritic polymer.

A method of effecting cell transfection and bioavailability of genetic material comprising providing a complex of a dendritic polymer and genetic material, in solution with DEAE-dextran or glycerol, and making said complex available to cells to be transfected.

A method for effecting cell transfection and bioavailability of genetic material comprising:

• forming a complex of a first dendritic polymer and genetic material, followed by placing said complex in a solution containing a second dendritic polymer, wherein said second dendritic polymer is larger than said first dendritic polymer;
• and
• making the resulting complex and second dendritic polymer available to cells to be transfected.

A dense star polymer conjugate which comprises at least one dense star polymer associated with at least one unit of at least one bioactive agent, selected from the group consisting of therapeutic agents, diagnostic agents, and therapeutic/diagnostic agents.