Abstract: The present invention discloses a Plectin-1 receptor targeting novel cationic KTLLPTPK(SEQ ID NO: 1)-lipopeptide. The present invention further discloses a liposomal formulation comprising the cationic KTLLPTPK(SEQ ID NO: 1)-lipopeptide, at least two co-lipids, a therapeutic agent, and a pharmaceutically acceptable carrier. The present invention also provides a method for regressing established pancreatic tumors comprising administering a therapeutically effective amount of the liposomal formulation with the therapeutic agents in combination with targeted genetic immunization (DNA vaccination) i.e. by immunizing mice with electrostatic complexes (direct in-vivo DC-targeting cationic liposomes) of DNA vaccines encoding mesothelin (p-CMV-MSLN).

Abstract: Liposomal compositions comprising of liposomes of guanidinylated cationic amphiphiles as the main lipid and cholesterol/1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC)/aminopropyl polyethyleneglycol carbamyl-distearoylphosphatidyl-ethanolamine (DSPE-peg-NH2) as co-lipids are described. These liposomal compositions containing encapsulated or electrostatically complexed therapeutic small interfering RNAs (siRNAs) against Cdc20, a key cell cycle regulator, inhibit solid tumor growth and melanoma tumor growth on lung in C57BL/6J mice.

Abstract: The present invention relates to the mannose-receptor selective lysinylated cationic amphiphile and a process for preparation thereof. The compounds of the present invention can target DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterparts in genetic immunization in mice. The present invention discloses that immunization with electrostatic complexes (lipoplexes) of DNA vaccines encoding melanoma antigens (gp100 and tyrosinase) and liposome of the presently described novel lysinylated cationic amphiphiles with mannose-mimicking shikimoyl head-groups provides long-lasting (100 days post melanoma tumor challenge) protective immunity in all immunized mice.

Abstract: The present invention discloses a Plectin-1 receptor targeting novel cationic KTLLPTPK-lipopeptide. The present invention further discloses a liposomal formulation comprising the cationic KTLLPTPK-lipopeptide, at least two co-lipids, therapeutic agents and a pharmaceutically acceptable carrier. The present invention also provides a method for regressing established pancreatic tumors comprising administering therapeutically effective amount of the liposomal formulation with the therapeutic agents in combination with targeted genetic immunization (DNA vaccination) i.e. by immunizing mice with electrostatic complexes (direct in-vivo DC-targeting cationic liposomes) of DNA vaccines encoding mesothelin (p-CMV-MSLN).

Abstract: The present invention provides synthesis of a novel series of cationic lipopeptides with integrin-binding RGD functionalities. The invention also provides high L27 (transformed S1 80, mouse sarcoma cells) cell tropic gene transfer properties of these novel RGD-lipopeptides. Since L27 cell surface contains over expressed integrins, the present class of lipopeptides with integrin-binding RGD ligands are likely to find future applications in targeting anti-cancer genes/drugs to the endothelial cells of tumor vasculatures (possessing over expressed integrins).

Abstract: Liposomal compositions comprising of liposomes of guanidinylated cationic amphiphiles as the main lipid and cholesterol/1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC)/aminopropyl polyethyleneglycol carbamyl-distearoylphosphatidyl-ethanolamine (DSPE-peg-NH2) as co-lipids are described. These liposomal compositions containing encapsulated or electrostatically complexed therapeutic small interfering RNAs (siRNAs) against Cdc20, a key cell cycle regulator, inhibit solid tumor growth and melanoma tumor growth on lung in C57BL/6J mice.

Abstract: The present invention relates to the mannose-receptor selective lysinylated cationic amphiphile and a process for preparation thereof. The compounds of the present invention can target DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterparts in genetic immunization in mice. The present invention discloses that immunization with electrostatic complexes (lipoplexes) of DNA vaccines encoding melanoma antigens (gp100 and tyrosinase) and liposome of the presently described novel lysinylated cationic amphiphiles with mannose-mimicking shikimoyl head-groups provides long-lasting (100 days post melanoma tumor challenge) protective immunity in all immunized mice.

Abstract: Novel anti-cancer reagents capable of combating various types of tumors continue to be major research focus in many leading pharmaceutical companies round the globe. To this end, the present invention discloses processes for preparing a novel series of histidinylated cationic amphiphiles of formula I. The findings described herein also demonstrate that compounds of the present invention possess anti-proliferative activity such as anti” cancer activity and are useful in combating various types of cancer. The pharmaceutically active composition of cationic amphiphiles disclosed herein show enhanced cellular apoptosis through the Bax & Bcl-2 mediated signal transduction pathway. Cationic amphiphiles with histidine head-groups described in the present invention are likely to find future applications in the field of anti-cancer therapy.

Abstract: The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikimic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.

Abstract: The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikimic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.

Abstract: The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.

Abstract: The present invention provides method and pharmaceutical composition for efficient delivery of siRNA (small interfering ribonucleic acids) into cultured mammalian cells. In addition, the present invention provides methods and compositions for knocking down the expression of a specific target gene by treating cells with the formulations comprising cationic amphiphile, a neutral colipid and a small RNA molecule. We demonstrate that our method delivers siRNA efficaciously into animal cells for the purpose of RNA interference. The area of medical science that is likely to benefit most from the present invention is RNAi therapeutics.

Abstract: The present invention provides synthesis of a novel series of cationic lipopeptides with integrin-binding RGD functionalities. The invention also provides high L27 (transformed S1 80, mouse sarcoma cells) cell tropic gene transfer properties of these novel RGD-lipopeptides. Since 127 cell surface contains over expressed integrins, the present class of lipopeptides with integrin-binding RGD ligands are likely to find future applications in targeting anti-cancer genes/drugs to the endothelial cells of tumor vasculatures (possessing over expressed integrins).

Abstract: A process for producing a targeted gene and/or drug delivery system for liver cells comprising the steps of: i. chemical reduction of Sendai virus for reduction of HN protein; ii. subjecting the reduced virus to the step of dialysis for removal of the reducing agent; iii. solubilizing the reduced virus with a detergent to obtain a solution; iv. centrifuging the solution to separate the insolubles consisting of reduced HN protein and core of said virus; v. adding histidylated lipid to the supernatant; vi. adding the drug or gene after addition of the lipid; vii. removing the detergent from the envelope and then subjecting it to the step of centrifugation to obtain His lipid F-virosomes with entrapped drug or DNA.

Abstract: The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.

Abstract: The present invention provides novel cationic amphiphiles capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain cyclic head group having polar functional groups and pharmaceutical composition useful for delivering biologically active therapeutic molecules into body cells.

Abstract: The present invention provides novel cationic amphiphiles capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain cyclic head group having polar functional groups and pharmaceutical composition useful for delivering biologically active therapeutic molecules into body cells.

Abstract: The present invention provides processes for the synthesis of novel cationic amphiphiles capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain N-hydroxyalkyl group and have at least one hydroxyalkyl group containing 1-3 carbon atoms directly linked to the positively charged nitrogen atom.

Abstract: The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells.

Abstract: The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells.