IP Library Granted Patent US 12708671
Granted Patent B2
US 12708671 · App. 17/958,671 · Granted Aug 18, 2026

Nanometric pharmaceutical composition in the form of liposomes or nanoemulsion containing specific sequences of interference RNA

Inventors: Elizandra Braganhol (Porto Alegre, BR); Ana Maria Oliveira Battastini (Porto Alegre, BR); Helder Teixeira (Porto Alegre, BR); Marco Antonio Stefani (Porto Alegre, BR); Fernanda Bruxel (Uruguaiana, BR); Roselia Maria Spanevello (Pelotas, BR); Fernanda Cardoso Teixeira (Pelotas, BR); Juliana Hofstatter Azambuja (Porto Alegre, BR)
A61K47/6911A61K9/1075A61K9/127A61K31/713A61K38/465A61K47/20A61K47/24A61P35/00C12N15/1137C12N15/1138C12N15/87B82Y5/00C12N2310/14C12N2320/32C12Y301/03005
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Quick Facts
Patent No.
US 12708671
App. No.
17/958,671
Granted
Aug 18, 2026
Kind
B2
Abstract

A nanometric pharmaceutical composition in the form of liposomes or a nanoemulsion containing interference RNA strands comprising one or more of the following specific siRNA sequences: SEQ ID NO: 1; SEQ ID NO: 2; or SEQ ID NO: 3.

Claims (23)

1 . A nanometric pharmaceutical composition in the form of liposomes or a nanoemulsion containing interference RNA strands comprising one or more of the following specific siRNA sequences:

SEQ ID NO: 1;

SEQ ID NO: 2; or

SEQ ID NO: 3.

2 . The composition of claim 1 , wherein the composition is used to treat glioblastoma.

3 . The composition of claim 1 , comprising the interference RNA strands formed by SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3 present a sense and antisense strand comprised of 19 nucleotides in an inverted orientation, separated by a space of 1 base pair.

4 . The composition of claim 1 , comprising a pharmaceutically acceptable excipient capable of carrying siRNA SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3.

5 . The composition of claim 4 , wherein the pharmaceutically acceptable excipient is in the form of a liposome complex or nanoemulsion.

6 . The composition of claim 1 , wherein the nanoemulsion is composed of 8% (w/w) of medium chain triglycerides, 2% (w/w) of egg lecithin, 0.132% (w/w) of DOTAP (N-[1-(2,3-dioleoyloxy) propyl]-N, N, Ntrimethylammonium methylsulfate, 2.25% (w/w) glycerol and water to complete 100% (w/w).

7 . The composition of claim 1 , wherein the nanoemulsion undergoes a process of transfection of the interfering RNA of SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3.

8 . The composition of claim 1 , wherein the composition is a drug to silence genes responsible for the expression of overexposed proteins in glioblastoma.

9 . The composition of claim 8 , wherein the gene silenced by SEQ ID NO: 1 and SEQ ID NO: 2 is 58813/NT5E, and the gene silenced by SEQ ID NO:3 is 4907/NT5E.

10 . The composition of claim 1 , wherein a protein to be regulated is ecto-5′-nucleotidase/CD73.

11 . The composition of claim 1 , wherein the composition is administered intratumoral, parenteral, aerosol, oral, dermal, intradermal, inhalation, intramuscular injection, intranasal, intraocular, intrapulmonary, intravenous, intraperitoneal, nasal, ocular, optical, plaster, subcutaneous, sublingual, topical, or transdermal.

12 . The composition of claim 10 wherein the composition is used in gene silencing kits.

13 . A method for the treatment of glioblastoma comprising the step of administering to a patient an effective amount of the composition of claim 1 .

14 . A process for manufacturing a drug, wherein the process comprises forming a cationic nanometric lipid formulation and associating therewith an siRNA consisting of SEQ ID NO: 3 under conditions effective to form an electrostatic complex for treating a disease characterized by elevated CD73 expression.

15 . The process of claim 14 , wherein the process comprises combining SEQ ID NO:3 with a pharmaceutically acceptable carrier selected from the group consisting of a liposome complex and nanoemulsion, to produce the drug.

16 . A method of using the drug produced by the process of claim 15 for treating a tumor, wherein the drug is administered via a route selected from the group consisting of intratumoral, parenteral, aerosol, oral, dermal, intradermal injection, inhalation, intramuscular, intranasal, intraocular, intrapulmonary, intravenous, intraperitoneal, nasal, ocular, otic, patch, subcutaneous, sublingual, topical, and transdermal.

17 . The composition of claim 2 , comprising a pharmaceutically acceptable excipient capable of carrying siRNA SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3.

18 . The composition of claim 3 , comprising a pharmaceutically acceptable excipient capable of carrying siRNA SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3.

19 . The process of claim 14 , wherein the disease is selected from the group consisting of tumors, glioblastoma, multiple sclerosis, and sepsis.

20 . The method of claim 16 , wherein the tumor is a glioma.