Patent SG-11201805101R-A (SG)
Title: Nanoliposomes comprising corticosteroid as medicaments and methods to prepare them
Inventor: VENKATRAMAN SUBRAMANIAN
IPC: A61P9/10
Filed: 2016-11-28
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 1111111101111011101010111110101111101110101111110111111011111111101111011111 International Bureau ... .... ..Yjd (10) International Publication Number (43) International Publication Date ..... ....!;,„. WO 2017/105344 Al 22 June 2017(22.06.2017) WIPO I PCT (51) International Patent Classification: Nanyang Technological University, 50 Nanyang Avenue, A61K 9/127 (2006.01) A61P 9/10 (2006.01) Singapore 639798 (SG). A61K 31/56 (2006.01) (74) Agent: VIERING, JENTSCHURA & PARTNER LLP; (21) International Application Number: P.O Box 1088, Rochor Post Office, Rochor Road, Singa- PCT/SG2016/050584 pore 911833 (SG). (22) International Filing Date: (81) Designated States (unless otherwise indicated, for every 28 November 2016 (28.11.2016) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (25) Filing Language: English BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (26) Publication Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, (30) Priority Data: KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 10201510370T 17 December 2015 (17.12.2015) SG MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (71) Applicant: NANYANG TECHNOLOGICAL UNIVER- OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SITY [SG/SG]; 50 Nanyang Avenue, Singapore 639798 SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, (SG). TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (72) Inventors: VENKATRAMAN, Subramanian; c/o Nan- yang Technological University, 50 Nanyang Avenue, (84) Designated States (unless otherwise indicated, for every Singapore 639798 (SG). NATARAJAN, Jayaganesh V.; kind of regional protection available): ARIPO (BW, GH, c/o Nanyang Technological University, 50 Nanyang Aven- GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, ue, Singapore 639798 (SG). DARWITAN, Anastasia; c/o TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, [Continued on next page] Title: NANOLIPOSOMES COMPRISING CORTICOSTEROID AS MEDICAMENTS AND METHODS TO PREPARE (54) = THEM Figure 2 (57) : This invention relates to a nanoliposome comprising at least one outer lipid bilayer and at least one (a) Release Profiles of FA-Loaded Liposomes corticosteroid encapsulated bythe at leastone lipid bilayer, 120 wherein the ratio of the corticosteroid and lipids forming the 100 lipid bilayer is preferably between 0.01 - 0.5, 0.1 - 0.3 or Z 40 0.12 - 0.18. The corticosteroid may be a group B corticoster - so oid, including triamcinolone acetonide, fluocinolone acet - onide, triamcinolone alcohol, mometasone, amcinonide, e 40 budesonide, desonide, fluocinonide and halcinonide. Prefer- ably, the size of the nanoliposome is between 1 0 - 1 000 nm 0 or 50 - 150 nm. The present invention also relates to the use 0 5 10 15 20 25 ao 35 of the nanoliposome of the invention for use as a medicam Time (day) ent and for use in the treatment of a cardiovascular disease. ---4--- DA = 0.15 molimoi --e-- DA =0.15 motimol (with DSPE-PEG 2K) Further, the invention is directed to a method to prepare the nanoliposome of the invention, which may further include an (b) Comparison of Daily FA Release Between DPPC + FA extruding step. (D/1=0.15 mol/mol) with and without DSPE-PEG 2K _ 300 2 250 i 200 i 150 li ; 100 71' 71' 1 6 11 15 21 26 31 en ir) lima (day) 0 li —4-0/1=0.15 motimol —5-- DA = 0.15 mol/rnol (with OSPE-PEG 2K) ,-.... IN li © N O WO 2017/105344 Al MIDEDIMOMOIDIONOIDEMOMMIMBOORIMMEHOIMI TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Published: DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, LT, SE, GA, — with — with international search report (Art. 21(3)) sequence listing part of description (Rule 5.2(a)) GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).