Title:
POLYPEPTIDE EYE ABSORPTION ENHANCER AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/224053
Kind Code:
A1
Abstract:
The present invention belongs to the field of pharmaceutical preparations and relates to designing a series of lipophilic derivatives by using the wild-type membrane-penetrating peptide penetratin. These penetratin derivatives have a strong ability to penetrate the eye tissue, are not toxic to the eye tissue, and can achieve intraocular drug delivery by means of a non-invasive route as eye absorption enhancers, increasing the bioavailability of a drug in the eyes. These penetratin derivatives and an ocular drug delivery system constructed with same are used for ophthalmic instillation, can replace intraocular injection administration, the compliance thereof to patients being poor, and enhance the convenience and safety of treating intraocular diseases and diseases of the fundus.
Inventors:
WEI GANG (CN)
JIANG KUAN (CN)
LU WEIYUE (CN)
LIU CHANG (CN)
TAI LINGYU (CN)
GAO XIN (CN)
JIANG KUAN (CN)
LU WEIYUE (CN)
LIU CHANG (CN)
TAI LINGYU (CN)
GAO XIN (CN)
Application Number:
PCT/CN2018/095539
Publication Date:
December 13, 2018
Filing Date:
July 13, 2018
Export Citation:
Assignee:
UNIV FUDAN (CN)
International Classes:
A61K38/10; C07K7/08; A61K47/64; A61P27/02
Domestic Patent References:
| WO2010091294A2 | 2010-08-12 |
Foreign References:
| CN101355970A | 2009-01-28 | |||
| CN102405053A | 2012-04-04 | |||
| CN201610560173A | 2016-07-15 |
Other References:
SGOLASTRA, F. ET AL.: "Designing Mimics of Membrane Active Proteins", ACC. CHEM. RES., vol. 46, no. 12, 17 December 2013 (2013-12-17), pages 2977 - 2987, XP055557454
PROCHIANTZ, A. ET AL.: "Getting Hydrophilic Compounds into Cells: Lessons from Homeopeptides", CUURENT OPINION IN NEUROBIOLOGY, vol. 6, 31 December 1996 (1996-12-31), pages 629 - 634, XP001004716
ESBJORNER, E.K. ET AL.: "Counterion-mediated Membrane Penetration: Cationic cell - penetrating Peptides Overcome Born Energy Barrier by Ion-pairing with Phospholipids", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1768, no. 6, 19 March 2007 (2007-03-19), pages 1550 - 1558, XP022095204
LIU, C. ET AL.: "Facile Noninvasive Retinal Gene Delivery Enabled by Penetratin", ACS APPL. MATER. INTERFACES, vol. 8, no. 30, 20 July 2016 (2016-07-20), pages 19256 - 19267, XP055557489
JIANG, K. ET AL.: "Discerning the Composition of Penetratin for Safe Penetration from Cornea to Retina", ACTA BIOMATERIALIA, vol. 63, 18 September 2017 (2017-09-18), pages 123 - 134, XP085239146
LIU, C. ET AL.: "Penetratin, a Potentially Powerful Absorption Enhancer for Noninvasive Intraocular Drug Delivery", MOL. PHARMACEUTICS, vol. 11, no. 4, 24 February 2014 (2014-02-24), pages 1218 - 1227, XP055557495
TAI, L. ET AL.: "Noninvasive Delivery of Oligonucleotide by Penetratin-modified Polyplexes to Inhibit Protein Expression of Intraocular Tumor", NANOMEDICINE: NANOTECHNOLOGY, BIOLOGY, AND MEDICINE, vol. 13, no. 6, 20 April 2017 (2017-04-20), pages 2091 - 2100, XP085147077
ZHANG, W. ET AL.: "Mechanism of Penetration of Antp (43-58) into Membrane Bilayers", BIOCHEMISTRY, vol. 44, no. 30, 1 August 2005 (2005-08-01), pages 10110 - 10118, XP055557498
DRUG DISCOVERY TODAY, vol. 13, no. 3-4, 2008, pages 135 - 143
ADV. DRUG DELIVERY REV., vol. 58, no. 11, 2006, pages 1131 - 1135
J. CONTROLLED RELEASE, vol. 193, 2014, pages 100 - 112
INVEST. OPHTHALMOL. VISUAL SCI., vol. 41, no. 5, 2000, pages 961 - 964
EYE, vol. 27, no. 7, 2013, pages 787 - 794
TOXICOL. LETT., vol. 122, no. 1, 2001, pages 1 - 8
J. CONTROLLED RELEASE, vol. 155, no. 1SI, 2011, pages 26 - 33
BIOMATERIALS, vol. 34, no. 32, 2013, pages 7980 - 7993
MOL. PHARM., vol. 11, no. 4, 2014, pages 1218 - 1227
ACS APPL. MATER. INTERFACES, vol. 8, no. 30, 2016, pages 19256 - 19267
PROCHIANTZ, A. ET AL.: "Getting Hydrophilic Compounds into Cells: Lessons from Homeopeptides", CUURENT OPINION IN NEUROBIOLOGY, vol. 6, 31 December 1996 (1996-12-31), pages 629 - 634, XP001004716
ESBJORNER, E.K. ET AL.: "Counterion-mediated Membrane Penetration: Cationic cell - penetrating Peptides Overcome Born Energy Barrier by Ion-pairing with Phospholipids", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1768, no. 6, 19 March 2007 (2007-03-19), pages 1550 - 1558, XP022095204
LIU, C. ET AL.: "Facile Noninvasive Retinal Gene Delivery Enabled by Penetratin", ACS APPL. MATER. INTERFACES, vol. 8, no. 30, 20 July 2016 (2016-07-20), pages 19256 - 19267, XP055557489
JIANG, K. ET AL.: "Discerning the Composition of Penetratin for Safe Penetration from Cornea to Retina", ACTA BIOMATERIALIA, vol. 63, 18 September 2017 (2017-09-18), pages 123 - 134, XP085239146
LIU, C. ET AL.: "Penetratin, a Potentially Powerful Absorption Enhancer for Noninvasive Intraocular Drug Delivery", MOL. PHARMACEUTICS, vol. 11, no. 4, 24 February 2014 (2014-02-24), pages 1218 - 1227, XP055557495
TAI, L. ET AL.: "Noninvasive Delivery of Oligonucleotide by Penetratin-modified Polyplexes to Inhibit Protein Expression of Intraocular Tumor", NANOMEDICINE: NANOTECHNOLOGY, BIOLOGY, AND MEDICINE, vol. 13, no. 6, 20 April 2017 (2017-04-20), pages 2091 - 2100, XP085147077
ZHANG, W. ET AL.: "Mechanism of Penetration of Antp (43-58) into Membrane Bilayers", BIOCHEMISTRY, vol. 44, no. 30, 1 August 2005 (2005-08-01), pages 10110 - 10118, XP055557498
DRUG DISCOVERY TODAY, vol. 13, no. 3-4, 2008, pages 135 - 143
ADV. DRUG DELIVERY REV., vol. 58, no. 11, 2006, pages 1131 - 1135
J. CONTROLLED RELEASE, vol. 193, 2014, pages 100 - 112
INVEST. OPHTHALMOL. VISUAL SCI., vol. 41, no. 5, 2000, pages 961 - 964
EYE, vol. 27, no. 7, 2013, pages 787 - 794
TOXICOL. LETT., vol. 122, no. 1, 2001, pages 1 - 8
J. CONTROLLED RELEASE, vol. 155, no. 1SI, 2011, pages 26 - 33
BIOMATERIALS, vol. 34, no. 32, 2013, pages 7980 - 7993
MOL. PHARM., vol. 11, no. 4, 2014, pages 1218 - 1227
ACS APPL. MATER. INTERFACES, vol. 8, no. 30, 2016, pages 19256 - 19267
Attorney, Agent or Firm:
TEE & HOWE INTELLECTUAL PROPERTY ATTORNEYS (CN)
Download PDF: