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1. WO2017184436 - SYSTEMS AND METHODS FOR STEROIDAL GELS

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[ EN ]

CLAIMS

A composition, comprising:

a steroid comprising a phosphate moiety and a core portion, the core portion having a logP value greater than or equal to 1, complexed via Ca2+ and/or Ba2+ metal ions to form a hydrogel, wherein the steroid forms at least 50% by dry weight of the hydrogel.

The composition of claim 1, wherein the phosphate moiety is bonded to a carboxylate within the steroid.

The composition of claim 2, wherein the carboxylate is bonded to a D-ring of the steroid.

The composition of any one of claims 1-3, wherein the core portion of the steroid comprises a gonane structure.

The composition of any one of claims 1-4, wherein the core portion of the steroid comprises a methyl group at the 10 position, a methyl group at the 13 position, and/or a carboxylate moiety at the 17 position.

The composition of claim 5, wherein the core portion of the steroid further comprises an oxo moiety at the 3 position.

The composition of any one of claims 5 or 6, wherein the core portion of the steroid further comprises a hydroxyl moiety at the 17 position.

The composition of any one of claims 1-7, wherein the steroid comprises a carboxylate at the 17 position.

The composition of any one of claims 5-8, wherein the core portion of the steroid comprises an acetyl moiety at the 17 position.

The composition of claim 9, wherein the phosphate moiety is bonded to the methyl group of the acetyl moiety.

11. The composition of any one of claims 1-9, wherein the phosphate moiety is attached at the 17 position of the core portion of the steroid.

12. The composition of any one of claims 1-11, wherein the core portion of the steroid does not comprise a carboxylic acid group.

13. The composition of any one of claims 1-12, wherein the core portion of the steroid

comprises at least one hydroxyl group.

14. The composition of any one of claims 1-13, wherein each face of the steroid comprises an equal number of hydroxyl groups.

15. The composition of any one of claims 1-14, wherein the steroid comprises a

corticosteroid.

16. The composition of any one of claims 1-15, wherein the steroid comprises a

glucocorticoid.

17. The composition of any one of claims 1-16, wherein the steroid has the following

structure:


The composition of any one of claims 1-16, wherein the steroid has the following structure:


19. The composition of any one of claims 1-16, wherein the steroid has the following

structure:


20. The composition of any one of claims 1-19, wherein the steroid forms at least 75% by dry weight of the hydrogel.

21. The composition of any one of claims 1-20, wherein the core portion of the steroid has a logP value greater than or equal to 1.2.

22. The composition of any one of claims 1-21, wherein the core portion of the steroid has no formal charged moieties at a pH of 7.

23. The composition of any one of claims 1-22, wherein the steroid is present within the hydrogel at a concentration of at least 2.5 mM.

24. The composition of any one of claims 1-23, wherein the steroid is present within the hydrogel at a concentration of at least 8 mM.

25. The composition of any one of claims 1-24, wherein the steroid is present within the hydrogel at a concentration of at least 10 mM.

26. The composition of any one of claims 1-25, wherein the concentration of steroid within the hydrogel is at most 25 mM.

27. The composition of any one of claims 1-26, wherein the metal ions are present within the hydrogel at a concentration of at least 2.5 mM.

28. The composition of any one of claims 1-27, wherein the metal ions are present within the hydrogel at a concentration of at least 8 mM.

29. The composition of any one of claims 1-28, wherein the metal ions are present within the hydrogel at a concentration of at least 10 mM.

30. The composition of any one of claims 1-29, wherein the steroid and the metal ion are present at a molar ratio of between about 2: 1 and about 1:2.

31. The composition of any one of claims 1-30, wherein the metal ion comprises Ca2+.

32. The composition of any one of claims 1-31, wherein at least 50 mol% of the metal ions are Ca2+.

33. The composition of any one of claims 1-32, wherein the metal ion comprises Ba2+.

34. The composition of any one of claims 1-33, wherein at least 50 mol% of the metal ions are Ba2+.

35. The composition of any one of claims 1-34, wherein the hydrogel further comprises a salt.

36. The composition of any one of claims 1-35, wherein the hydrogel further comprises an anesthetic.

37. The composition of claim 36, wherein the anesthetic comprises bupivacaine.

38. The composition of any one of claims 1-37, wherein the hydrogel comprises nanofibers.

39. The composition of any one of claims 1-38, wherein the hydrogel is shear-thinning.

40. The composition of any one of claims 1-39, wherein the hydrogel is exhibits decreased viscosity when subjected to shear strain.

41. The composition of any one of claims 1-40, wherein the hydrogel is self-healing.

42. The composition of any one of claims 1-41, wherein the hydrogel is thixotropic.

43. A needle, comprising the composition of any one of claims 1-42.

44. A syringe, comprising the composition of any one of claims 1-42.

45. An implant, comprising the composition of any one of claims 1-42.

46. A composition, comprising:

a steroid comprising a phosphate moiety and a core portion, the core portion having no formal charged moieties at a pH of 7, the steroid complexed via Ca2+ and/or Ba2+ metal ions to form a nanofiber.

47. The composition of claim 46, wherein the nanofiber has an average cross-sectional diameter between 5 nm and 25 nm.

The composition of any one of claims 46 or 47, wherein the nanofiber has an average cross-sectional diameter between 5 nm and 15 nm.

The composition of any one of claims 46-48, wherein the phosphate moiety is bonded to a carboxylate within the steroid.

50. The composition of claim 49, wherein the carboxylate is bonded to a D-ring of the

steroid.

51. The composition of any one of claims 46-50, wherein the core portion of the steroid comprises a gonane structure.

52. The composition of any one of claims 46-51, wherein the core portion of the steroid comprises a methyl group at the 10 position, a methyl group at the 13 position, and/or a carboxylate moiety at the 17 position.

53. The composition of claim 52, wherein the core portion of the steroid further comprises an oxo moiety at the 3 position.

54. The composition of any one of claims 52 or 53, wherein the core portion of the steroid further comprises a hydroxyl moiety at the 17 position.

55. The composition of any one of claims 46-54, wherein the steroid comprises a carboxylate at the 17 position.

56. The composition of any one of claims 52-55, wherein the core portion of the steroid comprises an acetyl moiety at the 17 position.

57. The composition of claim 56, wherein the phosphate moiety is bonded to the methyl group of the acetyl moiety.

The composition of any one of claims 46-56, wherein the phosphate moiety is attached at the 17 position of the core portion of the steroid.

The composition of any one of claims 46-58, wherein the core portion of the steroid does not comprise a carboxylic acid group.

60. The composition of any one of claims 46-59, wherein the core portion of the steroid comprises at least one hydroxyl group.

61. The composition of any one of claims 46-60, wherein each face of the steroid comprises an equal number of hydroxyl groups.

62. The composition of any one of claims 46-61, wherein the steroid comprises a

corticosteroid.

63. The composition of any one of claims 46 62, wherein the steroid comprises a

glucocorticoid.

64. The composition of any one of claims 46 63, wherein the steroid has the following

structure:


The composition of any one of claims 46-63, wherein the steroid has the following structure:


The composition of any one of claims 46-63, wherein the steroid has the following structure:


The composition of any one of claims 46-66, wherein the steroid forms at least 75% by dry weight of the nanofiber.

The composition of any one of claims 46-67, wherein the core portion of the steroid has a logP value greater than or equal to 1.

The composition of any one of claims 46-68, wherein the core portion of the steroid has a logP value greater than or equal to 1.2.

The composition of any one of claims 46-69, wherein the steroid and the metal ion are present at a molar ratio of between about 2: 1 and about 1:2.

The composition of any one of claims 46-70, wherein the metal ion comprises Ca2+.

72. The composition of any one of claims 46-71, wherein at least 50 mol% of the metal ions are Ca2+.

73. The composition of any one of claims 46-72, wherein the metal ion comprises Ba2+.

74. The composition of any one of claims 46-73, wherein at least 50 mol% of the metal ions are Ba2+.

75. The composition of any one of claims 46-74, wherein the nanofiber is a component of a hydrogel.

76. The composition of claim 75, wherein the steroid is present within the hydrogel at a concentration of at least 2.5 mM.

77. The composition of any one of claims 75 or 76, wherein the steroid is present within the hydrogel at a concentration of at least 8 mM.

78. The composition of any one of claims 75-76, wherein the steroid is present within the hydrogel at a concentration of at least 10 mM.

79. The composition of any one of claims 75-78, wherein the concentration of steroid within the hydrogel is at most 25 mM.

80. The composition of any one of claims 75-79, wherein the metal ions are present within the hydrogel at a concentration of at least 2.5 mM.

81. The composition of any one of claims 75-80, wherein the metal ions are present within the hydrogel at a concentration of at least 8 mM.

82. The composition of any one of claims 75-81, wherein the metal ions are present within the hydrogel at a concentration of at least 10 mM.

83. The composition of any one of claims 75-82, wherein the hydrogel further comprises a salt.

84. The composition of any one of claims 75-83, wherein the hydrogel further comprises an anesthetic.

85. The composition of claim 84, wherein the anesthetic comprises bupivacaine.

86. The composition of any one of claims 75-85, wherein the hydrogel comprises nanofibers.

87. The composition of any one of claims 75-86, wherein the hydrogel is shear-thinning.

88. The composition of any one of claims 75-87, wherein the hydrogel exhibits decreased viscosity when subjected to shear strain.

89. The composition of any one of claims 75-88, wherein the hydrogel is self-healing.

90. The composition of any one of claims 75-89, wherein the hydrogel is thixotropic.

91. A needle, comprising the composition of any one of claims 75-90.

92. A syringe, comprising the composition of any one of claims75-90.

93. An implant, comprising the composition of any one of claims 75-90.

94. A composition, comprising:

a hydrogel comprising a steroid and Ca2+ and/or Ba2+ metal ions, the steroid comprising a phosphate moiety and being present within the hydrogel at a concentration of at least 8 mM, and the metal ions being present within the hydrogel at a concentration of at least 8 mM.

A composition, comprising:

a nanofiber formed from a complex of (a) a steroid comprising a phosphate moiety, and (b) Ca2+ and/or Ba2+ metal ions, the steroid and the metal ions present within the nanofiber at a molar ratio of between about 2: 1 and about 1:2.