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US 2002/0153508 A1Published application
Cubic liquid crystalline compositions and methods for their preparation
OwnerMatthew Lawrence Lynch, Patrick Thomas Spicerinventors
Life of this patent
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Abstract
Cubic liquid crystalline gel precursors, bulk cubic liquid crystalline gels, and dispersions of cubic liquid crystalline gel particles, and methods for their preparation, are disclosed. The precursors, gels, and dispersions can be used as skin penetration enhancers. The precursors, gels, and dispersions are prepared by methods employing hydrotropes that do not detrimentally affect the cubic liquid crystalline structure of the gels and particles.
Claims49
A cubic gel precursor comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase, and optionally
- (C) a solvent,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c≧0;
- and with the proviso that a, b, and c do not fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C).
4 more elements
A bulk cubic liquid crystalline gel comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase, and
- (C) a solvent,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c>0;
- and with the proviso that a, b, and c fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C).
4 more elements
A dispersion comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase, and
- (C) a solvent,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c>0;
- and with the proviso that a, b, and c fall within a region representing cubic liquid crystalline phase in combination with at least one other phase on a phase diagram representing phase behavior of ingredients (A), (B), and (C), with the proviso that the dispersion is formed as cubic liquid crystalline gel particulates dispersed in the other phase.
4 more elements
Cubic liquid crystalline gel particles comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase,
- (C) a solvent, and
- (D) a stabilizer,
- wherein ingredients (A), (B), and (C) are present in relative mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c>0;
- and with the provisos that a, b, and c fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C), and that ingredients (A), (B), and (C) have a particulate form.
5 more elements
A method for preparing a cubic gel precursor comprising the steps of:
- 1) combining (A) a hydrotrope with (B) an amphiphile capable of forming a cubic liquid crystalline phase, and
- 2) optionally adding (C) a solvent,
- wherein ingredients (A), (B), and (C) are combined in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c≧0;
- and with the proviso that a, b, and c do not fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C), and with the proviso that amounts of each ingredient in the composition are such that cubic phase gel forms upon occurrence of a stimulus.
3 more elements
A method for preparing a cubic liquid crystalline gel composition comprising the steps of:
- 1) combining in a composition, ingredients comprising (A) a hydrotrope and (B) an amphiphile capable of forming a cubic liquid crystalline phase, and
- 2) mixing the product of step 1) with (C) a solvent,
- wherein ingredients (A), (B), and (C) are combined in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c>0;
- and with the proviso that a, b, and c fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C).
3 more elements
A method for preparing a dispersion of cubic gel particles directly from a precursor comprising the steps of:
- 1) dispersing a cubic gel precursor comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase, and optionally
- (C) a solvent,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c≧0;
- and with the proviso that a, b, and c do not fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C)
- wherein dispersing is carried out by a method selected from the group consisting of
- a) dispersing the precursor in additional (C) solvent, and
- b) dispersing additional (C) solvent in the precursor, and thereafter diluting.
8 more elements
A method for preparing a dispersion of cubic liquid crystalline gel particles comprising fragmenting a bulk cubic liquid crystalline gel comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase, and
- (C) a solvent,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c>0;
- and with the proviso that a, b, and c fall within a cubic liquid crystalline phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C).
4 more elements
A method for preparing dispersions of cubic liquid crystalline gel particles comprising the steps of:
- 1) heating (B) a solid amphiphile capable of forming a cubic liquid crystalline phase to a temperature greater than or equal to its melting point,
- 2) combining the product of step 1) with (A) a hydrotrope,
- 3) adding (C) water,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c≧0;
- and with the proviso that a, b, and c fall within an isotropic liquid phase region on a phase diagram representing phase behavior of ingredients (A), (B), and (C)
- 4) forming a dispersion by a route selected from the group consisting of
- i) dispersing the product of step 3) into (C) the water, and thereafter stabilizing;
- ii) spraying the isotropic liquid into a humid environment, diluting with sufficient water to form a colloidally unstable dispersion of cubic gel particles, and thereafter stabilizing;
- iii) diluting the isotropic liquid with sufficient water to form an interfacially stabilized emulsion phase, sterically stabilizing said emulsion phase, and thereafter, further diluting with additional water;
- and
- iv) dispersing water into the isotropic liquid, further diluting with sufficient water to form an unstable particle dispersion, and thereafter stabilizing.
10 more elements
A method for manufacturing a cubic liquid crystalline phase material comprising the steps of:
- 1) preparing a precursor comprising
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase, and optionally
- (C) a solvent,
- wherein ingredients (A), (B), and (C) are present in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c≧0;
- and with the proviso that a, b, and c fall at a starting point on a phase trajectory within an isotropic liquid region on a phase diagram representing phase behavior of ingredients (A), (B), and (C);
- 2) diluting the product of step 1) with ingredient (C) until an end point is reached on the phase trajectory, wherein the end point lies on a tie line between the isotropic liquid region and a cubic phase containing region on the phase diagram.
6 more elements
A method for delivering an active ingredient to a substrate comprising:
- 1) preparing a cubic gel precursor comprising:
- (A) a hydrotrope,
- (B) an amphiphile capable of forming a cubic liquid crystalline phase,
- (C) a solvent, and
- (D) an active ingredient,
- wherein ingredients (A), (B), and (C) are combined in mass fractions relative to each other such that
- 1.0=a+b+c
- wherein a is the mass fraction of ingredient (A), b is the mass fraction of ingredient (B), and c is the mass fraction of ingredient (C), and wherein 1.0>a>0, 1.0>b>0, 1.0>c≧0;
- and with the proviso that a, b, and c fall within an isotropic liquid region on a phase diagram representing phase behavior of ingredients (A), (B), and (C), and with the proviso that amounts of each ingredient in the composition are such that cubic phase gel forms upon occurrence of a stimulus;
- and
- 2) spraying the precursor onto a substrate.
8 more elements
Dependencies are inferred from the claim text.