Topical formulations having enhanced bioavailability
Inventors
McCook, John Patrick • Persaud, Indushekhar • Narain, Niven Rajin
Assignees
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Publication Number
US-10588859-B2
Publication Date
2020-03-17
Expiration Date
Abstract
The present disclosure provides compositions suitable for delivering lipophilic bioactive agents. The compositions may be utilized to treat numerous diseases and conditions that would benefit from the application of a lipophilic bioactive agent.
Core Innovation
The invention relates to topical/transdermal delivery compositions in which Coenzyme Q10 is formulated in a liposomal concentrate combined with a pharmaceutically acceptable carrier that includes a permeation enhancer comprising ethoxydiglycol. The liposomal concentrate includes a phospholipid selected from a defined group, Coenzyme Q10, and at least one solubilizer, and the overall composition fixes ethoxydiglycol and Coenzyme Q10 by weight within specified ranges.
The compositions emphasize a two-phase liposome formation approach, with a first phase of lipophilic bioactive including Coenzyme Q10 with a solubilizer and a second phase containing phospholipid. The formulation further supports topical/transdermal delivery by including permeation enhancers, with ethoxydiglycol described as especially relevant, and embodiments that report enhanced topical bioavailability and skin penetration at lower ethoxydiglycol amounts.
In addition, the document describes multi-phase topical carriers that may include oil phase, water phase, neutralization/buffer phase, and pigment phase components such as TiO2. The disclosure includes stability testing assertions and skin penetration data comparing ethoxydiglycol-containing creams versus controls and reporting measurable epidermal CoQ10 and statistically significant penetration differences.
The document also provides example embodiments for a CoQ10 liposomal concentrate using specific components including polysorbate 80 as a solubilizer with PHOSPHOLIPON 85G as the phospholipid, and cream formulations at multiple CoQ10 levels, along with quantitative skin penetration outcomes and additional performance and stability testing assertions.
Claims Coverage
The independent claim coverage is based on one independent claim. It defines an ethoxydiglycol-containing permeation-enhancer carrier combined with a liposomal concentrate that includes specified phospholipid options, Coenzyme Q10, and at least one solubilizer, with fixed ethoxydiglycol and Coenzyme Q10 weight ranges.
Ethoxydiglycol permeation-enhancer carrier with liposomal concentrate for Coenzyme Q10
A composition comprising a liposomal concentrate in combination with at least one pharmaceutically acceptable carrier possessing at least one permeation enhancer that comprises ethoxydiglycol, wherein the composition comprises ethoxydiglycol in an amount from about 4% by weight to about 6% by weight and Coenzyme Q10 in an amount from about 3% to about 3.3% by weight.
Liposomal concentrate with defined phospholipid class plus solubilizer
A liposomal concentrate wherein the liposomal concentrate comprises a phospholipid selected from the group consisting of lecithin, lysolecithin, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, phosphatidylglycerol, phosphatidic acid, phosphatidylserine, lysophosphatidylcholine, lysophosphatidylethanolamine, lysophosphatidylglycerol, lysophosphatidic acid, lysophosphatidylserine, PEG-phosphatidylethanolamine, PVP-phosphatidylethanolamine, and combinations thereof; Coenzyme Q10; and at least one solubilizer.
Overall, the independent claim ties together a liposomal concentrate with a pharmaceutically acceptable carrier that contains a permeation enhancer comprising ethoxydiglycol, while fixing the ethoxydiglycol and Coenzyme Q10 amounts to specific weight ranges.
Stated Advantages
Enhanced topical bioavailability and skin penetration of Coenzyme Q10 is asserted, including findings that lower ethoxydiglycol amounts can enhance skin penetration.
Documented Applications
Topical/transdermal delivery compositions for lipophilic bioactives, notably Coenzyme Q10, including creams and lotions with optional multi-phase carriers and permeation enhancers.
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