Poloxamer compositions with reduced sol-gel transition temperatures and methods of reducing the sol-gel transition temperature of poloxamer compositions
Inventors
Salamone, Joseph C. • McMahon, Rebecca Erin • Poleon, Suprena Emanuella Zariah • SALAMONE, ANN BEAL
Assignees
Rochal Industries LLC • Rochal Technologies LLC
Publication Number
US-12090205-B2
Publication Date
2024-09-17
Expiration Date
2039-10-28
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Abstract
The reduction in the sol-gel temperature of aqueous poloxamer surfactant compositions by the addition of hydrophobic vicinal diols is provided. Lowering of the sol-gel temperature and the gelling efficiency of water-soluble poloxamer block copolymers of polyethylene oxide-b-polypropylene oxide-b-polyethylene oxide has been markedly improved by the addition of small amounts of at least one hydrophobic vicinal diol, such as monoalkyl glycols, monoalkyl glycerols, or monoacyl glycerols. The decrease in the sol-gel temperature facilitates gel formation, and such gels exhibit greater residence time on a surface, particularly those with biological properties.
Core Innovation
The invention concerns the reduction of the sol-gel temperature in aqueous poloxamer surfactant compositions through the addition of hydrophobic vicinal diols, including monoalkyl glycols, monoalkyl glycerols, and monoacyl glycerols. By introducing small amounts of these hydrophobic vicinal diols, the sol-gel transition temperature of water-soluble poloxamer block copolymers of polyethylene oxide-b-polypropylene oxide-b-polyethylene oxide is significantly lowered. This facilitates gel formation and improves the gelling efficiency of the compositions.
The main problem addressed is the short residence time of topical formulations at the intended site of application, notably for delivery of active agents like wound-healing agents and drugs. Specifically, there is difficulty in maintaining sufficient retention of a formulation on biological surfaces to ensure effective localized treatment. The quick transformation back to a liquid phase or insufficient viscosity limits the extended presence of pharmaceutical or cosmetic agents at the site of action.
According to the patent, incorporating hydrophobic vicinal diols in concentrations ranging from 0.1 to 1.8 wt. % into poloxamer gel compositions lowers the sol-gel transition temperature by up to 12° C. These lowered transition temperatures make it easier for the gels to form and adhere to surfaces, particularly biological ones, thereby allowing for higher viscosity at lower temperatures and increased residence times. This approach also accommodates the addition of biologically active agents to the gel, ensuring proximity to the biological surface for extended periods.
Claims Coverage
There are two independent claims that establish the main inventive features of the patent.
Poloxamer gel composition comprising hydrophobic vicinal diol component
A poloxamer gel composition includes: - 0.05 to 5 wt. % hydrophobic vicinal diol component, - 17 to 46 wt. % of a poloxamer component selected from Poloxamer 407, Poloxamer 188, or their combination, - 0.5 wt. % or less of a water-soluble polymer other than poloxamer, - Hydrophobic vicinal diol component is 6-carbon to 16-carbon length monoalkyl glycols, 6-carbon to 16-carbon length monoalkyl glycerols, or their combination, - The monoalkyl group of the monoalkyl glycerols is 6-carbons to 16-carbons in length, - The hydrophobic vicinal diol component depresses the sol-gel temperature of an aqueous poloxamer equivalent by at least 1° C.
Method of lowering the sol-gel temperature of an aqueous poloxamer gel composition
A method of lowering the sol-gel temperature of an aqueous poloxamer gel composition by at least 3° C., comprising: - Adding 0.1 to 1.8 wt. % of a hydrophobic vicinal diol component to the aqueous poloxamer gel composition, - The poloxamer gel composition comprises 17 to 46 wt. % of a poloxamer component selected from Poloxamer 407, Poloxamer 188, or their combination, - The hydrophobic vicinal diol component comprises monoalkyl glycols, monoalkyl glycerols, or a combination thereof.
The inventive features cover specific compositions of poloxamer gels containing defined amounts of hydrophobic vicinal diols to lower sol-gel temperatures, as well as methods for achieving this effect, enabling improved gel formation and performance.
Stated Advantages
Addition of hydrophobic vicinal diols lowers the sol-gel temperature of poloxamer compositions, facilitating gel formation at lower temperatures.
Lower sol-gel transition temperatures result in higher viscosity compositions that allow for greater residence time on surfaces, especially biological surfaces.
The formulations enable extended proximity of active agents, such as pharmaceuticals or wound-healing compounds, to biological surfaces for more effective treatment.
The approach enables formation of stable gels with a variety of biologically active or therapeutic agents included.
Documented Applications
Topical biomaterials for sustained release of active pharmaceutical agents, aiding in therapeutic delivery with extended residence time.
Wound treatment compositions for enhanced wound healing, including the delivery of wound antimicrobial agents and wound debriding agents.
Delivery systems for biologically active agents such as antibiotics, antifungal agents, antiviral agents, anti-acne agents, anticlotting agents, anti-inflammatory agents, and moisturizers.
Formulations for use as topical applications in forms like liquids, creams, foams, lotions, gels, and aerosols, or imbibed by swabs, cloth, sponges, foams, dressing materials, and wipes.
Treatment of microbial biofilms on patient or inanimate surfaces using gelled poloxamer compositions containing antimicrobial agents and/or APIs.
Inclusion of UV absorbing agents such as avobenzene and zinc oxide for potential sunscreen or sunburn treatment formulations.
Use in compositions for analgesics, anti-itch, anti-burn, chelating, and enzymatic agents as documented in example formulations.
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