Topical pharmaceutical bases for treating skin conditions

Abstract

The present disclosure refers to topical pharmaceutical bases that possess scar healing properties. Further, these topical pharmaceutical bases are proposed for treating skin conditions, such as, for example keloids, hypertrophic scars, wounds, and burns, among others. The topical pharmaceutical bases include Amazonian oils and resins, such as pracaxi oil and breu-branco resin. The synergistic effect of pracaxi oil combined with breu-branco resin results in a highly effective scar and wound treatment. Suitable active pharmaceutical ingredients (APIs) can be incorporated to the topical pharmaceutical bases to formulate topical pharmaceutical compositions, which improve healing effects. The synergistic effect provided by the combination of pracaxi oil and breu-branco resin enables lower dosage requirements of the associated APIs when topical pharmaceutical compositions are employed for treating skin conditions.

Claims

1. A topical pharmaceutical composition comprising: about 1% w/w to about 95% w/w pracaxi oil, a synergistically effective amount of breu-branco resin, and a pharmaceutically effective amount of at least one active pharmaceutical ingredient.

2. The topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition comprises about 5% w/w to about 50% w/w breu-branco resin.

3. The topical pharmaceutical composition of claim 2, wherein the topical pharmaceutical composition comprises about 10% w/w to about 20% w/w pracaxi oil.

4. The topical pharmaceutical composition of claim 2, wherein the topical pharmaceutical composition comprises about 10% w/w breu-branco resin.

5. The topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition further comprises at least one natural component selected from the group consisting of buriti oil, copaiba balsam, bacaba oil, acai oil, ojon oil, andiroba oil, murumuru butter, and tucuma oil.

6. The topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition further comprises at least one natural component selected from the group consisting of about 1% w/w to about 20% w/w buriti oil, about 1% w/w to about 20% w/w copaiba balsam, about 1% w/w to about 20% w/w bacaba oil, about 1% w/w to about 20% w/w acai oil, about 1% w/w to about 20% w/w ojon oil, about 1% w/w to about 20% w/w andiroba oil, about 1% w/w to about 20% w/w murumuru butter, and about 1% w/w to about 20% w/w tucuma oil.

7. The topical pharmaceutical composition of claim 3, wherein the topical pharmaceutical composition further comprises at least one natural component selected from the group consisting of about 1% w/w to about 20% w/w buriti oil, about 1% w/w to about 20% w/w copaiba balsam, about 1% w/w to about 20% w/w bacaba oil, about 1% w/w to about 20% w/w acai oil, about 1% w/w to about 20% w/w ojon oil, about 1% w/w to about 20% w/w andiroba oil, about 1% w/w to about 20% w/w murumuru butter, and about 1% w/w to about 20% w/w tucuma oil.

8. The topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition further comprises at least one natural component selected from the group consisting of about 5% w/w buriti oil, about 5% w/w copaiba balsam, about 5% w/w bacaba oil, about 5% w/w acai oil, about 5% w/w ojon oil, about 5% w/w andiroba oil, about 5% w/w murumuru butter, and about 5% w/w tucuma oil.

9. The topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition is selected from the group consisting of a pharmaceutically acceptable liquid, a cream, an oil, a lotion, an ointment, a gel, a roll-on liquid, a skin patch, a spray, and a synthetic polymer dressing.

Description

DETAILED DESCRIPTION

(1) The present disclosure is here described in detail with reference to embodiments. Other embodiments may be used and/or other changes may be made without departing from the spirit or scope of the present disclosure. The illustrative embodiments described in the detailed description are not meant to be limiting of the subject matter presented herein.

Definitions

(2) As used here, the following terms have the following definitions:

(3) Abnormal scar refers to the over-expression of collagen at a wound site or in a scar, leaving an unaesthetic mark. Abnormal scars may include keloids and hypertrophic scars, among others.

(4) Active Pharmaceutical Ingredients (APIs) refer to chemical compounds that induce a desired effect, and include agents that are therapeutically effective, prophylactically effective, or cosmeceutical effective.

(5) Excessive scarring refers to a process that result from an imbalance in the anabolic and catabolic wound healing processes, causing overgrowth of dense fibrous tissue and which bring about one or more abnormal scars. Excessive scarring is characterized by overproduction of cells, collagen, and/or proteoglycan.

(6) Hypertrophic scars refer to abnormal scars in which dense fibrous tissue does not extend beyond borders of an original wound or incision, and which tend to be wider than necessary for normal wound healing to occur.

(7) Keloids refer to abnormal scars resulting from benign fibrous growths that occur after trauma or wounding of the skin, which extend beyond original areas of skin injury, and which tend to remain elevated.

(8) Oil refers to a vegetable substance that may be clear, odorless, viscous, hydrophobic, liquid or liquefiable at room temperature. Oils are widely used in cosmetics due to its hypoallergenic and non-comedogenic properties.

(9) Patient refers to warm-blooded animals, such as mammals, for example, humans, who are in need of treatment.

(10) Resin refers to a hydrocarbon secretion of many plants, which possesses valuable chemical properties.

(11) Therapeutically effective amount refers to the amount of subject compound that will elicit the biological or medical response of a tissue, system, animal or human that is being sought.

(12) Treating and Treatment refers to reduction in severity and/or frequency of symptoms, elimination of symptoms and/or underlying cause, prevention of the occurrence of symptoms and/or their underlying cause, and improvement or remediation of damage.

DESCRIPTION OF THE DISCLOSURE

(13) The present disclosure refers to topical pharmaceutical bases that possess scar healing properties. Further, these topical pharmaceutical bases are proposed for treating skin conditions. In some embodiments, skin conditions include keloids, hypertrophic scars, wounds, and burns, among others.

Formulation

(14) In some embodiments, the topical pharmaceutical bases include natural components from the Amazon forest. In these embodiments, the topical pharmaceutical bases include pracaxi oil and breu-branco resin. Further to these embodiments, aforementioned natural components exhibit moisturizing, antimicrobial, and healing properties.

(15) In an example, the topical pharmaceutical bases include: pracaxi oil in a concentration from about 1% w/w to 20% w/w, preferably from about 5% to 10% w/w; and breu-branco in a concentration from about 1% w/w to 20% w/w, preferably from about 5% w/w to 10% w/w.

(16) Pracaxi Oil

(17) Pracaxi oil is obtained from the seed oil of the Pentaclethara macroloba tree, or pracaxi tree. The pracaxi tree is a deciduous tree from the legumes family, growing in altitudes below 600 meters in many parts of northern Brazil, Guyana, Trinidad, and parts of Central America, and may reach between about 8 and about 35 meters in height. Pracaxi trees may sometimes be found in wetlands, and are resistant to water logging.

(18) Pracaxi seeds include from about 45% to 48% fat, about 27% to 28% protein, and about 12% to 14% carbohydrates (see Table 1). Pracaxi seed oil includes the highest known natural concentration of behenic acid (about 20%) in a vegetable fat, more than six times higher than in peanut oil, and also includes about 35% of oleic acid. In some cases, pracaxi seed oil may include greater percentages of the aforementioned behenic acid and oleic acid. The oleic acid and lauric acid, contained within pracaxi oil are effective vehicles for delivering drugs through the skin.

(19) TABLE-US-00001 TABLE 1 General composition of pracaxi oil. Components Composition % Fat 45-48 Protein 27-28 Carbohydrates 12-14

(20) In an example, the fatty acid composition of the pracaxi oil is illustrated below in Table 2. Compositions vary depending on the region and conditions in which the pracaxi tree grows.

(21) TABLE-US-00002 TABLE 2 Fatty acid composition of the pracaxi oil. Fatty Acids Carbon Atoms Composition % Lauric 12:00 1.30 Myristic 14:00 1.21 Palmitic 16:00 2.04 Stearic 18:00 2.14 Oleic 18:10 44.32 Linoleic 18:20 1.96 Linolenic 18:30 2.31 Behenic 22:00 9.67 Lignoceric 24:00 14.81

(22) TABLE-US-00003 TABLE 3 Specifications of the pracaxi oil. Indicators Reference Value Texture Solid below 18.5 C., liquid viscous texture above this temperature Color Translucent yellow, yellowish-white when solid Odor Almost odorless Melting point 18.5 C. Refractive index (40 C.) 1.4690 Iodine value 65-70 g I2/100 g Saponification value 170-180 mg kOH/g Acid value 3-5 mg KOH/g Peroxide value 5-10 mEQ/kg Density (25) 0.917 g/cm.sup.3

(23) Pracaxi oil has been widely employed within pharmaceutical compositions because of its cosmetic, therapeutic, and medicinal properties. Pracaxi oil is rich in organic acids with antioxidant, antibacterial, antiviral, antiseptic, antifungal, anti-parasitic, and anti-hemorrhagic properties. Because pracaxi oil possesses many of the aforementioned properties, pracaxi oil can be suitable oil for helping in the treatment of wounds and scars.

(24) Pracaxi oil has a high amount of solid matter, not fatty acids, which makes pracaxi oil solidifies in cooler temperatures. The solid matter has gentle moisturizing and high cellular renewal promoting properties. It includes vitamin E, and has essential fatty acids, which makes pracaxi oil suitable for topical pharmaceutical compositions.

(25) Breu-Branco Resin

(26) Breu-branco resin (Protium heptaphyllum, Burseraceae) is extracted from an Amazon jungle tree called Almcega. Almcega is a tree that grows in dry forests and is native to most of Brazil. The Almcega trees give off an aromatic fragrance and have a dark red bark. Additionally, Almcega trees grow from about 10 to 20 meters in height, and from about 50 to 60 centimeters in diameter at the base.

(27) When a cut is made in the trunk of Almcega trees, the breu-branco resin exudes. This resin has a white-green color and a very pleasant fragrant aroma. Additionally, the breu-branco resin hardens when coming in contact with air. In several areas of Brazil, the resin is collected from the trunk of Almcega trees, and then ground manually after it hardens. Typically, breu-branco resin is collected year round, but especially in the summer season. After the resin is collected, the resin is dried in the shade and then stored in sacks made of fibers, such as jute. Cuts on an Almcega tree to extract the resin are first made when the tree is about 8 to 10 years old. To harvest the resin of this species sustainably, it is recommended that each Almcega tree receives only about 2 to about 3 cuts per year.

(28) Additionally, yields vary according to the process of extraction. For example, the process of hydro-distillation yields about 11% resin, whereas steam distillation yields about 2.5% resin. The general composition of the resin of breu-branco is provided in Table 4, while the monoterpene composition within the resin of breu-branco is provided in Table 5.

(29) TABLE-US-00004 TABLE 4 Composition of Breu-Branco Resin. Ingredients Composition % Resinic acids 60-75 Terpenes 10-15 Various substances/water 5-10

(30) TABLE-US-00005 TABLE 5 Composition of Breu-Branco Resin Monoterpene. Monoterpenes Composition % -pyrene 10.50 Limonene 16.90 -phellandrene 16.70 Terpinolene 28.50 Others 27.40

(31) Breu-branco resin is often used in Amazonian regions for treating some physical conditions. Breu-branco resin is aromatic and rich in triterpenes , amyrins, which possess analgesic and anti-inflammatory properties. In traditional medicine, the resin of breu-branco is suggested for asthma, bronchitis, coughs, headaches stomach aches, liver disorders, memory loss, concentration, motor coordination, for soothing states of agitation and stress, as an anti-inflammatory and analgesic, for wound healing, and as a stimulating agent, among others. Due to breu-branco resin's aromatic properties, it is widely used in perfumes and toiletries as well as in soap manufacturing.

(32) In other embodiments, the topical pharmaceutical bases include one or more natural components, such as, for example buriti oil, copaiba balsam, bacaba oil, acai oil, ojon oil, andiroba oil, murumuru butter, and/or tucuma oil, among others. In these embodiments, aforementioned natural components improve skin penetration as well as healing properties. Further to these embodiments, the concentration of each natural component within topical pharmaceutical bases is from about 1% w/w to 20% w/w, preferably about 5% w/w.

(33) In further embodiments, active pharmaceutical ingredients (APIs) are incorporated into the topical pharmaceutical bases to formulate topical pharmaceutical compositions. In these embodiments, the topical pharmaceutical compositions are proposed for treating skin conditions, such as, for example keloids, hypertrophic scars, wounds, and burns, among others.

Administration

(34) In some embodiments, the topical pharmaceutical bases are in a dosage form selected from the group consisting of: pharmaceutically acceptable liquids, creams, oils, lotions, ointments, gels, roll-on liquids, skin patches, sprays, glass bead wound dressings, and synthetic polymer dressings, among others.

(35) In some embodiments, the topical pharmaceutical bases are directly administered onto the affected area. In these embodiments, suitable applicators are employed to administer the topical pharmaceutical bases. In an example, suitable applicators include a swab, brush, cloth, pad, and sponge, among others.

(36) In some embodiments, when the topical pharmaceutical bases are applied onto the affected area, the topical pharmaceutical bases deliver a therapeutically effective amount of fatty acids including behenic acid, triterpenes , amyrins, and other aforementioned components, which help in the treatment of wounds and scars. In these embodiments, the synergistic effect of pracaxi oil combined with breu-branco resin within the topical pharmaceutical bases results in a highly effective healing topical formulation, especially for wounds and excessive scarring. Further to these embodiments, the synergistic effect of the combination of pracaxi oil and breu-branco resin enables lower dosage requirements of the associated APIs when topical pharmaceutical compositions are employed for treating skin conditions.

(37) In some embodiments, various additives are included to facilitate the preparation of suitable dosage forms. For example, additives include gelling agents, thickening agents, pH adjusters, preservatives, colors, stabilizing agents, antioxidants, and surfactants, among others.

(38) While various aspects and embodiments have been disclosed, other aspects and embodiments are contemplated. The various aspects and embodiments disclosed are for purposes of illustration and are not intended to be limiting, with the true scope and spirit being indicated by the following claims.