WO2021048868A1 - A drug delivery carrier composition for brain disorders - Google Patents
A drug delivery carrier composition for brain disorders Download PDFInfo
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- WO2021048868A1 WO2021048868A1 PCT/IN2020/050175 IN2020050175W WO2021048868A1 WO 2021048868 A1 WO2021048868 A1 WO 2021048868A1 IN 2020050175 W IN2020050175 W IN 2020050175W WO 2021048868 A1 WO2021048868 A1 WO 2021048868A1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
- A61K47/544—Phospholipids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6905—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
- A61K47/6907—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a microemulsion, nanoemulsion or micelle
- A61K47/6909—Micelles formed by phospholipids
Definitions
- the present disclosure generally relates to the field of pharmaceutical compositions, and more particularly relates to the development of an effective drug delivery carrier composition with proven pharmacological activities for crossing blood-brain barriers and to treat numerous types of brain disorders.
- Brain disorders are one of the most prevalent identified disorders in a developed society. The food habits, lack of exercises, both physiological and psychological stress, lack of appropriate sleep, hormonal imbalance, infection, urbanized environmental change, and genetic disorders lead to overwhelming anarchy of brain function.
- the blood-brain barrier is a highly selective semipermeable border that separates the circulating blood from the brain and extracellular fluid in the central nervous system (CNS).
- the blood-brain barrier is formed by endothelial cells of the capillary wall, astrocyte end-feet ensheathing the capillary, and pericytes embedded in the capillary basement membrane. These cellular layers selectively permit the molecules into the brain to protect the neural milieu from foreign antigens and other toxic substances. But, due to the BBB selective permeability function in transporting the molecules, the physicians face the greatest challenge to target the drug during the brain diseased condition.
- the poly unsaturated fatty acids are the long chain hydrocarbon fatty acids contain a carboxylic group and multiple double bonds in the carbon chain. Based on the double position in the hydrocarbon chain the PUFA are classified into two categories those are omega 3 and omega 6 PUFAs. In the omega 3 PUFA, the double bond starts from the 3 rd position from the last carbon (omega) of hydrocarbon chain and continues towards the carboxylic end by leaving one methyl group between two double bonds.
- Drug carriers are primarily used to control the release of a drug into systemic circulation and can be accomplished either by slow release of the drug over a long period of time (typically diffusion) or by triggered release at the drug's target by some stimulus, such as changes in pH, application of heat, and activation by light.
- the drug carriers are also used to improve the pharmacokinetic properties, specifically the bioavailability, of many drugs with poor water solubility and/or membrane permeability.
- an antibody mimic conjugates are formulated with liposomes comprising folic acid to form a capsule.
- the pharmaceutical capsule comprises a suspension of polymeric microcapsules and polyunsaturated fatty acids of alkyl esters that belong to the omega-3 series, eicosapentaenoic acid, docosahexaenoic acid, and/or mixtures thereof.
- the capsule also comprises pharmaceutically acceptable salts i.e., sodium or potassium salts of salicylic acid and phosphoric acid thereby allowing the capsule to cross the blood-brain barrier.
- the capsule provides an effective outcome that helps in preventing cancer or infectious diseases. But, as the capsule is formulated by integrating with numerous acids to cross blood-brain barriers which lead to increase dosage limit of drug, poor solubility of the drug, expensive while preparing, and thereof.
- the primary objective of the invention is to provide a novel and effective drug delivery carrier composition with proven pharmacological activities.
- Another objective of the invention is to provide a carrier which can cross the blood-brain barrier (BBB) with ease for treating numerous brain disorders.
- BBB blood-brain barrier
- Further objective of the invention is to provide a composition which is useful in treating brain disorders such as neurodegenerative disorders, brain hemorrhages, bruising of brain tissue cerebral edema, or swelling inside the skull, concussions strokes and disorders due to brain tumors.
- brain disorders such as neurodegenerative disorders, brain hemorrhages, bruising of brain tissue cerebral edema, or swelling inside the skull, concussions strokes and disorders due to brain tumors.
- Yet another objective of the invention is to provide a carrier that alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
- Further objective of the invention is to provide a cost-effective drug without harmful side effects and enhance patient compliance.
- the invention relates to an effective drug delivery carrier composition with proven pharmacological activities for crossing blood-brain barriers and to treat numerous types of brain disorders.
- the lipidomer carrier composition is formulated by mixing equal proportions of compounds i.e., ranges from 0.001M to 1M of spingosine conjugated with ranges from 0.001M to 1M of salicylic acid mediated by ranges from 0.001M to 1M of phosphoric acid and ranges from 0.001M to 1M of poly unsaturated fatty acids, a biologically active compound, and ranges from 0.001M to 1M of folic acid added to the active compound.
- compounds i.e., ranges from 0.001M to 1M of spingosine conjugated with ranges from 0.001M to 1M of salicylic acid mediated by ranges from 0.001M to 1M of phosphoric acid and ranges from 0.001M to 1M of poly unsaturated fatty acids, a biologically active compound, and ranges from 0.001M to 1M of folic acid added to the active compound.
- the poly unsaturated fatty acids such as Arachidonic acid (AA), Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA) and the like that are used individually or the combination of selected fatty acids.
- AA Arachidonic acid
- DHA Docosahexaenoic acid
- EPA Eicosapentaenoic acid
- the Arachidonic acid used in this carrier molecule goes through the anti inflammatory pathway mediated by enzymes Lipoxygenases, co-factor salicylic acid and folic acid thereby soothing the inflammation produced due to various reasons.
- the lipidomer carrier itself alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
- the lipidomer carrier further contains the biologically active compound encapsulated with folic acid optionally as a suspension along with the spingosine, the salicylic acid, the phosphoric acid, and the poly unsaturated fatty acids.
- the structure of lipidomer carrier along with folic acid is represented by formula 2, Formula 2
- the lipidomer carrier composition is formulated by mixing equal proportions of compounds i.e., ranges from 0.001M to 1M of spingosine conjugated with ranges from 0.001M to 1M of salicylic acid mediated by ranges from 0.001M to 1M of phosphoric acid and ranges from 0.001M to 1M of poly unsaturated fatty acids.
- the poly unsaturated fatty acids may be selected from group of Arachidonic acid (AA), Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA) and the like that are used individually or the combination of selected fatty acids.
- the lipidomer carrier itself alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
- Inflammation is the innate immune response of the host body essential in neutralizing the pathogen. It is the first line of defense mechanism against foreign invading organisms.
- the proposed carrier composed of polyunsaturated fatty acid, salicylic acid, mediated by spingosine and phosphoric acid controls the onset of inflammation.
- the Arachidonic acid used in this carrier molecule goes through the anti-inflammatory pathway mediated by enzymes Lipoxygenases, co factor salicylic acid and folic acid.
- the anti-inflammatory molecules like LipoxinA4, resolvins, and protectins are produced when Lipoxygenases enzymes act upon the arachidonic acid thereby soothing the inflammation produced due to various reasons.
- a novel and effective drug carrier composition with proven pharmacological activities which can cross the blood-brain barrier (BBB) with ease for treating numerous brain disorders.
- BBB blood-brain barrier
- the composition helps in treating brain disorders such as neurodegenerative disorders, brain hemorrhages, bruising of brain tissue cerebral edema, or swelling inside the skull, concussions strokes and disorders due to brain tumors.
- the drug formulated is cost-effective without harmful side effects and enhance patient compliance.
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Abstract
The present disclosure provides a novel and effective drug delivery lipidomer carrier composition with proven pharmacological activities. Such a carrier composition has the ability to cross the blood‐brain barrier (BBB) with ease for treating numerous brain disorders. The formulation of carrier composition comprises of a spingosine, a salicylic acid, a phosphoric acid, a poly unsaturated fatty acids and a biologically active compound. Specifically, the suitable oral dosage form of a targeted drug is formulated and incorporated in the carrier with a synergistic effect for the treatment of multiple brain disorders. The carrier itself alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
Description
TITLE OF THE INVENTION:
A Drug Delivery Carrier Composition for Brain Disorders
The following specification particularly describes the invention and the manner in which it is to be performed:
4. DESCRIPTION:
Field of the invention:
[0001] The present disclosure generally relates to the field of pharmaceutical compositions, and more particularly relates to the development of an effective drug delivery carrier composition with proven pharmacological activities for crossing blood-brain barriers and to treat numerous types of brain disorders.
Background of the invention:
[0002] Brain disorders are one of the most prevalent identified disorders in a developed society. The food habits, lack of exercises, both physiological and psychological stress, lack of appropriate sleep, hormonal imbalance, infection, urbanized environmental change, and genetic disorders lead to overwhelming anarchy of brain function.
[0003] The brain is considered as a privileged center of the body separated by the blood-brain barrier (BBB), which is an important protective barrier between the brain and systemic circulation thereby permitting the brain to correspond to the rest of the body. Nevertheless, blood-borne infections of the brain or neuronal metabolic or genetic aberrations that occurred are often difficult to treat. The innate or humoral immunity are either hopeless to attenuate the dire conditions. The cellular or humoral mediated immune system unable to cross the blood brain barrier to abrogate the infection or the inflammatory state in the brain. However, the brain contains its own defensive cells termed microglia cells originated from the mesoderm acts like a macrophages in closed central nervous system. These Glial cells respond to any infection or abnormal condition in the brain by releasing the cytokines and trying to remove the infection or soothe the diseased state. In due course of action the released cytokines are pro-inflammatory in nature which even damages its own neuronal cells and leads to dreadful disorders like Alzheimer's, Parkinson, autism, cerebral lupus, encephalitis, Guillain-Barre syndrome, Tourette Syndrome, and other traumatic brain syndromes. Hence the action of glial cells in the brain makes the scenario worse than ever by increasing the inflammation in the brain. As antibodies are too large to cross the blood-brain barrier, only certain antibiotics can pass. In some cases, a drug has
to be administered directly, where it can enter the brain by crossing the blood-cerebrospinal fluid barrier.
[0004] The blood-brain barrier (BBB) is a highly selective semipermeable border that separates the circulating blood from the brain and extracellular fluid in the central nervous system (CNS). The blood-brain barrier is formed by endothelial cells of the capillary wall, astrocyte end-feet ensheathing the capillary, and pericytes embedded in the capillary basement membrane. These cellular layers selectively permit the molecules into the brain to protect the neural milieu from foreign antigens and other toxic substances. But, due to the BBB selective permeability function in transporting the molecules, the physicians face the greatest challenge to target the drug during the brain diseased condition.
[0005] The poly unsaturated fatty acids (PUFA) are the long chain hydrocarbon fatty acids contain a carboxylic group and multiple double bonds in the carbon chain. Based on the double position in the hydrocarbon chain the PUFA are classified into two categories those are omega 3 and omega 6 PUFAs. In the omega 3 PUFA, the double bond starts from the 3rd position from the last carbon (omega) of hydrocarbon chain and continues towards the carboxylic end by leaving one methyl group between two double bonds. The omega 3 fatty acids are eicosa-penta-enoic acid (EPA - 20:5), docosa-penta-enoic acid (DPA - 22:5), docosa-hexa-enoic acid (DHA - 22:6), and alpha Linolenic acid (ALA - 18:3). The products of omega 3 fatty acid are anti-inflammatory in nature. The other kind of PUFAs are n6 poly unsaturated fatty acids. They are gamma Linolenic acid (GLA - 18:3) and arachidonic acid (AA - 20:4). The cyclo-oxygenases (COX) products of n6 PUFA are pro-inflammatory in nature. And the Lipoxygenases (LOX) products of n6 PUFA are anti inflammatory in nature. The arachidonic acid is the precursor for both COX and LOX enzymes. The fate of arachidonic acid to evolve as a pro-inflammatory or anti-inflammatory is driven by various co-factors like Zn+2, folic acid, salicylic acid, pantothenic acid, cobalamine and other vitamin derivatives.
[0006] A drug carrier is any substrate used in the process of drug delivery which serves to improve the selectivity, effectiveness, and/or safety of drug administration. Drug carriers are primarily used to control the release of a drug into systemic circulation and can be accomplished either by slow release of the drug over a long period of time (typically diffusion) or by triggered release at the drug's target by some stimulus, such as changes in pH, application of heat, and activation by light. The drug carriers are also used to improve the pharmacokinetic properties, specifically the bioavailability, of many drugs with poor water solubility and/or membrane permeability.
[0007] Conventionally, an antibody mimic conjugates are formulated with liposomes comprising folic acid to form a capsule. The pharmaceutical capsule comprises a suspension of polymeric microcapsules and polyunsaturated fatty acids of alkyl esters that belong to the omega-3 series, eicosapentaenoic acid, docosahexaenoic acid, and/or mixtures thereof. The capsule also comprises pharmaceutically acceptable salts i.e., sodium or potassium salts of salicylic acid and phosphoric acid thereby allowing the capsule to cross the blood-brain barrier. The capsule provides an effective outcome that helps in preventing cancer or infectious diseases. But, as the capsule is formulated by integrating with numerous acids to cross blood-brain barriers which lead to increase dosage limit of drug, poor solubility of the drug, expensive while preparing, and thereof.
[0008] In updated technology, various compositions are formulated to cross blood-brain barriers for treating numerous brain disorders such as neurodegenerative disorders like Alzheimer's, Parkinson's, Huntington's disease ALS, mental disorders like depression Anxiety, bipolar disorder, post-traumatic stress disorder, brain hemorrhages like hematomas, blood clots, contusions, or bruising of brain tissue cerebral edema, disorders due to brain tumors either malignant or benign and thereof. But, existing compositions are only able to cross approximately 40 percent of blood- brain barriers for treating disorders. To treat more efficiently the drug has to be taken numerous times a day which leads to less patient compliance, more time to heal the disease and thereof.
[0009] In view of the above observations, there is a need for a novel and an effective drug delivery carrier composition with proven pharmacological activities. Such a carrier must have the ability to cross the blood-brain barrier (BBB) with ease for treating numerous brain disorders. There is a need to provide a carrier that alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain. There is a need to provide a cost-effective drug without any side effects and enhance patient compliance.
Objectives of the invention:
[0010] The primary objective of the invention is to provide a novel and effective drug delivery carrier composition with proven pharmacological activities.
[0011] Another objective of the invention is to provide a carrier which can cross the blood-brain barrier (BBB) with ease for treating numerous brain disorders.
[0012] The other objective of the invention is to prepare a suitable oral or intravenous or intramuscular or intrathecal or subcutaneous or intradermal or sublingual or ocular or nasal or intra-cerebral or any by other means of drug administration dosage form of a targeted drug incorporated in the carrier with a synergistic effect for the treatment of multiple brain disorders.
[0013] Further objective of the invention is to provide a composition which is useful in treating brain disorders such as neurodegenerative disorders, brain hemorrhages, bruising of brain tissue cerebral edema, or swelling inside the skull, concussions strokes and disorders due to brain tumors.
[0014] Yet another objective of the invention is to provide a carrier that alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
[0015] Further objective of the invention is to provide a cost-effective drug without harmful side effects and enhance patient compliance.
Summary of the invention:
[0016] The present disclosure proposes a drug delivery carrier composition for brain disorders. The following presents a simplified summary in order to provide a basic understanding of some aspects of the claimed subject matter. This summary is not an extensive overview. It is not intended to identify key/critical elements or to delineate the scope of the claimed subject matter. Its sole purpose is to present some concepts in a simplified form as a prelude to the more detailed description that is presented later.
[0017] According to an aspect, the invention relates to an effective drug delivery carrier composition with proven pharmacological activities for crossing blood-brain barriers and to treat numerous types of brain disorders.
[0018] The brain disorder drug with a lipidomer carrier composition comprises of a spingosine, a salicylic acid, a phosphoric acid, a poly unsaturated fatty acid and a biologically active compound for treating numerous brain disorders. The structure of lipidomer carrier is represented by formula 1,
Formula 1
[0019] In another aspect, the lipidomer carrier further contains the biologically active compound encapsulated with folic acid optionally as a suspension along with the spingosine, the salicylic acid, the phosphoric acid, and the poly unsaturated fatty acids. The structure of lipidomer carrier along with folic acid is represented by formula 2,
Formula 2
[0020] Specifically, the lipidomer carrier composition is formulated by mixing equal proportions of compounds i.e., ranges from 0.001M to 1M of spingosine conjugated with ranges from 0.001M to 1M of salicylic acid mediated by ranges from 0.001M to 1M of phosphoric acid and ranges from 0.001M to 1M of poly unsaturated fatty acids, a biologically active compound, and ranges from 0.001M to 1M of folic acid added to the active compound.
[0021] The poly unsaturated fatty acids such as Arachidonic acid (AA), Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA) and the like that are used individually or the combination of selected fatty acids. The Arachidonic acid used in this carrier molecule goes through the anti inflammatory pathway mediated by enzymes Lipoxygenases, co-factor salicylic acid and folic acid thereby soothing the inflammation produced due to various reasons. The lipidomer carrier itself alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
[0022] Further, objects and advantages of the present invention will be apparent from a study of the following portion of the specification, the claims, and the attached drawings.
Detailed Invention Disclosure:
[0023] Various embodiments of the present invention will be described in reference to the accompanying drawings. Wherever possible, same or similar reference numerals are used in the drawings and the description to refer to the same or like parts or steps.
[0024] According to an exemplary embodiment, disclosed herein is concerned with a novel series an effective drug delivery carrier composition with proven pharmacological activities for crossing blood-brain barriers and to treat numerous types of brain disorders.
[0025] The brain disorder drug with a lipidomer carrier composition comprises of a spingosine, a salicylic acid, a phosphoric acid, a poly unsaturated fatty acid and a biologically active compound for treating numerous brain disorders. The structure of lipidomer carrier is represented by formula 1,
[0026] Optionally the lipidomer carrier further contains the biologically active compound encapsulated with folic acid optionally as a suspension along with the spingosine, the salicylic acid, the phosphoric acid, and the poly unsaturated fatty acids. The structure of lipidomer carrier along with folic acid is represented by formula 2,
Formula 2
[0027] Specifically, the lipidomer carrier composition is formulated by mixing equal proportions of compounds i.e., ranges from 0.001M to 1M of spingosine conjugated with ranges from 0.001M to 1M of salicylic acid mediated by ranges from 0.001M to 1M of phosphoric acid and ranges from 0.001M to 1M of poly unsaturated fatty acids. The poly unsaturated fatty acids may be selected from group of Arachidonic acid (AA), Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA) and the like that are used individually or the combination of selected fatty acids. The lipidomer carrier itself alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
[0028] In another aspect, the biologically active compound is a targeted drug that can be formulated at better dosage form i.e., ranging from O.OOOlgm to lgm or from 0.001M to 1M.
[0029] Inflammation is the innate immune response of the host body essential in neutralizing the pathogen. It is the first line of defense mechanism against foreign invading organisms. The proposed carrier composed of polyunsaturated fatty acid, salicylic acid, mediated by spingosine and phosphoric acid controls the onset of inflammation. The Arachidonic acid used in this carrier molecule goes through the anti-inflammatory pathway mediated by enzymes Lipoxygenases, co factor salicylic acid and folic acid. The anti-inflammatory molecules like LipoxinA4, resolvins, and protectins are produced when Lipoxygenases enzymes act upon the arachidonic acid thereby soothing the inflammation produced due to various reasons.
[0030] Numerous advantages of the present disclosure may be apparent from the discussion above. In accordance with the present disclosure, a novel and effective drug carrier composition with proven pharmacological activities which can cross the blood-brain barrier (BBB) with ease for treating numerous brain disorders. The composition helps in treating brain disorders such as neurodegenerative disorders, brain hemorrhages, bruising of brain tissue cerebral edema, or swelling inside the skull, concussions strokes and disorders due to brain tumors. The drug formulated is cost-effective without harmful side effects and enhance patient compliance.
[0031] It will readily be apparent that numerous modifications and alterations can be made to the processes described in the foregoing examples without departing from the principles underlying the invention, and all such modifications and alterations are intended to be embraced by this application.
Claims
1. A brain disorder drug with a lipidomer carrier composition, comprising: a spingosine; a salicylic acid; a phosphoric acid; a poly unsaturated fatty acids; and a biologically active compound for treating numerous brain disorders, wherein said structure of lipidomer carrier is represented by formula 1,
Formula 1
wherein said lipidomer carrier further contains said biologically active compound encapsulated with folic acid optionally as a suspension along with said spingosine, salicylic acid, phosphoric acid, and poly unsaturated fatty acids represented by formula 2,
Formula 2
2. The brain disorder drug with a lipidomer carrier composition as claimed in claim 1, wherein said lipidomer carrier composition is formulated by mixing equal proportions of compounds i.e., ranges from 0.001M to 1M of spingosine, salicylic acid, phosphoric acid, poly unsaturated fatty acids and folic acid.
3. The brain disorder drug with a lipidomer carrier composition as claimed in claim 1, wherein said lipidomer carrier composition can be formulated by mixing all the compounds i.e., spingosine, salicylic acid, phosphoric acid, poly unsaturated fatty or the combination of selected compounds.
4. The brain disorder drug with a lipidomer carrier composition as claimed in claim 2, wherein said poly unsaturated fatty acids may be selected from group of Arachidonic acid (AA), Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA) and the like that are used individually or the combination of selected fatty acids.
5. The brain disorder drug with a lipidomer carrier composition as claimed in claim 1, wherein said Arachidonic acid used in this carrier molecule goes through the anti-inflammatory pathway mediated by enzymes Lipoxygenases, co-factor salicylic acid and folic acid thereby soothing the inflammation produced due to various reasons.
6. The brain disorder drug with a lipidomer carrier composition as claimed in claim 1, wherein said lipidomer carrier itself alleviates the diseased condition of the brain by balancing the levels of inflammatory mediated signal molecules in the brain.
6. DATE AND SIGNATURE:
Dated this 10th day of September, 2019
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| WO2022259958A1 (en) * | 2021-06-10 | 2022-12-15 | 日本精化株式会社 | Phospholipid |
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| NAOOMI TOMINAGA; KOSAKA NOBUYOSHI; ONO MAKIKO; KATSUDA TAKESHI; YOSHIOKA YUSUKE; TAMURA KENJI; LÖTVALL JAN; NAKAGAMA HITOSHI; OCHI: "BRAIN METASTATIC CANCER CELLS RELEASE MICRORNA-181C-CONTAINING EXTRACELLULAR VESICLES CAPABLE OF DESTRUCTING BLOOD-BRAIN BARRIER", NATURE COMMUNICATIONS, vol. 6, 1 April 2015 (2015-04-01), pages 6716-1 - 6716-12, XP055463954 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022259958A1 (en) * | 2021-06-10 | 2022-12-15 | 日本精化株式会社 | Phospholipid |
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