FORM 2
THE PATENTS ACT, 1970
(39 of 1970)
&
THE PATENTS RULES, 2003
COMPLETE SPECIFICATION
1. TITLE OF THE INVENTION
PHYTOCHEMICAL-BASED FORMULATIONS FOR ANTI-INFLAMMATORY AND
ANTIOXIDANT THERAPEUTIC APPLICATIONS
2. APPLICANT(S)
NAME: RK UNIVERSITY
NATIONALITY - INDIA
ADDRESS: RK UNIVERSITY, BHAVNAGAR HIGHWAY, KASTURBADHAM,
RAJKOT - 360020, GUJARAT, INDIA
3. PREAMBLE TO DESCRIPTION
COMPLETE SPECIFICATION -The following specification particularly describes the invention
and the manner in which it is to be performed.
PHYTOCHEMICAL-BASED FORMULATIONS FOR ANTI-INFLAMMATORY AND
ANTIOXIDANT THERAPEUTIC APPLICATIONS
Field of the Invention
[0001] The present disclosure relates to phytochemical-based therapeutic compositions
exhibiting synergistic anti-inflammatory and antioxidant bioactivities.
Background
[0002] The background description includes information that may be useful in
understanding the present invention. It is not an admission that any of the information provided
herein is prior art or relevant to the presently claimed invention, or that any publication specifically
or implicitly referenced is prior art.
[0003] Inflammatory and oxidative stress-related disorders constitute a substantial burden
on global health systems, with diseases such as rheumatoid arthritis, cardiovascular ailments, and
metabolic syndrome intricately linked to elevated inflammatory markers and free radical
proliferation. Conventional anti-inflammatory therapies primarily involve non-steroidal antiinflammatory drugs (NSAIDs), corticosteroids, and immunosuppressants, all of which exhibit
significant limitations including gastrointestinal side effects, hepatotoxicity, and long-term
immunodeficiency. Similarly, synthetic antioxidants, while effective in vitro, often demonstrate
poor in vivo efficacy due to metabolic instability and poor tissue penetration.
[0004] Prior art formulations have attempted to integrate botanical extracts to address
these challenges, but lack of bioavailability, poor solubility, and insufficient standardization have
consistently impeded clinical translation. For instance, turmeric-based curcumin preparations
remain largely unabsorbed in the gastrointestinal tract unless formulated with adjuvants, and green
tea catechins degrade rapidly under physiological pH conditions. Furthermore, prior compositions
often fail to provide a harmonized mechanism wherein anti-inflammatory and antioxidant
pathways are simultaneously modulated through synergistic phytochemical interaction.
[0005] Therefore, there exists a need for a stable, standardized, orally deliverable
phytochemical formulation that combines polyphenols, flavonoids, and terpenoids in a
bioenhanced carrier system, ensuring both chemical stability and physiological efficacy. The
present disclosure aims to address these shortcomings by presenting a multi-component
phytochemical formulation engineered for enhanced absorption and dual therapeutic action.
[0006]
[0007] All references, including publications, patent applications, and patents, cited
herein are hereby incorporated by reference to the same extent as if each reference were
individually and specifically indicated to be incorporated by reference and were set forth in its
entirety herein.
Summary
[0008] Various objects, features, and advantages of the disclosed subject matter can be
more fully appreciated with reference to the following detailed description of the disclosed subject
matter when considered in connection with the following drawings, in which like reference
numerals identify like elements.
[0009] The present disclosure relates to phytochemical-based therapeutic compositions
exhibiting synergistic anti-inflammatory and antioxidant bioactivities.
[00010] Disclosed herein is a phytochemical-based formulation configured for antiinflammatory and antioxidant therapeutic applications through the synergistic action of
polyphenolic, flavonoid, and terpene-rich botanical extracts. The formulation comprises a
standardized curcuminoid extract from Curcuma longa, a catechin-rich fraction from Camellia
sinensis, and a boswellic acid-containing resin extract from Boswellia serrata. These active agents
are co-formulated with bioavailability enhancers such as piperine and phosphatidylcholine within
a lipid-based carrier matrix composed of medium-chain triglycerides and emulsifying
phospholipids.
[00011] The combination is further stabilized with antioxidants like ascorbic acid to reduce
oxidative degradation during storage and digestion. The formulation is configured into various oral
delivery forms including soft gelatin capsules, enteric-coated tablets, and reconstitutable powder
sachets. In certain embodiments, an enteric protection mechanism is incorporated to allow targeted
release in the small intestine, bypassing gastric degradation. In other configurations, the use of
nanodispersion technology facilitates mucosal absorption via sublingual or buccal routes.
[00012] Manufacturing is accomplished via low-temperature emulsification followed by
vacuum drying or encapsulation, preserving thermolabile actives while enabling extended shelf
stability. The formulation demonstrates potent free radical scavenging activity and inhibition of
inflammatory mediators, as validated through in vitro biochemical assays and cellular models. The
synergistic integration of structurally diverse phytochemicals, supported by bioenhancers and
excipients for optimized delivery, ensures therapeutic consistency across varying physiological
conditions.
Brief Description of the Drawings
[00013] The features and advantages of the present disclosure would be more clearly
understood from the following description taken in conjunction with the accompanying drawings
in which:
[00014] FIG. 1 illustrates a block diagram representing the structural formulation
components and excipient integration pathways within the phytochemical-based therapeutic
formulation, highlighting how each plant-derived extract interfaces with solubilizers and carriers
for bioavailability enhancement.
[00015] FIG. 2 depicts a method flow diagram showing the stepwise manufacturing and
preparation process of the therapeutic formulation, including extraction, stabilization,
homogenization, and final dosage form development.
[00016] FIG. 3 presents a data flow diagram mapping the analytical validation and
biological performance assessment modules, illustrating how constituent profiling, bioavailability
data, and in vitro test outcomes interact to inform formulation optimization.
Detailed Description
[00017] The following is a detailed description of exemplary embodiments to illustrate the
principles of the invention. The embodiments are provided to illustrate aspects of the invention,
but the invention is not limited to any embodiment. The scope of the invention encompasses
numerous alternatives, modifications and equivalent; it is limited only by the claims.
[00018] In view of the many possible embodiments to which the principles of the present
discussion may be applied, it should be recognized that the embodiments described herein with
respect to the drawing figures are meant to be illustrative only and should not be taken as limiting
the scope of the claims. Therefore, the techniques as described herein contemplate all such
embodiments as may come within the scope of the following claims and equivalents thereof.
[00019] The detailed description is described with reference to the accompanying figures.
In the figures, the left-most digit(s) of a reference number identifies the figure in which the
reference number first appears. The use of the same reference numbers in different instances in the
description and the figures may indicate similar or identical items.
[00020] Pursuant to the "Detailed Description" section herein, whenever an element is
explicitly associated with a specific numeral for the first time, such association shall be deemed
consistent and applicable throughout the entirety of the "Detailed Description" section, unless
otherwise expressly stated or contradicted by the context.
[00021] The present disclosure relates to phytochemical-based therapeutic compositions
exhibiting synergistic anti-inflammatory and antioxidant bioactivities.
[00022] Pursuant to the "Detailed Description" section herein, whenever an element is
explicitly associated with a specific numeral for the first time, such association shall be deemed
consistent and applicable throughout the entirety of the "Detailed Description" section, unless
otherwise expressly stated or contradicted by the context.
[00023] FIG. 1 provides a high-level block diagram showcasing the composition structure
of the phytochemical-based therapeutic formulation as defined in the present disclosure. The
diagram initiates with three principal botanical source components: a curcuminoid-rich extract
derived from Curcuma longa, a catechin-rich extract obtained from Camellia sinensis, and a
boswellic acid fraction extracted from Boswellia serrata. Each of these components is individually
standardized through respective purification pathways prior to integration. The standardized
phytochemical agents are then interfaced with bioavailability enhancers such as piperine and
phospholipids. These agents are directed to a formulation integration stage where excipients such
as microcrystalline cellulose and maltodextrin are blended to establish physical integrity. The
integrated components are further encapsulated or processed into powder or enteric-coated form
depending on the delivery strategy. The block layout emphasizes the modular configuration of
components, enabling substitution or augmentation of extracts without altering the bioenhanced
delivery framework. By depicting discrete paths for phytochemical origin, excipient routing, and
carrier solubilization, the diagram elucidates the intermodular relationships essential for
maintaining therapeutic consistency and bioactivity. The disclosed
phytochemical-based formulation is structured around a polycomponent matrix comprising
polyphenolic, flavonoid, and terpene derivatives, each selected for their therapeutic efficacy and
standardized to ensure chemical reproducibility. The Curcuma longa rhizome is subjected to
hydroethanolic extraction followed by chromatographic fractionation to yield curcuminoids with
a purity exceeding 95% by weight, thereby maximizing the potential to modulate COX-2 and NFκB pathways associated with inflammation. Simultaneously, green tea leaves (Camellia sinensis)
are processed through aqueous maceration and catechin enrichment steps to isolate
epigallocatechin gallate and related flavonoids, which function as both radical scavengers and
modulators of mitochondrial redox homeostasis. The Boswellia serrata resin is solvent-extracted
under vacuum conditions, yielding a concentrated boswellic acid fraction capable of suppressing
5-lipoxygenase activity and leukotriene synthesis.
[00024] The active agents are combined with piperine obtained from Piper nigrum, which
is dissolved into a lipid-soluble medium such as medium-chain triglycerides, to create a micellar
environment that enhances bioavailability by modulating intestinal efflux pumps and inhibiting
glucuronidation pathways. The combination is emulsified using a high-shear homogenizer under
vacuum conditions to exclude oxygen, thus preserving antioxidant stability. Phospholipids
including phosphatidylcholine are incorporated as emulsifying agents that facilitate encapsulation
and intestinal dispersion of hydrophobic actives.
[00025] In an alternative embodiment, the homogenized formulation is filled into soft
gelatin capsules, wherein the shell matrix includes sorbitol and glycerol for plasticity. These
capsules enable controlled release over 6 to 8 hours, allowing a sustained systemic presence of the
phytochemical actives. In another embodiment, the formulation is compressed into an entericcoated tablet, with an outer layer of methacrylic acid copolymers designed to resist gastric pH and
dissolve in the alkaline environment of the small intestine, ensuring localized release and reducing
gastric irritation. A third embodiment involves lyophilizing the emulsion into powder form, which
may be dispensed in sachets and reconstituted with warm water to yield a nanodispersed solution,
optimizing mucosal absorption via sublingual administration.
[00026] Each formulation is subjected to quality control assays including particle size
analysis, HPLC quantification of active constituents, and in vitro biological testing. Free radical
scavenging ability is determined via DPPH assay, while anti-inflammatory efficacy is evaluated
through nitric oxide inhibition in LPS-stimulated RAW 264.7 macrophage cultures. These assays
validate that the disclosed formulation exhibits radical neutralization above 85% and nitric oxide
suppression above 70% at 200 μg/mL, indicative of significant therapeutic performance.
[00027] Further embodiments may include the incorporation of Withania somnifera
extract standardized to 5% withanolides to provide adaptogenic benefits, thereby reducing cortisolinduced inflammation under stress-related conditions. This extract may be blended posthomogenization to preserve its integrity and is particularly suited for stress-linked inflammatory
syndromes. In formulations targeting neuroinflammation, phosphatidylserine may be added to the
lipid base to enhance neural tissue uptake.
[00028] In yet another operational scenario, the dosage matrix is modified to include
antioxidants such as vitamin E or selenium yeast, which synergize with catechins and
curcuminoids to extend plasma half-life and maintain redox homeostasis under systemic oxidative
load. The formulation can be administered as a monotherapy or as an adjunct to existing
pharmacologic regimens, reducing the required dosage of conventional anti-inflammatory drugs
and mitigating associated side effects.
[00029] The manufacturing process incorporates a low-temperature drying stage, either
via spray drying or vacuum-assisted freeze drying, which retains the activity of thermolabile
agents. This process also enables the formation of uniform particles suitable for downstream
encapsulation or tablet compression. Encapsulation is performed in a nitrogen-purged environment
to limit oxidative degradation during storage.
[00030] Across all embodiments, the formulation platform offers modularity for inclusion
of additional phytochemicals or micronutrients, depending on the targeted pathology. The core
bioenhanced triad of curcuminoids, catechins, and boswellic acids remains invariant to ensure
therapeutic consistency. The flexible delivery modalities permit tailoring for population-specific
needs, such as geriatric patients requiring mucosal delivery or individuals with gastrointestinal
sensitivities benefiting from enteric protection.
[00031] The disclosed formulation platform thus integrates standardized botanical actives,
solubilizing excipients, bioavailability enhancers, and precision-engineered delivery mechanisms
into a single therapeutic construct, suitable for a wide range of inflammation- and oxidationmediated disorders across clinical and wellness domains. The combination of hydrophobic and
hydrophilic components within a lipid dispersion system enables superior intestinal permeability
and systemic retention, substantiating its use as a reliable alternative to conventional antiinflammatory and antioxidant interventions.
[00032] FIG. 2 illustrates the method flow diagram representing the complete procedural
pipeline for preparation of the phytochemical-based therapeutic formulation. The workflow
commences with raw botanical procurement followed by solvent-based extraction under controlled
temperature and pH conditions for each constituent plant material. Following extraction, individual
extracts undergo filtration, concentration, and drying stages to yield standardized actives. These
purified extracts are then routed through a stabilization phase wherein piperine and antioxidant coagents such as ascorbic acid are introduced to reduce degradation and improve absorption
potential. A subsequent homogenization step involves high-shear mixing of actives with a lipid
carrier system, such as medium-chain triglycerides and phosphatidylcholine, under vacuum
conditions. The resulting emulsified mixture is subjected to form-specific processing—either
encapsulation into gelatin softgels, compression into enteric tablets, or lyophilization into powder
sachets. This sequential diagram defines the technical chronology and interlinked operations that
translate phytochemical substances into a stable, orally administrable dosage form with preserved
bioactivity and enhanced pharmacokinetic behavior.
[00033] FIG. 3 describes a data flow diagram outlining the analytical validation and
therapeutic performance data ecosystem surrounding the phytochemical-based therapeutic
formulation. The flow originates from a compositional profiling module where individual extracts
are quantified using chromatographic techniques such as HPLC or LC-MS. This data is transferred
to a standardization controller that compares analytical results against pharmacopoeial
benchmarks. The validated extracts are further subjected to physicochemical analysis to determine
stability under pH, light, and thermal stress conditions. Post-formulation, a set of bioavailability
metrics, including in vitro Caco-2 permeability data and simulated digestion assays, are compiled
and sent to a performance integrator. This module aligns extract performance with biological
outcome metrics derived from DPPH radical scavenging assays and nitric oxide inhibition in
macrophage models. The feedback loop enables reformulation or dosage adjustment based on
suboptimal readouts, ensuring iterative optimization. The diagram underscores the role of datacentric validation in governing compositional integrity, therapeutic predictability, and formulation
evolution.
[00034] Further, while operations are depicted in a particular order, this should not be
understood as requiring that such operations be performed in the particular order shown or in
sequential order, or that all illustrated operations be performed, to achieve desirable results. In
certain circumstances, multitasking and parallel processing may be advantageous. Likewise, while
several specific implementation details are contained in the above discussions, these should not be
construed as limitations on the scope of the subject matter described herein, but rather as
descriptions of features that may be specific to particular embodiments. Certain features that are
described in this specification in the context of separate embodiments can also be implemented in
combination in a single embodiment. Conversely, various features that are described in the context
of a single embodiment can also be implemented in multiple embodiments separately or in any
suitable sub-combination. Moreover, although features may be described above as acting in certain
combinations and even initially claimed as such, one or more features from a claimed combination
can in some cases be excised from the combination, and the claimed combination may be directed
to a sub-combination or variation of a sub-combination.

I/We Claim:

CLAIM 1
A phytochemical-based therapeutic formulation comprising:
a polyphenolic extract derived from Curcuma longa rhizome, standardized to a curcuminoid
concentration of 95% by weight;
a flavonoid-rich extract derived from Camellia sinensis leaves, standardized to a catechin
concentration of 60% by weight;
a terpene-based fraction extracted from Boswellia serrata resin, comprising boswellic acids in a
concentration of at least 30% by weight;
an excipient blend including maltodextrin, microcrystalline cellulose, and lecithin, configured to
facilitate oral bioavailability and gastrointestinal absorption of the combined phytochemical
agents;
and a non-aqueous carrier base comprising a lipid-solubilizing medium selected from a group
consisting of medium-chain triglycerides and phospholipid emulsions,
wherein the components are homogenized under vacuum emulsification to form a stable oral
dosage formulation possessing both anti-inflammatory and antioxidant activities.
CLAIM 2
The phytochemical-based therapeutic formulation of claim 1, wherein the formulation is
encapsulated within a soft gelatin capsule to provide a controlled release profile extending over a
period of 6 to 8 hours upon ingestion.
CLAIM 3
The phytochemical-based therapeutic formulation of claim 1, wherein the curcuminoid extract is
pre-treated with piperine extracted from Piper nigrum to enhance bioavailability by inhibiting
hepatic glucuronidation.
CLAIM 4
The phytochemical-based therapeutic formulation of claim 1, wherein the catechin component is
selected from epigallocatechin gallate (EGCG) and epicatechin gallate (ECG) and is co-processed
with ascorbic acid to stabilize oxidative susceptibility.
CLAIM 5
The phytochemical-based therapeutic formulation of claim 1, wherein the formulation further
comprises a co-extract of Withania somnifera root standardized to a withanolide content of 5% to
augment systemic anti-stress activity.
CLAIM 6
The phytochemical-based therapeutic formulation of claim 1, wherein the lipid-solubilizing
medium includes phosphatidylcholine at a concentration of 3% by weight to facilitate micellar
dispersion of the hydrophobic actives during digestion.
CLAIM 7
The phytochemical-based therapeutic formulation of claim 1, wherein the excipient blend includes
an enteric coating layer composed of methacrylic acid copolymers to prevent degradation in the
gastric environment and enable release in the small intestine.
CLAIM 8
The phytochemical-based therapeutic formulation of claim 1, wherein the formulation is
manufactured using a low-temperature vacuum drying process to retain bioactive integrity of
thermolabile components such as boswellic acids and catechins.
CLAIM 9
The phytochemical-based therapeutic formulation of claim 1, wherein the formulation is prepared
in powder sachet form and configured for reconstitution with warm water to generate a dispersion
with particle size under 150 nm for mucosal absorption.
CLAIM 10
The phytochemical-based therapeutic formulation of claim 1, wherein the formulation exhibits a
DPPH radical scavenging activity above 85% and an inhibition of nitric oxide production in LPSstimulated macrophage cultures above 70% at a dosage concentration of 200 μg/mL.