Description:1
FORM-2
THE PATENTS ACT, 1970
(39 of 1970)
&
THE PATENTS RULES, 2003
COMPLETE
SPECIFICATION
(See section 10 and rule 13)
Quercetin loaded Nanostructured Lipid Carrier for the Breast Cancer
G D Goenka University, an Indian university of Sohna Gurugram Road, Sohna, Haryana, India, 122103
THE FOLLOWING SPECIFICATION PARTICULARLY DESCRIBES THE INVENTION AND THE MANNER IN WHICH IT IS TO BE PERFORMED
2
FIELD OF INVENTION:
The present invention relates to pharmaceutical science field, which aims at design and development of Integrin (avß3) receptor-targeted PLGA nanoparticles containing cisplatin and upconversion nanoparticles improved theranostic effect in lung cancer therapy
BACK GROUND:
Breast Cancer remains the leading cancer-related cause of disease burden for women, affecting one in 20 globally and as many as one in eight in high-income countries. Quercetin, the most abundant flavonoid in plants is a promising natural compound in Cancer prevention or treatment. However , its application in Cancer is limited due to its low aqueous solubility, poor cellular bioavailability and high instability .Quercetin has extremely low aqueous solubility so one of the strategies to circumvent these problems is to encapsulate Quercetin into nanoparticles. Nanoparticle Drug Delivery has gained great attention in Cancer research recently.
Danhier et al., have demonstrated the clinical applications of RGD grafted PLGA nanoparticles containing paclitaxel and JNJ-7706621. The study concluded that the prepared PLGA nanoparticles decorated with RGD peptide have shown signifiant effect in cytotoxicty study in HeLa cells and achieved lower IC50 vales at 5.5 µg/ ml in compared to free paclixatel. The observed result was further matched with the observation of cellular uptake study which revealed that after RGD peptide decorated PLGA nanoparticles were more effective to penetrate in cancer cells in compared without peptide modifid nanoparticles. Furthermore, the tumor inhibition study have also proved the effectiveness of RGD peptide decorated PLGA nanoparticles which achieved higher tumor growth inhibition in compared to other drug counterparts
3
Dragana et al., have evaluate the synergetic effect of loading natural plant-oil-based nanostructured lipid carriers with quercetin (QR-NPO-NLCs) as a topical delivery system for the treatment of bacterial skin infections. Five nanostructured lipid carrier systems containing different oils (sunflower, olive, corn, coconut, and castor) were engineered. The particles’ stability, structural properties, bioavailability, and antimicrobial activity were studied. NLCs with an average size of <200 nm and Z-potential of -40 mV were developed. Stable QR-NPO-NLCs were obtained with high encapsulation efficiency (>99%). The encapsulation of QR decreased cytotoxicity and increased the antioxidant effect of nanocarriers. An increase in antibacterial activity of the systems containing QR was demonstrated against Staphylococcus aureus. QR-NPO-NLCs could transport QR to an intranuclear location within HaCaT cells, indicating that QR-NPO-NLCs are promising candidates for controlled topical drug delivery.
Anisha D'Souza et al screens types of oils used till date in combination with solid lipids to form NLCs. These oils are broadly classified into two categories: Natural oils and Essential oils. NLCs offer range of advantages in drug delivery due to the formation of an imperfect matrix owing to the presence of oil. The type and percentage of oil used, determine optimal drug loading and stability. Literature shows that a variety of oils is/are used in NLCs mainly as the matrix, which is from natural origin, triglycerides class. On the other hand, essential oils not only serve as a matrix but also as an active moiety. In short, oil is the key ingredient in the formation of NLCs, hence it needs to be selected wisely as per the performance criteria expected. The aim of this article is to discuss shortly the role of liquid lipids and highlight the use of variety of oils in NLCs preparation.
The line of research can help develop a novel preventive and therapeutic modality for breast cancer using natural compounds and biocompatible nanocarriers with enhanced anticancer activities, minimized immunology and side effects. Many researchers have formulated Q loaded NLCs for topical use only.
To date, pharmaceutical scientists and researchers have managed to develop different types of nanoformulations for the delivery of quercetin, such as
4
nanovesicles, nanospheres, nanocapsules,nanogels, nanofibres, nanoemulsions, micelles, goldnanoparticles, silica nanoparticles, solid lipid nanoparticles (SLN), and nanostructured lipid carriers (NLC).
Due to the limitations of Quercetin , it has to be encapsulated into the nano drug delivery systems.In my invention , I have encapsulated in nanostructured lipid carriers but many other researchers have synthesized other Quercetin loaded Nanopaticle systems like SLN but to overcome their great disadvanges, NLCs were sysnthesized.
Therefore, the present invention overcome the said problems and synthesizing Q-NLCs , increases aqueous solubility and stability of Quercetin, enhances sustained release of Quercetin, elevate cellularuptake of Q by MCF-7 breast cancer cells, decrease the viability of those breast cancer cells, and induce their apoptosis.
OBJECTIVE OF THE INVENTION:
1. It is an object of the invention to provide a method for preparing Quercetin loaded Nanostructured Lipid Carriers (NLCs).
2. It is another object of the invention to provide Quercetin loaded Nanostructured Lipid Carrier (NLC).
3. It is another object of the invention to pharmaceutical composition for delivering Quercetin.
4. It is another object of the invention to method for enhancing Quercetin's bioavailability and stability, comprising encapsulating Quercetin within a Nanostructured Lipid Carrier (NLC) prepared using Compritol 888ATO and Transcutol HP.
SUMMARY
Quercetin (Q), a common dietary flavonoid, derived from plants has gained tremendous attention from the researchers for Cancer Chemoprevention due to its many beneficial roles but its low degree of water solubility, stability, and cellular bioavailability has hampered its applicability. Therefore synthesized Q-NLCs using hot High Pressure Homogenization technique because nanocarriers can increase drug
5
absorption, protect drugs from premature degradation, prolong drug circulation time, exhibit high differential uptake efficiency in the target cells (or tissues) over normal cells (or tissues), lower toxicity through preventing the drug from prematurely interacting with the biological environment. The Quercetin loaded nanostructured lipid carriers were formulated by High Shear homogenization (high stirring homogenization) followed by bath ultrasonication. The technique is based on the reduction of droplet and particle size. It is one of the simplest and the most effective ways of producing NLCs. The Quercetin NLCs were prepared using Compritol 888ATO and Transcutol HP as solid and liquid lipids,respectively, selected after lipid screening for the preparation NLCs. The liquid phase was prepared by melting the solid lipid at a temperature 10? higher than its melting point. Further , the calculated amount of liquid lipid was added to the melted solid lipid followed by slow addition of drug with constant stirring to get a clear solution. The aqueous phase containing Kolliphor HS 15 as a surfactant was heated separately at the same temperature as that of the molten lipids, followed by the addition of the aqueous solution drop wise into the drug- lipid melt. The mixture was homogeneously dispersed using a high shear mixer. High speed stirring was performed at 10,000 rpm for 6-10 minutes followed by the constant stirring at 1600 rpm for 1-4 hours to produce the Quercetin NLCs with lower particle size and polydispersity index. This high-speed stirring is usually followed by ultra-sonication, which breaks droplets based on the formation, growth, and implosive collapse of bubbles. The optimized formulation exhibited a particle size of 302 nm, which falls within the acceptable range for oral drug delivery. It displayed a higher entrapment efficiency ranging from 42.3% to 76.5%, as well as an elevated drug release profile with a subsequent sustained release of 77.6%. The experimental findings revealed that Q-NLC improved the solubility and stability of Quercetin in aqueous solutions and facilitated its sustained release. This study represents a promising advancement in breast cancer prevention through the utilization of a novel, biodegradable, and biocompatible Q-NLC. It possesses enhanced anti-cancer properties while minimizing immunogenicity and side effects.
BRIEF DESCRIPTION OF FIGURES
6
These and other features, aspects, and advantages of the present invention will become better understood when the following detailed description is read with reference to the accompanying figures in which like characters represent like parts throughout the figures, wherein:
Figure 1, illustrates a view of the optimized clear Quercetin nanostructured lipid carrier formulation for the present invention.
Fig. 2: illustrates a view of The FTIR Spectra of Q-NLCs (a) pure drug, (b) Compritol 888ATO, (c) Solutol HS 15, (d) transcutol HP, (e) physical mixture, (f) Q-NLC formulation for the present invention.
Fig.3: illustrates a view of TEM photomicrograph of Q-NLC for the present invention. Fig.4: illustrates a view of DSC Thermogram of Q-NLC for the present invention.
Fig: 5: illustrates a view of DSC thermogram of Physical mixture of drug and excipients for the present invention.
Fig: 6: illustrates a view of the in vitro Drug Release Profile of Q-bio-SNEDDS and Pure Drug Solution for the present invention.
Further, skilled artisans will appreciate that elements in the figures are illustrated for simplicity and may not have been necessarily been drawn to scale. For example, the flowcharts illustrate the method in terms of the most prominent steps involved to help to improve understanding of aspects of the present invention. Furthermore, in terms of the construction of the device, one or more components of the device may have been represented in the figures by conventional symbols, and the figures may show only those specific details that are pertinent to understanding the embodiments of the present invention so as not to obscure the figures with details that will be readily apparent to those of ordinary skill in the art having benefit of the description herein.
DETAILED DESCRIPTION:
For the purpose of promoting an understanding of the principles of the invention, reference will now be made to the embodiment illustrated in the figures and specific
7
language will be used to describe the same. It will nevertheless be understood that no limitation of the scope of the invention is thereby intended, such alterations and further modifications in the illustrated system, and such further applications of the principles of the invention as illustrated therein being contemplated as would normally occur to one skilled in the art to which the invention relates.
It will be understood by those skilled in the art that the foregoing general description and the following detailed description are exemplary and explanatory of the invention and are not intended to be restrictive thereof.
Reference throughout this specification to “an aspect”, “another aspect” or similar language means that a particular feature, structure, or characteristic described in connection with the embodiment is included in at least one embodiment of the present invention. Thus, appearances of the phrase “in an embodiment”, “in another embodiment” and similar language throughout this specification may, but do not necessarily, all refer to the same embodiment.
The terms "comprises", "comprising", or any other variations thereof, are intended to cover a non-exclusive inclusion, such that a process or method that comprises a list of steps does not include only those steps but may include other steps not expressly listed or inherent to such process or method. Similarly, one or more devices or systems or elements or structures or components proceeded by "comprises... a" does not, without more constraints, preclude the existence of other devices or other systems or other elements or other structures or other components or additional devices or additional systems or additional elements or additional structures or additional components.
Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. The system, methods, and examples provided herein are illustrative only and not intended to be limiting.
8
The terms “a” and “an” herein do not denote a limitation of quantity, but rather denote the presence of at least one of the referenced items.
The terms “having”, “comprising”, “including”, and variations thereof signify the presence of a component.
Now the present invention will be described below in detail with reference to the following embodiment.
Example 1
Preparation of Quercetin loaded Nanostructured Lipid Carrier
The Quercetin loaded nanostructured lipid carriers were formulated by High Shear homogenization (high stirring homogenization) followed by bath ultrasonication. The technique is based on the reduction of droplet and particle size. It is one of the simplest and the most effective ways of producing NLCs. The Quercetin NLCs were prepared using Compritol 888ATO and Transcutol HP as solid and liquid lipids,respectively, selected after lipid screening for the preparation NLCs. The liquid phase was prepared by melting the solid lipid at a temperature 10? higher than its melting point. Further , the calculated amount of liquid lipid was added to the melted solid lipid followed by slow addition of drug with constant stirring to get a clear solution. The aqueous phase containing Kolliphor HS 15 as a surfactant was heated separately at the same temperature as that of the molten lipids, followed by the addition of the aqueous solution drop wise into the drug- lipid melt. The mixture was homogeneously dispersed using a high shear mixer. High speed stirring was performed at 10,000 rpm for 6-10 minutes followed by the constant stirring at 1600 rpm for 1-4 hours to produce the Quercetin NLCs with lower particle size and polydispersity index. This high-speed stirring is usually followed by ultra-sonication, which breaks droplets based on the formation, growth, and implosive collapse of bubbles.
Example 2
9
The optimum formulation responses were predicted using CCRD, which were then correlated with the obtained results. The optimized formulation consisted of solid lipid:liquid lipid ratio(75.49:24.51) of Compritol 888ATO : Transcutol HP respectively , surfactant concentration of 2.61 and the ultrasonication time of 5.6 min. The predicted response of particle size and entrapment efficiency was 369.7 nm and 70.5% respectively. While the response obtained after using this composition was found to be 302.9 nm and 77.6 % respectively. The results suggested that a good correlation existed between the predicted and obtained responses, which established the accuracy in the formulation of Quercetin NLCs. The responses of the optimized formulation were generated with a desirability factor close to 0.8. The image of clear optimized drug loaded Quercetin NLCs is shown in Fig 1.
Example 3
Characterization of Quercetin loaded Nanostructured lipid carrier
FT-IR Spectra
FTIR spectra of the pure drug, physical mixture of the drug and excipients and final formulation were performed to study the possible interactions between the drug (Quercetin), solid and the liquid lipids and the other excipients used in the formulation. The FTIR spectra of Quercetin, physical mixture of Quercetin, lip-ids and other excipients and the final NLC formulation are shown in the figure down below. In the figure 2(a) shows the FTIR Spectra of the pure drug which showed all the characterisitic peaks of Quercetin where where its characteristic bands were detected, OH groups stretching was detectable at 3412.22 cm-1, whereas OH bending of the phenol function was detectable at 1381.09 cm-1. The C=O aryl ketone stretching was marked at 1664.64 cm-1. C=C aromatic ring stretch bands were measurable at 1610.63, 1562.41, and 1518 cm-1. The in-plane bending of C–H aromatic hydrocarbon was detectable at 1319.37 cm-1, the C–O stretching in phenol was marked at 1261.50, and the C–CO–C stretch and bending in ketone was seen at 1168.91. 2(e) in the figure depicts the FTIR spectra of physical mixture of Quercetin and Compritol 888ATO / Transcutol HP( Lipids) and Kolliphor HS15 (Surfactant) .Peaks at 2953 and 2845 cm-1 were detectable at C-H
10
stretching, the C-H bending is observed at peak in the range 1641 to 1973 cm-1. . O-H bending was oberseved btw the peaks in the range 1087-1354 cm-1 and C=C bending is detected at 717 cm-1. The spectra of NLC (f) showed high intensity characteristic peak at 2916 cm and 2850 cm-1.. Strong C=0 stretching was observed at 1730 cm-1. Medium peak in the range 1629 was observed at C-C stretching. Peak in the range 1105-1383 cm-1 was observed at O-H bending of the carboxylic acid.
Example 4
Surface morphology and structure
Q-NLCs after preparation were characterized for their morphological and structural examination. They were investigated using transmission electron microscopy (TEM, Talos) on an H7500 machine operating at 100 kV. Briefly, a droplet of the diluted formulation (1:10) was directly placed on the copper electron microscopy grids supported by the formvar films. Approximately 3–4 minutes after sample deposition, the excess surface water was removed by tapping on the grid with filter paper and air-dried. Then, the grid was stained with phospho-tungstic acid for 30 seconds, and again, the excess was drawn off. The grid was then observed by TEM. The combination of different bright-field images was taken at increasing magnification to expose the structure and size of the NLC formulation as well. The TEM images show the particle size ranges between 92.8-213 nm but the particle size analysis shows the droplet size 302 nm as it gives the average particle size (Fig 3).
Example 5
Entrapment efficiency
The entrapment efficiency of various nanostructured lipid carrier (NLC) formulations ranged from 66.09% to 93.70%. The differences in entrapment efficiency among the different formulations can be attributed to various factors, including the content of solid and liquid lipids. Increasing the concentration of Compritol® 888 resulted in a higher entrapment efficiency. However, the formulation with the highest ratio of solid to liquid lipid (80:20) exhibited comparatively lower entrapment efficiency than the formulation
11
with a middle ratio (75:25). This observation could be explained by the reduced content of liquid lipid in the formulation. The presence of liquid lipid is crucial for maintaining an irregular arrangement of the solid lipid matrix, which facilitates the entrapment of more drug within the NLC. Previous studies have also reported that Compritol® 888 promotes drug entrapment in NLCs due to its higher content of mono-, di-, and triglycerides, which enhance the solubilization of the drug in the lipid matrix. Additionally, the liquid lipid acts in synergy and makes sufficient space for drug entrapment. The % entrapment efficiency of the prepared formulation was found between the range 42.31-76.55%. The results indicated that the entrapment efficiency of the formulation is directly proportional to the lipid ratio while inversely proportional to the surfactant concentration and ultrasonication time.
Example 6
Differential Scaaning Calorimetry (DSC)
Thermal properties and phase change behavior of pure drug Quercetin, physical mixture of drug and excipients and optimized NLC formulations were analyzed by Differential Scanning Calorimetry (DSC). A comparative assessment between the pure drug, lipid, physical mixture and drug-loaded lipid nanocarrier confirms the characteristics of the pure drug and lipid. Also, it provides a clear idea about changes in drug properties upon loading into the nanocarrier. DSC thermogram of the pure drug Quercetin ,physical mixture of lipid phase, Compritol® 888 ATO and transcutol HP, and l NLC are shown in figures down bellow . The Differential Scanning Calorimetry curve of Quercetin showed a sharp endothermic peak at 130.34°C as shown in the figure (4), while the onset of temperature is 109.98 and the end point was 139.01°C which is concordant with the reference value which is 119°C. These obtained value indicated the purity of drug samples.
Example 7
In vitro drug release:
12
The in vitro release of drugs of Q-NLCs and pure Quercetin were performed in 250 ml of phosphate buffer pH 6.8 separately. After 60 minutes, the percentage of drugs release of the NLC was reached to be 53.2±0.72 , which further reached to 77.6 ± 0.879 after 24 hours and the percentage release of pure quercetin was 72.19 ± 1.651 after 24 hrs which shows that the percentage release of Q-NLCs was significantly higher (p ? 0.05) than the pure quercetin solution as shown in the table below.. Increased availability of Quercetin in the dissolved state could give the better absorption and improved bioavailability. The drug released rate were fitted in the different kinetics models including zero order, first order, Higuchi’s model, Korsmeyer Peppas and Hixon–Crowell. The finding of this study indicated the slow and sustained release of drugs from the Q-NLCs. Time (minutes) % Cumulative Drug Release (% CDR)* Q-NLCs Drug Solution 0 0 0 5 9.88 ± 1.25 9.072 ± 0.72 10 11.05 ± 1.22 12.21 ±1.41 15 11.16 ± 3.49 12.45 ± 1.22 30 14.77 ± 1.25 14.31 ± 1.32 45 17.92 ± 1.39 15.82 ± 1.25 60 21.88 ± 2.13 17.22 ± 0.34 120 27.35± 1.25 18.85 ± 1.06 240 47.7 ± 0.87 21.41 ± 0.69 360 52.63 ± 0.72 40.51 ± 0.87 720 62.06 ± 0.53 53.91 ± 1.04
13
1440 77.55 ± 0.87 59.62 ± 0.72
Table. 1: The Percentage Drug Release of Q-NLCs and Pure Quercetin
The NLC loaded with the drug was effectively prepared through a combination of hot shear homogenization and ultrasonication methods. The experimental design and optimization process employed response surface methodology utilizing the Central Composite Design approach. The objective of this study was to optimize the formulation variables and create a nanocarrier that is cost-effective, biodegradable, and stable, while also achieving higher drug entrapment and a sustained release profile.The optimized formulation exhibited a particle size of 302 nm, which falls within the acceptable range for oral drug delivery. It displayed a higher entrapment efficiency ranging from 42.3% to 76.5%, as well as an elevated drug release profile with a subsequent sustained release of 77.6%. The experimental findings revealed that Q-NLC improved the solubility and stability of Quercetin in aqueous solutions and facilitated its sustained release. This study represents a promising advancement in breast cancer prevention through the utilization of a novel, biodegradable, and biocompatible Q-NLC. It possesses enhanced anti-cancer properties while minimizing immunogenicity and side effects.
Variations and modifications of the foregoing are within the scope of the present invention. Accordingly, many variations of these embodiments are envisaged within the scope of the present invention.
The foregoing descriptions of specific embodiments of the present invention have been presented for purposes of description. They are not intended to be exhaustive or to limit the present invention to the precise forms disclosed, and obviously many modifications and variations are possible in light of the above teaching.
The embodiments were chosen and described in order to best explain the principles of the present invention and its practical application, and to thereby enable others skilled in the art to best utilize the present invention and various embodiments with various
14
modifications as are suited to the particular use contemplated. It is understood that various omissions and substitutions of equivalents are contemplated as circumstances may suggest or render expedient, but such omissions and substitutions are intended to cover the application or implementation without departing from the spirit or scope of the present invention.
15
We claim,
1. A method for preparing Quercetin loaded Nanostructured Lipid Carriers (NLCs), comprising the steps of:
a) Formulating the Quercetin NLCs using High Shear homogenization (high stirring homogenization) followed by bath ultrasonication.
b) Selecting Compritol 888ATO as the solid lipid and Transcutol HP as the liquid lipid after lipid screening for NLC preparation.
c) Melting the solid lipid at a temperature 10? higher than its melting point to prepare the liquid phase.
d) Adding the calculated amount of liquid lipid to the melted solid lipid and slowly adding the Quercetin drug with constant stirring to obtain a clear solution.
e) Preparing an aqueous phase containing Kolliphor HS 15 as a surfactant and heating it separately at the same temperature as the molten lipids.
f) Adding the aqueous solution dropwise into the drug-lipid melt.
g) Homogeneously dispersing the mixture using a high shear mixer at 10,000 rpm for 6-10 minutes, followed by constant stirring at 1600 rpm for 1-4 hours to achieve Quercetin NLCs with reduced particle size and polydispersity index.
h) Optionally, subjecting the mixture to ultrasonication to further reduce droplet size and improve NLC stability through bubble formation, growth, and implosive collapse.
2. A Quercetin loaded Nanostructured Lipid Carrier (NLC) prepared by the method of claim 1, comprising Compritol 888ATO as the solid lipid and Transcutol HP as the liquid lipid, with Quercetin encapsulated within the NLC structure.
3. A pharmaceutical composition for delivering Quercetin, comprising the Quercetin loaded Nanostructured Lipid Carrier (NLC) of claim 2, wherein the NLC's reduced
16
particle size and polydispersity index enhance Quercetin's bioavailability and therapeutic efficacy.
4. The pharmaceutical composition of claim 3, wherein the NLC formulation enables controlled release and targeted delivery of Quercetin, improving its performance in the treatment of various diseases.
5. A method for enhancing Quercetin's bioavailability and stability, comprising encapsulating Quercetin within a Nanostructured Lipid Carrier (NLC) prepared using Compritol 888ATO and Transcutol HP, as claimed in claim 2. The NLC's reduced particle size and polydispersity index facilitate improved absorption and prolonged release of Quercetin, enhancing its therapeutic effectiveness.
Dated this 28/07/2023 G D Goenka University, Sohna Gurugram Road, Sohna, Haryana, India, 122103
17
ABSTRACT
Quercetin loaded Nanostructured Lipid Carrier for the Breast Cancer
The present invention relates to formulate, optimize and evaluate the Quercetin loaded Nanostructured Lipid Carrier for the treatment of Breast Cancer. Quercetin (Q), a common dietary flavonoid, derived from plants has gained tremendous attention from the researchers for Cancer Chemoprevention due to its many beneficial roles but its low degree of water solubility, stability, and cellular bioavailability has hampered its applicability. Therefore we have successfully synthesized Q-NLCs using hot High Pressure Homogenization technique because nanocarriers can increase drug absorption, protect drugs from premature degradation, prolong drug circulation time, exhibit high differential uptake efficiency in the target cells (or tissues) over normal cells (or tissues), lower toxicity through preventing the drug from prematurely interacting with the biological environment. , Claims:We claim,
1. A method for preparing Quercetin loaded Nanostructured Lipid Carriers (NLCs), comprising the steps of:
a) Formulating the Quercetin NLCs using High Shear homogenization (high stirring homogenization) followed by bath ultrasonication.
b) Selecting Compritol 888ATO as the solid lipid and Transcutol HP as the liquid lipid after lipid screening for NLC preparation.
c) Melting the solid lipid at a temperature 10? higher than its melting point to prepare the liquid phase.
d) Adding the calculated amount of liquid lipid to the melted solid lipid and slowly adding the Quercetin drug with constant stirring to obtain a clear solution.
e) Preparing an aqueous phase containing Kolliphor HS 15 as a surfactant and heating it separately at the same temperature as the molten lipids.
f) Adding the aqueous solution dropwise into the drug-lipid melt.
g) Homogeneously dispersing the mixture using a high shear mixer at 10,000 rpm for 6-10 minutes, followed by constant stirring at 1600 rpm for 1-4 hours to achieve Quercetin NLCs with reduced particle size and polydispersity index.
h) Optionally, subjecting the mixture to ultrasonication to further reduce droplet size and improve NLC stability through bubble formation, growth, and implosive collapse.
2. A Quercetin loaded Nanostructured Lipid Carrier (NLC) prepared by the method of claim 1, comprising Compritol 888ATO as the solid lipid and Transcutol HP as the liquid lipid, with Quercetin encapsulated within the NLC structure.
3. A pharmaceutical composition for delivering Quercetin, comprising the Quercetin loaded Nanostructured Lipid Carrier (NLC) of claim 2, wherein the NLC's reduced
16
particle size and polydispersity index enhance Quercetin's bioavailability and therapeutic efficacy.
4. The pharmaceutical composition of claim 3, wherein the NLC formulation enables controlled release and targeted delivery of Quercetin, improving its performance in the treatment of various diseases.
5. A method for enhancing Quercetin's bioavailability and stability, comprising encapsulating Quercetin within a Nanostructured Lipid Carrier (NLC) prepared using Compritol 888ATO and Transcutol HP, as claimed in claim 2. The NLC's reduced particle size and polydispersity index facilitate improved absorption and prolonged release of Quercetin, enhancing its therapeutic effectiveness.