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result(s) for
"Patil, Archana S."
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Enhanced bioavailability of Quercetin-loaded niosomal in situ gel for the management of Parkinson’s disease
by
Patil, Priyanka
,
Karishetti, Reshma
,
Revankar, Abhishek A.
in
Animal models
,
Anti-inflammatory agents
,
Bioavailability
2025
Parkinson's disease (PD) is the second most prevalent neurological disorder, characterized by motor symptoms such as tremor and rigidity due to the degeneration of dopaminergic neurons in the substantia nigra. This study investigates the formulation of quercetin, a natural bioflavonoid with potent antioxidant and anti-inflammatory properties, as niosomes for intranasal delivery to enhance its bioavailability and therapeutic potential for PD.
The niosomal formulation was optimized for critical parameters including particle size, entrapment efficiency, and zeta potential. Male Wistar rats were utilized to assess the effects of quercetin-loaded niosomes on motor function, dopaminergic neuron protection, and oxidative stress alleviation.
The optimized niosomal formulation exhibited a particle size of 195 nm, a polydispersity index (PDI) of 0.29, a zeta potential (ZP) of -30.63 mV, and an entrapment efficiency (EE) of 82.77%.
evaluations conducted using the haloperidol-induced PD model revealed significant enhancements in behavioural, biochemical, and histopathological outcomes when compared to both disease controls and the standard treatment group. Additionally, short-term stability tests confirmed the robustness of the formulation.
The findings suggest that the quercetin-loaded niosomal formulation offers improved drug delivery and efficacy, indicating its potential as a superior treatment option for PD compared to conventional dosage forms. This approach may pave the way for enhanced therapeutic strategies targeting the neurodegenerative processes underlying Parkinson's disease.
Journal Article
Omega-3 fatty acids: a comprehensive scientific review of their sources, functions and health benefits
by
Bhat, Chetan T.
,
Patted, Pradnya G.
,
Masareddy, Rajashree S.
in
Alzheimer's disease
,
Cancer
,
Carbon
2024
Background
In recent years, public awareness of healthy diets has significantly increased, leading to a rise in the consumption of nutritional supplements. Among these, omega-3 fatty acids have become particularly popular.
n
− 3 polyunsaturated fatty acids (PUFAs) are widely distributed in marine and terrestrial environments. The primary sources of marine
n
− 3 fatty acid supplements are oily fish, such as anchovies, sardines and mackerel. Recently, they have drawn considerable attention for their potential therapeutic benefits in treating a range of illnesses, including cancer, neurological disorders, cardiovascular diseases, immunological and reproductive diseases, respectively.
Main text
This study explores the many activities of
n −
3 PUFAs, highlighting their importance in cellular processes that include signaling pathways, cell membrane integrity and structural maintenance. These fatty acids significantly regulate important physiological functions including the neurological system, blood pressure control, hematopoiesis, glucose metabolism and inflammatory responses. The latter highlights the wide therapeutic range of
n −
3 PUFAs is especially notable considering the implications for controlling inflammatory disorders. Furthermore, the chemistry and dietary sources of omega-3 fatty acids are clarified in this review, which also sheds light on the complex molecular pathways that support the therapeutic efficacy of these fats and their bioavailability. The most recent information on the FDA's approval of omega-3 oils for use in formulation development highlights the compounds' adaptability and potential influence on the development of novel medications.
Conclusion
A thorough analysis of omega-3 polyunsaturated fatty acids reveals both their remarkable therapeutic potential against a variety of diseases and their essential place in a normal diet. This study adds to the increasing amount of data that supports the use of
n
− 3 PUFAs in preventative and therapeutic approaches that are meant to improve human health and well-being by clarifying their mechanisms of action and emphasizing their applicability in formulation and development.
Journal Article
Phytochemical Evaluation and Screening of Anti-Depressant and Anxiolytic Activities of Bacopa monniera in rats
by
Gandla, Kumaraswamy
,
Mayasa, Vinyas
,
Nelson, Vinodh Kumar
in
Animal cognition
,
Antidepressants
,
Antifungal agents
2024
Around 21% of the global population suffers from MDD, making it one of the most common mental disorders. People who take antidepressant medications often are more likely to experience undesirable effects such as hypoplasia, cardiovascular toxicity, decreased libido, obesity, and sleep disorders. Studies investigating the potential medicinal benefits of natural remedies for psychiatric diseases have gained increasing attention throughout the past decade. The ethanolic extract of Bacopa monnieri (EEBM) was evaluated for potential anti-depressant effects and anxiolytic activityin animal models. The different phytochemical constituents like Alkaloids, steroids, triterpenoids, tannins and phenolic compounds, saponins were identified. Acute toxicity trials were performed in accordance with OECD standards 425, and the EEBM was shown to be safe at doses up to 2000mg/kg body weight. In vivoanti-depressant activity was conducted utilizing experimental procedures involving animal models, namely testing, TST, and FST.From the study and results, it was observed that the effect of Bacopa was significant and comparable to reference standards.
Journal Article
Apigenin-Loaded Stealth Liposomes: Development and Pharmacokinetic Studies for Enhanced Plasma Retention of Drug in Cancer Therapy
by
Jalalpure, Sunil S.
,
Shetti, Priya
,
Kaur, Kirtanjot
in
Animals
,
Anticancer properties
,
Antitumor activity
2024
Apigenin belongs to the class of compounds known as flavones. It possesses significant antioxidant, anti-inflammatory, and antitumor potential in various preclinical studies. Despite being a potent anticancer molecule, it suffers from significant pharmacokinetic limitations. As per Biopharmaceutical classification system, Apigenin has been categorized as a Class II drug. It has high permeability but low solubility which leads to lower bioavailability. To increase its bioavailability, it has to raise its solubility. Thus, the present work aimed to develop novel Apigenin loaded stealth liposomes to enhance its solubility, plasma residence time and better therapeutic efficacy. Apigenin loaded stealth liposomes (APISL) were prepared by utilizing the ethanol injection technique. The formulation was statistically optimized by DOE and evaluated for particle size, zeta potential, entrapment efficiency, morphology, in-vitro drug release study, in-vivo pharmacokinetic study and stability study. Among all of the preparations, the optimized stealth liposomal batch (APISL-L8) produced the best outcomes, with smallest particle size, the highest percent entrapment efficiency and the highest drug release percent at 48 h. The optimized Apigenin loaded stealth liposomes L8 was found to show higher percent drug release than the plain Apigenin as per Higuchi release model. According to in-vivo experiments, stealth liposomes had a longer exposure period in comparison to pure drug solution. When compared to standard drug, investigations revealed that Apigenin-loaded stealth liposomes demonstrated better plasma retention time and stability. Thus, the result reveals that, the Apigenin-loaded stealth liposome demonstrated an improved bioavailability with enhanced antitumor efficacy in the treatment of breast cancer.
Graphical Abstract
Journal Article
Fabrication of Polyisobutene Based Matrix Patches for Transdermal Delivery of Atenolol
by
S. Masareddy, Rajashree
,
S. Kamat, Shriraj
,
M. Dandagi, Panchaxari
in
Adhesives
,
Cellulose
,
Drug delivery systems
2023
One of the possible routes for local and systemic delivery of hypertensive drugs has been identified as transdermal administration. Monolithic drugs in adhesive patches have the advantages of being relatively simple to manufacture and having limited dimensions of both thickness and surface area. Polyisobutene is a pressure-sensitive adhesive polymer often used in transdermal patch preparation. Polyisobutenes with varying molecular weight distributions have differing viscosities, which can affect drug release. In the current study, Atenolol transdermal patches were made with different proportions of low and high molecular weight polyisobutene and ethyl cellulose as a thickening agent. Prepared patches were evaluated for their physicochemical properties like thickness, weight variation, folding endurance, tensile strength, moisture content, drug content and in- vitro permeation rate. Based on tensile strength (1.92kg/mm2), folding endurance (343) and in-vitro permeation rate (85.79%) at the end of 30th hour, F1 formulation was found to be optimum. Ex vivo permeation study was carried out using rat skin and 67.09% drug permeated at the end of 30th hour. Formulations were subjected to stability studies for 60 days and were found to be stable. Thus, an ideal combination of polyisobutenes in the ratio 3:1 (High Molecular Weight: Low Molecular Weight) and ethyl cellulose (200mg) would serve as the best choice for fabrication of Atenolol patches for its sustained effect.
Journal Article
Development of Bimatoprost-Loaded Nano Spanlastic In-Situ Gel for Ophthalmic Drug Delivery: A Box-Behnken Optimization Approach with In Vitro and Ex Vivo Characterization
by
Patted, Pradnya
,
Masareddy, Rajashree
,
Chougule, Krutuja R.
in
Aluminum
,
Bioavailability
,
Biochemical Engineering
2025
Purpose
The present study aimed to develop and optimize a Bimatoprost-loaded spanlastic in-situ gel to enhance precorneal retention, corneal penetration, and therapeutic efficacy while minimizing ocular side effects.
Methods
Spanlastic vesicles were prepared using the ethanol injection method and optimized using a 3³ Box-Behnken design. The optimized formulation was characterized for morphology using transmission electron microscopy (TEM), particle size, entrapment efficiency, and drug-excipient compatibility using FTIR and DSC. The in-situ gel was formulated using 18% poloxamer 407 and evaluated for viscosity, gelling capacity, and drug content. Drug release kinetics, ex vivo corneal permeation through goat cornea, and ocular irritation using the HET-CAM assay were assessed. Sterility, isotonicity, and stability studies were also conducted.
Results
TEM analysis revealed uniform spherical vesicles with a mean particle size of 156.1 ± 0.82 nm. The vesicles demonstrated high entrapment efficiency and compatibility with excipients. The in-situ gel exhibited favourable viscosity of 610 ± 1.09 cps, rapid gelation, and high drug content of 99.52 ± 1.28%. Drug release followed a sustained pattern best described by the Korsmeyer-Peppas model. Ex vivo studies showed enhanced corneal permeation of 89.56% for 8 h, while HET-CAM assays indicated minimal ocular irritation. The optimized formulation (SPs-ISG 18%) was sterile, isotonic, and stable at room temperature.
Conclusion
The developed Bimatoprost-loaded spanlastic in-situ gel demonstrates promising potential as a safe and effective ocular delivery system for glaucoma management, offering improved corneal penetration and sustained release.
Journal Article
Exploring the Solvent-Anti-solvent Method of Nanosuspension for Enhanced Oral Bioavailability of Lovastatin
2021
Lovastatin is an antilipidemic drug that belongs to the class of statins that has poor oral bioavailability due to its low solubility and variable dissolution rate. The main aim of this study was to enhance the solubility and dissolution rate of the drug and understand its oral bioavailability.
Lovastatin nanosuspension was formulated using a solventanti-solvent method using a probe sonication technique. A nanosuspension was prepared, using hydroxypropyl methylcellulose (HPMC) K15M and pluronic F68 as stabilizers. The formulated nanosuspensions were characterized for particle size, polydispersity index (PDI) zeta potential, surface morphology, and
release rate. Further, an
bioavailability study and stability studies were also performed.
Optimized formulation showed a particle size of 127±0.01 nm, a PDI of 0.492±0.001, and a zeta potential of -37.9 mV, which indicates good stability. Morphological study showed that the particles were in the nano range. The drug content was found to be in the range of 73-87%.
release revealed much faster release of the drug in one hour compared to the pure drug and its marketed formulation.
bioavailability study was carried out in Wistar rats, which showed improvement in bioavailability by approximately 2.5 folds compared with the marketed formulation. Stability studies indicated that the optimized formulation F2 was more stable at 4°C±2°C.
The prepared lovastatin nanosuspension showed improvement in solubility, dissolution rate, and oral bioavailability compared to the pure drug and its marketed formulation. Hence, lovastatin nanosuspension may be a potentially valuable tool for improving the oral bioavailability of lovastatin.
Journal Article
Effect of deposition potential and time substitution for Co(OH)2 on controlled synthesis and electrochemical performance for electrochemical supercapacitor
by
Dhas, Suprimkumar D.
,
Bhosale, Tushar T.
,
Patil, Raviraja T.
in
Characterization and Evaluation of Materials
,
Chemistry and Materials Science
,
Cobalt
2023
Interconnected nanoflakes of cobalt hydroxide Co(OH)
2
were deposited potentiostatically on nickel mesh (NM) at various potentials (− 0.9 V, − 1.0 V, − 1.1 V) and various times (1 min, 2 min, 3 min, 4 min, and 5 min). The FE-SEM, XRD, FT-IR, and EDS etc. studied the morphological and structural properties. The electrochemical properties evaluated in 1 M KOH electrolyte using cyclic voltammetry (CV), galvanostatic charge–discharge (GCD), and electrochemical impedance spectroscopy (EIS) techniques. The Co(OH)
2
nanoflakes deposited on nickel mesh with − 1.0 V for 5 min. electrode exhibits a good specific capacitance of 1035 F g
−1
, at a current density of 1 mA cm
−2
1 M KOH electrolyte. In conclusion, the deposition potential and the deposition time affect the surface morphology and the electrochemical performance of the deposited Co(OH)
2
electrode.
Journal Article
Chitosan-Graft-Poly (N-Isopropylacrylamide)Co-Polymer as a Carrier for Targeted Delivery and Enhanced Catalytic Activity of Capecitabine
by
Patil, Archana S
,
Kummara, Sivaiah
,
Ambhore, Nitin P
in
Angiogenesis
,
Antineoplastic drugs
,
Cancer therapies
2022
The efficient biodistribution and controlled release of medications or genes at specific site are made possible by the use of stimuli-responsive or intelligent polymers. Pathologically challenged tissue has fundamental qualities that are very different from those of typical, healthy cells. These characteristics have been useful in creating endostimuli-responsive nanocarriers for the efficient delivery of drug cargoes. The site-specific release of medications delivered by nanocarriers can take advantage of the tumour microenvironment's increased temperature and acidic pH. Capecitabine, is enzymatically catalysed to 5-FU, the active compound by sequential enzymatic steps with the last step catalyzed by the tumor-associated angiogenic factor thymidine phosphorylase which is more abundantly expressed in many types of human tumours than in healthy tissues catalyses. Thus, the site specific delivery of capacitabine to tumor microenvironment enhance its catalytic activity and increase the selectivity of 5-FU for tumor cells and decrease plasma levels of 5-FU. The goal of this research was to synthesize the co-polymer chitosan-g- poly (N-isopropylacrylamide) (CS-g-PNIPAm) and evaluate it as a dual responsive carrier for targeted Capecitabine delivery. For this, the co-polymer was synthesized, its responsiveness was optimized to tumour microenvironment conditions of pH and temperature. The Capecitabine was subsequently encapsulated in the synthesised co-polymer, and the physicochemical properties of the produced nanoparticles were assessed. When comparing the physiological pH and temperature to acidic pH (6.8) and higher temperature (39 °C), the in vitro stimuli driven drug release investigation found that the percent drug release was greater at acidic pH (6.8) and higher temperature (39 °C). MTT assay as well asfluorescence microscopic study demonstrated significantly increased drug release in tumor microenvironment while showed minimal effect at physiological conditions. In conclusion, the synthesizedco-polymer appear to be an an efficient dual pH and temperature responsive carrier for targeted delivery of anti-cancer drug Capecitabine to enhance its catalytic activity. Higher levels of FU are thus produced within tumours with minimal exposure of healthy tissue to FU.Graphical Abstract
Journal Article