Kumar Shiva Gubbiyappa

• Doctor of Pharmacy
• Professor & Principal at GITAM University

Objective: The objective of the present research is to develop, analyze, and evaluate the cytotoxic effects of nanobubbles loaded with irinotecan and sunitinib for colorectal cancer therapy. Methods: Drug-loaded dextran sulfate nanobubbles were formulated using the emulsification technique and the prepared nanobubbles were evaluated for qualitative...

Background In the present study, a new and sensitive UPLC method for stability-indicating study has been established and validated as per the ICH guidelines. To date, no work has been reported on the forced degradation studies of alpelisib using the UPLC technique. Box–Behnken design was used to study the response surface for method optimisation to...

Objective: The use of dextran nanobubbles is aimed at function as a delivery system for drugs like sunitinib. These specially designed nanobubbles enhance the drug's solubility, stability, and bioavailability, thus improving the therapeutic effectiveness. Moreover, they offer controlled release characteristics and can potentially enhance drug deliv...

Background Piperidines are among the essential synthetic fragments for designing drugs and play a significant role in the pharmaceutical industry. The synthesis of newer derivatives by incorporating different amines paves the way for the introduction of novel drug combinations for current cancer treatments. Method The new combinations of 1-(4-brom...

Objective: A unique liquid chromatography-mass spectrometry technique is essential for determining the concentration of asciminib in biological matrices, and its development is of the utmost importance. Methods: The samples that were processed were separated using a Reversed Phase-Phenomenex (100 mm x 4.6 mm, 5 µm) C18 analytical column. The column...

The objective of the present research is to develop, analyze, and evaluate the cytotoxic effects of nanobubbles loaded with irinotecan and sunitinib for colorectal cancer therapy.Drug loaded dextran sulfate nanobubbles were formulated using the emulsification technique and the prepared nanobubbles were evaluated for qualitative and quantitative par...

Alzheimer’s malady (Advertisement) is neurodegenerative disarranges that have developed as among the genuine wellbeing issues of the 21st century. The drugs as of now accessible to treat Advertisement have restricted adequacy and are related with side impacts. Characteristic items are one of the foremost imperative and traditionalist sources of sol...

The anticancer drug lurbinectedin was measured in plasma samples using a newly designed and validated LC-ESI-MS/MS method. The drug’s examination was conducted using ledipasvir as the internal standard. Following the liquid liquid extraction of 200 μL of plasma, the samples were separated using a ZorbaxSB (25 0mm x4.6 mm, 5 µm)C18 column. The mobil...

Objective: The present investigation explored the binding affinities of phytoconstituents present in Indigofera prostrata and lantana camara that acted as Anti-Alzheimer's drug. Also the phytoconstituents were identified by Gas chromatography–Mass spectrometry (GC-MS) against selected targets, i. e., β-amyloid and acetylcholinesterase (AchE). Metho...

The chemical flexibility of the pyrrolidine nucleus and its ability to generate a wide range of structural variations may have a significant impact on the therapeutic effectiveness. In present study, 17 analogs of 1-(4-bromo-2-(pyrrolidin-1-yl)benzyl)pyrrolidin-3-amine (7a-q) were synthesized and characterized. All the synthesized compounds were pu...

Chemotherapeutic experts have been utilised to cure a variety of disorders, but their practical application is restricted due to their regrettable selectivity and outrageous fundamental optional effects. Short single-stranded DNA or RNA oligonucleotides known as aptamers are released from randomised libraries and have strong propensity and differen...

Objective: The research aims to enhance poorly water-soluble drug Simvastatin (SMV) solubility and bioavailability by solid dispersion (SD) using various sugar carriers like lactulose, xylitol, Sorbitol, and soluplus. Methods: First, the drug was subjected to determine bulk density, carr’s index, Hausner’s ratio, angle of repose, solubility analysi...

Objective: Pemigatinib is an active component in treatment of cholangiocarcinoma, but the low solubility and bioavailability of Pemigatinib limit its wide application. The aim of the present study was to prepare and evaluate supersaturable self-nanoemulsifying drug delivery systems (sSNEDDS) followed by investigating and comparing the pharmacokinet...

A specific, linear and accurate LC-MS/MS method was developed for the determination of febuxostat in human K2 EDTA plasma and it was successfully applied for the pharmacokinetic study in wister rats. Chromatographic isolation of febuxostat and febuxostat D9 were attained on Purosphur C18, 100 × 4.6 mm, 5 μ column with 1.0 mL/min flowing rate. The t...

Entrectinib is a novel potent anticancer drug with poor aqueous solubility. A supersaturable self-nanoemulsifying drug delivery system of entrectinib is developed using a super saturation promoter. The components of the isotropic mixture of SNEDDS were selected based on solubility and emulsification study. The optimum composition was identified usi...

Irbesartan (IRB), an angiotensin II receptor AT1 blocker, is an antihypertensive agent commonly used with Sitagliptin (STG), a novel antidiabetic agent in diabetes. A finalised and validated LC-MS/MS method was used for the bioanalytical quantification of STG and IRB to be applicable to studies on the P.K drug-drug interactions between STG and IRB....

Background: A novel, sensitive and specific LC-MS/MS technique was developed and validated for the quantification of fostemsavir in human plasma and its pharmacokinetic application in rabbits. Methods: Chromatographic separation of the fostemsavir and fosamprenavir (internal standard) were achieved on Zorbax C18 (50 mm × 2 mm × 5 μm) column with...

A novel, sensitive, and specific LC-MS/MS technique was developed for the quantification of Relugolix in plasma and validated as per the regulatory guidelines. Elution of Relugolix and Canagliflozin was achieved on Inertsil C18 (150mm × 2.10mm i.d, 5.0 μm particles size) column with acetonitrile and 0.1% HCOOH as a mobile phasic system in the fract...

A new accurate LC–MS/MS methodology was needed for the simultaneous quantitation of remogliflozin etabonate and metformin in plasma samples. Chromatography was executed with BDS-Hyoersil, C18 (50mm×4.60mm, 5.0µ) reverse phasic analytical stationary system with movable solvent comprising of 0.10% HCOOH, methyl alcohol, and acetonitrile in the fracti...

The aim of present work is to develop cost effective, selective, precise and sensitive LC-MS method for the estimation of Lefamulin in rat plasma. The chromatographic separation of Lefamulin was successfully achieved with Zorbax Symmetry C18, (150mm x 4.6mm, 3.5µ) column and using mobile phase of 0.1%v/v formic acid: Acetonitrile (70:30 v/v) at a f...

Background: To develop a simple and accurate method for the determination of Darunavir in human plasma by liquid-liquid extraction method with Verapamil as an internal standard using UPLC-MS/MS. Methods: The separation was achieved on Agilent, Zorbax XDB C18 (2.1 x 50 mm ID, 5 μm) column. The samples were chromatographed using the mobile phase cons...

Background Pemigatinib is a small molecule tyrosine kinase inhibitor of fibroblast growth factor receptor inhibitors. The oral bioavailability of Pemigatinib is constricted due to its limited solubility at physiological pH. It is essential to develop a novel formulation of Pemigatinib to improve the intrinsic solubility and to reduce the pharmacoki...

The current research focuses on identifying the bioactive compounds from Ethanolic extraction of Cochlospermum religiosum and Justicia betonica by GC-MS technique followed by phytochemical screening. The ethanolic extraction of Cochlospermum religiosum and Justicia betonica revealed the presence of various components. The GC-MS results indicated th...

Objective: Cyclodextrin nanosponges have unfolded themselves as budding delivery aids for intractable molecules that face difficulty in formulation. Methods: The present research aimed at the preparation of cyclodextrin-based nanosponges employing diphenyl carbonate crosslinker as reported elsewhere. Box-Behnken design was adopted to evaluate the e...

Introduction The current research aims to formulate a controlled release formulation of Actarit utilizing cyclodextrin based nanosponges as a nanocarriers. β-Cyclodextrin built nanosponges were prepared by condensation reaction using diphenyl carbonate as crosslinking agent. Method A 3-level, 3-factor Box-Behnken design was used to optimize the re...

A simple, accurate, and precise method for estimating Aspirin, Atorvastatin, and Ramipril in Tablet dosage form was developed. Symmetry C18 (150 x 4.6 mm, 3.5) was used to run the chromatogram. At a flow rate of 1.0 ml/min, a mobile phase containing potassium dihydrogen ortho phosphate (pH adjusted to 3) and Methanol in the ratio 35:65 was pumped t...

The most fundamental important extensive constitutive of drug molecules to be available for systemic absorption is aqueous solubility; subsequently, that is the nature of GIT fluid. When the drug molecules become solubilized, it has to reach the systemic circulation via the biological membrane. The solubility problem of many effective pharmaceutica...

Lipid-based drug delivery systems are extensively reported in the literature for enhancing drug solubility, permeability, and bioavailability. Self-nanoemulsifying drug delivery systems (SNEDDS) are a superior strategy for enhancing solubility and bioavailability of poorly water-soluble compounds and the most prevailing and commercially viable oil-...

Carbon dots (CDs) have emerged as a potential material in the multifarious fields of biomedical applications due to their numerous advantageous properties including tunable fluorescence, water solubility, biocompatibility, low toxicity, small size and ease of modification, inexpensive scale-up production, and versatile conjugation with other target...

Among various epithelial-to-mesenchymal transition (EMT)-related transcription factors (TFs), altered expression levels of Snail-1, Snail-2/Slug, Twist, and ZEB1 have shown a significant association in different cancers having a higher risk of metastasis. However, their role in the circulation of endometriosis patients is not well understood. Hence...

Sepsis aggregates undesirable immune response causing depression of ventricular myocardium and diastolic dysfunction. This present study examined the effect of a plant-derived flavone tangeretin (TG) on autophagy and reduction in myocardial dysfunction. The sepsis was induced by cecum ligation and puncture (CLP) in male Sprague–Dawley rats. Abnorma...

Li P, Bukhari SNA, Khan T, et al. Int J Nanomedicine. 2020;15:9115–9124. The Editor and Publisher of International Journal of Nanomedicine wish to retract the published article. Concerns were raised regarding the alleged duplication of H&E images in Figure 4. Specifically, Figure 4A, Control, appears to have been duplicated with the same image for...

Background A simple and sensitive quantitation analytical technique by liquid chromatography–tandem mass spectrometry (LC-MS/MS) is essential for fedratinib in biological media with kinetic study in healthy rabbits. Objective The main objectives of the present research work are to LC-MS/MS method development and validate procedure for the quantita...

Multiple effects on cancer cells are exerted by the peroxisome proliferator-activated receptor γ (PPAR-γ). Recent studies have shown that rosiglitazone, a synthetic PPAR-γ ligand, inhibits the growth of cells. This research was designed to assess the impact of rosiglitazone on diethylnitrosamine (DENA)-induced lung carcinogenesis in Wistar rats and...

Background: Rheumatoid arthritis (RA) is associated with joint damage. Effectiveness of embelin has been established in a wide variety of inflammatory disorders, but its utility as a therapeutic agent is limited by its poor absorption, rapid metabolism, and fast systemic elimination. To apprehend these limitations, we propose to use highly bioavai...

Rheumatoid arthritis (RA) is a chronic and accelerated autoimmune illness with proliferative and damaging synovitis, resulting in joint death and cartilage and bone erosion. This study focused on the potential therapeutic effect of wogonin on complete Freund's adjuvant (CFA) induced RA in rats and the underlying mechanisms. Arthritis was experiment...

Dipeptidyl peptidase‐4 inhibitor (DPP‐4 inhibitor) such as sitagliptin has been presented as antidiabetic drugs and has numerous restorative advantages over different diseases; however, its defensive role against aflatoxin b1 (AFB1) liver toxicity has not been previously examined. Wistar rats (65 weeks, male) were utilized in the investigation. Ani...

Homocysteine [HSCH2CH2CH(NH2)COOH] (Hcy), is a sulfur‐containing amino acid of 135.18 Da of molecular weight, generated during conversion of methionine to cysteine. If there is a higher accumulation of Hcy in the blood, i.e. usually above 15 µmol/L, it leads to a condition referred to as hyperhomocysteinemia. A meta‐analysis of observational study...

A reverse phase high performance liquid chromatography (RP HPLC) method was developed and validated for the simultaneous estimation of atenolol and chlorthalidone in marketed formulation. The determination was carried out on an Xterra RP8 (150 x 4.6 mm, 5 µm) column using a mobile phase of potassium dihydrogen phosphate buffer solution: methanol (5...

Major challenges of dealing elder patients with diabetes mellitus (DM) are the individualization of consideration in persons with various comorbid types of conditions. In spite of the fact that microvascular and macrovascular problems associated with DM are well documented, there is only a few numbers of reports viewing different conditions, for ex...

The current study is a review of the literature on patients with diabetes who are diagnosed with colorectal cancer (CRC), encompassing recent research on CRC and the molecular level changes occurring in these patients on the basis of varying environmental as well as non-environmental factors. It has been noted that nearly 50% of all patients underg...

Objectives: Flipped classroom (FC) is a pedagogical model to engage students in learning process by replacing the didactic lectures. Using technology, lectures are moved out of the classroom and delivered online as means to provide interaction and collaboration. Poll Everywhere is an audience response system (ARS) which can be used in an FC to make...

India has rich tradition of plants based knowledge on healthcare. The aim of present study to assess the wound healing activity of various extracts of Acacia suma Roxb. leaf (Fabaceae). The chloroform, ethanol and aqueous extracts of A. suma leaves were evaluated for their wound healing activities in rats using excision and incision wound models re...

A selective, specific and sensitive stability-indicating high-performance liquid chromatographic method was developed and validated for the determination of Tamsulosin in in pharmaceutical dosage forms. Celecoxib was used as Internal Standard (IS). The chromatographic conditions comprised of a reversed-phase Lichrocart / Lichrosphere C18 column (25...

Propionibacterium acnes and Staphylococcus epidermidis have been recognized as pus-forming bacteria triggering an inflammation in acne. The present study was conducted to evaluate antimicrobial activities of Indian medicinal plants against these etiologic agents of acne vulgaris. Ethanolic extracts of Hemidesmus indicus (roots), Eclipta alba (fruit...