Influence of polymer and surfactant-based precipitation inhibitors on supersaturation-driven absorption of Ibrutinib from high-dose lipid-based formulations.

There is a growing pharmaceutical interest in supersaturated lipid-based formulations (Super-LbF) as an innovative strategy to enhance drug loading capacities while simultaneously reducing pill burden. This approach involves increasing the drug concentration above its equilibrium solubility in a lipid solution, achieved through temperature-induced supersaturation or the dissolution of lipophilic ionic salts. However, the physical instability and potential drug precipitation upon the dispersion of LbF remain critical.

Development of 3-indolyl substituted phenyl pyrazolo-carboxamide hybrids as potential type II VEGFR-2 inhibitors and in vitro cytotoxicity studies.

The progression of tumors is intricately linked to angiogenesis, the formation of new blood vessels, driven primarily by the release of growth factors such as Vascular Endothelial Growth Factor (VEGF). Targeting VEGF signaling through its receptor kinase (VEGFR-2) has emerged as a promising anti-angiogenic strategy for cancer therapy. In this study, we designed and synthesized a series of novel chemical entities based on 3-indolyl substituted phenyl pyrazole-carboxamides through docking studies upon considering the structure of sorafenib and its pattern of type II inhibition of VEGFR-2.

Traditional uses, phytochemistry, pharmacology, and nutraceutical potential of horse gram (Macrotyloma uniflorum): A systematic review.

Macrotyloma uniflorum is known for being a rich source of protein, fat, fiber, carbohydrates, vitamins, and micronutrients. Since ancient times, it has been used as a pulse and traditional remedy in the Himalayan Mountains for curing kidney and bladder stones, bronchitis, asthma, piles, leukoderma, and heart diseases. Horse gram contains bioactive compounds such as phenolic acids, flavonoids, and tannins, which contribute to its health advantages.

Memantine Alleviates PTSD-like Symptoms and Improves Dendritic Arborization through Modulation of the HPA Axis and Neuroinflammation in Rats.

Post-traumatic stress disorder (PTSD) poses significant neurological and psychiatric challenges. Investigations into the glutamatergic system, particularly the N-methyl-D-aspartate (NMDA) receptor, are crucial for understanding PTSD mechanisms. This study aimed to evaluate the therapeutic potential of the non-competitive NMDA receptor antagonist memantine in mitigating PTSD symptoms and to explore its underlying cellular and molecular impacts.

Diagnosing Respiratory Variability: Convolutional Neural Networks for Chest X-ray Classification Across Diverse Pulmonary Conditions.

The global burden of lung diseases is a pressing issue, particularly in developing nations with limited healthcare access. Accurate diagnosis of lung conditions is crucial for effective treatment, but diagnosing lung ailments using medical imaging techniques like chest radiograph images and CT scans is challenging due to the complex anatomical intricacies of the lungs. Deep learning methods, particularly convolutional neural networks (CNN), offer promising solutions for automated disease classification using imaging data.

Capsaicin nanocrystals burdened topical polymeric gel: An encouraging tactic for alleviation of paclitaxel-induced peripheral neuropathy.

Chemotherapy-induced peripheral neuropathy (CIPN) is triggered by clinically recommended chemotherapeutics. Topical capsaicin (CAP) is a US-FDA-approved therapeutic entity for the mitigation of CIPN. Besides good skin permeation efficiency, CAP concentration in a topical dermal dosage form must be controlled due to its dose-dependent therapeutic and adverse effects.

Exploring role of citrus fruits in comorbid neurodegenerative disorders associated with psoriasis.

A neurodegenerative illness is a disorder in which the brain and/or spinal cord's neurons, or nerve cells, gradually deteriorate and disappear. These illnesses often get worse with time and can seriously affect movement, cognition, and other neurological functions. Psoriasis is a long-term autoimmune skin condition marked by fast skin cell growth that results in red, elevated areas coated in silvery-white scales.

Discovery of novel hybrid tryptamine-rivastigmine molecules as potent AChE and BChE inhibitors exhibiting multifunctional properties for the management of Alzheimer's disease.

Contemporary research evidence has corroborated a gradual loss of central cholinergic neurons in Alzheimer's Disease (AD). This progressive deterioration leads to cognitive dysfunction and impaired motor activity, culminating in the brain cell's death in the disease. The approved drugs for AD treatment can only offer relief from symptoms without addressing the underlying pathological hallmarks of the disease.

Aminocarbonylation using CO surrogates.

Aminocarbonylation reactions play a critical role in the synthesis of amides. Traditional aminocarbonylation processes often rely on carbon monoxide (CO) gas, a highly toxic and challenging reagent to handle. Recent advancements in CO surrogates address these challenges.

Development of bioengineered 3D patient derived breast cancer organoid model focusing dynamic fibroblast-stem cell reciprocity.

Three-dimensional (3D) models, such as tumor spheroids and organoids, are increasingly developed by integrating tissue engineering, regenerative medicine, and personalized therapy strategies. These advanced 3Dmodels are not merely endpoint-driven but also offer the flexibility to be customized or modulated according to specific disease parameters. Unlike traditional 2D monolayer cultures, which inadequately capture the complexities of solid tumors, 3D co-culture systems provide a more accurate representation of the tumor microenvironment.

Biomimetic Approach for Optimal Designing of the Shape and Controlled Release of Therapeutics from Tricompartmental Microcarriers for Managing Parkinson's Disease.

Inspired by the intricate cellular morphology and the discoid shape of red blood cells (RBCs), biomimetic tricompartmental microcarriers (TCM) with controlled release profiles were engineered using an electrohydrodynamic--jetting technique for efficient management of Parkinson's disease (PD). While jetting, Levodopa (LD), CD (Carbidopa), and ENT (Entacapone) (3 PD drugs) were directly encapsulated in the three individual compartments of the TCM used for oral administration. The optimal shape and controlled release profiles were obtained by employing the Taguchi orthogonal L9 design-of-experiment approach by systematically varying the processing parameters, i.

Role of Flavonoids in Mitigating the Pathological Complexities and Treatment Hurdles in Alzheimer's Disease.

With the passage of time, people step toward old age and become more prone to several diseases associated with the age. One such is Alzheimer's disease (AD) which results into neuronal damage and dementia with the progression of age. The existing therapeutics has been hindered by various enkindles like less eminent between remote populations, affordability issues and toxicity profiles.

Forced Degradation Study of an Anti-Diabetic Drug Imeglimin: Impurity Profiling and Structure Elucidation Using LC-Q-ToF-MS/MS and NMR.

Rationale: The present study aims to establish structures of the degradation products of an anti-diabetic drug, Imeglimin (IMG) approved for the treatment of type 2 diabetes mellitus in the year 2021. Degradation pathways are proposed along with in silico toxicity assessments of the observed degradation products (DPs) of the drug.

Methods: A reversed-phase high-performance liquid chromatography (RP-HPLC), equipped with a photodiode array detector, was used to separate the observed DPs with a Phenomenex Luna PFP (250 × 4.

Revisiting the Emerging Role of Light-Based Therapies in the Management of Spinal Cord Injuries.

The surge in spinal cord injuries (SCI) attracted many neurobiologists to explore the underlying complex pathophysiology and to offer better therapeutic outcomes. The multimodal approaches to therapy in SCI have proven to be effective but to a limited extent. The clinical basics involve invasive procedures and limited therapeutic interventions, and most preclinical studies and formulations are yet to be translated due to numerous factors.

Combination Therapy for Post-Kala-Azar Dermal Leishmaniasis: A Literature Review of Current Evidence.

Post-kala-azar dermal leishmaniasis (PKDL) is a neglected skin disease that has tremendous epidemiological significance as a reservoir of Leishmania parasites. Relapse, drug resistance, non-compliance to prolonged treatment, poor health-seeking behaviour, along with limited therapeutic options pose a significant impact on the management of PKDL. In this study, we aimed to review the efficacy, safety and tolerability data of combination therapies for PKDL in the published literature.

Costus igneus: A Versatile Herbal Remedy for Multiple Health Conditions.

Costus igneus, commonly known as the insulin plant, is a potent medicinal herb with a wide range of pharmacological activities. Traditionally used in diabetes management, recent studies have highlighted its antidiabetic, antioxidant, antimicrobial, hepatoprotective, and kidney stone-inhibitor properties. Phytochemical analyses reveal the presence of saponins, flavonoids, alkaloids, steroids, and terpenoids, which contribute to its therapeutic effects.

Molecular signature-based labeling techniques for vascular endothelial cells.

Vascular endothelial cells (VECs) play a crucial role in the development and maintenance of vascular biology specific to the tissue types. Molecular signature-based labeling and imaging of VECs help researchers understand potential mechanisms linking VECs to disease pathology, serving as valuable biomarkers in clinical settings and trials. Labeling techniques involve selectively tagging or marking VECs for visualization.

Effect of ethyl acetate extract of the whole plant Clerodendrum phlomidis on improving bleomycin (BLM)-induced idiopathic pulmonary fibrosis (IPF) in Rats: In vitro and in vivo research.

Idiopathic pulmonary fibrosis (IPF) is a prevalent chronic lung condition of unknown etiology characterized by fibrosis and inflammation. Lung scarring progresses owing to cytokines and immune cells that promote inflammation and fibrosis in idiopathic pulmonary fibrosis (IPF). The anti-inflammatory and anti-fibrotic properties of the ethyl acetate extract of Clerodendrum phlomidis (CPEA), derived from the Indian plant "agnimantha," are recognized in traditional Ayurvedic medicine.

Evaluation of 1-vinyl-3-alkyl imidazolium-based ionic liquid monomers towards antibacterial activity: An in-silico & in-vitro study.

In this study 1-vinyl-3-alkyl imidazolium-based ionic liquid monomers (ILs) with different alkyl chain lengths {R = hexyl (A), octyl (B) and decyl (C)} have been synthesized for antibacterial applications. The prepared ILs have been characterized using UV, FT-IR and NMR spectroscopy. The antibacterial activities of the synthesized ILs against Staphylococcus aureus (S.

Biopharmaceutical and pharmacokinetic attributes to drive nanoformulations of small molecule tyrosine kinase inhibitors.

Buoyed by the discovery of small-molecule tyrosine kinase inhibitors (smTKIs), significant impact has been made in cancer chemotherapeutics. However, some of these agents still encounter off-target toxicities and suboptimal efficacies due to their inferior biopharmaceutical and/or pharmacokinetic properties. Almost all of these molecules exhibit significant inter- and intra-patient variations in plasma concentration-time profiles.

Fabrication of lactoferrin-chitosan-etoposide nanoparticles with melatonin via carbodiimide coupling: In-vitro & in-vivo evaluation for colon cancer.

This study presents the development of melatonin-coated lactoferrin-chitosan nanoparticles (ETP-CS-LF-MLT-NPs) using ionic gelation and carbodiimide coupling for colorectal cancer treatment. The nanoparticles were characterized by an average size of 208.7 ± 1.

Protective Effects of NRF2 Activator Sulforaphane in Polyinosinic:Polycytidylic Acid-Induced In Vitro and In Vivo Model.

NRF2 is a nuclear transcription factor involved in the cellular protection against oxidative stress and inflammatory signaling. Sulforaphane is a known NRF2 activator used for its strong antioxidant and anti-inflammatory activity through regulation of Keap-1-HO-1 pathway. However, there is a limited exploration about the role of NRF2 activator, sulforaphane in regulation of poly(I:C)-induced oxidative stress, inflammation and injury in lung.

Bifunctional Oxaliplatin (IV) Prodrug Based pH-Sensitive PEGylated Liposomes for Synergistic Anticancer Action Against Triple Negative Breast cancer.

Triple negative breast cancer (TNBC) exhibits higher susceptibility towards oxaliplatin (OXA) due to a faulty DNA damage repair system. However, the unfavorable physicochemical properties and risk of toxicities limit the clinical utility of OXA. Therefore, to impart kinetic inertness, site-specific delivery, and multidrug action, an octahedral Pt(IV) prodrug was developed by using chlorambucil (CBL) as a choice of ligand.