American Journal of PharmTech Research

Isatin (1H-indole-2,3-dione) and its derivatives belong to an important class of indole-fused heterocyclic compounds. Isatin serves as a versatile intermediate for the synthesis of a wide range of biologically active heterocycles. The present work provides a detailed account of the synthesis of isatin-based Schiff bases and their corresponding thiazolidine-4-one derivatives, which can be further utilized for the development of novel heterocyclic molecules.The isatin moiety exhibits a broad spectrum of biological and pharmacological activities, including antihypertensive, analgesic, anthelmintic, antitumor, antiviral, antifungal, anticonvulsant, anti-Parkinson, anti-HIV, anti tubercular, and antioxidant activities.In the present study, a series of isatin and Schiff base derivatives were synthesized. Initially, isatin was reacted with acetaldehyde in the presence of sodium hydroxide and ethanol to yield an aldol-condensed product at the C-2 position. This intermediate was further reacted with nitro-substituted benzene diamines in ethanol under basic conditions to form Schiff base derivatives. The synthesized Schiff bases were subsequently cyclized with thioglycolic acid to obtain thiazolidine-4-one derivatives.The progress and completion of the reactions were monitored by thin-layer chromatography (TLC). The synthesized compounds were evaluated for anthelmintic activity using earthworms as the experimental model. Structural characterization of the compounds was carried out using ¹H-NMR spectroscopy and mass spectrometry, which confirmed the proposed structures.

Doxorubicin is a potent chemotherapeutic agent, but its clinical use is limited by dose-dependent cardiotoxicity, which can lead to cardiomyopathy and heart failure. This review discusses the potential of phyto constituent-based nanoformulations as cardioprotective adjuvants against doxorubicin. Encapsulating cardioprotective agents like herbal extracts, antioxidants, and anti-inflammatory co0mpounds encompassing nanoparticles enhances their bioavailability and targeted delivery to cardiomyocytes. Various nanoparticle systems including polymeric (solid lipid), inorganic (mesoporous silica, gold), and nanocomposites have shown promise in mitigating doxorubicin-induced oxidative stress, apoptosis, and cardiac injury in preclinical studies. The therapeutic effects of curcumin, resveratrol, thymoquinone, L-carnitine, and other agents were improved when delivered via nanoparticle. However, optimization of nanoparticle properties, targeted delivery strategies, long-term safety assessments, and clinical translation remain to be addressed. Nonetheless, nanoparticle-mediated delivery of cardioprotective agents holds great potential for reducing doxorubicin-associated cardiotoxicity and improving chemotherapeutic outcomes for cancer patients.

Depression is a chronic neuropsychiatric disorder characterized by emotional instability, sadness, sleep disturbances, cognitive impairment, and loss of interest in daily activities. Conventional antidepressant therapies are associated with delayed onset of action, systemic adverse effects, poor patient compliance, low bioavailability, and inadequate blood–brain barrier penetration. Advanced pharmaceutical technologies including bilayer tablet systems and nanotechnology-based drug delivery approaches have emerged as promising strategies for improving antidepressant therapy. Bilayer tablets provide immediate and sustained drug release profiles within a single dosage form, thereby improving therapeutic efficacy and patient adherence. Nanotechnology-based systems including nanoparticles, nanoemulsions, lipid carriers, and intranasal formulations improve targeted brain delivery and reduce systemic toxicity. The present review discusses depression pathophysiology, antidepressant mechanisms, bilayer tablet technologies, tablet preparation methods, evaluation parameters, marketed antidepressant formulations, and recent advancements in nano-based antidepressant delivery systems. The review further highlights the future potential of advanced pharmaceutical approaches in depression management.