Design and optimization of polyherbal tablets for anti-inflammatory therapy: A design of experiment approach with in vitro and in vivo evaluation Mahantesh Kunchanur, V.S. Mannur, Rahul Koli, Prakash Biradar Journal of Holistic Integrative Pharmacy, 2026 To develop and optimize polyherbal tablets containing Terminalia chebula , Moringa oleifera , and Ocimum sanctum as a multi-targeted therapeutic approach for the management of chronic inflammatory disorders. Polyherbal tablets were formulated and optimized using a 3 2 central composite design within a Quality by Design framework. The optimized formulation (F-11) was evaluated for physicomechanical properties, stability under ambient and accelerated conditions for 60 days, in vitro drug release of key phytoconstituents (gallic acid, stigmasterol, and rosmarinic acid), in vitro anti-inflammatory activity using the human red blood cell (HRBC) membrane stabilization assay, and in vivo anti-inflammatory efficacy using the carrageenan-induced paw edema model in Wistar rats. The optimized formulation (F-11) exhibited acceptable physicomechanical characteristics and remained stable over 60 days under both storage conditions. Sustained in vitro release was observed, with cumulative releases of gallic acid (72.47%), stigmasterol (81.20%), and rosmarinic acid (76.21%) within 180 min. The formulation demonstrated strong in vitro anti-inflammatory activity, achieving 83.63% inhibition of hemolysis at 500 μg/mL, exceeding that of diclofenac sodium. In vivo studies revealed a significant, dose-dependent reduction in paw edema comparable to the standard drug. The developed polyherbal tablets demonstrated promising anti-inflammatory efficacy, sustained phytoconstituent release, and short-term stability, supporting their potential for further development as an alternative therapeutic option for inflammatory conditions.
Novel Intranasal Fisetin-Loaded Mucoadhesive Microemulsion for Schizophrenia Management: A Nanotherapeutic Approach to Enhance Brain Bioavailability and Improved Efficacy Tamizmaran V, V. S. Mannur, Rahul Koli, Prakash Biradar Molecular Pharmaceutics, 2025 Schizophrenia, a complex neuropsychiatric disorder originating in the central nervous system, poses significant therapeutic challenges primarily due to the restrictive nature of the blood-brain barrier (BBB). In this study, a fisetin-loaded mucoadhesive microemulsion (fisetin-MME) was successfully developed and optimized via Box-Behnken Design (BBD) to enhance the solubility and brain-targeting potential of fisetin following intranasal administration. The optimized formulation exhibited a mean droplet size of 64.0 nm ± 0.05, a polydispersity index (PDI) of <0.5, and high entrapment efficiency (94.9%), alongside favorable thermodynamic stability, rheological characteristics, and mucoadhesive strength (3.24 ± 0.95 g). Physicochemical characterization by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier-transform infrared spectroscopy (FT-IR), and transmission electron microscopy (TEM) confirmed the structural integrity and compatibility of the formulation. A validated reverse-phase high-performance liquid chromatography (RP-HPLC) method consistently quantified fisetin with a retention time of 6.01 ± 0.23 min. The fisetin-MME demonstrated enhanced in vitro release (85.2 ± 2.345%) and ex vivo nasal mucosal permeation (87.6 ± 0.25%), with significantly improved flux (40.23 ± 0.06 μg/cm2/h) and permeability coefficient (81.23 × 10-6 cm/s), indicating efficient transmucosal transport. Pharmacokinetic evaluation revealed a marked improvement in both systemic and brain bioavailability following intranasal administration, with a brain C_max of 261.53 ± 0.14 ng/g and AUC0-t of 2564.0 ± 232.0 h·ng/g, surpassing the reference standard (C_max of 228.50 ± 0.36 ng/g; AUC0-t of 2257.6 ± 245.9 h·ng/g). Behavioral assessments, including the Forced Swim Test and Balance Beam Test, demonstrated significant amelioration of schizophrenia-like symptoms, including hyperlocomotion, catalepsy, and impaired motor coordination, with fisetin-MME showing superior neuroprotective and antidepressant effects compared to the standard drug by Day 14 (p < 0.001). Histopathological analysis further supported these findings, demonstrating marked neuroprotective effects in the cortical and hippocampal regions, as evidenced by reduced neuronal degeneration and attenuation of neuroinflammatory markers. These results highlight the potential of intranasally delivered fisetin-MME as a promising nanotherapeutic strategy for the management of schizophrenia.
Effect of cilnidipine on depression-like behaviour in male Swiss mice: A study using the tail suspension test Nandhini Devi Saravanan, Anil Pandharinath Hogade, Prakash R Biradar Indian Journal of Physiology and Pharmacology, 2025 Objectives: The objective is to evaluate cilnidipine and compare it with fluoxetine on the depression model in male Swiss mice, utilising the tail suspension test and locomotor activity test. Materials and Methods: The animals were categorised into four groups, each consisting of six individuals (n = 6 per group). The subjects were given the test drug doses of cilnidipine at 5 mg/kg and 10 mg/kg, as well as fluoxetine at 10 mg/kg, for a duration of 21 days through an intraperitoneal route. On days 1, 14 and 21, the locomotor activity was assessed using the actophotometer, while the antidepressant activity was assessed using the tail suspension test (TST). The duration of immobility was assessed using the total sleep time method for a 5-minute period, while the number of counts was monitored for 10 min using an actophotometer. Results: Cilnidipine at a dosage of 10 mg/kg demonstrates a reduction in symptoms of depression when compared to the standard control. Neither cilnidipine 5 mg/kg nor 10 mg/kg resulted in a noteworthy decrease in locomotor activity. Conclusion: The present study demonstrated a substantial antidepressant effect of cilnidipine 10 mg/kg dosage. More research is needed to validate the results reported.
Quality by Design Approach for the Development of Cariprazine Hydrochloride Loaded Lipid-Based Formulation for Brain Delivery via Intranasal Route Pallavi Chiprikar, Vinayak Mastiholimath, Prakash Biradar, Nisha Shirkoli Current Drug Metabolism, 2024 Background: Cariprazine (CPZ) is a third-generation antipsychotic medication that has been approved for treating schizophrenia. This study aimed to develop a cariprazine-loaded nanostructured lipid carrier (CPZ-NLCs) to prevent first-pass metabolism and improve bioavailability and site-specific delivery from nose to the brain. Methods: The CPZ-NLCs were prepared using melt emulsification. The formulation was optimized using the Box–Behnken design (BBD); where the influence of independent variables on critical quality attributes, such as particle size and entrapment efficiency was studied. Results: The optimized batch (F6) had a particle size of 173.3 ± 0.6 nm and an entrapment efficiency of 96.1 ± 0.57%, respectively. The in vitro release showed >96% release of CPZ from NLC within 30 min. The optimized formulation's ex vivo studies revealed significantly increased CPZ permeability (>75%) in sheep nasal mucosa compared to the CPZ suspension (~26%). The ciliotoxicity study of the nasal mucosa revealed that the CPZ-NLC formulation did not affect the nasal epithelium. The intranasal administration of the formulation achieved 76.14±6.23 μg/ml concentration in the brain which was significantly higher than the oral CPZ suspension administration (30.46±7.24 μg/ml). The developed formulation was stable for 3 months. Conclusion: The study concluded that the developed CPZ-NLC could significantly improve the bioavailability with quick delivery to the brain.
Antianaphylactic and mast cell stabilization activity of Cynodon dactylon International Journal of Pharmacy and Pharmaceutical Sciences, 2010
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PATENT: Patent No. 68307 BERBERINE NANOETHOSOMAL VAGINAL IN-SITU GEL FOR POLYCYSTIC OVARY SYNDROME
AN INNOVATIVE PREFOMULATION STUDIES & NOVEL ANALYTICAL HPLC METHOD DEVELOPMENT & VALIDATION FOR&NBSP;EST
A NOVEL FORMULATION DEVELOPMENT & OPTIMIZATION OF CHRYSIN-LOADED CUBOSOMAL GEL THEREOF
A PROCESS OF PRECLINICAL EVALUATION OF NOVEL CHYRSIN-LOADED CUBOSOMAL GEL FOR THE MANAGEMENT OF INFL
Patent No. 431185 DEVELOPMENT OF BERBERINE LOADED CUBOSOMAL NANOFORMULATION FOR THE TOPICAL TREATMENT OF ACNE
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