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This study describes the synthesis of N5‐(4‐(1H‐benzo[d]imidazol‐2‐yl)phenyl)‐N2‐phenylpyridine‐2,5‐diamine derivatives from Orthophenylenediamine (1) and 4‐aminobenzoic acid (2) and all the synthesized chemical moieties screened against a panel of cancer cell lines resulted in the identification compound 6 a with good anti‐cancer potential and a GI50 of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM and 1.56 μM against MDAMB‐231, MCF‐7, A‐549, NCI‐H23 and A‐498 respectively. As the second greatest cause of death globally, cancer continues to pose a serious threat to public health. An essential enzyme called aromatase catalyses the last, rate‐limiting step in the production of oestrogens. As a well‐researched endocrine therapeutic strategy, aromatase inhibitors (AIs) efficiently block the production of oestrogen, which is necessary for aromatase activity. [ABSTRACT FROM AUTHOR]

Background: The present study is designed to develop a novel dosage form i.e. microemulgel which will enhance the rate of absorption in the systemic circulation and ultimately enhance the pharmacological effect of the Mentha piperita L. extract as anti-inflammatory agent. Its primary components include with constituents including menthol (46.32%), menthofuran (13.18%), menthyl acetate (12.10%), menthone (7.42%) and 1,8-cineole (6.06%). Materials and Methods: The research aimed to formulate and assess herbal microemulgel containing M. piperita extract, focusing on its in vitro anti-inflammatory properties. M. piperita herb extraction was carried out using a hydro-alcoholic solvent, followed by phytochemical analysis. Four separate sets of herbal microemulgel were crafted and underwent a series of assessments, encompassing pH levels, spreadability, viscosity, consistency, appearance, color and ease of washing. Additionally, the in vitro anti-inflammatory potential of both the extract and the microemulgel formulation was assessed using the HRBC membrane stabilization assay and the protein denaturation assay. Results: The findings of this study suggest that the newly developed herbal microemulgel, enriched with M. Piperita extract, exhibits promising anti-inflammatory effects. Conclusion: The M. piperita microemulgel exhibited a remarkable 94.35% drug content with high solubility and compatibility of the drug with the excipients. Permeability studies revealed that the M. piperita microemulgel achieved 94% permeability within 48 hr, showcasing enhanced drug permeability facilitated by the microemulsion-based gel system. Moreover, the formulated microemulgel demonstrated significant anti-inflammatory activity. It can be concluded that topical herbal M. piperita microemulgel has potential for future applications in this regard. [ABSTRACT FROM AUTHOR]

Background and Aims: The aim of the present research work was to develop and optimize statistically carvedilol floating beads for chronotherapeutic drug delivery. Methods: Multiple unit floating pulsatile beads of carvedilol were prepared by simple ionotropic gelation method intended for chronotherapy of hypertension. Pectin and sodium alginates were used as matrix forming, polymer and sodium bicarbonate was used as floating agent. A 2³ full factorial design was applied to investigate the combined effect of three independent formulation variables namely amount of sodium alginate, sodium bicarbonate and calcium chloride on the dependent variables as % entrapment efficiency, floating lag time and drug release percentage. Results: The formulation was optimized and tested based on its drug release pattern which presented minimum drug release in 0.1 N HCl and after 6 h lag time period and showed maximum drug release in 6.8 pH phosphate buffer by burst release within 45 mins. Surface response plots were presented graphically to represent the effect of independent variables on floating lag time, entrapment efficiency and drug release in 0.1 N HCl. The generated mathematical model for each response was validated and checked by formulating three extra-design checkpoint batches. There were no significant changes in drug content, floating lag time, entrapment efficiency and drug release of the formulation following its stability studies at 40 0C and 75% relative humidity. Conclusion: It was concluded that the floating beads were successfully formulated for chronotherapy of hypertension giving site- and time specific release of drug. [ABSTRACT FROM AUTHOR]

In order to overcome some of the drawbacks of traditional formulations, increasing emphasis has recently been paid to lipid-based drug delivery systems. Solid lipid nanoparticles (SLNs) are among these delivery methods, and they hold promise because of their simplicity in production, capacity to scale up, biocompatibility, and biodegradability of formulation components. Other benefits could be connected to a particular route of administration or the makeup of the ingredients being placed into these delivery systems. This article aims to review the significance of solid lipid nanocarriers, their benefits and drawbacks, as well as their types, compositions, methods of preparation, mechanisms of drug release, characterization, routes of administration, and applications in a variety of delivery systems with a focus on their efficacy., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Nanostructured lipid carriers (NLCs) are explored as vehicles for ophthalmic drug delivery owing to their better drug loading, good permeation, and satisfactory safety profile., Objective: The purpose of the study was to fabricate and characterize an in situ ocular gel of loratadine as a model drug based on NLCs to enhance the drug residence time., Methods: NLCs were fabricated using the microemulsion method in which solid lipid as Compritol 888 ATO, lipid as oleic acid, surfactant as Tween 80, and isopropyl co-surfactant as alcohol, were used. Based on the evaluation of formulation batches of NLCs, the optimized batch was selected and further utilized for the formulation of in situ gel containing Carbopol 934 and HPMC K15M as gelling agents, and characterized., Results: The optimized NLCs of loratadine exhibited entrapment efficiency of 83.13 ± 0.13 % and an average particle size of 18.98 ± 1.22 nm. Drug content and drug release were found to be 98.67 and 92.48 %, respectively. Excellent rheology and mucoadhesion were demonstrated by the loratadine NLC-loaded in situ gel to enhance its attachment to the mucosa. NLC-based in situ ocular gel showed the desired results for topical administration. The prepared gel was observed to be non-irritating to the eye., Conclusion: The optimized NLC-based in situ gel formulation presented better corneal retention and it was found to be stable, offering sustained release of the drug. Thus, the joined system of sol-gel was found promising for ophthalmic drug delivery., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)