Cationic microemulsion of voriconazole for the treatment of fungal keratitis: and evaluation.

This investigation aimed to develop a voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat fungal keratitis. Microemulsions were prepared using water titration, and the optimized microemulsion was coated with chitosan to prepare CVME. The physicochemical parameters, ocular irritation potential, antifungal efficacy and release studies were performed.

Step-Economical Mechanosynthesis of Hybrid Azoles: Deciphering Their π-Orbital and Pharmacological Characteristics.

A hybrid pharmacophore strategy for unifying 1,2,3-triazole with 1,2,4-triazole cores to prepare mixed triazoles was accomplished by a ball-milling approach. The developed chemistry works under the catalysis of cupric oxide nanoparticles with salient features like one-jar operation, lower number of synthetic steps, catalyst recyclability, time-dependent product control, and good overall yields. π-Orbital properties based on theoretical calculations supported the suitability of these molecules for pharmacological screening.

Synthesis and Optoelectronic Features of Rhodamine-Triazole Dyads as Metallochromic Probes for Copper-Selective Chemosensing.

Rhodamine-based chromic materials have attracted significant interest owing to their cation recognition ability with high sensitivity. However, rhodamine chromophores with controllable sensing selectivity towards transition metal species are only at the advent. Herein, three triazole-conjugated rhodamine dyads with different peripheral substituents were synthesized.

Mechanosynthesis of Triazolyl-bis(indolyl)methane Pharmacophores via Gold Catalysis: A Prelude to Their Molecular Electronic Properties and Biological Potency.

Chemical structures possessing both 1,2,3-triazole and bis(indolyl)methane fragments gained considerable interest in drug synthesis owing to their established biological efficacies. However, 1,2,3-triazoles linked at the bridging position of bis(indolyl)methane is a logical and unexplored design approach. In this regard, nine new triazolyl-bis(indolyl)methane conjugates under AuCl catalyzed ball-milling conditions were accomplished.

Cationic Chitosan/Pectin Polyelectrolyte Nanocapsules of Moxifloxacin as Novel Topical Management System for Bacterial Keratitis.

Purpose: Moxifloxacin (MOX) is a fourth-generation fluoroquinolone and a broad spectrum antibiotic used in the management of bacterial keratitis (BK). This investigation aimed to formulate MOX-loaded chitosan/pectin cationic polyelectrolyte nanocapsules (CPNCs) for the effective topical treatment of BK.

Methods: Physicochemical properties like nanocapsule size, charge, drug entrapment efficiency (EE), viscosity, pH, and release profile of CPNCs were evaluated.

Experimental infection of Enterocytozoon hepatopanaei parasite (EHP) of penaeid shrimp in Indian marine crabs.

Enterocytozoon hepatopanaei parasite (EHP) is identified as an emerging pathogenic microsporidium parasite in shrimp culture industry. Though the etiology, disease pattern and sustainability of shrimp are well known, significantly less research has been carried out about the disease transmission and symptoms of infected aquatic animals. The present study aims is to determine the disease carrier status of five different species of Indian marine crabs (Scylla olivacea, Scylla serrata, Portunus pelagicus, Ocypode quadrata and Portunus sanquinolentus) using EHP.

Mechanochemical Access to Functional Clickates with Nitro-Retentive Selectivity via Organocatalyzed Oxidative Azide-Olefin Cycloaddition.

4-Nitro-1,2,3-triazoles are crucial precursors for high energy materials, and their practical synthesis is a long-standing problem. Herein, we communicate a mechanochemical route for the selective synthesis of 4-nitro-1,2,3-triazoles via organocatalyzed oxidative [3 + 2] cycloaddition between β-nitrostyrenes and organic azides. Our conditions avoid divergent pathways and permit the retention of the valuable NO group on the product.

Cationic Polyelectrolyte Nanocapsules of Moxifloxacin for Microbial Keratitis Therapy: Development, Characterization, and Pharmacodynamic Study.

Microbial keratitis (MK) is a vision-threatening disease and the fourth leading cause of blindness worldwide. In this work, we aim to develop moxifloxacin (MXN)-loaded chitosan-based cationic mucoadhesive polyelectrolyte nanocapsules (PENs) for the effective treatment of MK. PENs were formulated by polyelectrolyte complex coacervation method and characterized for their particle size, surface charge, morphology, mucoadhesive property, in-vitro and ex-vivo release, ocular tolerance, and antimicrobial efficacy studies.

Phase Transition Microemulsion of Brimonidine Tartrate for Glaucoma Therapy: Preparation, Characterization and Pharmacodynamic Study.

: The aim of this study was to formulate brimonidine tartrate loaded phase transition microemulsions (PMEs), which undergo phase transition from water in oil (W/O) microemulsions to liquid crystalline (LC) and then oil in water (O/W) microemulsions after instilled into the eye and prolong the precorneal residence time and ocular bioavailability for the effective treatment of glaucoma.: The pseudo-ternary phase diagram was developed and various PMEs were prepared using Tween 80 and Span 80 with isopropyl myristate and water. Globule size and shape, physicochemical parameters, and drug release of PMEs were studied.

Topical Ocular Delivery of Nanocarriers: A Feasible Choice for Glaucoma Management.

Topical ocular delivery is an acceptable and familiar approach for the treatment of common ocular diseases. Novel strategies for the treatment of inherited eye diseases include new pharmacologic agents, gene therapy and genome editing, which lead to the expansion of new management options for eye disorders. The topical ocular delivery of nanocarriers is a technique, which has the potential to facilitate novel treatments.

Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.

Aim: Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. The aim of this study was to prepare BNZ loaded chitosan-pectin mucoadhesive nanocapsules (CPNCs) by polyelectrolyte complex coacervation method for ocular delivery and evaluated for its anti glaucoma efficacy.

Methods: The prepared CPNCs were characterized for their particle size, polydispersity index, zeta-potential, surface morphology, entrapment efficiency, drug loading efficiency, mucoadhesive strength in-vitro and ex-vivo release.

Harnessing the TEMPO-Catalyzed Aerobic Oxidation for Machetti-De Sarlo Reaction toward Sustainable Synthesis of Isoxazole Libraries.

A practical synthesis of isoxazole/isoxazoline derivatives via Machetti-De Sarlo reaction under sustainable conditions has been accomplished. This protocol involves the use of readily available 2,2,6,6-tetramethylpiperidine--oxyl (TEMPO) to catalyze the cyclocondensation of primary nitroalkanes with alkynes/alkenes to afford a library of isoxazole/isoxazoline products. From an eco-benign perspective, notable advantages of this method are as follows: (i) water as the solvent, (ii) air as the oxidant, (iii) transition metal-free, (iv) no base required, (v) no toxic byproduct, (vi) no need of solvent extraction, (vii) diverse substrate scope, (viii) high chemical yields, (ix) excellent chemo- and regioselectivity, (x) short reaction time, (xi) gram-scale synthesis, (xii) extension to heterogeneous version, and (xiii) catalyst recyclability.

Experimental horizontal transmission of Enterocytozoon hepatopenaei in post-larvae of whiteleg shrimp, Litopenaeus vannamei.

Enterocytozoon hepatopenaei (EHP) is a microsporidian parasite that causes hepatopancreatic microsporidiosis (HPM) in penaeid shrimp. HPM was observed in several countries, including Thailand and India; it has become a prominent pathogen in shrimp culture. Based on observations on EHP infection in the wild, the route of transmission has been hypothesized.

Tamoxifen citrate loaded chitosan-gellan nanocapsules for breast cancer therapy: development, characterisation and in-vitro cell viability study.

The objective of this study was to evaluate the potential of chitosan-gellan nanocapsules (CGNCs) for encapsulation and sustained release of Tamoxifen citrate (TMC) for breast cancer therapy. Polyelectrolyte complex coacervation method was used for production of CGNCs. Interaction studies were conducted by Fourier-transform infra-red (FT-IR), differential scanning colorimetric (DSC), and X-ray diffraction (XRD) to investigate any interaction between drug and excipients.

Ocular Self-Microemulsifying Drug Delivery System of Prednisolone Improves Therapeutic Effectiveness in the Treatment of Experimental Uveitis.

Purpose: The purpose of this study was to investigate the self-microemulsifying drug delivery systems (SMEDDS) for ophthalmic delivery of Prednisolone (PDN) to treat uveitis.

Materials And Methods: The pseudo-ternary phase diagrams were developed, and various SMEDDS were prepared using Linoleic acid as oil, Cremophore RH 40 as a surfactant, and propylene glycol as a co-surfactant. Physicochemical parameters (globule size, zeta potential, viscosity, and pH) and in vitro release of SMEDDS were studied.

Development of microemulsions for ocular delivery.

Microemulsions (MEs) are thermodynamic stable dispersion of oily phase and aqueous phase stabilized by surfactants and co-surfactants, and are a small droplet size of less than 100 nm. MEs are appropriate systems for ocular drug delivery because they improve ocular drug retention, extended duration of action, high ocular absorption, permeation of loaded drugs and effortlessness of preparation and administration. This review is an effort to summarize the recent development in the area of MEs, self-emulsifying drug delivery systems, which are examined in relation to their uses in ocular drug delivery.

Effect of chitosan coating on microemulsion for effective dermal clotrimazole delivery.

Clotrimazole (CTZ) is a broad spectrum antimycotic agent known to be very effective locally for the treatment of fungal skin infections. The aim of this study was to study the effect of chitosan-coated microemulsion (CME) for topical delivery of CTZ and also evaluate its in vitro antifungal efficacy, ex vivo permeation and retention ability on the skin surface. The pseudo-ternary phase diagrams were developed using clove oil as oil phase, Tween 80 and propylene glycol as surfactant and co-surfactant, respectively, and distilled water as aqueous phase.

Phase-transition W/O Microemulsions for Ocular Delivery: Evaluation of Antibacterial Activity in the Treatment of Bacterial Keratitis.

Purpose: Moxifloxacin (MXN) is widely prescribed for the treatment of bacterial keratitis. The conventional MXN solution has several limitations, including short precorneal residence time and poor intrastromal bioavailability, requiring frequent instillation of the drug to achieve the desired therapeutic effect. To circumvent this problem, the W/O (water-in-oil) microemulsion (ME) system was utilized for sustained release and improved precorneal retention.

Therapeutic Effectiveness in the Treatment of Experimental Bacterial Keratitis with Ion-activated Mucoadhesive Hydrogel.

Purpose: To investigate the therapeutic effectiveness of ion-activated mucoadhesive hydrogel system in the treatment of experimental bacterial keratitis.

Materials And Methods: Mucoadhesive systems were prepared using gellan or sodium alginate alone and combined with sodium carboxymethylcellulose (NaCMC) to enhance the gel bioadhesion properties. The in vivo antimicrobial efficacy of selected mucoadhesive systems was studied in an experiment on bacterial keratitis in rabbit's eyes and compared with that of the marketed conventional eyedrops.

Positively charged microemulsions of dexamethasone: comparative effects of two cosurfactants on ocular drug delivery and bioavailability.

Background: The objective of this investigation was to evaluate the potential of mucoadhesive chitosan-coated positively charged microemulsions (CH-MEs) of dexamethasone with respect to the change in nonionic cosurfactants.

Methods: CH-MEs were prepared with different concentrations of surfactant and cosurfactant using the water titration method and coated with low-molecular-weight chitosan.

Results: All formulations displayed an average globule size between 85 and 187 nm and a positive surface charge.

Chitosan-sodium alginate blended polyelectrolyte complexes as potential multiparticulate carrier system: colon-targeted delivery and gamma scintigraphic imaging.

Objectives: The objective of this study is to develop stable, biodegradable chitosan-sodium alginate-based dual, ionic cross-linked multiparticulate system (microbeads) of tinidazole for targeted colon delivery and sustained drug release for the treatment of amoebiasis and thereby evaluating its targeting approach through in vivo gamma scintigraphic imaging technique.

Methods: The chitosan-sodium alginate-based multiparticulate system developed was producing sustained effect by virtue of its mechanical strength using double ionotropic gelation method utilizing calcium chloride and sodium sulfate as first and second cross-linkers respectively. Prepared formulations were evaluated for percent yield, drug entrapment efficiency, particle size, degree of swelling, in vitro kinetics, and in vivo targeting potentials using gamma scintigraphic imaging technique.

Effect of hydroxypropyl-β-cyclodextrin on the ocular bioavailability of dexamethasone from a pH-induced mucoadhesive hydrogel.

Purpose: Dexamethasone (DXN) is an effective anti-inflammatory drug in the treatment of acute and chronic eye disease such as uveitis. It is relatively lipophilic and permeates biological membranes quite easily. However, its low aqueous solubility limits its clinical usefulness.

Phytochemical and pharmacological evaluation of prop roots of Pandanus fascicularis Lam.

Objective: To evaluate the anti-inflammatory and analgesic activities of the ethanol and aqueous extracts of prop roots of Pandanus fascicularis (P. fascicularis) Lam (pandanaceae). And provide experimental evidence for its traditional use such as rheumatoid arthritis and spasmodic.