Thymoquinone (THQ) is known for its neuroprotective and anti-convulsant properties in preclinical studies. We herewith describe a simple, rapid, selective, sensitive and stability-indicating UPLC method for the estimation of THQ and its application to biopharmaceutical studies such as in vitro release from nanoparticulate system and in vivo pharmacokinetic study. The method employed gradient elution using a Waters Acquity HSS-T3 C(18) (100 × 2.1 mm, 1.8 µm) UPLC column. The mobile phase consisted of water and acetonitrile, pumped at a flow rate of 0.5 mL/min. The injection volume was 5 µL and THQ was monitored at 294 nm wavelength with a total run time of 6 min. In solution as well as in plasma, the method was found to be linear (r ≥ 0.998), precise (CV ≤ 2.45%) and accurate (recovery ≥ 84.8%) in the selected concentration range of 0.1-0.8 µg/mL. Forced degradation studies revealed that THQ undergoes degradation under acidic, basic, oxidation and UV light stress conditions. However, the developed UPLC method could effectively resolve degradation product peaks from THQ. Further, no interference was found at the retention time of THQ from any plasma components, indicating selectivity of the developed method. For solutions, the limits of detection and quantitation of the method were found to be 0.001 and 0.0033 µg/mL, respectively; while in plasma they were 0.006 and 0.02 µg/mL, respectively. The validated method was successfully applied to quantify THQ in dissolution medium as well as oral in vivo pharmacokinetic study of THQ suspension and THQ- solid lipid nanoparticle (THQ-SLN) formulation. A 2-fold increase in the relative bioavailability was observed with the THQ-SLN compared with THQ. The results indicate that the SLN significantly increased plasma concentrations and retention within the systemic circulation.
Current investigation aimed to develop a novel Amiloride loaded mucoadhesive nanoemulsion formulation for nose-to-brain delivery. Furthermore, nasal irritation study and histopathological examination of the nasal mucosa were also carried out to assess nonirritant nature of the nanoemulsion. The optimized formulation, surface epithelium lining and the granular cellular structure of the nasal mucosa were totally intact, whereas KCl caused major changes in the ultrastructure of mucosa. Amiloride loaded mucoadhesive nanoemulsion formulations are non toxic on nasal mucosa and can be administered by intranasal route for effective treatment of epilepsy.
Ganciclovir (GCV) plays an important role in the treatment of ocular viral infections. A high dose results in dose-related toxicity including bone marrow suppression and neutropenia. The aim of the present study was to investigate the comparative potential of different mucoadhesive nano formulations for the topical ocular delivery of Ganciclovir. GCV mucoadhesive Nanoemulsions (GCV-NEs), chitosan nanoparticles (GCV-NPs), GCV mucoadhesive niosomal dispersion (GCV-NDs) were prepared by the reverse-phase evaporation technique. All of the three formulations were evenly round in shape with mean particle size in the range of 23-200 nm. These results indicated the nonirritant and nontoxic nature of the developed formulations. The achieved results may be useful for formulation development of GCV, which could be effective in the treatment of ocular infections by topical instillation.
The phytosome technology was developed by Indena markedly enhancing the bioavailability of selected phytomedicines, by incorporating phospholipids into standardized plant extract, which improve their absorption and utilization. Phytosome are advanced form of herbal extract that shows better absorption profile than conventional herbal extract. The present review focus on the preparation and characterization techniques of phytosomes, merits and various landmarks in the field of phytosomes.
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