No abstract

Local controlled delivery sustained anti-inflammatory activity of dexamethasone has been achieved using kaolin incorporated HPMC film.

The present study was undertaken for characterization of the steady state and non steady state corneal permeation kinetics of diclofenac potassium (DCP) using statistical moment theory.

Analysis of the binding interactions of ibuprofen and silicified-microcrystalline cellulose (SMCC) has been undertaken. Co-processing of ibuprofen with SMCC was carried out by solid state ball milling, and aqueous state equilibration followed by freeze drying to investigate the effect of silicified-microcrystalline cellulose on ligand. Molecular docking study revealed that ibuprofen formed complex through hydrogen bond with microcrystalline cellulose (MCC) and silicon dioxide (SiO 2); the binding energy between MCC and SiO 2 , and ibuprofen and SMCC were found as-1.11 and-1.73 kcal/mol respectively. The hydrogen bond lengths were varying from 2.028 to 2.056 Å. Interaction of Si atom of SMCC molecule with Pi-Orbital of ibuprofen has shown the bond length of 4.263 Å. Significant improvement in dissolution of ibuprofen has been observed as a result of interaction. Binary and ternary interactions revealed more stabilizing interactions with ibuprofen and SMCC compared to SMCC formation.

Pramanik et al.: Molecular Docking of Kaolin Based Cellulosic FilmOphthalmic delivery of dexamethasone can control inflammation and also some forms of uveitis. But it is effective therapeutically over a short period of time and frequent instillation is required. hydroxypropyl methylcellulose matrix films containing dexamethasone were prepared by casting method in presence and absence of particulate kaolin for extending ophthalmic drug delivery. Fourier-transform infrared spectroscopy confirmed the complexation of dexamethasone and kaolin in the film via formation of hydrogen bond and the observed shouldering at 1032 cm -1 increased with corresponding higher amount of kaolin binding. Differential scanning calorimetry thermogram resulted in almost complete amorphization of dexamethasone in the film. X-ray diffractogram demonstrated almost disappearance of kaolinite diffraction and the reduced order of dexamethasone crystal lattice in all the film formulations. Submicrons, tubular and nano-fibrous morphology of the kaolin and drug particles were seen in the scanning electron microscope images of the film. Relatively extended diffusion controlled drug release and ophthalmic permeation behavior were observed with the increase of kaolin loading in the film. Stable complex facilitated the sustained ophthalmic delivery of dexamethasone and prolonged anti-inflammatory activity. Molecular docking study also revealed the complex formation of dexamethasone with kaolin and hydroxypropyl methyl cellulose to understand the fitting and stable configuration of drug-carrier interaction. Kaolin-based hydroxypropyl methyl cellulose hydrogel film containing dexamethasone as a model drug can enhance the corneal residence time for anti-inflammation for an extended period of time.

Hydration behavior of hydrogel-based polymeric film possesses great importance in mucosal drug delivery. Modified Lag phase sigmoid model was used for the investigation of hydration of the film. Kaolin incorporated HPMC K100LVCR (HL) and K100M (HH) films containing dexamethasone as a model drug have been prepared for studying swelling kinetics. Swelling of HL and HH films was decreased with the gradual increase of kaolin content and HH of higher viscosity has shown higher value than HL matrix. Kaolin also inhibited the film erosion process. Mathematically modified lag phase sigmoid model demonstrated similarity of the predicted swelling content with the observed value. High R2 and small RMSE value confirmed the successful fitting of the modified lag phase sigmoid model to the experimental data of swelling content. τ value similar to the observed one was obtained. This modified model could be reliable enough for estimating hydration process in food grains, food packaging films etc.

Proliferative retinopathy is described as a progressive neovascularization in the inner surface of the retina or vitreous, which subsequently threatens vision by causing retinal detachment or vitreous hemorrhage. Reactive oxygen species generation and its related vasoproliferative factor up regulation play a major role in progression of the disease. The present study focuses on Carr induced reactive species generation with its related vasoproliferative factor up regulation and ameliorative activity of AML. Biochemical estimation of catalase, lipid peroxidation, hypoxia inducing factor (HIF-1α) and guanyl-s-transferase (GST) were done. AML treated group showed significant increase in catalase enzyme, guanyl-s-transferase and significantly reduced the lipid peroxidation. Western blotting assay showed a significant decrease in HIF-1α in AML treated group. The progression of PR alters the endogenous cell signalling thus causing havoc in retinal cells. Therefore, it could be hypothesized that use of AML can be a new detection method for therapeutic strategies to prevent blindness in PR.

This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms