Vildagliptin (VID) is a dipeptidyl peptidase-4 (DPP-4) inhibitor used in controlling blood glucose level in type 2 diabetes. Vildagliptin improves beta cells function and is also suggested to effectively control the inflammation. The possible ocular anti-inflammatory property of vildagliptin has been explored using topically applied plasticized ocular film formulation. Film formulation was prepared by solvent cast and evaporation method using triethanolamine (TEA), dimethyl sulphoxide (DMSO), and polyethylene glycol 400 (PEG 400) as the plasticizer in HPMC hydrogel matrix base. Anti-inflammatory study was carried out in the carrageenan induced ocular rabbit model. Analytical methods confirmed that the drug was present almost in completely amorphized form in the film formulation. Level of hydration, swelling and erosion rate of the film played the controlling factor in the process of drug release, ocular residence and permeation. Maximum swelling rate of 363 h−1 has been shown by VHT compared to other formulation of VHD and VHP (174 and 242 h−1 respectively). Film containing DMSO exhibited highest in vitro release as well as ex vivo ocular permeation. Film formulation has shown a fast recovery of ocular inflammation in contrast to the untreated eye after inducing inflammation. Plasticized vildagliptin hydrogel film formulation could be utilized in the management and control of ocular inflammation particularly with diabetic retinopathy after proper clinical studies in higher animal and human individuals.
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.
Background and Objectives: Ornidazole is widely used as an antiprotozoal and antiamoebic drug and its onset of action is within 2 h. The major extent of the drug is metabolized in the liver and excreted in the urine and faeces. Hence, the present study of suppository formulation for sustained systemic delivery of ornidazole is significant which could minimize abdominal disturbances and nausea and delayed onset of action particularly after oral administration. Methods: Bioadhesive suppository formulations were prepared for systemic delivery of ornidazole via rectal and vaginal route. Results: The physical drug-excipient-interaction was confirmed by in-silico docking study. The affinity between drug-HPMC and drug-PEG was found to be-2 and-0.9 k cal/mol respectively. In vitro drug release of the suppositories varied depending on the viscosity grade of HPMC used and all have followed mostly diffusion controlled mechanism. The formulation containing HPMC K100 showed the most sustained release of ornidazole in both the dissolution fluid of pH 7.4 and 4.5 (54.53 and 41.89 % respectively after 360 min). Conclusion: In conclusion, present bio adhesive suppositories could be utilized for sustained systemic delivery of ornidazole via rectal and vaginal route. The findings of this work will contribute to the current knowledge and encourage future pre-clinical research.
Background: Tablet manufacturing with direct compression is one of the leading industrial technique that consumes less time, labour and economic also. But the choice of excipients are critical in this case which will allow the drug to get compressed without granulation techniques. Purpose: Aceclofenac is a BCS class II non-steroidal anti-inflammatory drug, which exerts a low oral bioavailability because of low solubility in aqueous medium. The drug also suffers from compressibility and also shows poor tabletibility. Methods: We have attempted to improve tabletability by incorporating titanium dioxide (TiO 2) through kneading and solvent evaporation technique. Results: In the FTIR study revealed that NH and Cl aromatic stretching of aceclofenac has been affected significantly due to binding with TiO 2. DSC thermogram ascertained the partial amorphization of the drug in the formulations. Evaluated tabletability from the area under the applied pressure vs tensile strength curve (AUTC) of A1T1 has shown a poor value in contrast to other formulations.
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