Introduction: Psoriasis (Ps) is a well-known chronic non-infectious, inflammatory skin disease affecting about 2–3% of the worldwide Population. Pathogenesis includes the environmental trigger factors with other factors like genetic factors, trauma, chemicals, bacterial infection etc. Currently there is no drug which can permanently cure the skin lesions as well as completely eradicate this dermatosis. The purpose of this research is to investigate the anti-psoriatic activity of phytoconstituents of Tribulus terrestris by predicting the ligand-receptor binding and by predicting the ADMET parameters using Lipinski's rule. Methodology: The process of research work starts with protein and ligand structure preparation. Further docking was done using PyRxAutodock Vina. Afterward, analysis and visualisation of the interaction between protein-ligands was done, and ADMET profiling was carried out according to lipinski's rules using Swiss ADME. Result: we selected four phytoconstituents of Tribulus terrestris. Molecular docking simulation showed all four compounds had better binding affinities. Based on the results of prediction of ADMET values using the Lipinski rule, compound that are thought to have good activity. Conclusion: Based on results these molecules have discovered that they may be able to produce anti-psoriatic activity and found that they have a lower toxicity, and ADME analysis determined the easily absorbability to the tissue site. Hence, these compounds can be analysed by further in vitro studies and can be a leader in the designing of the potential drug for the psoriasis management.
24 March 2022 in Research Journal of Pharmacy and Technology
Psoriasis is an inflammatory skin condition characterised by scaling with inflammation (pain, edema, warmth, and redness) that results in regions of thick, red skin covered in silvery scales. These spots can be itchy or painful. Systemic treatment, topical therapy, and phototherapy are all now used to treat psoriasis. These treatments have a variety of negative and perhaps fatal side effects. Patients with psoriasis are more likely to acquire other conditions such as psoriatic arthritis, anxiety and depression, cancer, metabolic syndrome, cardiovascular disease, and Crohn's disease. The majority of people use herbal medicine because it is readily available, inexpensive, and effective. Many plants have promising features, including significant results in the treatment of psoriasis. The present study plans to emphasize such plants, herbal formulations, and associated therapy, which could add value to the development of a better, safe, and efficacious formulation to treat psoriasis that may help new researchers in this field.
Transdermal systems are ideally suited for diseases that demand chronic treatment. Hence, an anti-diabetic agent of both therapeutic and prophylactic usage has been subjected to transdermal investigation. Gliclazide, a second-generation hypoglycemic agent, faces problems like its poor solubility, poor oral bioavailability with large individual variation and extensive metabolism. In the present work, transdermal matrix-type patches were prepared by film casting techniques on mercury using polymers like HPMC, Eudragit RL-100, and chitosan. Also an attempt was made to increase the permeation rate of drug by preparing an inclusion complex with hydroxypropyl β-cyclodextrin (HP β-CD). The possibility of a synergistic effect of chemical penetration enhancers (CPE) (propylene glycol and oleic acid) on the transdermal transport of the drug was also studied. Folding endurance was found to be high in patches containing higher amount of the Eudragit. There was increase in tensile strength with an increase in Eudragit in the polymer blend. In vitro drug release profile indicates that the drug release is sustained with increasing the amount of Eudragit in patches. The patches containing inclusion complex of drug showed higher permeation flux compared with patches containing plain drug. The result of the synergistic effect indicates that the HP β- CD in conjunction with other CPE showed a higher permeation flux.
Objective: The objective of the present study was to the preparation of a coamorphous (COAM) system of paracetamol (PA) (Biopharmaceutics Classification System [BCS] Class-III) and ibuprofen (IB) (BCS Class-II) for enhancement of solubility and dissolution of IB. Methods: The COAM system was prepared by chemical electric magnetic field microwave-assisted method. Several batches with different concentrations of COAM PA and IB were prepared at constant temperature, pressure, and holding time. Solubility studies were carried out in different pH condition and the batch, which show the highest increase in solubility 98.00%. COAM samples were characterized by solubility, dissolution, Fourier transform infrared (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC) studies. Results: FTIR results showed evidence of molecular interactions between both the drugs. Maximum increase in aqueous solubility of IB was seen 500:200 mg dose ratio (COAM) batch E in phosphate buffer 7.4. The COAM system increased solubility of IB about 98.70%. The solubility and dissolution rate of IB were also enhanced. In vitro drug release study, 100% of the drug was released within 120 min. Thus, saturation solubility and dissolution rate of IB were found significant improved unlike PA. XRD and DSC results confirmed amorphization of IB. FTIR results evidenced hydrogen bonding interactions between both the drugs. In accelerated stability studies, powder XRD and DSC results demonstrated insignificant changes, thus confirming successful stabilization of IB by PA. Conclusion: Hence, it concluded that the study of COAM of PA and IB successfully prepared by microwave-assisted method to enhance solubility, dissolution, stability, and bioavailability.
7 June 2020 in International Journal of Applied Pharmaceutics
Objective: The objective of the present investigation was to the development of floating pulsatile drug delivery system of Losartan potassium (LP) tablets for obtaining no drug release during floating followed by pulsed, rapid drug release to achieve chronotherapeutic release. In hypertension, the risk of getting heart attacks early in the morning is high and therefore, there was need to develop drug delivery, which will release drugs at morning hours and provide efficacious therapy. LP is a short biological half-life (1.5-2.5h) and readily absorbed from the stomach and upper gastrointestinal tract. Methods: Tablet formulation was prepared by press coating of rapid release core tablets and core tablets were further top coated with a buoyant layer of HPMC K4M and sodium bicarbonate. Various grades of HPMC polymer (E5/E15/E50) were used for the pulsatile coating layer. The developed formulations were characterized for physical characteristics, floating lag time, floating time, release lag time, drug content, swelling index, in vitro dissolution studies, DSC and XRD. Results: The FTIR and DSC studies predicted that there was no chemical interaction between drug and excipients. The core tablet coated with HPMC E50 showed a high swelling index and release the drug 97.60±1.2% at 6h. Buoyant layer with 80 mg HPMC K4M and 25 mg sodium bicarbonate gave satisfactory floating lag time. Conclusion: The system showed an excellent lag phase followed by burst release in the distal small intestine, which gives site and time-specific delivery of LP acting as per chronotherapy for treatment of hypertension.