The objective of present work was to prepare nanocrystals of Lopinavir (LPN) to enhance its solubility and dissolution rate with aim of dose reduction and minimising the side effects associated with it's oral administration. Nanocrystals of LPN were prepared by anti-solvent precipitation method using a 3 2 full factorial design, employing stirring speed (X1) and concentration of surfactant (X2) as independent variables. The nanocrystals obtained were characterised mainly for particle size (PS), zeta potential (ZP), crystallinity, saturation solubility, in vitro dissolution and permeability. Results demonstrated profound effect of concentration of surfactant (pluronic F-68) on both the PS and polydispersity index (PDI) values. The optimised nanocrystals formulation had particle size 265nm, PDI 0.260 and ZP in the range of-18.0 to-22.5mv. X-Ray diffraction studies (XRPD) and Differential scanning calorimetry (DSC) studies suggested nanocrystal formation and absence of crystalline peaks, indicating loss of crystallinity, additionally confirmed by scanning electron microscopy (SEM). Nanocrystals showed 30.45 fold enhancements in aqueous solubility, and 38.5 fold in phosphate buffer pH 6.8, as compared to pure LPN. In vitro release studies have demonstrated 92.20% cumulative drug release within 3 hrs from nanocrystals compared to 42.65% from pure LPN. Even, increase in permeation flux from 423.1 μg/cm 2 /hr to 632.93 μg/cm 2 /hr in case of nanocrystals was also indication of enhanced dissolution. Stable LPN nanocrystals formulated by anti-solvent precipitation method shows improved solubility and dissolution. It has been concluded that LPN nanocrystals were obtained with significant improvement in saturation solubility and drug losing it's crystalline nature when compared with plain drug.
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.
Objective: The aim of present study was to prepare triamcinolone acetonide (TA) loaded NLCs hydrogel for antipsoriatic activity. Methods: A Nanostructured lipid carrier (NLCs) was prepared by using solvent diffusion and high pressure homogenization methods. NLCs dispersion was characterized by particle size, zeta potential, scanning electron microscopy (SEM), differential scanning calorimetry, and an in vitro release study. Optimized NLC incorporated into the hydrogel and characterized for rheological properties, drug content, in vitro drug release, stability study, skin irritation and antipsoriatic activity for optimized batch of hydrogel. Results: Optimized NLCs loaded with TA were exhibited spherical shape with particle size 286±0.07 nm, polydispersity index 0.317, zeta potential-21.91±0.05mV and entrapment efficiency 86.19±0.06% respectively. The drug release of optimized batch was 8.34 % and 88.84±0.08% at 1h and 8h respectively. The release kinetics of the optimized NLCs best fitted the peppas-korsmeyer model. The results of NLC hydrogel formulations were spreadability 27.4±0.06-11.76±0.07 g. cm2/sec, drug content 65.60±0.05%-74.50±0.02%, in vitro drug release 87.52±0.04%, primary irritation index was 0.0752, it indicates barely perceptible irritation. Histopathological studies showed that, in psoriasis-induced animal treated with TA loaded NLC hydrogel, marked reduction in thickness of epidermis, as compared to conventional gel formulation. It shows the increase % orthokeratosis 88.69% and % drug activity 54.23% than the marketed formulation. Conclusion: The present results demonstrated that hydrogel based NLC shows the better and effective drug delivery for the management of psoriasis.
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.
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