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27 result(s) for "Thorat, P V"
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Development and Evaluation of Acitretin Loaded Solid Lipid Nanoparticles for Topical Drug Delivery System
In order to understand the in vitro drug release of the produced gel, the goal of the current investigation was to construct and characterize. Acitretin loaded Solid Lipid Nanoparticles (ActSLNs). Act SLNs were created utilizing the Box Benhken design and the hot homogenization procedure. Act SLN's average diameter and surface morphology were assessed. Act SLNs were lyophilized, then they underwent stability testing, powder X-Ray diffraction, Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared (FT-IR) tests to characterize them. The SLNs were added to a 0.25% w/w Carbopol 940 gel base the Stability study, ex vivo drug release in vitro drug releases in rat skin were carried out. The optimized Act SLNs had a spherical form, an entrapment efficiency of 78.82% to 85.73%, and an average particle size of 123.24nm to 409nm. The generation of SLNs was confirmed by DSC, FTIR, and XRD data. ActSLN gel (0.056mg/cm2) significantly increased the amount of accutane deposited in rat skin compared to Act plain gel (0.012mg/cm2).No discernible change was found in the stability studies, according to stability studies.
Enhancement of Solubility of Leflunomide with β-cyclodextrin inclusion complexation
4 mg/ 100 ml at 25°C), which limits its dissolution and consequently its bioavailability. [...]it is important to enhance the solubility and dissolution rate of Leflunomide to improve its oral bioavailability. Phase solubility analysis of Leflunomide: Phase solubility study was done to determine the stoichiometric proportion of Leflunomide with complexing agent ß-CD. Inclusion complexes prepared by kneading method showed higher saturation solubility than those prepared by other methods8,9. 3) IR spectral analysis: IR Spectra of pure drug and inclusion complexes of Leflunomide with ß-CD prepared by different methods are given in Fig. 1. The spectra of inclusion complexes and physical mixtures of components revealed disappearance of characteristic peaks of aromatic C-H stretching, N-H stretching and Amide at 3250 cm-1, 3400 cm-1 and 1670 cm-1respectively. [...]it suggests that vibrating and bending movements of guest molecule that is Leflunomide were restricted due to formation of inclusion complex.
Fast Dissolving Drug Delivery System of Cilnidipine using Gelucire 50/13
Formulations were analyzed using Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) analysis, Fourier Transform-Infrared spectroscopy (FT-IR) and in-vitro release studies followed by various release kinetics. The solid dispersion is defined as dispersion of one or more active ingredients in an inert carrier matrix at solid-state prepared by the melting (fusion), solvent evaporation or melting-solvent method.1 Gelucires are a family of lipid-based excipients comprising glycerides and esters of (PEG), these two components conferring hydrophobic and hydrophilic properties to the vehicle. Powder X ray Diffraction: PXRD pattern of the solid dispersion prepared with Gelucire was characterized by less intensity of diffraction peaks as compared to pure drug, suggesting conversion of microcrystalline form of the drug to an amorphous state, which may helps to improve solubility and dissolution of drug (Fig. 1 and 2).17, 18,19,22,25 Factorial Design: Response surface plot for cumulative % drug release in 15 minutes and for disintegration time is as shown in Figure No.3, 4. The enhanced drug release rates of solid dispersions (SDs) may be due to many factors such as decreased particle size of drug, specific form of drug in these SDs, in addition to the increase in drug wettability.
Synthesis and Characterization of Water Based Silver Nanofluids
This present research is focus to synthesis water based silver nanofluids by chemical reduction which increase the thermal conductivity to enhance the rate of heat transfer, also to characterize the thermal properties and heat transfer performance of nanofluids over heat exchangers to enhance the efficiency and overall heat transfer coefficient of heat exchanger with simultaneous reduction in the area of heat exchanger. As noted above the basic concept of dispersing solids in fluids to enhance thermal conductivity. Solid particles are added because they conduct heat much better than do liquids. Compared with micro particles, nanoparticles stay suspended much longer and possess a much higher surface area. The surface/volume ratio of nanoparticles is 1000 times larger than that of microparticles. The high surface area of nanoparticles enhances the heat conduction of nanofluids since heat transfer occurs on the surface of the particle. The number of atoms present on the surface of nanoparticles, as opposed to the interior, is very large. Therefore, these unique properties of nanoparticles can be exploited to develop nanofluids.
Porous NiCo2O4 electrodes for high-energy asymmetric supercapacitor: effect of annealing
Nickel–cobalt hydroxide thin films were synthesized using the chemical bath deposition method, and the effect of thermal annealing (373–673 K) on their physicochemical and electrochemical characteristics was explored. The X-ray diffraction study showed a cubic crystalline structure of NiCo 2 O 4 electrode formed above annealing temperature of 573 K. Field emission scanning electron spectroscopy (FE-SEM) study revealed that after annealing, NiCo 2 O 4 electrode showed urchin-like microspheres morphology with superhydrophilic nature. The electrode annealed at 573 K exhibited outstanding electrochemical performance with a specific capacitance of 470 F g −1 at 0.4 A g −1 current density. Over 2000 cycles, electrode demonstrated capacitive retention of 75.55%. Finally, NiCo 2 O 4 and Fe 2 O 3 thin films were used to construct the asymmetric supercapacitor (ASC) device. The ASC device manifested energy density of 40 Wh kg −1 at power density of 1.66 kW kg −1 and 82% retention after 2000 CV cycles. Graphical Abstract
AB0937 TOFACITINIB EFFICACY AND SAFETY IN PATIENTS WITH ANKYLOSING SPONDYLITIS BY BASELINE C‑REACTIVE PROTEIN LEVELS: A POST HOC ANALYSIS
BackgroundElevated baseline (BL) C-reactive protein (CRP) levels can predict treatment response in patients (pts) with ankylosing spondylitis (AS). Tofacitinib is a Janus kinase inhibitor for the treatment of AS.ObjectivesTo evaluate the impact of BL CRP levels on tofacitinib efficacy and safety in pts with AS.MethodsPost hoc analysis of pooled data from placebo (PBO)-controlled, randomised, double-blind trials (NCT01786668, Phase [P]2, 16 weeks; NCT03502616, P3, 48 weeks) in pts with AS on ≥1 dose of tofacitinib or PBO (P3: PBO-treated pts switched to tofacitinib after Week [W]16), by BL CRP: normal (NML) <5 mg/L; elevated (ELV) ≥5 mg/L. Tofacitinib 5 mg twice daily (BID) efficacy was assessed to W12/W16–48 (P3). Endpoints: Assessment of SpondyloArthritis international Society (ASAS) 20/40, Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) 50, AS-Disease Activity Score-CRP inactive disease (ASDAS-CRP ID), least squares mean change from BL (Δ) in nocturnal pain and Functional Assessment of Chronic Illness Therapy-Fatigue (FACIT-F). Safety was assessed to W16 and W48.ResultsOf 372 pts, 30.4/69.6% had NML/ELV BL CRP. Both groups had generally similar BL characteristics; more pts with ELV CRP were male, current smokers and had prior biologic disease-modifying antirheumatic drug use. At W12, ASAS20 response was greater for tofacitinib vs PBO in both groups (Figure 1); efficacy maintained to W48. At W12, the difference in response from PBO for tofacitinib was numerically greater for ELV vs NML CRP for ASAS20 (44.7% vs 15.9%), ASAS40 (34.6% vs 17.3%), BASDAI50 (33.8% vs 15.3%), ASDAS-CRP ID (9.5% vs 8.2%), Δnocturnal spinal pain (-2.1 vs -1.4) and ΔFACIT-F (5.2 vs 3.5). For tofacitinib, rates of treatment-emergent adverse events (TEAEs) and infections to W16 trended numerically higher for tofacitinib vs PBO in pts with NML CRP, but were similar to PBO in pts with ELV CRP (Table 1). There were few serious AEs (SAEs), serious infections (SIs) or herpes zoster (HZ) across groups and no deaths. Limitations: small sample size, differences in BL characteristics.Table 1.Safety outcomes by BL CRP (NML <5 mg/L; ELV ≥5 mg/L)n (%)IRd [95% CI]To W16To W48Tofacitinib 5 mg BIDaPBOAll tofacitinib 5 mg BIDbAll tofacitinibcNML N=58ELV N=127NML N=55ELV N=132NML N=91ELV N=225NML N=129ELV N=291TEAEs39 (67.2)365.4[259.9, 499.6]61 (48.0)222.7[170.4, 286.1]27 (49.1)240.7[158.6, 350.2]64 (48.5)235.4[181.3, 300.6]60 (65.9)188.2[143.7, 242.3]138 (61.3)146.5[123.1, 173.1]80 (62.0)202.5[160.6, 252.0]168 (57.7)155.6[133.0, 181.0]SAEs1 (1.7)5.6[0.1,31.0]2 (1.6)5.1[0.6,18.6]00.0[0.0,21.9]1 (0.8)2.5[0.1,14.0]5 (5.5)7.8[2.5,18.2]3 (1.3)1.8[0.4,5.3]5 (3.9)6.6[2.1,15.4]4 (1.4)2.2[0.6,5.5]All infections23 (39.7)158.0 [100.2, 237.1]28 (22.0)81.5[54.2, 117.8]13 (23.6)87.9 [46.8, 150.2]30 (22.7)83.9[56.6, 119.8]37 (40.7)82.1[57.8, 113.2]74 (32.9)56.7[44.5, 71.2]46 (35.7)84.1[61.6, 112.2]86 (29.6)58.0[46.4, 71.6]SIs1 (1.7)5.6[0.1, 31.0]00.0[0.0, 9.5]00.0[0.0, 21.9]00.0[0.0, 9.2]1 (1.1)1.5[0.0, 8.5]00.0[0.0, 2.2]1 (0.8)1.3[0.0, 7.3]00.0 [0.0, 2.0]HZ00.0[0.0,20.4]00.0[0.0,9.5]00.0[0.0, 21.9]00.0[0.0,9.2]2 (2.2)3.1[0.4,11.1]3 (1.3)1.8[0.4,5.3]3 (2.3)3.9[0.8,11.5]4 (1.4)2.2[0.6,5.5]Dis-continuationdue to AEs1 (1.7)5.6[0.1,31.0]3 (2.4)7.7[1.6,22.6]2 (3.6)11.9[1.4,43.0]2 (1.5)5.0[0.6,18.0]4 (4.4)6.1[1.6,15.7]7 (3.1)4.2[1.7,8.7]4 (3.1)5.2[1.4,13.4]8 (2.7)4.3[1.9,8.5]aTo W12: P2; W16: P3b To W12: P2; W48: P3c P2: tofacitinib 2, 5 or 10 mg BID to W12; P3: 5 mg BID to W48d Pts with events/100 pt-yearsCI, confidence interval; n, number of pts with an event within risk period (on treatment); N, number of pts in safety analysis setConclusionRegardless of BL CRP, at W12, tofacitinib was more efficacious vs PBO; and across endpoints, the differences in response from PBO for tofacitinib were numerically greater in pts with ELV vs NML CRP. Tofacitinib safety rates were consistent with PBO in pts with ELV CRP, but trended higher for tofacitinib vs PBO in pts with NML CRP.AcknowledgementsThis study was sponsored by Pfizer. Medical writing support, under the direction of the authors, was provided by Lavanyaa Manjunatha, PhD, CMC Connect, a division of IPG Health Medical Communications, and was funded by Pfizer, New York, NY, USA, in accordance with Good Publication Practice (GPP 2022) guidelines (Ann Intern Med 2022; 175: 1298-1304).Disclosure of InterestsAtul Deodhar Consultant of: AbbVie, Amgen, Aurinia, Bristol Myers Squibb, Celgene, Eli Lilly, GSK, Janssen, MoonLake, Novartis, Pfizer Inc and UCB, Grant/research support from: AbbVie, Bristol Myers Squibb, Celgene, Eli Lilly, GSK, Janssen, Novartis, Pfizer Inc and UCB, Xenofon Baraliakos Speakers bureau: AbbVie, Amgen, Chugai, Eli Lilly, Galapagos, Janssen, MSD, Novartis, Pfizer Inc, Roche, Sandoz and UCB, Consultant of: AbbVie, Amgen, Chugai, Eli Lilly, Galapagos, Janssen, MSD, Novartis, Pfizer Inc, Roche, Sandoz and UCB, Marina Magrey: None declared, Lianne S. Gensler: None declared, Amit V Thorat Shareholder of: Pfizer Inc, Employee of: Pfizer Inc, Cassandra Kinch Shareholder of: Pfizer Inc, Employee of: Pfizer Inc, Surya Pemmaraju Shareholder of: Pfizer Inc, Employee of: Pfizer Inc, Mary Jane Cadatal Shareholder of: Pfizer Inc, Employee of: Pfizer Inc, Peter Nash Speakers bureau: AbbVie, Bristol Myers Squibb, Celgene, Eli Lilly, Janssen, Novartis, Pfizer Inc, Galapagos and GSK, Grant/research support from: AbbVie, Bristol Myers Squibb, Celgene, Eli Lilly, Pfizer Inc, Galapagos, GSK, Janssen and Novartis.
Effect of low energy argon ion irradiation on work function of AISI 304L stainless steel
The effect of low-energy Ar + ion irradiation on the work function of stainless steel AISI 304L (SS-304L) was studied by varying energy and fluence of Ar + ion. The irradiation of Ar + ions on stainless steel creates several vacancies in the target material which resulted a change in work function. The retarding field diode method was used for the measurement of work function. Results reveal work function decreases with an increase in ion energy (for fixed ion fluence) of irradiated Ar + ion. Furthermore, it was observed that at varying ion fluence (for fixed ion energy) the decrease in work function value was more prominently, but at higher fluence, it again increases. In both (energy and fluence) cases of irradiation, the displacement per atom (DPA) in the material has been estimated with the stopping range using the SRIM-2013.00 program and is correlated with the experimental observation. Overall, the maximum work function was observed to be decreased by ~ 7.28% relative to the pristine sample in the case of fluence variation keeping the energy constant at 30 keV. The results indicate that low-energy ion irradiation can be utilized for work function modulation of materials and can be optimized by controlling ion fluence. The results are useful for further understanding of corrosion rate of materials and the data are extremely important for various nuclear reactors, where these materials are used.
Porous NiCo.sub.2O.sub.4 electrodes for high-energy asymmetric supercapacitor: effect of annealing
Nickel-cobalt hydroxide thin films were synthesized using the chemical bath deposition method, and the effect of thermal annealing (373-673 K) on their physicochemical and electrochemical characteristics was explored. The X-ray diffraction study showed a cubic crystalline structure of NiCo.sub.2O.sub.4 electrode formed above annealing temperature of 573 K. Field emission scanning electron spectroscopy (FE-SEM) study revealed that after annealing, NiCo.sub.2O.sub.4 electrode showed urchin-like microspheres morphology with superhydrophilic nature. The electrode annealed at 573 K exhibited outstanding electrochemical performance with a specific capacitance of 470 F g.sup.-1 at 0.4 A g.sup.-1 current density. Over 2000 cycles, electrode demonstrated capacitive retention of 75.55%. Finally, NiCo.sub.2O.sub.4 and Fe.sub.2O.sub.3 thin films were used to construct the asymmetric supercapacitor (ASC) device. The ASC device manifested energy density of 40 Wh kg.sup.-1 at power density of 1.66 kW kg.sup.-1 and 82% retention after 2000 CV cycles.
N-Benzylation of 6-aminoflavone by reductive amination and efficient access to some novel anticancer agents via topoisomerase II inhibition
Series of novel N-benzyl derivatives of 6-aminoflavone (9a–n) were synthesized and evaluated for anticancer and topoisomerase II enzyme inhibition activity. All the synthesized compounds were screened for in vitro anticancer activity against human breast cancer cell line (MCF-7) and human lung cancer cell line (A-549). Among the synthesized compounds, 9f and 9g were found to be the most potent anticancer agents against human breast cancer cell line (MCF-7) with IC50 values of 9.35 µM and 9.58 µM, respectively. Compounds 9b, 9c and 9n exhibited promising anticancer activity against human lung cancer cell line (A-549) with 43.71%, 46.48% and 44.26% inhibition at the highest concentration of 10 µM, respectively. Compounds 9c, 9f and 9g have ability to inhibit the topoisomerase II enzyme. Compound 9f showed most potent topoisomerase II enzyme inhibition activity with IC50 value of 12.11 µM. Further, these compounds have a high potential to be developed as a promising topoisomerase II inhibitors.