The purpose of this research was to develop a matrix-type transdermal therapeutic system containing carvedilol with different ratios of hydrophilic and hydrophobic polymeric combinations by the solvent evaporation technique. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy and differential scanning calorimetry. The results suggested no physicochemical incompatibility between the drug and the polymers. In vitro permeation studies were performed by using Franz diffusion cells. The results followed Higuchi kinetics (r = 0.9953-0.9979), and the mechanism of release was diffusion mediated. Based on physicochemical and in vitro skin permeation studies, patches coded as F3 (ethyl cellulose:polyvinylpyrrolidone, 7.5:2.5) and F6 (Eudragit RL:Eudragit RS, 8:2) were chosen for further in vivo studies. The bioavailability studies in rats indicated that the carvedilol transdermal patches provided steady-state plasma concentrations with minimal fluctuations and improved bioavailability of 71% (for F3) and 62% (for F6) in comparison with oral administration. The antihypertensive activity of the patches in comparison with that of oral carvedilol was studied using methyl prednisolone acetate-induced hypertensive rats. It was observed that both the patches significantly controlled hypertension from the first hour (P < .05). The developed transdermal patches increase the efficacy of carvedilol for the therapy of hypertension.

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Environmental pollution caused by heavy metals is a serious threat. In the present work, removal of chromium was carried out using chitosan-magnetite nanocomposite strip. Magnetite nanoparticles (Fe 3 O 4 ) were synthesized using chemical co-precipitation method at 80°C. The nanoparticles were characterized using UVvisible spectroscopy, fourier transform infrared spectroscopy, X-ray diffraction spectrometer, atomic force microscope, dynamic light scattering and vibrating sample magnetometer, which confirm the size, shape, crystalline nature and magnetic behaviour of nanoparticles. Atomic force microscope revealed that the particle size was 15-30 nm and spherical in shape. The magnetite nanoparticles were mixed with chitosan solution to form hybrid nanocomposite. Chitosan strip was casted with and without nanoparticle. The affinity of hybrid nanocomposite for chromium was studied using K 2 Cr 2 O 7 (potassium dichromate) solution as the heavy metal solution containing Cr(VI) ions. Adsorption tests were carried out using chitosan strip and hybrid nanocomposite strip at different time intervals. Amount of chromium adsorbed by chitosan strip and chitosan-magnetite nanocomposite strip from aqueous solution was evaluated using UV-visible spectroscopy. The results confirm that the heavy metal removal efficiency of chitosan-magnetite nanocomposite strip is 92.33 %, which is higher when compared to chitosan strip, which is 29.39 %.

Niosome vesicles of cytarabine hydrochloride were prepared by a lipid hydration method that excluded dicetylphosphate. The sizes of the vesicles obtained ranged from 600 to 1000 nm, with the objective of producing more blood levels in vivo. The study of the release of drug from niosomes exhibited a prolonged release profile as studied over a period of 16 hr. The drug entrapment efficiency was about 80% with Tween 80, Span 60 and Tween 20; for Span 80, it was 67.5%. The physical stability profile of vesicular suspension was good as studied over a period of 4 weeks.

Solid Lipid Nanoparticles (SLN) containing Methotrexate (MTX), an anticancer drug for intravenous administration was formulated and characterized. The SLN dispersions with MTX, stearic acid, and soya lecithin in the ratio of 1:4:1, 1:4:1.5, and 1:4:2, sodium taurodeoxycholate and distilled water were prepared by micro emulsification solidification method. The results show that the prepared MTX-SLN particles (with MTX-Stearic acid-Soya lecithin--1:4:2) have an average size of 270 nm with 51.3% drug entrapment. The in-vitro release was attained up to 15th h. The pharmacokinetic study reveals that the half-life and MRT of SLNs were higher than MTX solution. The life span of EAC (Ehrlich Ascite Carcinoma) bearing mice was increased when treated with MTX-SLNs (Methotrexate nanoparticles). These results clearly indicate that SLNs are a promising sustained release drug targeting system for lipophilic antitumour drugs.

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Methicillin-resistant Staphylococcus aureus (MRSA) infections are easily spread among infected patients, where resistance has dramatically increased resulted in serious health issues. Therefore, there is a need to develop alternative natural or combination drug therapies. Apigenin (AP) is a natural poly phenolic flavonoid has been found to possess many beneficial biological actions. The aim of this study was to investigate the anti-MRSA efficacy and synergistic effect of apigenin (AP) and in combination with ampicillin (AM) and ceftriaxone (CEF). The antibacterial activity of apigenin was assessed by the broth macro dilution, checkerboard micro dilution method and time-kill assay. The mode of action was studied by outer and inner membrane permeabilisation assays, scanning electron microscopy and transmission electron microscopy. The minimum inhibitory concentration (MIC) of apigenin against gram positive and gram negative strain ranged from 32.5 to 62.5µg/ml. In checkerboard method apigenin markedly reduced the MIC of the antibiotics ampicillin 800 µg/ml shifted to 107 µg/ml (AM+AP) and ceftriaxone 58 µg/ml shifted to 2.6 µg/ml (CEF+AP) against MRSA. The synergistic activity of ampicillin and ceftriaxone plus apigenin combinations with FIC indices (CI) between 0.18-0.47. The modulation of methicillin-resistance by apigenin significantly enhanced the activities of ampicillin and ceftriaxone. The result of time-kill assays of the two drug combinations AM +AP and CEF+AP against MRSA showed significant inhibitory effect and reduced the colony count by approximately 99% after 8 h The results for outer membrane (OM) and inner membrane (IM) permeabilization showed that ampicillin and ceftriaxone in combination with apigenin damaged MRSA cytoplasmic membrane and caused subsequent leakage of intracellular constituents. Electron microscopy clearly showed that the above said combination also caused marked morphological damage of cell wall, cell shape and plasma membrane of this strain. From these results, it can be concluded that apigenin has the synergistic effect with ampicillin and ceftriaxone to reverse bacterial resistance against MRSA.