Current Issue : April - June Volume : 2019 Issue Number : 2 Articles : 5 Articles
Flexible liposomes (FLs) were developed as promising nano-carriers for anticancer drugs.\nCoating them with chitosan (CS) could improve their drug delivery properties. The aim of this study\nwas to investigate the physicochemical characteristics, pharmacokinetics behavior, and cytotoxic\nefficacy of docetaxel (DTX)-loaded CS-coated FLs (C-FLs). DTX-loaded FLs and C-FLs were produced\nvia thin-film evaporation and electrostatic deposition methods, respectively. To explore their\nphysicochemical characterization, the particle size, zeta potential, encapsulation efficiency (EE%),\nmorphology, and DTX release profiles were determined. In addition, pharmacokinetic studies\nwere performed, and cytotoxic effect was assessed using colon cancer cells (HT29). Various FLs,\ndependent on the type of surfactant, were formed with particle sizes in the nano-range, 137.6 Â} 6.3\nto 238.2 Â} 14.2 nm, and an EE% of 59â??94%. Moreover, the zeta potential shifted from a negative to\na positive value for C-FL with increased particle size and EE%, and the in vitro sustained-release\nprofiles of C-FL compared to those of FL were evident. The optimized C-FL containing sodium\ndeoxycholate (NDC) and dicetyl phosphate (DP) elicited enhanced pharmacokinetic parameters and\ncytotoxic efficiency compared to those of the uncoated ones and Onkotaxel®. In conclusion, this\napproach offers a promising solution for DTX delivery....
Pain is inadequately relieved by escalating doses of a strong opioid analgesic such as\nmorphine in up to 25% of patients with cancer-related severe pain complicated by a neuropathic\n(nerve damage) component. Hence, there is an unmet medical need for research on novel painkiller\nstrategies. In the present work, we used supercritical fluid polymer encapsulation to develop\nsustained-release poly(lactic-co-glycolic acid) (PLGA) biodegradable microparticles containing the\nanalgesic adjuvant drug ketamine, for injection by the intrathecal route. Using this approach with a\nrange of PLGA co-polymers, drug loading was in the range 10â??60%, with encapsulation efficiency\n(EE) of 60â??100%. Particles were mainly in the size rangeâ?¦â?¦â?¦â?¦â?¦...
The objective of this study was to optimize and develop fast disintegrating liquisolid compact of sertraline hydrochloride to enhance the dissolution and study the dissolution in different pH conditions. Fast disintegrating liquisolid compacts were prepared from Neusilin US2 as a carrier material, Aeroperl 300 as a coating material, crospovidone as a superdisintegrants and Tween80 as a non-volatile liquid vehicle. In liquisolid formulations the ratio of carrier to coating material was kept enhancing. The ratio 40 gives optimal results relative to other ratios. The pre-compression evaluation includes: flow properties, angle of slide and FT-IR study for drug-excipient compatibility. The post-compression evaluation which includes: friability, hardness, wetting time, in-vitro disintegration time, drug content and % drug release-1 h. Among the superdisintegrants, crospovidone was found to be best to give the fastest disintegration. The optimized batch (F7c) was prepared using 5% crospovidone, shows the shortest disintegration time (44 sec), superior drug release profile (almost 90% drug release). Selected formulation minimizes the pH effect on dissolution. Complete solubilization of drug into non-volatile liquid, provides enhanced drug release due to an improved surface area, wettability and drug solubility....
The feasibility of upscaling the formulation of co-amorphous indomethacin-lysine from\nlab-scale to pilot-scale spray drying was investigated. A 22 full factorial design of experiments (DoE)\nwas employed at lab scale. The atomization gas flow rate (Fatom, from 0.5 to 1.4 kg/h) and outlet\ntemperature (Tout, from 55 to 75 Degree Centigrade ) were chosen as the critical process parameters. The obtained\namorphization, glass transition temperature, bulk density, yield, and particle size distribution were\nchosen as the critical quality attributes. In general, the model showed low Fatom and high Tout to\nbe beneficial for the desired product characteristics (a co-amorphous formulation with a low bulk\ndensity, high yield, and small particle size). In addition, only a low Fatom and high Tout led to the\ndesired complete co-amorphization, while a minor residual crystallinity was observed with the\nother combinations of Fatom and Tout. Finally, upscaling to a pilot scale spray dryer was carried out\nbased on the DoE results; however, the drying gas flow rate and the feed flow rate were adjusted to\naccount for the different drying chamber geometries. An increased likelihood to achieve complete\namorphization, because of the extended drying chamber, and hence an increased residence time of\nthe droplets in the drying gas, was found in the pilot scale, confirming the feasibility of upscaling\nspray drying as a production technique for co-amorphous systems....
The scope of this work was to determine the possibility of the application of the pulsed\nelectric field (PEF) technique to the production of extracts from Moringa oleifera plant material\n(freeze-dried leaves). Various PEF conditions (pulse durationâ??PD; and pulse intervalâ??PI) were\ntested. A field strength of 7 kV/cm was used. The total phenols in the extracts were evaluated by\nthe Folinâ??Ciocalteu method and the antioxidant activity was evaluated by the radical scavenging\nactivity (DPPHâ?¢), ferric reducing antioxidant power (FRAP) and Rancimat methods. The results\nwere compared with those of the extracts obtained using other extraction techniques, namely\nmicrowave-assisted and ultrasound-assisted extractions, simple boiling water extraction, and plain\nmaceration with water (as the control). The highest extraction of total phenols was achieved by\nthe PEF procedure using 40 min treatment at a PD of 20 msec and a PI of 100..................
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