Current Issue : October - December Volume : 2019 Issue Number : 4 Articles : 5 Articles
Three-dimensional printing (3DP) has demonstrated great potential for multi-material\nfabrication because of its capability for printing bespoke and spatially separated material\nconformations. Such a concept could revolutionise the pharmaceutical industry, enabling the\nproduction of personalised, multi-layered drug products on demand. Here, we developed a novel\nstereolithographic (SLA) 3D printing method that, for the first time, can be used to fabricate multi-layer\nconstructs (polypills) with variable drug content and/or shape. Using this technique, six drugs,\nincluding paracetamol, caffeine, naproxen, chloramphenicol, prednisolone and aspirin, were printed\nwith different geometries and material compositions. Drug distribution was visualised using Raman\nmicroscopy, which showed that whilst separate layers were successfully printed, several of the drugs\ndiffused across the layers depending on their amorphous or crystalline phase. The printed constructs\ndemonstrated excellent physical properties and the different material inclusions enabled distinct drug\nrelease profiles of the six actives within dissolution tests. For the first time, this paper demonstrates the\nfeasibility of SLA printing as an innovative platform for multi-drug therapy production, facilitating a\nnew era of personalised polypills....
The improvement of the loading content of hydrophilic drugs by polymer nanoparticles\n(NPs) recently has received increased attention from the field of controlled release. We developed a\nnovel, simply modified, drop-wise nanoprecipitation method which separated hydrophilic drugs\nand polymers into aqueous phase (continuous phase) and organic phase (dispersed phase), both\nindividually and involving a mixing process. Using this method, we produced ciprofloxacin-loaded\nNPs by Poly (d,l-lactic acid)-Dextran (PLA-DEX) and Poly lactic acid-co-glycolic acid-Polyethylene\nglycol (PLGA-PEG) successfully, with a considerable drug-loading ability up to 27.2 wt% and an\nin vitro sustained release for up to six days. Drug content with NPs can be precisely tuned by\nchanging the initial drug feed concentration of ciprofloxacin. These studies suggest that this modified\nnanoprecipitation method is a rapid, facile, and reproducible technique for making nano-scale drug\ndelivery carriers with high drug-loading abilities...
The aim of this research was to investigate the stability of a lidocaine-loaded nanostructured\nlipid carrier dispersion at different temperatures, formulate a nanostructured lipid carrier gel, and test\nthe penetration profile of lidocaine from the nanostructured lipid carrier gel using different skin\npenetration modeling methods. The formulations were characterized by laser diffraction, rheological\nmeasurements and microscopic examinations. Various in vitro methods were used to study drug\nrelease, diffusion and penetration. Two types of vertical Franz diffusion cells with three different\nmembranes, including cellulose, Strat-M®, and heat separated human epidermis were used and\ncompared to the Skin-parallel artificial membrane permeability assay (PAMPA) method. Results\nindicated that the nanostructured lipid carrier dispersion had to be gelified as soon as possible for\nproper stability. Both the Skin-PAMPA model and Strat-M® membranes correlated favorably with\nheat separated human epidermis in this research, with the Strat-M® membranes sharing the most\nsimilar drug permeability profile to an ex vivo human skin model. Our experimental findings suggest\nthat even when the best available in vitro experiment is selected for modeling human skin penetration\nto study nanostructured lipid carrier gel systems, relevant in vitro/in vivo correlation should be made\nto calculate the drug release/permeation in vivo. Future investigations in this field are still needed to\ndemonstrate the influence of membranes and equipment from other classes on other drug candidates....
Human African trypanosomiasis (HAT), also commonly known as sleeping sickness, is a\nneglected tropical disease affecting millions of people in poorly developed regions in sub-Saharan\nAfrica. There is no satisfactory treatment for this infection. The investment necessary to bring new\ndrugs to the market is a big deterrent to drug development, considering that the affected communities\nform a non-lucrative sector. However, natural products and many sesquiterpene lactones (STLs) in\nparticular are very strong trypanocides. Research and applications of nano-drug delivery systems\nsuch as nanoparticles (NPs) have undergone unprecedented growth in the recent past. This is\nmainly due to the advantages offered by these systems, such as targeted delivery of the drug to\nthe place of action (cell, parasite, etc), sustained release of the drug, increased bioavailability,\nreduced drug dosage, and reduction of undesired side effects, among others. In this study,\nthe STLs alpha-santonin, arglabin, schkuhrin II, vernolepin, and eucannabinolide, all trypanocides,\nwere loaded into polylactic acid (PLA) NPs through an emulsification-diffusion method. The NPs\nwere stable, homogenous, and spherical in shape with a rounded knotty depression like a navel\norange. The average particle sizes were 202.3, 220.3, 219.5, 216.9, and 226.4 nm for alpha-santonin,\narglabin, schkuhrin II, vernolepin, and eucannabinolide, respectively. The NPs had encapsulation\nefficiencies of 94.6, 78.1, 76.8, 60.7, and 78.9% for Alpha-santonin, arglabin, schkuhrin II, vernolepin,\nand eucannabinolide, respectively. The NPs loaded with arglabin, vernolepin, and eucannabinolide\nexhibited considerable antitrypanosomal activity against Trypanosoma brucei rhodesiense (Tbr) with\nfree drug equivalent IC50 values of 3.67, 1.11 and 3.32 microM, respectively. None of the NP formulations\ndisplayed cytotoxicity towards mammalian cells (rat skeletal myoblast cell line L6). These results\nprovide new insights into the possibility of incorporating STLs into nanoparticles, which may provide\nnew options for their formulation in order to develop new drugs against HAT....
Solvents purification mainly used in pharmaceutical field such as acetone and\nmethyl ethyl ketone (MEK) were performed through hybrid silica membranes and from\nbinary and multi-components mixtures. Two hybrid silica membranes-zirconia doped\nbis(triethoxysilyl)methane and bis(triethoxysilyl)ethane (BTESE)-were studied. Flux, permeance,\nand separation factor were evaluated depending on temperature, composition, and number of organic\ncompounds in the feed. Dehydration tests of acetone were operated at 30 and 45 DegreeC following\nby acetone and MEK purification at 50 Degree C from multi-components hydro-organic mixtures where\nhydrophilic compounds (water, methanol) but also hydrophobic (dichloromethane (DCM) and/or\ntoluene) were present. Results showed that the presence of Zr nanoparticles affected flux and\nimproved selectivity in the case of dehydration. Experiments related to acetone and MEK purification,\nrevealed a mass transfer alteration and a decrease of performance, from 99 to 97 wt% and from 98 to\n95 wt% respectively, when the number of compounds in the initial feed grown up and more precisely,\nin the presence of DCM and toluene thus highlighting a possible coupling effect....
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