Current Issue : January - March Volume : 2019 Issue Number : 1 Articles : 5 Articles
Sustained-release preparation is a hot spot in antitumor drug research, where the first task\nis to select suitable drug carriers. Research has revealed that carboxylic acid iron metalâ??organic\nframeworks (MOFs), constructed from iron (Fe) ions and terephthalic acid, are nontoxic and\nbiocompatible. Due to the breathing effect, the skeleton of this mesoporous material is flexible\nand can reversibly adapt its pore size through drug adsorption. Therefore, we chose one kind of\nFe-MOF, MIL-53(Fe), as a carrier for the anticancer drug oridonin (Ori). In this work, we report\nthe design and synthesis of MIL-53(Fe) and explore its ability as a transport vehicle to deliver Ori.\nMIL-53(Fe) is characterized by scanning electron microscopy and X-ray powder diffraction. A loading\ncapacity of 56.25 wt % was measured by high performance liquid chromatography. This carrier was\nsafe and nontoxic (cell viability > 95.27%), depending on the results of 3-(4,5-dimethylthiazol-2-yl)â??\n2,5-diphenyltetrazolium bromide assays, lactate dehydrogenase assays, and Annexin V-fluoresce\nisothiocyanate/propidium iodide double-staining assays. After loading the drug, the structure of the\nMIL-53(Fe) was not destroyed, and Ori was amorphous in MIL-53(Fe). Based on an analysis of the Ori\nrelease profile, results suggest that it lasts for more than seven days in vitro. The cumulative release\nrate of Ori at the seventh day was about 82.23% and 91.75% in phosphate buffer saline solution at ..... under pH 7.2 and pH 5.5, respectively. HepG2 cells were chosen to study the cytotoxicity of\nOri@MIL-53(Fe), and the results show that the anticancer ratio of Ori@MIL-53(Fe) system reaches\n90.62%. Thus, MIL-53 can be used as a carrier for anticancer drugs and Ori@MIL-53(Fe) is a promising\nsustained-release drug delivery system for the cancer therapy....
N-Palmitoyl-Glycine-Histidine (Pal-GH) is a novel low molecular weight gelator. In our\nprevious report, ivermectin, a lipophilic drug, was effectively delivered to skin tissue after topical\napplication with Pal-GH as a spray gel formulation, and a much higher skin concentration was\nconfirmed than with the administration of a conventional oral formulation. The objective of this\nstudy was to increase the skin permeation of metronidazole (MTZ), a hydrophilic drug, after the\ntopical application of Pal-GH gel. An evaluation of the combined effect of chemical penetration\nenhancers (CPEs), such as isopropyl myristate (IPM), propylene glycol (PG), ethanol, diethylene glycol\nmonoethyl ether, and dimethyl sulfoxide (DMSO), on skin permeation was also conducted. We found\nthat a 5% Pal-GH gel containing 1% MTZ (F5MTZ) exhibited a 2.7-fold higher MTZ permeation\nthrough excised hairless rat skin than its solution. Furthermore, F5PG-MTZ and F5IPM-MTZ further\nincreased the skin permeation of MTZ when compared to F5MTZ. Interestingly, F5PG-MTZ enhanced\nthe skin penetration of MTZ, although no enhancement effect was observed for an MTZ solution\ncontaining PG. Thus, a Pal-GH formulation containing PG and IPM may enhance the skin permeation\nof MTZ....
Nowadays, the safety of parabens as pharmaceutical preservatives is debated.\nRecent studies investigated their interference with the oestrogen receptors, nevertheless\ntheir carcinogenic activity was also proved. That was the reason why the re-evaluation\nof the biocompatibility and antimicrobial activity of parabens is required using modern\ninvestigation methods. We aimed to test the cytotoxic, antifungal and antibacterial effect of\nparabens on Caco-2 cells, C. albicans, C. parapsilosis, C. glabrata, E. coli, P. aeruginosa and S. aureus.\nTwo complex systems (glycerolâ??Polysorbate 20; ethanolâ??Capryol PGMCâ?¢) were formulated to\nstudyâ??with the MTT-assay and microdilution method, respectivelyâ??how other excipients may\nmodify the biocompatibility and antimicrobial effect of parabens. In the case of cytotoxicity, the\ntoxicity of these two systems was highly influenced by co-solvents and surfactants. The fungi\nand bacteria had significantly different resistance in the formulations and in some cases the\nexcipients could highly modify the effectiveness of parabens both in an agonistic and in a\ncounteractive way. These results indicate that with appropriate selection, non-preservative excipients\ncan contribute to the antimicrobial safety of the products, thus they may decrease the required\npreservative concentration....
Purpose: Drug coated balloons (DCB) are continually improving due to advances in\ncoating techniques and more effective excipients. Paclitaxel, the current drug choice of\nDCB, is a microtubule-stabilizing chemotherapeutic agent that inhibits smooth muscle\ncell proliferation. Excipients work to promote coating stability and facilitate paclitaxel\ntransfer and retention at the target lesion, although current excipients lack sustained,\nlong-term paclitaxel retention. Keratose, a naturally derived protein, has exhibited unique\nproperties allowing for tuned release of various therapeutic agents. However, little\nis known regarding its ability to support delivery of anti-proliferative agents such as\npaclitaxel. The goal of this project was to thus demonstrate the feasibility of keratose\nas a DCB-coating excipient to promote the release and delivery of paclitaxel.\nMethods: Keratose was combined with paclitaxel in vitro and the release kinetics of\npaclitaxel and keratose were evaluated through high performance liquid chromatographmass\nspectroscopy (HPLC-MS) and spectrophotometry, respectively. A custom coating\nmethod was developed to deposit keratose and paclitaxel on commercially available\nangioplasty balloons via an air spraying method. Coatings were then visualized under\nscanning electron microscopy and drug load quantified by HPLC-MS. Acute arterial\ntransfer of paclitaxel at 1 h was assessed using a novel ex vivo model and further\nevaluated in vivo in a porcine ilio-femoral injury model. ... Results: Keratose demonstrated tunable release of paclitaxel as a function of keratose\nconcentration in vitro. DCB coated via air spraying yielded consistent drug loading Under scanning electron microscopy, the keratose-paclitaxel\nDCB showed uniform coverage with a consistent, textured appearance. The acute drug\ntransfer of the keratose-paclitaxel DCB was 43.60 ... 14.8 ng/mg at 1 h ex vivo. These\nmeasurements were further confirmed in vivo as the acute 1 h arterial paclitaxel levels\nwere .... Conclusion: The keratose-paclitaxel coated DCB exhibited paclitaxel uptake and\nachieved acute therapeutic arterial tissue levels, confirming the feasibility of keratose\nas a novel excipient for DCB....
The objective of this work was to study in vitro propranolol permeation and skin retention after topical application of different\nsemisolid vehicles, with the final aim of developing new topical formulations intended for the treatment of infantile hemangioma,\nable to produce therapeutic drug levels in the skin, avoiding systemic absorption. Propranolol ointments, creams, and gels were\nprepared and tested on pig skin, an accepted model of human skin. Fromthe results obtained in the present work it is clear that the\npermeation of propranolol across the skin is a poor predictor of its skin retention, at least in the time-frame considered. With an\napplication time of 4 h, reasonably close to the permanence time of a semisolid formulation on the skin surface, the best performance\n(high retention and lowskin penetration)was obtained with lipophilic formulations, in particular with a lipophilic creamcontaining\nolive oil. Hydrophilic formulations, such as gels, are characterized by a significant permeation across the skin, probably leading to\nsystemic side effects, accompanied by a limited skin retention. Overall, the results obtained in the present work pose the basis for\nthe development of new topical formulations, containing propranolol, with better performance and reduced systemic absorption....
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