Current Issue : October - December Volume : 2020 Issue Number : 4 Articles : 5 Articles
This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon\ncancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100)\nmicroparticles. The release of EAdouble-coatedmicroparticles (MPs) was tested at simulative pH values.\nMaximum release was observed at 24 h and pH7.4. The cytotoxicity of EAMPs onHCT 116 colon cancer\ncells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry\nsuggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher\ncell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic\nactivity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation\nof the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and\ntotal cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the\ndouble-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography.\nIn conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting\nas well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared\nwith the administration of raw EA....
Orodispersible tablets (ODTs) offer rapid disintegration of the dosage form when placed on\nthe tongue, which leads to fast release of the active pharmaceutical ingredient. Despite increased use\nin diverse patient populations, there have been numerous challenges associated with ODTs. One\nsuch concern is the lack of standardised assessment of disintegration behaviour. In the European\nPharmacopoeia, â??orodispersiblesâ?? are defined as such if disintegration time is faster than 3 min.\nCommon in vitro measurement methods only provide single time point data and have limited\nphysiological accuracy. To determine more bio-predictive disintegration kinetics, a bench-top in vitro\noral cavity model (OCM) was modified and piloted to assess disintegration of three ODTs of differing\nhardness. All ODTs disintegrated similarly within the OCMâ??surface breakdown/swelling, initial\nâ??wash awayâ?? and final â??wash awayâ??. The distinct advantage presented within this pilot study using\nthe OCM is the opportunity to ascertain disintegration behaviour profiles of ODTs by evaluating\nchanges in the observable area during simulated oral processing. The model could be implemented\nas a decision-support tool during the early stages of the drug design process to improve acceptability\nand further understand ODT disintegration behaviour....
Amphotericin B (AmpB), one of the most commonly used agents in the treatment of\nsevere fungal infections and life-threatening parasitic diseases such as visceral Leishmaniasis, has a\nnegligible oral bioavailability, primarily due to a low solubility and permeability. To develop an\noral formulation, medium chain triglycerides and nonionic surfactants in a self-nano-emulsifying\ndrug delivery system (SNEDDS) containing AmpB were combined with room temperature ionic\nliquids (RTILs) of imidazolium. The presence of ionic liquids significantly enhanced the solubility of\nAmpB, exhibited a low toxicity and increased the transport of AmpB across Caco-2 cell monolayers.\nThe combination of RTILs with a lipid formulation might be a promising strategy to improve the oral\nbioavailability of AmpB....
Opportunistic fungal infections are responsible for over 1.5 million deaths per year.\nThis has created a need for highly effective antifungal medication to be as potent as possible. In this\nstudy, we improved the effcacy of a common over the counter (OTC) antifungal skin medication,\nmiconazole, by encapsulating nano-molecules of the drug in cholesterol/sodium oleate nano-vesicles.\nThese nano-vesicles were characterized to optimize their size, zeta potential, polydispersity index\nand encapsulation effciency. Furthermore, these nano-vesicles were compared to a conventional\nmiconazole-based commercially available cream to determine potential improvements via permeation\nthrough the stratum corneum, cytotoxicity, and antifungal capabilities. Our results found that the\nvesicle size was within the nano range (~300 nm), with moderate polydispersity and stability.\nWhen compared with the commercially available cream, Actavis, as well as free miconazole,\nthe miconazole nano-vesicle formulation displayed enhanced fungal inhibition by a factor of three\nor more when compared to free miconazole. Furthermore, with smaller nanoparticle (NP) sizes,\nhigher percentages of miconazole may be delivered, further enhancing the effcacy of miconazoleâ??s\nantifungal capability. Cytotoxicity studies conducted with human dermal fibroblast cells confirm its\nbiosafety and biocompatibility, as cell survival rate was observed to be twofold higher in nano-vesicle\nformulation than free miconazole. This formulation has the potential to treat fungal infections through\nincreasing the retention time in the skin, improving the treatment approach, and by enhancing the\necacy via the use of nano-vesicles....
Amorphous solid dispersions (ASDs) improve the oral delivery of poorly water-soluble\ndrugs. ASDs of olanzapine (OLZ), which have a high melting point and low solubility, are performed\nusing a complicated process. Three-dimensional (3D) printing based on hot-melt pneumatic extrusion\n(HMPE) is a simplified method for producing ASDs. Unlike general 3D printing, printlet extrusion is\npossible without the preparation of drug-loaded filaments. By heating powder blends, direct fused\ndeposition modeling (FDM) printing through a nozzle is possible, and this step produces ASDs\nof drugs. In this study, we developed orodispersible films (ODFs) loaded with OLZ as a poorly\nwater-soluble drug. Various ratios of film-forming polymers and plasticizers were investigated\nto enhance the printability and optimize the printing temperature. Scanning electron microscopy\n(SEM) showed the surface morphology of the film for the optimization of the polymer carrier ratios.\nDifferential scanning calorimetry (DSC) was used to evaluate thermal properties. Powder X-ray\ndiffraction (PXRD) confirmed the physical form of the drug during printing. The 3D printed ODF\nformulations successfully loaded ASDs of OLZ using HMPE. Our ODFs showed fast disintegration\npatterns within 22 s, and rapidly dissolved and reached up to 88% dissolution within 5 min in\nthe dissolution test. ODFs fabricated using HMPE in a single process of 3D printing increased the\ndissolution rates of the poorly water-soluble drug, which could be a suitable formulation for fast\ndrug absorption. Moreover, this new technology showed prompt fabrication feasibility of various\nformulations and ASD formation of poorly water-soluble drugs as a single process. The immediate\ndissolution within a few minutes of ODFs with OLZ, an atypical antipsychotic, is preferred for drug\ncompliance and administration convenience....
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