In the present research work mouth dissolving tablets of domperidone were developed with superdisintegrants like crospovidone, croscarmellose sodium and sodium starch glycollate in various concentrations like 3%, 4% and 6% w/w by direct compression method. All formulations were evaluated for physical characteristics of compressed tablets such as weight variation, hardness, friability, content uniformity, in vitro disintegration time, wetting time and in vitro dissolution study. Among all, the formulation F3 (containing 6% w/w concentration of crospovidone) was considered to be the best formulation, having disintegration time of 9 s, wetting time of 15 s and in vitro drug release of 99.22% in 15 min.
Objective: The objective of the current study is to optimize and evaluate the potential of polyethylene glycolylated (PEG) glyceride Labrasol® nanostructured lipid carrier (NLC) composites of methotrexate (MTX) to achieve enhanced sustained release delivery in cancer treatment.
Materials and Methods: MTX-NLC was successfully prepared by hot melt emulsification and probe sonication method for spatial and controlled release of this therapeutic agent.
Results: The solubility screening of MTX and lipids resulted in the selection of Monostearin as solid lipid, PEGylated glyceride Labrasol® and olive oil as liquid lipids for the formulation of MTX-loaded NLC composites. Particle size, zeta potential, and polydispersity index of both the composites were confirmed using dynamic light scattering, whereby Labrasol® MTX-NLC showed high entrapment efficiency and drug loading. A spherical particle shape with smooth surface of all the composites was confirmed from the scanning electron microscope and transmission electron microscopy analysis. Labrasol® MTX-NLC showed remarkably increased cytotoxic response, augmented cellular uptake, and low half maximal inhibitory concentration value in MCF-7 cells. In vitro release study confirmed that encapsulation of MTX in PEGylated glyceride Labrasol® MTX-NLC resulted in enhanced sustained release of MTX for a period of 48 h.
Conclusion: The present study establishes that PEGylated glyceride Labrasol® MTX-NLC can be considered as a promising anticancer delivery system, thereby improving antitumor efficacy of the drug.
Cancer is one of the most leading causes of morbidity and mortality worldwide causing 9.6 million deaths in 2018. However, for a variety of cancers the efficacy of current standard treatments is suboptimal. For, most of the cytotoxics are highly toxic which restrains their use in cancer treatment. Second, almost all cancer treatments lack specificity, affecting both the cancerous cells and their normal counterparts. Finally, hydrophobicity and short half lives exhibited by a number of chemotherapeutic agents restrict their efficacy. However, application of nanotechnology has led to the development of effective nanosized drug delivery systems known commonly as nanoparticles. Amid the different lipid based oral delivery systems, Solid lipid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) specifically, have shown to be quite effective in manifesting the potentiality to; a) enhance selectivity of cytotoxics b) reduce the cytotoxicity to normal tissues c) improving the solubility of hydrophobic cytotoxics and d) offer a sustained and controlled release of agents. The current review summarizes the strategies using SLN's and NLC's in overcoming the challenges and enhancement of anticancer efficacy of cytotoxic agents to specific tumor targeting, including active and passive targeting, long circulating and MDR reversing.
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