Purpose: The size of polymeric nanoparticles is considered as an effective factor in cancer therapy due to enterance into tumor tissue via the EPR effect. The purpose of this work was to investigate the effective parameters on poly(lactic-co-glycolic acid)-paclitaxel (PLGA –PTX) nanoparticles size.Methods: We prepared PLGA-PTX nanoparticles via single emulsion and precipitation methods with variable paremeters including drug concentration, aqueous to organic phase volume ratio, polymer concentration, sonication time and PVA concentration.Results: PLGA-PTX nanoparticles were characterized by dynamic light scattering (DLS) and scanning electron microscopy (SEM). The results exhibited that the diameter of nanoparticles enhanced with increasing drug, polymer and PVA concentrations whereas organic to aqueous phase volume ratio and sonication time required to the optimization for a given size.Conclusion: The precipitation method provides smaller nanoparticles compared to emulsion one. Variable parameters including drug concentration, aqueous to organic phase volume ratio, polymer concentration, sonication time and PVA concentration affect diameter of nanoparticles.
Indirubin, an ingredient in traditional Chinese medicine, is considered as an anti-cancer agent. However, due to its hydrophobic nature, clinical efficiency has been limited. Drug delivery via nanotechnology techniques open new windows toward treatment of cancerous patients. Glioblastoma multiforme (GBM) is the most severe and common type of brain primary tumors. Of common problems in targeting therapies of glioblastoma is the availability of drug in tumoric tissues. In this study, Indirubin loaded solid lipid nanoparticles were prepared and their therapeutic potentials and antitumoric effects were assessed on GBM cell line (U87MG). The SLNs were prepared with Cetyl palmitate and Polysorbat 80 via high-pressure homogenization (HPH) methods in hot mode. Then, properties of SLNs including size, zeta potential, drug encapsulation efficacy (EE %) and drug loading were characterized. SLNs morphology and size were observed using SEM and TEM. The crystalinity of formulation was determined by different scattering calorimetry (DSC). The amount of drug release and antitumor efficiency were evaluated at both normal brain pH of 7.2 and tumoric pH of 6.8. The prapared SLNs had mean size of 130 nm, zeta potential of -16 mV and EE of 99.73%. The results of DSC showed proper encapsulation of drug into SLNs. Drug release assessment in both pH displayed sustain release property. The result of MTT test exhibited a remarkable increment in antitumor activity of Indirubin loaded SLN in comparison with free form of drug and blank SLN on multiform GB. This study indicated that Indirubin loaded SLNs could act as a useful anticancer drugs.
Imatinib is a useful drug for inhibiting some receptors such as c-Kit and PDGFRs which are overexpressed in glioblastoma. However, imatinib is easily effluxed by the proteins of endothelial cells. The aim of this work was to synthesize an imatinib base (IMTb) in the nanoscale and also investigate the amount of its loading into human serum albumin (HSA) nanoparticles. A desolvation method was used to synthesize IMTb loaded HSA with a mean size about 80-90 nm. Fourier transform infrared spectroscopy (FT-IR) demonstrated that the non-covalent interactions between IMTb and HSA could not affect the chemical structure of IMTb.Differential scanning calorimetry (DSC) analysis indicated the amorphous form of IMTb in the HSA nanoparticles. Moreover, the encapsulation efficiency and drug loading capacity were found to be 98% and 6.9%, respectively. The obtained results also exhibited that IMTb loaded HSA and free IMTb at a concentration of 40 mg ml À1 had an approximately 90% and 55% cytotoxicity effect on U87MG glioblastoma cells, respectively. Therefore, IMTb loaded HSA nanoparticles can be introduced as a potential candidate for drug delivery in the treatment of glioblastoma.
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