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Preparation, evaluation and pharmacokinetic studies of spray dried PLGA polymeric submicron particles of simvastatin for the effective treatment of breast cancer

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Abstract In the current study, simvastatin-loaded PLGA submicron particles (SIM SP) were prepared by the spray drying method. Different parameters of the nanospray drying method, such as the inlet temperature,… Click to show full abstract

Abstract In the current study, simvastatin-loaded PLGA submicron particles (SIM SP) were prepared by the spray drying method. Different parameters of the nanospray drying method, such as the inlet temperature, spray mesh diameter, the spray rate, and the gas flow rate, were optimized and a particle of size 259.1 nm was obtained, utilizing a 7 μm mesh sieve. Percent drug entrapment efficiency and drug loading capacity were calculated as 63.07% and 85.23 μg/mg, respectively. A 66.61% cumulative drug release was recorded after 72 h, in accordance to the Higuchi diffusion pattern followed by Fickian transport. An amorphous form drug was entrapped inside the polymer, and no interaction of the drug with the polymer was observed. An MTT assay was conducted in the MCF-7 cell lines to search for anti-cancerous activity. The pharmacokinetic studies clearly demonstrated that SIM SP exhibited significant increase in AUC0–24, T1/2 and Cmax and decrease in Kel, compared to pure SIM. Therefore, it can be concluded that submicronic particles acquired by nanospray drying were found to be appropriate for the treatment of solid tumor.

Keywords: pharmacokinetic studies; treatment; drug; submicron particles; preparation evaluation

Journal Title: Journal of Molecular Liquids
Year Published: 2018

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