ABSTRACT

Aprepitant (AP) is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors that is used for the prevention of acute and delayed nausea and vomiting caused by initial and repeat courses of highly emetogenic cancer chemotherapy. It has low aqueous solubility that delays the absorption from the gastrointestinal tract (GIT) when administered through oral route. Solubility parameter of a drug substance is one of the key factor of its oral bioavailability and low oral bioavailability requires development of drug delivery systems able to improve its solubility and bypass hepatic effect. The purpose of the present research paper was to investigate the possibility to encapsulate Aprepitant into nanostructured lipid carriers (NLCs) to improve the drug release and in long run oral bioavailability by using of Quality by Design (QbD) approach for the design, development, optimization and characterization of nanostructured lipid carriers containing Aprepitant (AP-NLCs). For this purpose, AP-NLCs were fabricated by emulsification using high-speed homogenization followed by ultrasonication. The 23 full factorial plan was utilized to assess the connection between the Critical Material Attributes (CMAs) and Critical Process Parameters (CPPs) variable. The most basic critical quality attributes (CQAs) studied were particle size analysis and entrapment efficiency. The particle size of prepared NLCs were found to be between 179.2 - 485.5 nm while zeta potential values varied between 40.02 ± 0.24 and 15.42 ± 0.31 mV. They also showed high encapsulation efficiency (>80%) and amorphous state of the drug in lipid matrix. Keywords: Aprepitant, Nanostructured Lipid Carriers (NLCs), Ultrasonication, Quality by Design (QbD), factorial design
Publication date: 01/10/2020

https://ijbpas.com/pdf/2020/October/MS_IJBPAS_2020_5497.pdf

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https://doi.org/10.31032/IJBPAS/2020/9.10.5497