Drug development and industrial pharmacy · 2025
Box-Behnken based furosemide-nanostructured lipid carriers (NLCs) delivery system for improving oral bioavailability.
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Ilyas Muzzamil, Rehman Asim Ur, Tayyab Muhammad, Nawaz Malik Marya, Ahmed Naveed, Fatima Humaira
Аннотация
OBJECTIVE: The fabrication of furosemide (FSM) with enhanced oral bioavailability and encapsulation was achieved using a nanostructured lipid carriers (NLCs) drug delivery system.
SIGNIFICANCE: The uniform drug distribution is a barrier due to its low dose. The lipid-based delivery system was selected based on its poor solubility and permeability, limiting its poor partitioning and solubility in water-based polymeric delivery systems. The lipophilicity of the FSM makes it favorable to partition with triglyceride-based Compritol 888 ATO and oleic acid with minimized drug expulsion, high drug payload, and sustained release over extended time frames.
METHODS: The Organic and aqueous phases of the microemulsion were stabilized using Tween 80, a hydrophilic surfactant. Box-Behnken design-based optimization was done using alteration in various formulation variables to obtain nano-formulation with the lowest particle size and polydispersity, maximal zeta potential and entrapment efficiency.
RESULTS: Design-Expert yielded several optimized formulations with the desirability function. Maximum desirability was obtained at a particle size of around 178 nm, a surface charge of -19.6 mV, and an EE of above 85%.The in vitro release profile depicted 86.5% of cumulative release after 24 h whereas, in vivo pharmacokinetic study revealed an increase in Cmax from 0.48 µg/mL (FSM-Suspension) to 0.77 µg/mL (FSM NLCs) to increase the bioavailability to approx. 241% in FSM NLCs. The half-life escalation demonstrated that the residence time of the nanoparticles prolonged at the physiologic pH.
CONCLUSIONS: FSM-NLCs exhibited sustained release over a prolonged period, improved residence time in the body, and their action was prolonged.
SIGNIFICANCE: The uniform drug distribution is a barrier due to its low dose. The lipid-based delivery system was selected based on its poor solubility and permeability, limiting its poor partitioning and solubility in water-based polymeric delivery systems. The lipophilicity of the FSM makes it favorable to partition with triglyceride-based Compritol 888 ATO and oleic acid with minimized drug expulsion, high drug payload, and sustained release over extended time frames.
METHODS: The Organic and aqueous phases of the microemulsion were stabilized using Tween 80, a hydrophilic surfactant. Box-Behnken design-based optimization was done using alteration in various formulation variables to obtain nano-formulation with the lowest particle size and polydispersity, maximal zeta potential and entrapment efficiency.
RESULTS: Design-Expert yielded several optimized formulations with the desirability function. Maximum desirability was obtained at a particle size of around 178 nm, a surface charge of -19.6 mV, and an EE of above 85%.The in vitro release profile depicted 86.5% of cumulative release after 24 h whereas, in vivo pharmacokinetic study revealed an increase in Cmax from 0.48 µg/mL (FSM-Suspension) to 0.77 µg/mL (FSM NLCs) to increase the bioavailability to approx. 241% in FSM NLCs. The half-life escalation demonstrated that the residence time of the nanoparticles prolonged at the physiologic pH.
CONCLUSIONS: FSM-NLCs exhibited sustained release over a prolonged period, improved residence time in the body, and their action was prolonged.