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Development, Optimization, and Pharmacokinetics Study of Bufalin/Nintedanib Co-loaded Modified Albumin Sub-microparticles Fabricated by Coaxial Electrostatic Spray Technology.

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Coaxial electrostatic spray technology has received extensive attention in fabricating micro/nanoparticles for drug delivery. However, there are few reports on applying this technology in preparing albumin nanoparticles. In this study,… Click to show full abstract

Coaxial electrostatic spray technology has received extensive attention in fabricating micro/nanoparticles for drug delivery. However, there are few reports on applying this technology in preparing albumin nanoparticles. In this study, the bufalin (BF) and nintedanib (NDNB) co-loaded ursodeoxycholic acid and p-biguanides benzoic acid decorated albumin sub-microparticles (BN-DUB subMPs) were fabricated by coaxial electrostatic spray technology and optimized by central composite design. Five percent of albumin (contained 0.7% polyethylene oxide) solution was selected as the shell solution which ejected through outer axis with the flow rate of 0.07 mm/min, while the core solution which contained by BF and NDNB ethanol solution was ejected through inner axis with the flow rate of 0.05 mm/min. In vitro cell studies revealed that the modified albumin possessed good biocompatibility. What's more, the BN-DUB subMPs enhanced the inhibitory effect on the growth of LLC cells efficiently. The pharmacokinetics study showed that the t1/2 and AUC0-t of BN-DUB subMPs increased significantly compared with that of the drug solution, which indicated the improved in vivo stability of modified albumin nanoparticles. Thus, this study provided a novel and simple technical platform for the development of albumin-based drug carriers.

Keywords: coaxial electrostatic; technology; electrostatic spray; spray technology; modified albumin

Journal Title: AAPS PharmSciTech
Year Published: 2021

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