Jong-Suep Baek1, Cheong-Weon Cho. 1. College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Yuseong-gu, Daejeon, South Korea.
Abstract
OBJECTIVES: This study aimed to evaluate the potential of solid lipid nanoparticles (SLNs) of paclitaxel (PTX) modified with a 2-hydroxypropyl-β-cyclodextrin system to enhance cellular accumulation of PTX into p-glycoprotein (p-gp)-expressing cells. METHODS: The PTX-loaded-SLNs consisted of lipid (stearic acid) and surfactants (lecithin and poloxamer 188) and were then modified with 2-hydroxypropyl-β-cyclodextrin by a sonication method. KEY FINDINGS: In terms of cytotoxicity, PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin showed higher cytotoxicity than other formulations. In particular, the cellular uptake of PTX from PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin was about 5.8- and 1.5-fold higher than that from PTX solution and unmodified PTX-loaded SLNs in MCF-7/ADR cells, respectively. After a 4-h incubation, clear fluorescence images inside cells were observed over time. When PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin were incubated with MCF-7/ADR cells for 4 h, cellular uptake of PTX increased 1.7-fold versus that of PTX in the presence of verapamil. CONCLUSIONS: These results suggest that optimized SLNs modified with 2-hydroxypropyl-β-cyclodextrin may have potential as an oral drug delivery system for PTX.
OBJECTIVES: This study aimed to evaluate the potential of solid lipid nanoparticles (SLNs) of paclitaxel (PTX) modified with a 2-hydroxypropyl-β-cyclodextrin system to enhance cellular accumulation of PTX into p-glycoprotein (p-gp)-expressing cells. METHODS: The PTX-loaded-SLNs consisted of lipid (stearic acid) and surfactants (lecithin and poloxamer 188) and were then modified with 2-hydroxypropyl-β-cyclodextrin by a sonication method. KEY FINDINGS: In terms of cytotoxicity, PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin showed higher cytotoxicity than other formulations. In particular, the cellular uptake of PTX from PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin was about 5.8- and 1.5-fold higher than that from PTX solution and unmodified PTX-loaded SLNs in MCF-7/ADR cells, respectively. After a 4-h incubation, clear fluorescence images inside cells were observed over time. When PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin were incubated with MCF-7/ADR cells for 4 h, cellular uptake of PTX increased 1.7-fold versus that of PTX in the presence of verapamil. CONCLUSIONS: These results suggest that optimized SLNs modified with 2-hydroxypropyl-β-cyclodextrin may have potential as an oral drug delivery system for PTX.
Authors: Nabil F Saba; Kelly R Magliocca; Sungjin Kim; Susan Muller; Zhengjia Chen; Taofeek K Owonikoko; Nicholas J Sarlis; Carrie Eggers; Vanessa Phelan; William J Grist; Amy Y Chen; Suresh S Ramalingam; Zhuo G Chen; Jonathan J Beitler; Dong M Shin; Fadlo R Khuri; Adam I Marcus Journal: Head Neck Pathol Date: 2013-07-24
Authors: María Carmen Leiva; Raúl Ortiz; Rafael Contreras-Cáceres; Gloria Perazzoli; Iryna Mayevych; Juan Manuel López-Romero; Francisco Sarabia; Jose Manuel Baeyens; Consolación Melguizo; Jose Prados Journal: Sci Rep Date: 2017-10-18 Impact factor: 4.379