作者： Priyanka S. Jahagirdar1; Pramod K. Gupta2; Savita P. Kulkarni2; Padma V. Devarajan1
1Dept. of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai, MH, India
2Radiation Medicine Centre, Bhabha Atomic Research Centre, Parel, Mumbai, MH, India
摘要：Targeting macrophages is a promising strategy for improved therapy of intracellular infections as macrophages exhibit rapid phagocytosis of particles >200 nm. Entrapment of Curcumin (CUR) in nanocarriers could provide bioenhancement and macrophage targeting. We present a simple and facile in situ nanoprecipitation approach for instantaneous and on‐site generation of curcumin nanoparticles (ISCurNP). ISCurNP optimised by Box‐Behnken design exhibited average size of 208.25 ± 7.55 nm and entrapment efficiency of 90.16 ± 1.17%. Differential scanning calorimetry and X‐Ray diffraction confirmed amorphization of CUR in ISCurNP. Sustained release was observed over 72 hr in vitro at lysosomal pH 4.5. Rapid and high uptake in RAW 264.7 macrophages was confirmed by flow cytometry and high performance liquid chromatography. Confocal microscopy established localisation of ISCurNP in lysosomal compartment. The facile in situ nanoprecipitation method provides simple, scalable technology to enable macrophage targeted delivery of CUR, with great promise for improved therapy of intracellular infections.
