17β-Estradiol-Loaded PEGlyated Upconversion Nanoparticles as a Bone-Targeted Drug Nanocarrier.

Hormone replacement therapy (HRT) plays an important role in the treatment and prevention of osteoporosis. Here, 17β-estradiol (E2)-loaded PEGlyated upconversion nanoparticles (E2-UCNP@pPEG) were synthesized that retained E2 bioactivity and improved delivery efficiency over a relatively long time-period. E2-UCNP@pPEG was synthesized and characterized using transmission electron microscopy (TEM), X-ray diffraction (XRD), and Fourier transform infrared (FTIR), among other methods. The loading efficiency of E2 was determined to be 14.5 wt %, and the nanocarrier effectively facilitated sustained release. Confocal upconversion luminescence (UCL) imaging using the CW 980 nm laser as excitation resource revealed significant interactions of E2-UCNP@pPEG with preosteoblasts. E2-UCNP@pPEG treatment of preosteoblasts induced positive effects on differentiation, matrix maturation, and mineralization. Moreover, in situ and ex vivo UCL imaging studies disclosed that E2 encapsulated in the nanocomposite was passively delivered to bone. Our results collectively suggest that this nanoreservoir provides an effective drug-loading system for hormonelike drug delivery and support its considerable potential as a therapeutic agent for osteoporosis.