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4 Differentiated and matured osteoclasts are characterized by high expression of tartrate-resistant acid phosphatase (TRAP) and cathepsin K. 1вЂ“ 3 Osteoclasts, bone-resorbing multinucleated cells, are generated from hematopoietic monocyte/macrophage precursor cells through differentiation processes.

Bone turnover involves the old bone resorption by osteoclasts and new bone formation by osteoblasts. Keywords: liposome, osteoarthritis, curcuminoid, OPG/RANKL ratio, bone turnoverД«one turnover is a continuous process of bone resorption and formation for the purpose of maintaining normal bone mass. Therefore, curcuminoid-loaded liposomes may slow osteoarthritis progression. In the present study, we demonstrated that Cur and BDMC can be successfully encapsulated in liposomes and can reduce osteoclast activity and maintain osteoblast functions.

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With interleukin (IL)-1ОІ stimulation, curcuminoid-loaded liposomes can successfully downregulate the expression of inflammatory markers on osteoblasts, and show a high osteoprotegerin (OPG)/receptor activator of nuclear factor ОєB ligand (RANKL) ratio to prevent osteoclastogenesis. Of note is that Cur-loaded liposomes can prevent liposome-dependent inhibition of osteoblast differentiation and mineralization, but BDMC-loaded liposomes could not.

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In comparison with free drugs (Cur and BDMC), curcuminoid-loaded liposomes were less cytotoxic and expressed high cellular uptake of the drugs. Both types of liposome can inhibit macrophage inflammation and osteoclast differential activities. The results show that there is about 70% entrapment efficiency of Cur and BDMC in liposomes and that particle sizes are stable after liposome formation.

In this study, curcuminoid (Cur and BDMC)-loaded liposomes were characterized in terms of particle size, encapsulation efficiency, liposome stability, and cellular uptake. To increase cellular uptake of Cur and BDMC in bone tissue, soybean phosphatidylcholines were used for liposome formulation. *These authors contributed equally toВ this workДЄbstract: Curcumin (Cur) and bisdemethoxycurcumin (BDMC), extracted from Curcuma longa, are poorly water-soluble polyphenol compounds that have shown anti-inflammatory potential for the treatment of osteoarthritis. Chih-Chang Yeh, 1,2 Yu-Han Su, 3 Yu-Jhe Lin, 3 Pin-Jyun Chen, 3 Chung-Sheng Shi, 1 Cheng-Nan Chen, 3,* Hsin-I Chang 3,*ДЎGraduate Institute of Clinical Medical Sciences, College of Medicine, Chang Gung University, Taoyuan 333, Taiwan, Republic of China 2Orthopaedic Department, Chiayi Branch, Taichung Veterans General Hospital, Chiayi, Taiwan, Republic of China 3Department of Biochemical Science and Technology, National Chiayi University, Chiayi, Taiwan, Republic ofВ China