Abstract
BackgroundOsteoporosis is a bone-incapacitating malady and it is characterized by obvious bone mass loss and bone microarchitecture deterioration. Current treatments for osteoporosis have many limitations, including the non-obvious therapeutic effect and long-term safety issues. Icariin is a pharmacologically active flavonoid glycoside, which shows potential application in treatment of osteoporosis. But its clinical application is limited by the inherent disadvantages such as poor water solubility, first pass effect after oral administration, and low bioavailability. Moreover, due to lack of targeting ability, icariin cannot accumulate at the local diseased region to provide early protection from fractures. To solve the application problems of icariin and enhance its therapeutic effects on osteoporosis, this work aimed to design a targeting drug delivery system of biomineral-binding liposomes (BBL) mediated by pyrophosphate ions.ResultsBiomineral-binding liposomes enhanced the binding ability of liposomes with hydroxyapatite particles. It increased the serum level of alkaline phosphatase and reduced that of tartrate-resistant acid phosphatase 5b. Meanwhile, BBL increased the mechanical strength of femoral midshaft, preserving the trabecular bone microarchitecture. Moreover, BBL could initiate bone turnover/remodeling of rats with osteoporosis.ConclusionsThis drug targeting delivery system of BBL loading with icariin showed more therapeutic advantages than the free icariin for the treatment of osteoporosis, which may be a kind of valid candidate in future osteoporosis therapy.
Highlights
Osteoporosis is a bone-incapacitating malady and it is characterized by obvious bone mass loss and bone microarchitecture deterioration
Characterization of biomineral-binding liposomes (BBL) preparations The trans-mission electron microscopy (TEM) detection demonstrated that both BBL and non-binding liposome (NBL) showed a uniform spherical shape (Fig. 2a–f )
The polydispersity index (PDI) resulted from BBL and NBL is 0.19 ± 0.01 and 0.24 ± 0.01, respectively. It suggested that these liposomes might have a narrow size distribution, which was confirmed by the results shown in Fig. 2g, h
Summary
Osteoporosis is a bone-incapacitating malady and it is characterized by obvious bone mass loss and bone microarchitecture deterioration. Current treatments for osteoporosis have many limitations, including the nonobvious therapeutic effect and long-term safety issues. Osteoporosis is characterized by fragile bones and microarchitectural deterioration, which causes approximately 9 million cases of the bone fractures every year [2]. Current clinical treatments on osteoporosis mainly include estrogen therapy, bisphosphonates, and selective estrogen receptor modulators [3]. These treatments showed obvious restrictions, including non-obvious therapeutic effect and long-term safety issues. Bisphosphonates were widely used for osteoporosis therapeutics, which avoided further bone deterioration in osteoporosis It can’t replenish the already lost bone [3, 4].
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