Bone-targeting drug delivery system of biomineral-binding liposomes loaded with icariin enhances the treatment for osteoporosis

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.Electronic supplementary materialThe online version of this article (10.1186/s12951-019-0447-5) contains supplementary material, which is available to authorized users.

Icariin-Functionalized Coating on TiO2 Nanotubes Surface to Improve Osteoblast Activity In Vitro and Osteogenesis Ability In Vivo

“…It has been reported that nearly 90% of currently used drugs in implant modification are hydrophobic, and icariin is no exception [19]. That said, icariin has a number of shortcomings, such as the first-pass effect after oral administration and low bioavailability, which limit its clinical application [20]. Previous studies have shown that icariin could be combined with small intestine submucosa scaffold to enhance bone regeneration [21].…”

Untargeted metabolomics using liquid chromatography coupled with mass spectrometry for rapid discovery of metabolite biomarkers to reveal therapeutic effects ofPsoralea corylifoliaseeds against osteoporosis

“…As the pathogenesis of OP is still unclear and no effective early diagnosis basis has been determined, therapeutic drugs with denite curative effect and high cure rate have not been developed. 40 However, medical and pharmaceutical researchers have never stopped their exploration. A variety of advanced scientic research methods and strategies are applied to the study of diseases.…”

Icariin/Aspirin Composite Coating on TiO2 Nanotubes Surface Induce Immunomodulatory Effect of Macrophage and Improve Osteoblast Activity

“…The drug release percentage scatter diagrams as a function of time and sketch view of the established substrate were shown in Figure 6A-C. The sustained release mechanism of ICA may partly be interpreted by its poor water solubility [42] and the existence of the outside ASP/PLGA coating, which generate a viscous layer that further retarded the drug diffusion to the solvent, similar to a previous report [43]. In the future, drug release amount at more time points, especially for ASP, are needed to be measured to evaluate the kinetic mechanism much accurately.…”