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. 2012 May 11;18(5):323–340. doi: 10.1089/ten.teb.2011.0737

Table 2.

Systems Containing Bisphosphonates That Can be Used to Develop Scaffolds for Bone Tissue Engineering

Delivery systems that can be used as scaffolds BP incorporate Experimental trial BP release quantification Most important contributions References
Chitosan microspheres Pamidronate In vitro, In vivo - The release of BP from microspheres was faster in vitro than in vivo. After implantation, drugs exhibited a relatively increased disposition in the adjacent tibia. 139
Poly-D,L-lactic acid (PDLLA) scaffolds Pamidronate In vivo - PDLLA pellets containing Bone Morphogenetic Protein (BMP) and PAM showed an increase in bone formation after 3 weeks when low doses of PAM were used (0.02 mg). Polymer degradation remained until 8 weeks. 147
Mesoporous silica-based materials (MCM41, SBA15) Alendronate In vitro release of Alendronate - Amine functionalization on mesopores enhances 3 times the incorporation of ALN and reduces the mesopore surface area. The diffusive behavior of the absorbed molecule through the mesopores can be calculated using a zero-order or lineal model. 134
Mesoporous silica-based materials (SBA15) Alendronate In vitro release of Alendronate RP-HPLC Mesopores functionalizatiwith aminopropyl groups was made using a catalytic or an anhydrous procedure. The catalytic method induces a more gradual ALN loading (approximately 3 mg ALN/25 mg SiO2) that depends on the functionalization degree and offers a better control in the release of ALN molecules showing a deviation from the theoretical first-order behavior. 135
HA-coated starch scaffold Clodronate In vitro HPLC-UV detection The microhardness increases by increasing the BP concentration on the coating (from 0.004 to 1 mg/cm2). A zero-order kinetic was observed during 14 days at pH 7.4. The CLO that is incorporated promoted osteoblast-like cell adhesion, and it has influenced cellular proliferation in a way dependent of the concentration, being 0.02 mg/cm2 of BP the ideal concentration for enhancing cell viability. 138
PLGA/HA microspheric system Alendronate In vitro Spectrophotometrically, as a Fe(III) complex ALN was encapsulated using a single emulsion method, which showed a higher encapsulation efficiency (about 90%) than the double emulsion one. A controlled zero-order release during 30 days was achieved, without a remarkable initial burst effect: composites with 50% of HA showed a better controlled release. Inhibition on the growth of macrophages and enhancement in the proliferation of osteoblasts were observed. 7
PCL fibres loaded with HA and BP Clodronate In vitro characterization - PCL fiber scaffolds were developed by using electro- and wet-spinning techniques and loaded with HA nanoparticles, which had CLO linked (about 75 mg ALN/250 mg HA). Release kinetics of CLO, through the tuning of fiber dimensions and mesh porosity, could be controlled. 140
PLA/PEO-ZOL/PLA nanofiber meshes Zoledronate In vitro release of Zoledronate HPLC-UV detection The sandwich structure-like meshes show the main advantages of facile preparation condition and the possibility of including hydrophobic or hydrophilic drugs. In vitro experiments revealed that with an increase in the thickness of inner drug-loaded mesh, the drug release rate and initial burst release decreased. 141
HA microspheric system Alendronate In vitro Spectrophotometrically, as a Fe(III) complex They fabricated a microsphere-type carrier where ALN loading and microsphere formation can occur through a simultaneous process, and the loading content was much higher than other CaP carrier systems (approximately 19.5 wt.% ALN). A controlled drug release for 40 days was achieved, which was dependent on the dissolution rate of the HA microspheres. The release showed linear kinetics, except for a burst effect during the initial 24 h. In addition, the inhibition of osteoclast formation was observed. 40

BP, bisphosphonates; RP, reverse phase; ALN, alendronate; HA, hydroxyapatite; PCL, poly(ε-caprolactone); CLO, clodronate; PLA, Poly (L-lactic acid); PEO, polyethylene oxide; ZOL, Zoledronate; CaP, calcium phosphates; UV, ultraviolet.