Preparation And Study Of Drug-loading Performance Of Calcium Phosphate/Carboxymethyl-β-cyclodextrin Composite Microspheres

In this paper, the hybrid nanoparticles consisting of calcium phosphate andβ-cyclodextrin were studied. Nanospheres combine the advantages of calciumphosphate and β-cyclodextrin such as the pH response of calcium phosphate,β-cyclodextrin-enhancing water-soluble of drugs to improve drug loading capacity, andboth materials having good biocompatibility and biodegradation, which promptedmicrospheres loaded with hydrophilic and hydrophobic drugs.Firstly, Carboxymethyl-β-cyclodextrin was prepared, as the solubility ofβ-cyclodextrin derivative in water would be increased significantly, so that the capacityof embedding hydrophobic drug would be enhanced. The three most importantexperimental conditions influencing on the rate of carboxylation product were explored,the orthogonal experiment to get the best experimental conditions: the system reactiontemperature is60℃, the molar ratio of chloroacetic acid and β-cyclodextrin is8, thefinal pH of the reaction system is10.Then the composite nanospheres consist of calcium phosphate andcarboxymethyl-β-cyclodextrin loaded drugs were prepared successfully with rhodamineB and azobenzene as hydrophilic and hydrophobic model drug in the aqueous phasewith soap-free physical method. Drug loading of the two drug-loaded calciumphosphate/carboxymethyl-β-cyclodextrin complex nanospheres were0.82%and3.10%respectively. The vitro studies showed that the drug release properties of the compositemicrospheres achieved a sustained release, and eliminated the "burst" effect basically.Secondly, stable calcium phosphate/carboxymethyl-β-cyclodextrin complexnanospheres containing docetaxel that is treated as typical hydrophobic anticancer drugwere prepared successfully. The vitro release studies showed that the drug releaseperformance reached "slow-release" purpose, eliminating the "burst" effect basically.Finally, the calcium phosphate/carboxymethyl-β-cyclodextrin complex nanospherescontaining docetaxel were used to inhibit MDA-MB-231breast cancer cells and A549lung cancer cells for the experimental evaluation of biological activity. The blanknanospheres experimental activity evaluation proved the safety of the carrier material.The results showed that the effect of the drug-loaded composite nanospheres inhibitingMDA-MB-231breast cancer cells and A549lung cancer cells was significant.