Ethinylestradiol (EE) is a potent estrogen widely used to treat diseases such as breast cancer, prostate cancer, and menopausal syndrome. The poor aqueous solubility of EE leads to erratic oral absorption, resulting in suboptimal plasma levels. Developing a formulation to enhance the solubility of EE in the gastrointestinal tract would be beneficial to increase the bioavailability of EE. Thereafter, we prepare diethylenetriamine-β-cyclodextrin/ethinylestradiol (DETA-β-CD/EE) complex, aiming to increase the solubility of EE in water, and design and prepare core-shell composite hydrogel capsules with aldocellulose and hydroxyethyl cellulose as the core and sodium alginate as the shell. The stability, swelling, drug release behavior and biocompatibility of the core-shell hydrogel capsules are carefully investigated. And the results show that the prepared hydrogel capsules have the controlled and sustained release ability of soluble DETA-β-CD/ EE, can achieve pH-responding to intestinal fluid, and are non-toxic to normal human cells.

Betulinic acid (BA), a natural pentacyclic lupine‐type triterpene, has shown its prominent efficiency on the selective antitumor activity. However, its poor water solubility and bioavailability have limited its application. Herein, targeting nanoparticles were prepared to improve BA‐based liposome (BL)'s restricted chemotherapeutic efficacy. Multi‐layers membranes from the cancer cells were added as highly penetrative targeting ligands to functionalize the BA‐based liposomes. In vitro experiments including the MTT assay and the fluorescence imaging of live/dead staining were adopted to prove its great inhibition in the growth of tumor cells. And it manifests that the antitumor efficacy of BL coated with cell membranes (BLCM) achieves nearly 4.3 times as that of BL under the same conditions in the MTT experiments. In addition, the fluorescence imaging stained with DAPI‐FITC was applied to prove the targeting positioning effects on the BLCM. In a nutshell, the nanomedicine has good targeting antitumor efficacy and has great potential in being applied for the personalized cancer clinical treatment.

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Ethinylestradiol (EE), is widely used to treat conditions such as breast cancer, prostate cancer and climacteric syndrome. However, due to the low water solubility of EE, the bioavailability of EE is low. Herein, to improve the bioavailability of EE, a hydrosoluble cyclodextrin drug carrier system, diethylenetriamine‐β‐cyclodextrin/ethinylestradiol (DETA‐β‐CD/EE) was prepared. High performance liquid chromatography (HPLC), fourier transform infrared (FTIR), 2D rotating frame overhauser effect spectroscopy (ROESY) spectrum and scanning electron microscope (SEM) were used to characterize the DETA‐β‐CD/EE. HPLC test showed that DETA‐β‐CD was the optimal host molecule, which can improve the solubility of EE to 496 mg L−1. Phase solubility indicated the formation of a soluble inclusion complex with 1 : 1 stoichiometry. In terms of practical application, the solubility and stability of DETA‐β‐CD/EE in blood was proved by dissolution rate studies. Overall, by the encapsulation in polysaccharide DETA‐β‐CD, the water solubility of EE is increased by 100 times. The establishment of hydrosoluble cyclodextrin drug carrier system provides support for the sustained release system or large dose drug delivery.