BackgroundApatinib is a newly approved antitumor drug (molecular targeted agent/small molecular
kinase inhibitor) for advanced hepatocellular carcinoma (HCC) treatment. However,
current oral administration of apatinib could induce the even distribution of drugs in
the body and cause the concentration of apatinib in the HCC location to be limited or
insufficient. Therefore, it is urgent to develop novel formulations of apatinib to
improve its efficiency.Materials and methodsApatinib was prepared to form a stable and even dispersion with cyclodextrin (a
clathrate complex/inclusion complex named Apa-Cyc). A temperature-sensitive phase-change
hydrogel of apatinib (named Apa-Gel) was prepared using apatinib–cyclodextrin
and poloxamer 407. Apa-Gel was injected into HCC tissues in nude mice to examine the
long-term antitumor effect.ResultsApa-Gel can transform from liquid to hydrogel at near body temperature and maintain
slow release of apatinib in HCC tumor tissues. When injected subcutaneously, one-time
administration of Apa-Gel has a long-acting antitumor effect on the subcutaneous growth
or epithelial–mesenchymal transition process of HCC cells.ConclusionThis novel slow-releasing system allows apatinib to be released effectively on the long
term and facilitates tissue attachment, thereby preserving the efficiency of apatinib
over the long term.
The present study focused on the development of Cur-loaded SOHA nanogels (Cur-SHNGs) to enhance the topical administration of Cur. The physiochemical properties of Cur-SHNGs were characterized. Results showed that the morphology of the Cur-SHNGs was spherical, the average size was 171.37 nm with a zeta potential of −13.23 mV. Skin permeation experiments were carried out using the diffusion cell systems. It was found that the skin retention of Cur-SHNGs was significantly improved since it showed the best retention value (0.66 ± 0.17 μg/cm2). In addition, the hematoxylin and eosin staining showed that the Cur-SHNGs improved transdermal drug delivery by altering the skin microstructure. Fluorescence imaging indicated that Cur-SHNGs could effectively deliver the drug to the deeper layers of the skin. Additionally, Cur-SHNGs showed significant analgesic and anti-inflammatory activity with no skin irritation. Taken together, Cur-SHNGs could be effectively used for the topical delivery of therapeutic drugs.
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