Abstract
Ginsenoside CK is one of the intestinal bacterial metabolites of ginsenoside prototype saponins, such as ginsenoside Rb1, Rb2, Rc, and Rd. Poor water solubility and low bioavailability have limited its application. The nanogel carriers could specifically deliver hydrophobic drugs to cancer cells. Therefore, in this study, a nanogel was constructed by the formation of Schiff base bonds between hydrazide-modified carboxymethyl cellulose (CMC-NH2) and aldehyde-modified β-cyclodextrin (β-CD-CHO). A water-in-oil reverse microemulsion method was utilized to encapsulate ginsenoside CK via the hydrophobic cavity of β-CD. β-CD-CHO with a unique hydrophobic cavity carried out efficient encapsulation of CK, and the drug loading and encapsulation efficiency were 16.4% and 70.9%, respectively. The drug release of CK-loaded nanogels (CK-Ngs) in vitro was investigated in different pH environments, and the results showed that the cumulative release rate at pH 5.8 was 85.5% after 140 h. The methylthiazolyldiphenyl-tetrazolium bromide (MTT) toxicity analysis indicated that the survival rates of A549 cells in CK-Ngs at 96 h was 2.98% compared to that of CK (11.34%). In vivo animal experiments exhibited that the inhibitory rates of CK-Ngs against tumor volume was 73.8%, which was higher than that of CK (66.1%). Collectively, the pH-responsive nanogel prepared herein could be considered as a potential nanocarrier for CK to improve its antitumor effects against lung cancer.
Highlights
In recent years, hydrophobic ginsenosides with broad anticancer activity had been considered as one of the most promising Chinese herbal medicines
Drug loading (DL) and entrapment efficiency (EE) of compound K (CK)-loaded nanogels (CK-Ngs) were calculated by Equations (2) and (3)
The characterization of β-CD-CHO was confirmed by Fourier transform infrared spectroscopy (FTIR, Thermo Scientific, Wilmington, DE, USA), accumulating 36 scans from 400 to 4000 cm−1 with a resolution of 4 cm−1.The morphological characteristics of CK-Ngs were observed by scanning electron microscope (HITACH S4800, Hitachi, Tokyo, Japan)
Summary
Hydrophobic ginsenosides with broad anticancer activity had been considered as one of the most promising Chinese herbal medicines. They were divided into protopanaxadiol (PPDs) and protopanaxatriol (PPTs), which demonstrate a variety of pharmacological properties [1]. Β-cyclodextrin (β-CD), consisting of seven glucose units, possesses a truncated cone structure containing a hydrophobic inner ring and a hydrophilic outer ring [6,7]. The integration of β-cyclodextrin into a cross-linked polymer network improved the ability of hydrogels to deliver drugs and control drug release [11]. 2-phenylindole (DAPI) and Fluorescein isothiocyanate (FITC) were purchased from Beijing Solarbio Science & Technology Co., Ltd. 2-phenylindole (DAPI) and Fluorescein isothiocyanate (FITC) were purchased from Beijing Solarbio Science & Technology Co., Ltd. (Beijing, China)
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