期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 172, 期 -, 页码 655-664出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2018.09.025
关键词
N-acetylcysteine; Ryaluronic acid; Paclitaxel; Amphiphilic polymers; Mucoadhesion; Oral bioavailability
资金
- National Natural Science Foundation of China [81503027]
- College Students Innovation Project for the R&D of Novel Drugs [J1310032]
N-acetylcysteine modified hyaluronic acid-paclitaxel (NAC-HA-PTX) conjugate was designed to improve the water solubility and oral bioavailability of PTX through mucosal bioadhesion ability. The average size of spherical NAC-HA-PTX micelles was 187 rim with a zeta potential of -25.38 mV. Mucin adhesion study showed that the amount of mucin adhered to NAC-HA-PTX micelles was 1.98-fold greater than that of hyaluronic acid-paclitaxel (HA-PTX) micelles. The fluorescence micrographs showed that the biodistribution sequence of coumarin 6-loaded micelles in the gastrointestinal tract was duodenum > jejunum > ileum, and NAC-modified micelles significantly exhibited better mucoadhesive properties than the corresponding unmodified ones. The pharmacokinetic study showed that the area under the curve (AUC(0.24h)) of NAC-HA-PTX micelles was 2.32-fold and 2.56-fold higher compared to that of HA-PTX micelles and PTX solution (Taxol) after oral administration, respectively. NAC-HA-PTX micelles appear to be a promising drug delivery system to improve the bioavailability of insoluble drugs for efficient tumor therapy via oral administration.
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