PEG-PCL modification and intestinal sustained-release of solid lipid nanoparticles for improving oral bioavailability of 2-methoxyestradiol

Paclitaxel-Loaded TPGS2k/Gelatin-Grafted Cyclodextrin/Hyaluronic Acid-Grafted Cyclodextrin Nanoparticles for Oral Bioavailability and Targeting Enhancement

“…35 A similar phenomenon was observed in other studies on sustained-release formulations. 36,37 As indicated, the T max and t 1/2 increased from 1.50 § 0.84 and 9.04 § 5.67 to 3.33 § 0.51 and 100.04 § 7.40 h when TGHC-PTX-NPs were employed for drug delivery. Such finding aligns with that of drug release experiment in vitro, and may be mainly related to the steric hindrance of the PEG long chain of TPGS 2k , which can impart stealth properties to the nanoparticles, increase their stability in the circulatory system, 10,38 and then prolong the half-life of PTX.…”

“…Different endocytosis inhibitors (colchicine, chlorpromazine, indomethacin, quercetin) of intestinal epithelial cells were added, and the samples were incubated for 45 min in a shaker at 37 °C. The inhibitor solution was discarded, and the intestinal segments were washed with 37 °C KRPH buffer twice. In addition, TGHC-PTX-NPs in the 37 °C KRPH buffer were added, and the intestinal segments without inhibitor treatment were regarded as the positive control.…”

Glucose-Modified Zein Nanoparticles Enhance Oral Delivery of Docetaxel

“…For the biodistribution study, 24 tumor-bearing mice were randomly assigned to three groups and treated with IR-780 iodide-labeled DTX-NPs according to a method described previously [ 25 ]. IR-780 solution (composed of polyoxymethylene castor oil, ethanol, and 5% glucose solution at a mass ratio of 1:1:9) was assigned as the control group; IR780-DTX-NPs and IR780-DTX-GNPs were assigned as study groups (the preparation method was the same as that of C6 coated nanoparticles).…”

Solid Lipid Nanoparticles: An Approach to Improve Oral Drug Delivery

“…Moreover, the oral bioavailability of curcumin-loaded SLN was 9.5-fold higher than that of the control solution. In 2019, an exciting approach was developed by Xing et al (108) to enhance the oral bioavailability of 2methoxyestradiol, an anti-tumor, anti-angiogenic, and anti-inflammatory estradiol metabolite characterized by low solubility and rapid elimination. The authors prepared modified SLN with PEG-PLC (polycarbonate) and embedded them in pH-sensitive microparticles to decrease the release of methoxyestradiol in the stomach but increase it in the intestinal tract and prolong the retention and absorption time of the carriers.…”