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In the present study, a novel nonionic surfactant vesicles (NSVs) system consisting of cholesterol, Tween 80 and Span 80 was developed for the delivery of Ginsenoside Rb 1 with an improved oral bioavailability. The prepared vesicles were hollow and spherically shaped with acceptable diameter (264.68 ± 4.17 nm), zeta potential (−11.58 ± 0.87 mV) and encapsulation efficiency (69.034 ± 0.045%). XRD analysis provided affirmed the encapsulation of Rb 1 in the vesicles. The in vitro release profile of Rb 1 from the vesicles in the two different media (double distilled water, pH 7.0, phosphate buffer solution, pH 7.4) showed statistical insignificant difference when compared with the free Ginsenoside Rb 1. Notably, the pharmacokinetic analysis of optimized Ginsenoside Rb 1 -NSVs exhibited a higher C max (9.55 ± 0.5 μg/mL versus 6.22 ± 0.53 μg/mL) with 1.82-fold increase in relative oral bioavailability. Collectively, these findings revealed that the developed vesicles could be a novel alternative in improving the oral bioavailability of Ginsenoside Rb 1 and extending its application in the clinical setting. [Display omitted] • Ginsenoside Rb 1 was purified from Panax Ginseng extract. • Oral bioavailability of Ginsenoside Rb 1 was improved after encapsulation in vesicles. [ABSTRACT FROM AUTHOR]

Isoliquiritigenin (ISL) is known to have a variety of pharmacological activities, but its poor water solubility limits its application. In order to improve the bioavailability of ISL and its anti-colitis activity, this study aims to develop an effective drug delivery system loaded with ISL. In this study, ISL pH-sensitive micelles (ISL-M) were prepared by thin film hydration method. The micellar size (PS), polydispersity index (PDI), electrokinetic potential (ζ-potential), drug loading (DL), encapsulation rate (EE) and other physical parameters were characterized. The storage stability of ISL-M was tested, release in vitro and pharmacokinetic studies in rats were performed, and the anti-inflammatory effect of ISL-M on ulcerative colitis induced by dextran sulfate sodium (DSS) was evaluated. The results showed that PS, PDI, ZP, EE% and DL% of ISL-M were 151.15±1.04 nm, 0.092±0.014, -31.32±0.721 mV, 93.97±1.53 % and 8.42±0.34 %, respectively. Compared with unformulated ISL (F-ISL), the cumulative release rate of ISL-M in the three different media was significantly increased and showed a certain pH sensitivity. The area under drug curve (AUC 0-t) and peak concentration (C max) of ISL-M group were 2.94 and 4.06 times higher than those of ISL group. In addition, ISL-M is expected to develop new methods for increasing the bioavailability and anti-inflammatory activity of ISL. [Display omitted] [ABSTRACT FROM AUTHOR]

Isoliquiritigenin (ISL) has a great variety of pharmacological effects especially liver cancer therapy, but its poor solubility, bioavailability and liver targeting have limited its clinical use. In order to solve the aforementioned shortcomings, the TPGS-modified proliposomes loaded with ISL (ISL-TPGS-PLP) was prepared in this study. ISL-TPGS-PLP was fabricated via thin-film dispersion method and was characterized by the appearance, particle size, zeta potential and morphology. HPLC was used to evaluate entrapment efficiency (EE), in vitro release and stability of ISL-TPGS-PLP single or combined while appropriate physicochemical parameters were measured with DLS. Meanwhile, the pharmacokinetics and tissue distribution were also studied after oral administration. The results demonstrated that ISL-TPGS-PLP had a mean size of 23.8 ± 0.9 nm, high EE of 97.33 ± 0.40%. More importantly, nearly 90% ISL was released from ISL-TPGS-PLP within 24 h while only 50% was released from ISL suspension. In the pharmacokinetics study, the area under the curve (AUC 0-24h) of ISL-TPGS-PLP was 1.53 times higher than that of ISL suspension. The Tissue distribution study showed that the ISL released from ISL-TPGS-PLP was higher in the liver than the free ISL suspension. Altogether, ISL-TPGS-PLP could ameliorate the ISL solubility, bioavailability and liver targeting ability, suggesting that ISL-TPGS-PLP could serve as a promising nanocarrier for liver cancer therapy. [ABSTRACT FROM AUTHOR]

This study sought to prepare a self-microemulsion drug delivery system containing zingerone (Z-SMEDDS) to improve the low oral bioavailability of zingerone and anti-tumor effect. Z-SMEDDS was characterized by particle size, zeta potential and encapsulation efficiency, while its pharmacokinetics and anti-tumor effects were also evaluated. Z-SMEDDS had stable physicochemical properties, including average particle size of 17.29 ± 0.07 nm, the zeta potential of -22.81 ± 0.29 mV, and the encapsulation efficiency of 97.96% ± 0.02%. In vitro release studies have shown the release of zingerone released by Z-SMEDDS was significantly higher than free zingerone in different release media. The relative oral bioavailability of Z-SMEDDS was 7.63 times compared with free drug. Meanwhile, the half inhibitory concentration （IC50）of Z-SMEDDS and free zingerone was 8.45 μg/mL and 13.30 μg/mL, respectively on HepG2. This study may provide a preliminary basis for further clinical research and application of Z-SMEDDS. [ABSTRACT FROM AUTHOR]

The purpose of this study was to develop a precursor liposome nano-delivery system for liquiritin (LT) to improve its solubility, oral bioavailability, and efficacy. The characterizations of the particle diameter, zeta potential, polydispersity index (PDI), droplet morphology, drug release in vitro , and oral bioavailability of the prepared LT precursor liposomes (LTMs) were carried out. In addition, streptozotocin intraperitoneal injection successfully induced diabetic mouse model, while the LT hypoglycemic effect, oral glucose tolerance, biochemical parameters and pathological sections were studied. The prepared LTMs were diluted to obtain a clear and transparent solution with a diameter of 91.84 ± 1.85 nm, zeta potential of −38.59 ± 2.65 mV and PDI of 0.215 ± 0.016. The in vitro release of the LTMs was superior to that of the free LT suspension, which may be related to the increased solubility of LT, as well as the small diameter and increased surface area. The obtained pharmacokinetic parameters indicated that the relative oral bioavailability of LTMs was increased by 8.8 times compared with the free LT suspension. Pharmacodynamic studies showed that LTMs effectively improved LT's hypoglycemic effect and diabetes-related organ repair, simultaneously confirmed its antioxidant activity. These results implied that the LTMs was an effective method to improve the solubility, oral bioavailability, and hypoglycemic activity of LT. [ABSTRACT FROM AUTHOR]