These results indicate that the developed microemulsion represents a safe and orally effective carrier for poorly soluble substances. The formulation could be used for clinical trials and expand the application of capsaicin.
This study innovatively investigated the anticancer effect of Flammulina velutipes sterols (FVSs), the in vivo pharmacokinetics, and the tissue distribution of FVS-loaded liposomes. The FVS consisting of mainly 54.8% ergosterol and 27.9% 22,23-dihydroergosterol exhibited evident in vitro antiproliferative activity (liver HepG-2, IC50 = 9.3 μg mL(-1); lung A549, IC50 = 20.4 μg mL(-1)). To improve the poor solubility of FVS, F. velutipes sterol liposome (FVSL) was originally prepared. The encapsulation efficiency of ergosterol was 71.3 ± 0.1% in FVSL, and the encapsulation efficiency of 22,23-dihydroergosterol was 69.0 ± 0.02% in FVSL. In comparison to its two free sterol counterparts, the relative bioavailability of ergosterol and 22,23-dihydroergosterol in FVSL was 162.9 and 244.2%, respectively. After oral administration in Kunming mice, the results of tissue distribution demonstrated that the liposomal FVS was distributed mostly in liver and spleen. The drug was eliminated rapidly within 4 h. These findings support the fact that FVS, a potential nutraceutical and an effective drug for the treatment of liver cancer, could be encapsulated in liposomes for improved solubility and bioavailability.
An efficient HPLC method was developed and validated for the simultaneous determination of ergosterol and 22,23-dihydroergosterol in Flammulina velutipes sterol-loaded microemulsions (FVSMs). The different chromatographic conditions for in vitro and in vivo determinations were investigated, with the application examined by tissue distribution. Chromatographic separation was achieved on an Inertsil ODS-SP (250 × 4.6 mm, 5 µm) analytical column using a mobile phase of 98% methanol (in vitro), and 93% methanol for stomach samples and 96% methanol for other samples (in vivo) at 1.0 mL/min. The sterol content was detected at 282 nm. The established in vitro linearity ranges for ergosterol and 22,23-dihydroergosterol were 0.58-72.77 µg/mL (r1 = 0.9999) and 0.59-73.25 µg/mL (r2 = 0.9999), respectively, with the biological (in vivo) samples following the same trend. The accuracy of the method was >99% (in vitro) and between 93%-108% (in vivo). The LOQ was 2.15 µg/L for ergosterol and 2.41 µg/L for 22,23-dihydroergosterol in the in vitro studies. Also, the precisions met the acceptance criterion. These results indicate that the established HPLC method was specific, linear, accurate, precise and sensitive for the separation and simultaneous determination of ergosterol and 22,23-dihydroergosterol.
The study confirms the different pharmacokinetic and toxicity profiles of PLD compared with non-liposomal doxorubicin. The pharmacokinetic profiles in Chinese patients with breast tumours is different from those reported for European patients with metastatic breast cancer. The correlation between toxicities, neutropenia grade and nausea and two of the pharmacokinetic parameters, AUC and Cl, may be useful for guiding the dosing of the agent.
Using three‐dimensional current collectors (3DCC) as frameworks for lithium metal anodes (LMAs) is a promising approach to inhibit dendrite growth. However, the intrinsically accumulated current density on the top surface and limited Li‐ion transfer in the interior of 3DCC still lead to the formation of lithium dendrites, which can pose safety risks. In this study, it reports that gradient lithiophilic structures can induce uniform lithium deposition within the interior of the 3DCC, greatly suppressing dendrite formation, as confirmed by COMSOL simulations and experimental results. With this concept, a gradient‐structured zinc oxide‐loaded copper foam (GSZO‐CF) is synthesized via an easy solution‐combustion method at low cost. The resulting Li@GSZO‐CF symmetric cells demonstrate stable cycling performance for over 800 cycles, with an ultra‐deep capacity of 10 mAh cm−2 even under an ultra‐high current density of 50 mA cm−2, the top results reported in the literature. Moreover, when combined with a LiFePO4 (LFP) cathode under a low negative/positive (N/P) capacity ratio of 2.9, the Li@GSZO‐CF||LFP full cells exhibit stable performance for 200 cycles, with a discharge capacity of 130 mAh g−1 and retention of 85.5% at a charging/discharging rate of 1C. These findings suggest a promising strategy for the development of new‐generation LMAs.
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