The curcumin (CUR)-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex (CUR-HP-β-CD) was prepared to erase its therapeutic restrictions of poor aqueous solubility and low oral bioavailability. CUR-HP-β-CD was prepared by a simple procedure of water-ethanol cosolvent incubation-lyophilization which may be suitable for scale up production, and characterized by Fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), phase solubility method and dissolution study; the in vitro cytotoxicity was assayed by MTT, whereas the in vivo pharmacokinetics was tested by HPLC in rats receiving formulations via intravenous and oral administration, respectively. CUR was successfully encapsulated in HP-β-CD with a loading capacity of about 1:7 of CUR to HP-β-CD mole ratio, which remarkably enhanced drug water solubility and maintained well the antitumour activity of CUR. The CUR-HP-β-CD and free CUR have a similar pharmacokinetic behaviour in rats after intravenous administration; however, the oral bioavailability of CUR was enhanced to 2.77-fold by the HP-β-CD. The CUR-HP-β-CD can be successfully prepared by a simple method, which may be feasible for industrial scaling up, to remarkably increase drug water solubility and oral bioavailability while maintaining its bioactivity and may be a promising therapeutic preparation.
Vulnerability of respiratory mucosa to invasions of airborne pathogens, such as SARS-CoV, MERS-CoV and avian viruses which sometimes cause a life-threatening epidemic and even pandemic, underscores significance of developing a pulmonary vaccine adjuvant-delivery system (VADS). Herein, 30-nm aluminum nanoparticles (ANs), unlike the mostly used adjuvant alum which is unsuitable for delivering pulmonary vaccines due to side effects, proved able to act as a VADS fitting inhalation immunization to elicit wide-spread anti-antigen immunity. In vitro ANs facilitated cellular uptake of their cargos and, after pulmonary vaccination, induced mouse production of high levels of anti-antigen IgG in serum and IgA in saliva, nasal, bronchoalveolar and also vaginal fluids. Besides, IFN-γ and anti-antigen IgG2a enriched in immunized mice which meanwhile showed no obvious lung inflammation indicated balanced Th1/Th2 responses were safely induced. These outcomes suggest ANs may be an efficient pulmonary VADS for defending against pathogens, especially, the ones invading hosts via respiratory system.
Graphic AbstractAluminum nanoparticles can safely induce humoral and cellular immunity at systemic and mucosal level through pulmonary vaccination to contrast the conventional adjuvant alum.
Cimetidine reacting with 1,5-dichloroanthraquinone in acetone solution can produce a charge-transfer complex that shows a strong absorption peak at 343 nm. The absorption value at 343 nm increased with cimetidine concentration in the range of 0.01-0.5 µg/mL, with regression coefficient of 0.9995 and detection limit of 0.006 µg/mL. This simple and sensitive method has been successfully applied to determine cimetidine in tablets and capsules, with average recovery of (98.47±0.92)% and (97.07±1.16)%, respectively. Furthermore, the mole ratio of the complex between cimetidine and 1,5-dichloroanthraquinone is 2∶1, and the mechanism of charge-transfer reaction is explored.
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