RESUMO
The aim of this work was to increase the solubility and oral bioavailability of isorhamnetin, kaempferol, and quercetin in the total flavones of Hippophae rhamnoides L. (TFH) by preparing their nanosuspensions (NSs) and an inclusion complex. Based on the particle size and zeta potential, P407, Soluplus, SDS, PEG-6000, and HP-ß-CD were selected as stabilizers. TFH NSs and a TFH/HP-ß-CD inclusion complex were prepared, and their morphology, crystallinity, molecular interactions, and cytotoxicity were investigated. Furthermore, the saturation solubility, dissolution, and pharmacokinetics of the three flavonoids in the TFH, TFH NSs, and TFH/HP-ß-CD inclusion complex were compared. The five obtained TFH NSs were physically stable, and their particle sizes were all below 200 nm. The solubility and dissolution of the three active components were obviously enhanced by the formation of the TFH NSs and TFH/HP-ß-CD inclusion complex. Correspondingly, the oral bioavailability of isorhamnetin, kaempferol, and quercetin increased up to 4.11-, 3.85-, and 6.73-fold, respectively, in the TFH NSs and 2.89-, 3.71-, and 9.51-fold, respectively, in the TFH/HP-ß-CD inclusion complexes compared to those in the raw TFH. In brief, both NSs and inclusion complexes can improve the oral bioavailability of the three flavonoids in TFH. Taking the drug loading and the stable ratio of the multiple components into consideration, the NSs is a more promising strategy than the inclusion complex for increasing the oral bioavailability of multiple water-insoluble components in herbal extracts. Graphical abstract.
Assuntos
Flavonas/farmacocinética , Hippophae/química , Nanopartículas , 2-Hidroxipropil-beta-Ciclodextrina/química , Administração Oral , Animais , Disponibilidade Biológica , Flavonas/administração & dosagem , Masculino , Ratos , Ratos Sprague-Dawley , SolubilidadeRESUMO
Magnetic fibrous membrane used to generate heat under the alternating magnetic field (AMF) has attracted wide attention due to their application in magnetic hyperthermia. However, there is not magnetic fibrous membrane prepared by melt electrospinning (e-spinning) which is a solvent-free, bio-friendly technology. In this work, polycaprolactone (PCL)/Fe3O4 fiber membrane was prepared by melt e-spinning and using homemade self-powered portable melt e-spinning apparatus. The hand-held melt e-spinning apparatus has a weight of about 450 g and a precise size of 24 cm in length, 6 cm in thickness and 13 cm in height, which is more portable for widely using in the medical field. The PCL/Fe3O4 composite fibers with diameters of 4-17 µm, are very uniform. In addition, the magnetic composite fiber membrane has excellent heating efficiency and thermal cycling characteristics. The results indicated that self-powered portable melt e-spinning apparatus and PCL/Fe3O4 fiber membrane may provide an attractive way for hyperthermia therapy.
Assuntos
Hipertermia Induzida , Nanopartículas Magnéticas de Óxido de Ferro/química , Membranas Artificiais , Nanofibras/química , Poliésteres/química , Humanos , Nanopartículas Magnéticas de Óxido de Ferro/ultraestrutura , Nanofibras/ultraestruturaRESUMO
An auxiliary electrode electrospinning method is proposed to deposit N-octyl-2-cyanoacrylate (NOCA) medical glue fibrous membrane on kidney for in-situ fast hemostasis. A metal electrode equipped to the spinning needle is used to confine the divergence angle of jet. Compared to the conventional electrospinning method, the fiber deposition area has reduced by 2.5 times, and it can achieve in-situ accurate deposition. Moreover, it reduces both the external dimension and over-reliance on electricity, which is superior to previous air-flow assisted electrospinning method. In addition, in situ accurate deposition of NOCA on the kidney exhibits fast hemostasis within 10â¯s, confirming that this auxiliary electrode method can be applied in outdoors for fast hemostasis. Further pathological studies indicate that this auxiliary electrode method can reduce the inflammatory response of tissues due to the better accurate deposition. This portable hand-held device with the auxiliary electrode method may have potential application in fast hemostasis for outdoors due to its accurate deposition and portability characteristics.
Assuntos
Adesivos/farmacologia , Galvanoplastia/métodos , Hemostasia/efeitos dos fármacos , Rim/efeitos dos fármacos , Animais , Contagem de Células Sanguíneas , Estimulação Elétrica , Eletrodos , Rim/patologia , Masculino , Ratos Sprague-Dawley , Espectroscopia de Infravermelho com Transformada de Fourier , SuínosRESUMO
Precise deposition of nanofibers is still an important issue in the applications of electrospinning (e-spinning), especially in rapid hemostasis of organs such as the liver, lung, and kidney. In this study, we propose an electric field-modified e-spinning technique with a metal cone attached to the spinning nozzle to realize controllable precise deposition of fibers. The deposition range of the e-spun fibers is tunable by changing the size of the metal cone, and the mechanism is attributed the focused electric field verified by theoretical simulations. This electric field-modified e-spinning method was further used to in situ precisely deposit medical glue N-octyl-2-cyanoacrylate (NOCA) fibers onto the resection site of rat liver to realize rapid hemostasis within 10 s. Postoperative pathological results indicate that less inflammatory response and tissue adhesion are observed in this electric field-modified e-spinning group compared with that of traditional airflow-assisted group. This technique combined with our designed handheld e-spinning device could be used in emergency medical treatment, clinics, field survival, and home care for its portability and precise deposition characteristics.