The Preparation and Evaluation of Cepharanthine-Nanostructured Lipid Carriers <i>In Vitro</i> and <i>In Vivo</i>

Li, Qianwen; Cai, Tiange; Huang, Yinghong; Cole, Susan P. C.; Cai, Yu-Dong

doi:10.1166/jbt.2017.1642

Cited by 4 publications

(3 citation statements)

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“…Increasing studies have indicated that CEP has a variety of pharmacological activities, implying that will play a crucial role in clinical trials. Nevertheless, CEP has the defect of low water solubility and low direct oral bioavailability which limit its pharmacological validity ( 35 ). The absolute bioavailability of CEP by oral route was only 5.65 ± 0.35% in rats ( 36 ).…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine

et al. 2021

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The aim of this article was to design a self-emulsifying drug delivery system (SEDDS) of loaded cepharanthine (CEP) to improve the oral bioavailability in rats. Based on the solubility determination and pseudo-ternary phase diagram, isopropyl palmitate (IPP) was chosen as the oil phase. Meanwhile, Cremophor RH40 and Macrogol 200 (PEG 200) were chosen as the emulsifier and co-emulsifier, respectively. This prescription was further optimized by using central composite design of response surface methodology. The optimized condition was CEP:IPP:Cremophor RH40:PEG 200=3.6:30.0:55.3:11.1 in mass ratio with maximum drug loading (36.21 mg/mL) and the minimum particle size (36.70 nm). The constructed CEP-SEDDS was characterized by dynamic light scattering, transmission electron microscopy, in vitro release and stability studies. The dissolution level of CEP-SEDDS was nearly 100% after 30 min in phosphate-buffered saline (PBS, pH 6.8) which was higher than that of the pure CEP (approximately 20%). In addition, in vivo pharmacokinetic study in rats showed that CEP-SEDDS dramatically improved bioavailability compared with active pharmaceutical ingredient (API) (the relative bioavailability was 203.46%). In this study, CEP-SEDDS was successfully prepared to enhance the oral bioavailability which might facilitate to increase its better clinical application. Graphical abstract

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Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine

et al. 2021

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“…The shape was observed using transmission electron microscopy (TEM; Tecnai 10; Philips Healthcare, DA Best, The Netherlands) following diluting of the NE with soybean oil. The particle size and polydispersity index (PDI) of the prepared NE were measured with a laser particle size analyzer (Nano ZS 90; Malvern Instruments, Inc., Westborough, MA, USA) ( 22 ).…”

Section: Methodsmentioning

confidence: 99%

Preparation and evaluation of spirulina polysaccharide nanoemulsions

Wang

Cai

Liu³

et al. 2018

Int J Mol Med

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The aim of the present study was to prepare spirulina polysaccharide (PSP) into an oral nanoemulsion (NE) with the aim of improving its oral bioavailability and prolonging its sustained release effect. The PSP-NE was prepared through a phase transformation method, and its formulation components were screened through the use of a pseudo-ternary phase diagram. The optimal formulation of PSP-NE was determined to be: 11.9% Span 80, 6.0% Tween-80, 9.0% ethanol, 62.8% soybean oil, and 10.3% PSP aqueous solution. The prepared PSP-NE was clear and transparent, had a uniform color and spherical morphology, exhibited stability and no adhesion. The average particle size was 79.93±19 nm, the polydispersity index was 0.185±0.04 (n=3), and the entrapment rate was 62%. Small-animal imaging results showed that the prepared PSP-NE exhibited a sustained release and tissue effect in contrast to the PSP aqueous solution. The present study showed that the prepared PSP-NE not only exhibited a sustained release and tissue effect in contrast to the PSP aqueous solution, but also had superior performance in terms of antitumor and antioxidant effects.

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“…The CEP encapsulation efficiency (EE) of the formulation was determined by the ultrafiltration method using HPLC to quantify the CEP in NLCs (Li et al., 2017 ) …”

Section: Methodsmentioning

confidence: 99%

Cepharanthine loaded nanoparticles coated with macrophage membranes for lung inflammation therapy

Zheng²,

Ding

et al. 2021

Drug Delivery

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Acute lung injury (ALI) is a disease associated with suffering and high lethality, but to date without any effective pharmacological management in the clinic. In the pathological mechanisms of ALI, a strong inflammatory response plays an important role. Herein, based on macrophage ‘homing’ into inflammation sites and cell membrane coating nanotechnology, we developed a biomimetic anti-inflammation nanosystem (MM-CEP/NLCs) for the treatment of ALI. MM-CEP/NLCs were made with nanostructured lipid carriers (NLCs) coated with natural macrophage membranes (MMs) to achieve effective accumulation of cepharanthine (CEP) in lung inflammation to achieve the effect of treating ALI. With the advantage of suitable physicochemical properties of NLCs and unique biological functions of the macrophage membrane, MM-CEP/NLCs were stabilized and enabled sustained drug release, providing improved biocompatibility and long-term circulation. In vivo , the macrophage membranes enabled NLCs to be targeted and accumulated in the inflammation sites. Further, MM-CEP/NLCs significantly attenuated the severity of ALI, including lung water content, histopathology, bronchioalveolar lavage cellularity, protein concentration, and inflammation cytokines. Our results provide a bionic strategy via the biological properties of macrophages, which may have greater value and application prospects in the treatment of inflammation.

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The Preparation and Evaluation of Cepharanthine-Nanostructured Lipid Carriers In Vitro and In Vivo

Cited by 4 publications

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Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine

Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine

Preparation and evaluation of spirulina polysaccharide nanoemulsions

Cepharanthine loaded nanoparticles coated with macrophage membranes for lung inflammation therapy

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