Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Wang, Zhouhua; Bao, Chen; Quan, Guilan; Li, Feng; Wu, Qi-Zhen; Dian, Linghui; Dong, Yixuan; Li, Ge; Wu, Chuanbin

doi:10.2147/ijn.s37650

Cited by 34 publications

(15 citation statements)

References 35 publications

(35 reference statements)

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“…2d). These results verified the typical two-dimensional structure of the material (Wang et al, 2012). For SBA-16 the mean pore size was about 6 nm (measured from the images).…”

Section: Resultssupporting

confidence: 84%

Synthesis and characterization of mesoporous SBA-15 and SBA-16 as carriers to improve albendazole dissolution rate

Adrover

Pedernera

Bonne

et al. 2020

Saudi Pharmaceutical Journal

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Albendazole (ABZ, anti-parasitic active pharmaceutical ingredient) is a crystalline low water-soluble drug, thus the dissolution rate in gastrointestinal fluids is limited. Consequently, the improvement of the water solubility and dissolution rate of ABZ implies a great challenge for a more efficient treatment of hydatidosis. In this context, SBA-15 and SBA-16 ordered mesoporous silica materials were synthetized and loaded with ABZ. X-ray diffraction, FT-IR spectroscopy, nitrogen physisorption manometry, particle size distribution and scanning electronic microscopy were used to characterize unloaded and loaded materials (ABZ/SBA-15 and ABZ/SBA-16). The loaded ABZ amount in the carriers was estimated by elemental analysis. For the loaded materials, the drug solubility and release profile were evaluated. In addition, mathematical models were compared to explain the dissolution kinetics of ABZ from mesoporous solids. ABZ was successfully loaded into the mesopores. The amorphous state of the adsorbed ABZ was confirmed by differential scanning calorimetry that resulted in a notable increment in the dissolution rate compared to crystalline ABZ. Drug release behaviors were well simulated by the Weibull model for ABZ/SBA-15 and by the Gompertz function for pure ABZ and ABZ/SBA-16. The SBA-15 carrier exhibited the highest drug loading and dissolution rate becoming a promising material to improve ABZ bioavailability.

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“…2d). These results verified the typical two-dimensional structure of the material (Wang et al, 2012). For SBA-16 the mean pore size was about 6 nm (measured from the images).…”

Section: Resultssupporting

confidence: 84%

Synthesis and characterization of mesoporous SBA-15 and SBA-16 as carriers to improve albendazole dissolution rate

Adrover

Pedernera

Bonne

et al. 2020

Saudi Pharmaceutical Journal

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“…For the CIP-loaded MCM-41 sample the broad halo in the range of 15-35° derived from the amorphous silica with significant reduction of peaks characteristic for the CIP. Two diffraction peaks at 8 and 27° 2 θ observed in CIP-loaded MCM-41 sample suggested the semi-crystalline nature of CIP molecules adsorbed onto the silica surface [38]. In the case of both the F3 and MCM-F3 the XRD patterns showed two broad amorphous halos at 10-15° and 15-30° 2 θ which clearly revealed the amorphous nature of the obtained films.…”

Section: Resultsmentioning

confidence: 97%

The Effect of Polydimethylsiloxane-Ethylcellulose Coating Blends on the Surface Characterization and Drug Release of Ciprofloxacin-Loaded Mesoporous Silica

2019

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In this study, we obtained novel solid films composed of ciprofloxacin-loaded mesoporous silica materials (CIP-loaded MCM-41) and polymer coating blends. Polymer coating blends were composed of ethylcellulose (EC) with various levels of polydimethylsiloxane (PDMS, 0, 1, 2% (v/v)). The solid films were prepared via the solvent-evaporation molding method and characterized by using scanning electron microscopy (SEM), optical profilometry, and wettability analyses. The solid-state of CIP present in the solid films was studied using X-ray diffraction (XRD) and differential scanning calorimetry (DSC). The release profiles of CIP were examined as a function of PDMS content in solid films. The surface morphology analysis of solid films indicated the progressive increase in surface heterogeneity and roughness with increasing PDMS content. The contact angle study confirmed the hydrophobicity of all solid films and significant impact of both PDMS and CIP-loaded MCM-41 on surface wettability. DSC and XRD analysis confirmed the presence of amorphous/semi-crystalline CIP in solid films. The Fickian diffusion-controlled drug release was observed for the CIP-loaded MCM-41 coated with PDMS-free polymer blend, whereas zero-order drug release was noticed for the CIP-loaded MCM-41 coated with polymer blends enriched with PDMS. Both the release rate and initial burst of CIP decreased with increasing PDMS content.

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“… 38 All the above mentioned structural characteristics indicated that synthetic MSn was suitable as an oral drug delivery carrier the same as other mesoporous materials. 39 , 40 …”

Section: Resultsmentioning

confidence: 99%

Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate

Bai

et al. 2018

DDDT

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BackgroundBiopharmaceutics classification system class II drugs have low solubility, which limits their extent and speed of absorption after oral administration. Over the years, mesoporous materials have been widely used to increase the dissolution rate and oral relative bioavailability of poorly water-soluble drugs.ObjectivesIn order to improve the dissolution rate and increase oral relative bioavailability of the poorly water-soluble drugs, a tin oxide carrier (MSn) with a mesoporous structure was successfully synthesized.MethodsIn this study, MSn was synthesized using mesoporous silica material (SBA-15) as the template. Fenofibrate (FNB) was adsorbed into the channels of MSn by an adsorption method. Characterizations of the pure FNB, MSn, physical mixture of the drug and MSn (PM; 1:1) and FNB-loaded MSn (FNB-MSn) samples were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), N2 adsorption/desorption, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopy. Cytotoxicity assay (MTT) was used to evaluate the cytotoxicity of MSn. In vitro dissolution studies were performed to investigate the dissolution rate of FNB-MSn. In vivo pharmacokinetic studies were used to investigate the changes of plasma drug concentrations of FNB-MSn tablets and commercial FNB tablets in rabbits.ResultsDetailed characterization showed that FNB in the channels of MSn was present in an amorphous state. The in vitro release tests demonstrated that MSn with a good biocompatibility could effectively enhance the dissolution rate of FNB. Pharmacokinetic results indicated that MSn significantly increased the oral relative bioavailability of FNB.ConclusionMSn can be regarded as a promising carrier for an oral drug delivery system.

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Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Cited by 34 publications

References 35 publications

Synthesis and characterization of mesoporous SBA-15 and SBA-16 as carriers to improve albendazole dissolution rate

Synthesis and characterization of mesoporous SBA-15 and SBA-16 as carriers to improve albendazole dissolution rate

The Effect of Polydimethylsiloxane-Ethylcellulose Coating Blends on the Surface Characterization and Drug Release of Ciprofloxacin-Loaded Mesoporous Silica

Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate

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