Application of commercially available mesoporous silica for drug dissolution enhancement in oral drug delivery

Author(s):  
Ana Baumgartner ◽  
Odon Planinšek
2018 ◽  
Vol 513 ◽  
pp. 736-747 ◽  
Author(s):  
Ying Wang ◽  
Yu Cui ◽  
Yating Zhao ◽  
Qinfu Zhao ◽  
Bing He ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 344
Author(s):  
Jong-Hwa Lee ◽  
Hyeong Sik Jeong ◽  
Jong-Woo Jeong ◽  
Tae-Sung Koo ◽  
Do-Kyun Kim ◽  
...  

Rivaroxaban (RXB), a novel oral anticoagulant that directly inhibits factor Xa, is a poorly soluble drug belonging to Biopharmaceutics Classification System (BCS) class II. In this study, a hot-melt extruded amorphous solid dispersion (HME-ASD) containing RXB is prepared by changing the drug:polymer ratio (Polyvinylpyrrolidione-vinyl acetate 64, 1:1–1:4) and barrel temperature (200–240 °C), fixed at 20% of Cremophor® RH 40 and 15 rpm of the screw speed, using the hot-melt extruding technique. This study evaluates the solubility, dissolution behavior, and bioavailability for application to oral drug delivery and optimizes the formulation of rivaroxaban amorphous solid dispersion (RXB-ASD). Based on a central composite design, optimized RXB-ASD (PVP VA 64 ratio 1:4.1, barrel temperature 216.1 °C, Cremophor® RH 40 20%, screw speed 15 rpm) showed satisfactory results for dependent variables. An in vitro drug dissolution study exhibited relatively high dissolution in four media and achieved around an 80% cumulative drug release in 120 min. Optimized RXB-ASD was stable under the accelerated condition for three months without a change in crystallinity and the dissolution rate. A pharmacokinetic study of RXB-ASD in rats showed that the absorption was markedly increased in terms of rate and amount, i.e., the systemic exposure values, compared to raw RXB powder. These results showed the application of quality by design (QbD) in the formulation development of hot-melt extruded RXB-ASD, which can be used as an oral drug delivery system by increasing the dissolution rate and bioavailability.


Nanoscale ◽  
2017 ◽  
Vol 9 (40) ◽  
pp. 15252-15277 ◽  
Author(s):  
Justyna Florek ◽  
Romain Caillard ◽  
Freddy Kleitz

Mesoporous silica nanocarriers are discussed as potential oral drug delivery systems, focusing on their advantages and limitations, and future perspectives.


Pharmaceutics ◽  
2018 ◽  
Vol 11 (1) ◽  
pp. 4 ◽  
Author(s):  
Wei Zhang ◽  
Nan Zheng ◽  
Lu Chen ◽  
Luyao Xie ◽  
Mingshu Cui ◽  
...  

The use of mesoporous silica nanoparticles (MSNs) in the field of oral drug delivery has recently attracted greater attention. However, there is still limited knowledge about how the shape of MSNs affects drug delivery capacity. In our study, we fabricated mesoporous silica nanorods (MSNRs) to study the shape effects of MSNs on oral delivery. MSNRs were characterized by transmission electron microscopy (TEM), nitrogen adsorption/desorption, Fourier transform infrared spectroscopy (FTIR), and small-angle X-ray diffraction (small-angle XRD). Indomethacin (IMC), a non-steroidal anti-inflammatory agent, was loaded into MSNRs as model drug, and the drug-loaded MSNRs resulted in an excellent dissolution-enhancing effect. The cytotoxicity and in vivo pharmacokinetic studies indicated that MSNRs can be applied as a safe and efficient candidate for the delivery of insoluble drugs. The use of MSNs with a rod-like shape, as a drug delivery carrier, will extend the pharmaceutical applications of silica materials.


2020 ◽  
Vol 26 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Beom-Jin Lee ◽  
Thao T.D. Tran

: Solid dispersions offer many advantages for oral drug delivery of poorly water-soluble drugs over other systems, including an increase in drug solubility and drug dissolution. The improvement of drug absorption and higher bioavailability of active pharmaceutical ingredients in the gastrointestinal tract have been reported in various studies. In certain circumstances, a rapid pharmacological effect is required for patients. Fast-dissolving solid dispersions provide an ideal formulation in such cases. This report will provide an overview of current studies on fast-dissolving solid dispersions, including not only solid dispersion powders with fast dissolution rates but also specific does forms for the controlled release of poorly water-soluble drugs. Specifically, the applications of fast-dissolving solid dispersions will be described in every specific case. Moreover, pharmaceutical approaches and the utilization of polymers will be summarized. The classification and analysis of fast-dissolving solid dispersions could provide insight into strategies and potential applications in future drug delivery developments.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 60-62
Author(s):  
Priya Mourya ◽  
Anindya Goswami ◽  
Neelesh Malviya ◽  

Medicated candies are solid oral dosage form containing medicaments in a flavored and sweetened base. The main advantages associated with buccal drug delivery are systemic absorption of drug, also increased bioavailability and avoidance of hepatic first pass metabolism. Tenofovir alafenamide fumarate is a drug of choice for the treatment of human immunodeficiency virus due to its potency and fewer side effects over tenofovir disoproxil fumarate. The aim of the present research work was to formulate and evaluate candy of tenofovir alafenamide fumarate for pediatric and geriatric patients for better patient acceptability. Medicated candies of tenofovir alafenamide fumarate were prepared by using heating and congealing method, and the prepared formulations were evaluated for various parameters such as organoleptic properties, weight variation, friability, hardness, drug content and in vitro drug dissolution time profile. On the basis of the above studies, it can be concluded that medicated candy can be utilized as alternative option for oral drug delivery for pediatric and geriatric patients.


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