scholarly journals A Comparative Study of the Use of Mesoporous Carbon and Mesoporous Silica as Drug Carriers for Oral Delivery of the Water-Insoluble Drug Carvedilol

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1770 ◽  
Author(s):  
Cuiyan Han ◽  
Haitao Huang ◽  
Yan Dong ◽  
Xiaoyu Sui ◽  
Baiyu Jian ◽  
...  
Keyword(s):  
Mesoporous Silica ◽  
Oral Delivery ◽  
Mesoporous Carbon ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Drug Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Adsorption Effect ◽  
Insoluble Drugs

Mesoporous carriers have been extensively applied to improve the dissolution velocity and bioavailability of insoluble drugs. The goal of this work was to compare the drug-loading efficiency (LE) and drug-dissolution properties of mesoporous silica nanoparticles (MSN) and mesoporous carbon nanoparticles (MCN) as drug vectors oral delivery of water-insoluble drugs. For this purpose, MSN and MCN with similar particle size, surface area, and mesoporous diameter were prepared to precisely evaluate the effects of different textures on the drug-loading and dissolution behavior of insoluble drugs. Carvedilol (CAR), a Bio-pharmaceutic Classification System (BCS) class II drug, was loaded in the MSN and MCN by the solvent adsorption method and solvent evaporation method with different carrier–drug ratios. The carboxylated MCN (MCN–COOH) had a higher LE for CAR than MSN for both the two loading methods due to the strong adsorption effect and π–π stacking force with CAR. In vitro drug dissolution study showed that both MSN and MCN-COOH could improve the dissolution rate of CAR compared with the micronized CAR. In comparison to MSN, MCN-COOH displayed a slightly slower dissolution profile, which may be ascribed to the strong interaction between MCN-COOH and CAR. Observation of cell cytotoxicity and gastrointestinal mucosa irritation demonstrated the good biocompatibility of both MSN and MCN–COOH. The present study encourages further research of different carriers to determine their potential application in oral administration.

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

scholarly journals Polymeric Mesoporous Silica Nanoparticles for Enhanced Delivery of 5-Fluorouracil In Vitro

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 288 ◽  
Author(s):  
Thashini Moodley ◽  
Moganavelli Singh
Keyword(s):  
Side Effects ◽  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Therapeutic Potential ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Hek293 Cells ◽  
Cancer Drug ◽  
Delivery Vehicles

There is a need for the improvement of conventional cancer treatment strategies by incorporation of targeted and non-invasive procedures aimed to reduce side-effects, drug resistance, and recurrent metastases. The anti-cancer drug, 5-fluorouracil (5-FU), is linked to a variety of induced-systemic toxicities due to its lack of specificity and potent administration regimens, necessitating the development of delivery vehicles that can enhance its therapeutic potential, while minimizing associated side-effects. Polymeric mesoporous silica nanoparticles (MSNs) have gained popularity as delivery vehicles due to their high loading capacities, biocompatibility, and good pharmacokinetics. MSNs produced in this study were functionalized with the biocompatible polymers, chitosan, and poly(ethylene)glycol to produce monodisperse NPs of 36–65 nm, with a large surface area of 710.36 m2/g, large pore volume, diameter spanning 9.8 nm, and a favorable zeta potential allowing for stability and enhanced uptake of 5-FU. Significant drug loading (0.15–0.18 mg5FU/mgmsn), controlled release profiles (15–65%) over 72 hours, and cell specific cytotoxicity in cancer cells (Caco-2, MCF-7, and HeLa) with reduced cell viability (≥50%) over the non-cancer (HEK293) cells were established. Overall, these 5FU-MSN formulations have been shown to be safe and effective delivery systems in vitro, with potential for in vivo applications.

scholarly journals In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 215 ◽  
Author(s):  
Marcelo Dutra Duque ◽  
Daniela Amaral Silva ◽  
Michele Georges Issa ◽  
Valentina Porta ◽  
Raimar Löbenberg ◽  
...  
Keyword(s):  
Reference Product ◽  
Plasma Concentrations ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Time Data ◽  
Simulation Results ◽  
Population Simulation

A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution. This study aimed to simulate plasma concentrations of fluconazole capsules with different dissolution profiles and run population simulation to evaluate their bioequivalence. The dissolution profiles of two batches of the reference product Zoltec® 150 mg capsules, A1 and A2, and two batches of other products (B1 and B2; C1 and C2), as well as plasma concentration–time data of the reference product from the literature, were used for the simulations. Although products C1 and C2 had drug dissolutions < 85% in 30 min at 0.1 M HCl, simulation results demonstrated that these products would show the same in vivo performance as products A1, A2, B1, and B2. Population simulation results of the ln-transformed 90% confidence interval for the ratio of Cmax and AUC0–t values for all products were within the 80–125% interval, showing to be bioequivalent. Thus, even though the in vitro dissolution behavior of products C1 and C2 was not equivalent to a rapid dissolution profile, the computer simulations proved to be an important tool to show the possibility of bioequivalence for these products.

scholarly journals Effectiveness of Diverse Mesoporous Silica Nanoparticles as Potent Vehicles for the Drug L-DOPA

Materials ◽  
2019 ◽  
Vol 12 (19) ◽  
pp. 3202
Author(s):  
Sumita Swar ◽  
Veronika Máková ◽  
Ivan Stibor
Keyword(s):  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Vis Spectroscopy ◽  
Bet Analysis ◽  
Silica Materials ◽  
Different Types ◽  
Mesoporous Silica Materials ◽  
Drug Vehicle

Our study was focused on the synthesis of selective mesoporous silica nanoparticles (MSNs: MCM-41, MCM-48, SBA-15, PHTS, MCF) that are widely studied for drug delivery. The resulting mesoporous surfaces were conveniently prepared making use of verified synthetic procedures. The MSNs thus obtained were characterized by Brunauer-Emmett-Teller (BET) analysis and scanning electron microscopy (SEM). The selected MSNs with various pore diameters and morphologies were examined to evaluate the capability of L-DOPA drug loading and release. L-DOPA is a well-known drug for Parkinson’s disease. The L-DOPA drug loading and release profiles were measured by UV-VIS spectroscopy and SBA-15 was proved to be the most effective amongst all the different types of tested mesoporous silica materials as L-DOPA drug vehicle.

scholarly journals Smart Protein‐Based Formulation of Dendritic Mesoporous Silica Nanoparticles: Toward Oral Delivery of Insulin

2020 ◽  
Vol 26 (23) ◽  
pp. 5195-5199 ◽  
Author(s):  
Estelle Juère ◽  
Romain Caillard ◽  
Doris Marko ◽  
Giorgia Del Favero ◽  
Freddy Kleitz
Keyword(s):  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Oral Delivery ◽  
Mesoporous Silica Nanoparticles

scholarly journals Core-Shell Structure Design of Hollow Mesoporous Silica Nanospheres Based on Thermo-Sensitive PNIPAM and pH-Responsive Catechol-Fe3+ Complex

Polymers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1832 ◽  
Author(s):  
Weili Peng ◽  
Zeping Zhang ◽  
Minzhi Rong ◽  
Mingqiu Zhang
Keyword(s):  
Mesoporous Silica ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Structure Design ◽  
Raw 264.7 Cells ◽  
Core Shell ◽  
Loading Capacity ◽  
Ph Responsive ◽  
Hierarchical Porous ◽  
Hollow Mesoporous Silica

A kind of core-shell hybrid nanoparticle comprised of a hollow mesoporous silica nanoparticles (HMS) core and a copolymer shell bearing N-(3,4-dihydroxyphenethyl) methacrylamide (DMA) and N-isopropylacrylamide (NIPAM) as responsive moieties was prepared. Moreover, the factors that could impact the surface morphology and hierarchical porous structure were discussed. In the presence of Fe3+, catechol-Fe3+ complexes were formed to achieve pH-responsive polymer shell, combining with thermal-sensitiveness of poly(N-isopropylacrylamide). Doxorubicin (DOX) was applied as a model drug and the behaviors of its loading/release behaviors were investigated to prove the idea. The results exhibited a significant drug loading capacity of 8.6% and embed efficiency of 94.6% under 1 mg ml–1 DOX/PBS solution. In fact, the loading capacity of drug can be easily improved to as high as 28.0% by increasing the DOX concentration. The vitro cytotoxicity assay also indicated that the as-prepared nanoparticles have no significant cytotoxicity on RAW 264.7 cells. The in vitro experiment showed that the cumulative release of DOX was obviously dependent on the temperature and pH values. This pH/temperature-sensitive hollow mesoporous silica nanosphere is expected to have potential applications in controlled drug release.

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