scholarly journals Oral Drug Delivery Systems Based on Ordered Mesoporous Silica Nanoparticles for Modulating the Release of Aprepitant

2021 ◽  
Vol 22 (4) ◽  
pp. 1896
Author(s):  
Theodora Christoforidou ◽  
Dimitra Giasafaki ◽  
Eleftherios G. Andriotis ◽  
Nikolaos Bouropoulos ◽  
Nikoleta F. Theodoroula ◽  
...  
Keyword(s):  
Silica Nanoparticles ◽  
Oral Drug Delivery ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Active Agent ◽  
Amorphous State ◽  
Diffusion Method ◽  
Oral Drug ◽  
Scanning Calorimetry ◽  
Ordered Mesoporous

Two different types of ordered mesoporous nanoparticles, namely MCM-41 and MCM-48, with similar pore sizes but different pore connectivity, were loaded with aprepitant via a passive diffusion method. The percentage of the loaded active agent, along with the encapsulation efficiency, was evaluated using High-performance Liquid Chromatography (HPLC) analysis complemented by Thermogravimetric Analysis (TGA). The determination of the pore properties of the mesoporous particles before and after the drug loading revealed the presence of confined aprepitant in the pore structure of the particles, while Powder X-ray Diffractometry(pXRD), Differential Scanning Calorimetry (DSC), and FTIR experiments indicated that the drug is in an amorphous state. The release profiles of the drug from the two different mesoporous materials were studied in various release media and revealed an aprepitant release up to 45% when sink conditions are applied. The cytocompatibility of the silica nanoparticles was assessed in Caco-2 cell monolayers, in the presence and absence of the active agent, suggesting that they can be used as carriers of aprepitant without presenting any toxicity in vitro.

Facile Synthesis of Chitosan Based-(AMPS-co-AA) Semi-IPNs as a Potential Drug Carrier: Enzymatic Degradation, Cytotoxicity, and Preliminary Safety Evaluation

2019 ◽  
Vol 16 (3) ◽  
pp. 242-253 ◽  
Author(s):  
Kaleem Ullah ◽  
Muhammad Sohail ◽  
Abdul Mannan ◽  
Haroon Rashid ◽  
Aamna Shah ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Cytotoxicity ◽  
Oral Drug ◽  
Specific Enzyme ◽  
Oral Toxicity ◽  
Scanning Calorimetry

Objective: The study describes the development of chitosan-based (AMPS-co-AA) semi-IPN hydrogels using free radical polymerization technique. Methods: The resulting hydrogels were characterized using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), X-Ray diffraction (XRD), and Scanning Electron Microscopy (SEM). The successful crosslinking of chitosan, 2- Acrylamido-2-Methylpropane Sulfonic Acid (AMPS), and Acrylic Acid (AA) was confirmed by FT IR. Unloaded and drug-loaded hydrogels exhibited higher thermal stability after crosslinking compared to the individual components. XRD confirmed the decrease in crystallinity after hydrogel formation and molecular dispersion of Oxaliplatin (OXP) in the polymeric network. SEM showed rough, vague and nebulous surface resulting from crosslinking and loading of OXP. Results: The experimental results revealed that swelling and drug release were influenced by the pH of the medium being low at acidic pH and higher at basic pH. Increasing the concentration of chitosan and AA enhanced the swelling, drug loading and drug release while AMPS was found to act inversely. Conclusion: It was confirmed that the hydrogels were degraded more by specific enzyme lysozyme as compared to the non-specific enzyme collagenase. In-vitro cytotoxicity suggested that the unloaded hydrogels were non-cytotoxic while crude drug and drug-loaded hydrogel exhibited dose-dependent cytotoxicity against HCT-116 and MCF-7. Results of acute oral toxicity on rabbits demonstrated that the hydrogels are non-toxic up to 3900 mg/kg after oral administration, as no toxicity or histopathological changes were observed in comparison to control rabbits. These pH-sensitive hydrogels appear to provide an ideal basis as a safe carrier for oral drug delivery.

Novel Self-Assembled Polycaprolactone–Lipid Hybrid Nanoparticles Enhance the Antibacterial Activity of Ciprofloxacin

2020 ◽  
Vol 25 (6) ◽  
pp. 598-607
Author(s):  
Mustafa E. Omer ◽  
Majed Halwani ◽  
Rayan M. Alenazi ◽  
Omar Alharbi ◽  
Shokran Aljihani ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Drug Loading ◽  
In Vitro Release ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Hybrid Nanoparticles ◽  
Diffusion Method ◽  
Prolonged Release ◽  
Scanning Calorimetry

Ciprofloxacin (CIP), a widely used antibiotic, is a poor biopharmaceutical resulting in low bioavailability. We optimized a CIP polymer–lipid hybrid nanoparticle (CIP-PLN) delivery system to enhance its biopharmaceutical attributes and the overall therapeutic performance. CIP-PLN formulations were prepared by a direct emulsification–solvent–evaporation method. Varying the type and ratio of lipid was tried to optimize a CIP-PLN formulation. All the prepared formulations were evaluated for their particle size, polydispersity index, zeta potential, physical stability, and drug entrapment efficiency. The drug in vitro release profile was also studied. Antibacterial activities were tested by the agar diffusion method for all CIP-PLN formulations against an Escherichia coli clinical bacterial isolate (EC04). CIP-PLN formulations showed average sizes in the range of 133.9 ± 1.7 nm to 217.1 ± 0.8 nm, exhibiting high size uniformity as indicated by polydispersity indices lower than 0.25. The entrapment efficiency was close to 80% for all formulations. The differential scanning calorimetry (DSC) thermograms indicated the existence of CIP in the amorphous state in all PLN formulations. Fourier transform infrared spectra indicated deep incorporation of molecular CIP within the polymer matrix. The release profile of CIP from PLN formulas showed a uniform prolonged drug profile, extended for a week from most formulations with a zero-order kinetics. The antibacterial activity of CIP-PLN formulations showed significantly higher antibacterial activity only with F4 containing lecithin as the lipid component. In conclusion, we successfully optimized a CIP-PLN formulation with a low nanoparticle size in a close range, high percentage of entrapment efficiency and drug loading, uniform prolonged release rate, and higher antibacterial activity against the EC04 clinical isolate.

scholarly journals Overcoming clofazimine intrinsic toxicity: statistical modelling and characterization of solid lipid nanoparticles

2018 ◽  
Vol 15 (139) ◽  
pp. 20170932 ◽  
Author(s):  
Luíse L. Chaves ◽  
Sofia Lima ◽  
Alexandre C. C. Vieira ◽  
Domingos Ferreira ◽  
Bruno Sarmento ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Delivery ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Amorphous State ◽  
Lipid Nanoparticles ◽  
Oral Drug ◽  
Solid Lipid ◽  
Cytotoxicity Studies

The aim of this work was to develop solid lipid nanoparticles (SLNs) loaded with clofazimine (CLZ) (SLNs-CLZ) to overcome its intrinsic toxicity and low water solubility, for oral drug delivery. A Box–Behnken design was constructed to unravel the relations between the independent variables in the selected responses. The optimized SLNs-CLZ exhibited the following properties: particle size ca 230 nm, zeta potential of −34.28 mV, association efficiency of 72% and drug loading of 2.4%, which are suitable for oral delivery. Further characterization included Fourier transformed infrared spectroscopy that confirmed the presence of the drug and the absence of chemical interactions. By differential scanning calorimetry was verified the amorphous state of CLZ. The storage stability studies ensured the stability of the systems over a period of 12 weeks at 4°C. In vitro cytotoxicity studies evidenced no effect of both drug-loaded and unloaded SLNs on MKN-28 gastric cells and on intestinal cells, namely Caco-2 and HT29-MTX cells up to 25 µg ml −1 in CLZ. Free CLZ solutions exhibited IC 50 values of 16 and 20 µg ml −1 for Caco-2 and HT29-MTX cells, respectively. It can be concluded that the optimized system, designed considering important variables for the formulation of poorly soluble drugs, represents a promising platform for oral CLZ delivery.

scholarly journals Effect of Shape on Mesoporous Silica Nanoparticles for Oral Delivery of Indomethacin

Pharmaceutics ◽  
2018 ◽  
Vol 11 (1) ◽  
pp. 4 ◽  
Author(s):  
Wei Zhang ◽  
Nan Zheng ◽  
Lu Chen ◽  
Luyao Xie ◽  
Mingshu Cui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Small Angle ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Mesoporous Silica Nanoparticles ◽  
Oral Drug ◽  
Pharmacokinetic Studies

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.

Programmable drug release using bioresponsive mesoporous silica nanoparticles for site-specific oral drug delivery

2014 ◽  
Vol 50 (42) ◽  
pp. 5547-5550 ◽  
Author(s):  
Amirali Popat ◽  
Siddharth Jambhrunkar ◽  
Jun Zhang ◽  
Jie Yang ◽  
Honwei Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Soy Protein ◽  
Oral Drug Delivery ◽  
Mesoporous Silica Nanoparticles ◽  
Oral Drug ◽  
Site Specific ◽  
Modified Surface

Programme Me! Programmable mesoporous silica based nanoparticles are produced via a combination of an amino modified surface and a coating of bio-responsive soy protein.

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.

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