scholarly journals Characterization of Drugs with Good Glass Formers in Loaded-Mesoporous Silica and Its Theoretical Value Relevance with Mesopores Surface and Pore-Filling Capacity

2022 ◽  
Vol 15 (1) ◽  
pp. 93
Author(s):  
Arif Budiman ◽  
Diah Lia Aulifa

The incorporation of a drug into mesoporous silica (MPS) is a promising strategy to stabilize its amorphous form. However, the drug within MPS has shown incomplete release, despite a supersaturated solution being generated. This indicates the determination of maximum drug loading in MPS below what is experimentally necessary to maximize the drug doses in the system. Therefore, this study aimed to characterize the drugs with good glass former loaded-mesoporous silica, determine the maximum drug loading, and compare its theoretical value relevance to monolayer covering the mesoporous (MCM) surface, as well as pore-filling capacity (PFC). Solvent evaporation and melt methods were used to load each drug into MPS. In addition, the glass transition of ritonavir (RTV) and cyclosporine A (CYP), as well as the melting peak of indomethacin (IDM) and saccharin (SAC) in mesoporous silica, were not discovered in the modulated differential scanning calorimetry (MDSC) curve, demonstrating that each drug was successfully incorporated into the mesopores. The amorphization of RTV-loaded MPS (RTV/MPS), CYP-loaded MPS (CYP/MPS), and IDM-loaded MPS (IDM/MPS) were confirmed as a halo pattern in powder X-ray diffraction measurements and a single glass transition event in the MDSC curve. Additionally, the good glass formers, nanoconfinement effect of MPS and silica surface interaction contributed to the amorphization of RTV, CYP and IDM within MPS. Meanwhile, the crystallization of SAC was observed in SAC-loaded MPS (SAC/MPS) due to its weak silica surface interaction and high recrystallization tendency. The maximum loading amount of RTV/MPS was experimentally close to the theoretical amount of MCM, showing monomolecular adsorption of RTV on the silica surface. On the other hand, the maximum loading amount of CYP/MPS and IDM/MPS was experimentally lower than the theoretical amount of MCM due to the lack of surface interaction. However, neither CYP or IDM occupied the entire silica surface, even though some drugs were adsorbed on the MPS surface. Moreover, the maximum loading amount of SAC/MPS was experimentally close to the theoretical amount of PFC, suggesting the multilayers of SAC within the MPS. Therefore, this study demonstrates that the characterization of drugs within MPS, such as molecular size and interaction of drug-silica surface, affects the loading efficiency of drugs within MPS that influence its relevance with the theoretical value of drugs.

2012 ◽  
Vol 486 ◽  
pp. 187-192
Author(s):  
Chun Feng Wang ◽  
Guo Wei Zhou ◽  
Lei Zhang

Porcine pancreatic lipase (PPL) was immobilized in ordered mesoporous silica materials, which were using PEG 2000 (poly (ethylene glycol)) and P123 as dual templates and synthesized via hydrothermal process. The materials were silylated by (3aminopropyl) triethoxysilane (APTES) by postsynthesis-grafting method. Samples were characterized by XRD, TEM, and BET. The results showed that the 2-dimensional hexagonal mesoscopic structure kept unchanging after modification. As compared to lipase immobilized mesoporous silica, the loading amount and hydrolization activity of lipase immobilized on aminopropyl-grafted mesoporous silica increased, respectively.


2017 ◽  
Vol 30 (3) ◽  
pp. 283-291
Author(s):  
Jie Geng ◽  
Quan Zhou ◽  
Juan Ge ◽  
Bo Bai ◽  
Lizhong Ni

This study focused on the preparation and characterization of silicon–acetylene resin by means of grafting functionalized mesoporous silica. (3-Aminopropyl) triethoxysilane was grafted to silica surface through the hydrolysis reaction to yield mesoporous silica functionalized with (3-Aminopropyl) triethoxysilane (MA). These MA nanoparticles were transferred to the chain of silicon–acetylene resin, poly(m-dietheynylbenzene-methylsilane) (PSA) to yield PSA-g-MA, with the help of the reaction of hydrochloric acid removal. PSA-g-MA was totally characterized by Fourier transform infrared spectroscopy, energy dispersive spectroscopy, differential scanning calorimetry, thermogravimetric analysis, scanning electron microscope, transmission electron microscope, and nuclear magnetic resonance, which certified the success of silica modification and functionalized nanoparticles grafted to chain of PSA. The char content of PSA-g-MA reached to 45% at 1000°C under air atmosphere, and the residual weight was increased by nearly 10%, compared with the unmodified PSA.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Zhen Li ◽  
Ying Peng ◽  
Xingyu Xia ◽  
Zhe Cao ◽  
Yuqing Deng ◽  
...  

AbstractA Sr-based metal-organic framework (MOF) is introduced as ketoprofen carrier to form a comprehensive system for treating osteoarthritis (OA), and the drug loading amount and release rate is investigated. Structural characterization of the samples showed that Sr/PTA-MOF had good crystal morphology and structure, and chemical and thermal stability. Ketoprofen was successfully loaded on the MOF carrier, which had been identified by high performance liquid chromatography (HPLC) and thermogravimetric analysis (TGA). The release experiment manifested that more than 90% of ketoprofen released from Sr/PTA-MOF after 24 h, and ketoprofen delivery was mainly governed by the Higuchi model. Furthermore, cytotoxicity experiment manifested that synthesized MOF carrier had no poisonous effect on OA chondrocytes, which provided a preliminary foundation for the realization of comprehensive treating OA.


2016 ◽  
Vol 223 ◽  
pp. 121-128 ◽  
Author(s):  
Chiranjit Santra ◽  
Sneha Shah ◽  
Aniruddha Mondal ◽  
Jai Krishna Pandey ◽  
Asit Baran Panda ◽  
...  

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak

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.


Author(s):  
Marcos de Oliveira Jr. ◽  
Kevin Herr ◽  
Martin Brodrecht ◽  
Nadia Berenice Haro-Mares ◽  
Till Wissel ◽  
...  

High-field Dynamic Nuclear Polarization is a powerful tool for the structural characterization of species on the surface of porous materials or nanoparticles. For these studies the main source of polarization...


Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 288 ◽  
Author(s):  
Thashini Moodley ◽  
Moganavelli Singh

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.


RSC Advances ◽  
2015 ◽  
Vol 5 (33) ◽  
pp. 25816-25823 ◽  
Author(s):  
Aigin Bashti ◽  
Ali Reza Kiasat ◽  
Babak Mokhtari

Application of SBA@BiPy2+ 2Cl− nanocomposite as a novel environmentally safe heterogeneous nanoreactor for the one-pot solvent-free synthesis of 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives.


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