“…As shown in Fig 2b, the phase inversion temperature of PAC powder was at 223 °C. However, the absence of a PAC melting peak in PAC-csMSN further confirmed that the PAC absorbed into csMSN existed in an amorphous state compared with that of the corresponding physical mixtures [24]. Fig 2PAC state characterization ( a XRD patterns, b DSC patterns)
…”
A nanodrug delivery system of paclitaxel-mesoporous silica nanoparticles with a core-shell structure (PAC-csMSN) was used to increase the dissolution of paclitaxel (PAC) and improve its treatment of lung cancer. PAC was loaded into the core-shell mesoporous silica nanoparticles (csMSN) by the adsorption equilibrium method and was in an amorphous state in terms of its mesoporous structure. In vitro and in vivo studies showed that csMSN increased the dissolution rate of PAC and improved its lung absorption. The area under concentration-time curve (AUC) value of PAC-csMSN used for pulmonary delivery in rabbits was 2.678-fold higher than that obtained with the PAC. After continuous administration for 3 days, a lung biopsy showed no signs of inflammation. Cell apoptosis results obtained by flow cytometry indicated that PAC-csMSN was more potent than pure PAC in promoting cell apoptosis. An absorption investigation of PAC-csMSN in A549 cells was carried out by transmission electron microscopy (TEM) and laser scanning confocal microscopy (LSCM). The obtained results indicated that the cellular uptake was time-dependent and csMSN was uptaken into the cytoplasm. All these results demonstrate that csMSN have the potential to achieve pulmonary inhalation administration of poorly water-soluble drugs for the treatment of lung cancer.
“…As shown in Fig 2b, the phase inversion temperature of PAC powder was at 223 °C. However, the absence of a PAC melting peak in PAC-csMSN further confirmed that the PAC absorbed into csMSN existed in an amorphous state compared with that of the corresponding physical mixtures [24]. Fig 2PAC state characterization ( a XRD patterns, b DSC patterns)
…”
A nanodrug delivery system of paclitaxel-mesoporous silica nanoparticles with a core-shell structure (PAC-csMSN) was used to increase the dissolution of paclitaxel (PAC) and improve its treatment of lung cancer. PAC was loaded into the core-shell mesoporous silica nanoparticles (csMSN) by the adsorption equilibrium method and was in an amorphous state in terms of its mesoporous structure. In vitro and in vivo studies showed that csMSN increased the dissolution rate of PAC and improved its lung absorption. The area under concentration-time curve (AUC) value of PAC-csMSN used for pulmonary delivery in rabbits was 2.678-fold higher than that obtained with the PAC. After continuous administration for 3 days, a lung biopsy showed no signs of inflammation. Cell apoptosis results obtained by flow cytometry indicated that PAC-csMSN was more potent than pure PAC in promoting cell apoptosis. An absorption investigation of PAC-csMSN in A549 cells was carried out by transmission electron microscopy (TEM) and laser scanning confocal microscopy (LSCM). The obtained results indicated that the cellular uptake was time-dependent and csMSN was uptaken into the cytoplasm. All these results demonstrate that csMSN have the potential to achieve pulmonary inhalation administration of poorly water-soluble drugs for the treatment of lung cancer.
“…39 Geng et al recently synthesized HMSNPs using hard template phenolic resin NPs to encapsulate two insoluble model drugs, namely carvedilol and fenofibrate. 40 The resulting drug-loading contents for carvedilol and fenofibrate were 26.2%±2.1% and 31.2%±2.7% in normal MSNPs and 37.5%±2.8% and 43.7%±3.2% in HMSNPs, respectively. These findings indicate that HMSNPs have higher drug-loading content than normal MSNPs under the same conditions.…”
Section: Mesoporous Silica-based Materials As Carriersmentioning
Drug molecules transformed into nanoparticles or endowed with nanostructures with or without the aid of carrier materials are referred to as “nanomedicines” and can overcome some inherent drawbacks of free drugs, such as poor water solubility, high drug dosage, and short drug half-life in vivo. However, most of the existing nanomedicines possess the drawback of low drug-loading (generally less than 10%) associated with more carrier materials. For intravenous administration, the extensive use of carrier materials might cause systemic toxicity and impose an extra burden of degradation, metabolism, and excretion of the materials for patients. Therefore, on the premise of guaranteeing therapeutic effect and function, reducing or avoiding the use of carrier materials is a promising alternative approach to solve these problems. Recently, high drug-loading nanomedicines, which have a drug-loading content higher than 10%, are attracting increasing interest. According to the fabrication strategies of nanomedicines, high drug-loading nanomedicines are divided into four main classes: nanomedicines with inert porous material as carrier, nanomedicines with drug as part of carrier, carrier-free nanomedicines, and nanomedicines following niche and complex strategies. To date, most of the existing high drug-loading nanomedicines belong to the first class, and few research studies have focused on other classes. In this review, we investigate the research status of high drug-loading nanomedicines and discuss the features of their fabrication strategies and optimum proposal in detail. We also point out deficiencies and developing direction of high drug-loading nanomedicines. We envision that high drug-loading nanomedicines will occupy an important position in the field of drug-delivery systems, and hope that novel perspectives will be proposed for the development of high drug-loading nanomedicines.
“…Nowadays, nanoparticle technology is being explored extensively for its ability to deliver proper drugs into tumor cells. 18,19 Nanoparticles (NPs) can change the pharmacokinetic and pharmacodynamic profiles of traditional therapeutics and thus may improve the efficacy of existing anticancer drugs. 20 Among them, hollow mesoporous silica nanoparticles (HMSNs) show great promise as a viable platform for effective delivery of anticancer drugs.…”
BackgroundThyroid cancer becomes the most common endocrine cancer with the greatest growing incidence in this decade. Sorafenib is a multikinase inhibitor for the treatment of progressive radioactive iodine-refractory differentiated thyroid cancer (DTC), while the off-target toxicity effect is usually inconvenient for patients taking.MethodsIn this study, hollow mesoporous silica nanoparticles (HMSNs) with transferrin modification (Tf-HMSNs) were loaded with sorafenib (sora@Tf-HMSNs) to help targeted delivery of sorafenib. Due to the biocompatible Tf shell, Tf-HMSNs exhibited excellent bio-compatibility and increased intracellular accumulation, which improved the targeting capability to cancer cells in vitro and in vivo.ResultsSora@Tf-HMSNs treatment exhibited the strongest inhibition effect of res-TPC-1 cells and res-BCPAP cells compared with sora@HMSNs and sorafenib groups and induced more cancer cell apoptosis. Finally, Western blot analysis was conducted to check the expression of RAF/MEK/ERK signaling pathway after sorafenib encapsulated Tf-HMSNs treatment.ConclusionOverall, sora@Tf-HMSNs can significantly increase the effective drug concentration in cancer cells and thus enhance the anticancer effect, which are expected to be promising nanocarriers to deliver anticancer drugs for effective and safe therapy for RAI-refractory DTC.
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