Drug loaded and ethylcellulose coated mesoporous silica for controlled drug release prepared using a pilot scale fluid bed system

Hacene, Youcef Chakib; Singh, Abhishek; Mooter, Guy Van den

doi:10.1016/j.ijpharm.2016.04.047

Cited by 30 publications

(15 citation statements)

References 19 publications

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“…However, because of high cytotoxicity and non-specificity to tumors, many chemotherapy drugs bring severe side effects, which exert pronounced suffering to patients and make them unfit for long-term therapy 3 - 5 . Currently, among the various approaches to improve the effectiveness of chemotherapy drugs, controlled drug delivery systems that can convey chemotherapeutic drugs safely and efficaciously have attracted great attention 6 - 12 . A desirable controlled release system should: 1) be easy to prepare with high purity; 2) accumulate more in cancer than normal cells; 3) exhibit minimal cytotoxicity to normal cells; 4) have favorable controlled release to prolong the acting time and avoid multiple dosing; 5) enable direct and real-time monitoring of the drug release dynamics with high accuracy in a noninvasive manner 13 - 15 .…”

Section: Introductionmentioning

confidence: 99%

Dual turn-on fluorescence signal-based controlled release system for real-time monitoring of drug release dynamics in living cells and tumor tissues

et al. 2018

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Controlled release systems with capabilities for direct and real-time monitoring of the release and dynamics of drugs in living systems are of great value for cancer chemotherapy. Herein, we describe a novel dual turn-on fluorescence signal-based controlled release system (CDox), in which the chemotherapy drug doxorubicin (Dox) and the fluorescent dye (CH) are conjugated by a hydrazone moiety, a pH-responsive cleavable linker. CDox itself shows nearly no fluorescence as the fluorescence of CH and Dox is essentially quenched by the C=N isomerization and N-N free rotation. However, when activated under acidic conditions, CDox could be hydrolyzed to afford Dox and CH, resulting in dual turn-on signals with emission peaks at 595 nm and 488 nm, respectively. Notably, CDox exhibits a desirable controlled release feature as the hydrolysis rate is limited by the steric hindrance effect from both the Dox and CH moieties. Cytotoxicity assays indicate that CDox shows much lower cytotoxicity relative to Dox, and displays higher cell inhibition rate to cancer than normal cells. With the aid of the dual turn-on fluorescence at different wavelengths, the drug release dynamics of CDox in living HepG2 and 4T-1 cells was monitored in double channels in a real-time fashion. Importantly, two-photon fluorescence imaging of CDox in living tumor tissues was also successfully performed by high-definition 3D imaging. We expect that the unique controlled release system illustrated herein could provide a powerful means to investigate modes of action of drugs, which is critical for development of much more robust and effective chemotherapy drugs.

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Section: Introductionmentioning

confidence: 99%

Dual turn-on fluorescence signal-based controlled release system for real-time monitoring of drug release dynamics in living cells and tumor tissues

et al. 2018

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“…The material temperature played an important role in the coating quality and the in vitro release profile of the products (Hacene, Singh, & Van den Mooter, ). Different material temperatures (26, 28, 30. and 32°C) were tested, and the results of the in vitro release behavior at pH 1.2 revealed that the release rate of DMOP at 26°C was significantly higher than that at other temperatures (Figure a).…”

Section: Resultsmentioning

confidence: 99%

“…The material temperature played an important role in the coating quality and the in vitro release profile of the products (Hacene, Singh, & Van den Mooter, 2016). Different material temperatures (26,28,30.…”

Section: Preparation and Optimization Of Dmopmentioning

confidence: 99%

Modified‐release oral pellets for duodenum delivery of doxycycline hyclate

Huang

et al. 2019

Drug Development Research

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To minimize the gastric and esophageal injury effect, a system to deliver doxycycline hyclate (DOXY) to the duodenum area is needed. DOXY‐containing modified‐release oral pellets (DMOP) coated with hydroxypropyl methylcellulose phthalate HP‐55 (HPMCP HP‐55) and hydroxypropyl methylcellulose E15 (HPMC E15) appear to be a reasonable choice. This coating layer dissolves at pH 5.5, which is the pH of the duodenum, but not at a gastric pH (1.2). The formulation and preparation of DMOP were optimized, and a scale‐up test was performed. The results showed that the production reproducibility was acceptable, and the quality of DMOP well met the standards of Chinese Pharmacopeia (Ch.P, 2015 edition). Notably, the accumulated DOXY release was lower than 50% at pH 1.2 (20 min) and higher than 85% at pH 5.5, which met the USP40‐NF35 standard for DOXY modified‐release formulations. Moreover, the storage stability of DMOP with different packages was investigated by stress testing, accelerated and long‐term testings. The stability of DMOP was maintained up to 12 months, in terms of DOXY content and in vitro release behavior. The results seem to suggest that DMOP could be a promising duodenum delivery system.

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“…First, the poor biodegradability of MSNs leads to toxic bioaccumulation after long‐term administration. Second, when the drug‐loaded MSNs are internalized into cancer cells, only a portion of the drug releases from the nanoparticles; much of the drug remains in the pore canal and cannot exert its anticancer effect . This incomplete release limits the therapeutic effect of the drug‐loaded MSNs.…”

Section: Introductionmentioning

confidence: 99%

A comparison of mesoporous silica nanoparticles and mesoporous organosilica nanoparticles as drug vehicles for cancer therapy

Yue

Luo

et al. 2018

Chem Biol Drug Des

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Mesoporous silica nanoparticles (MSNs) are promising drug carriers for use in cancer treatment owing to their excellent biocompatibility and drug-loading capacity. However, MSN's incomplete drug release and toxic bioaccumulation phenomena limit their clinical application. Recently, researchers have presented redox responsive mesoporous organosilica nanoparticles containing disulfide (S-S) bridges (ss-MONs). These nanoparticles retained their ability to undergo structural degradation and increased their local release activity when exposed to reducing agents. Disulfide-based mesoporous organosilica nanoparticles offer researchers a better option for loading chemotherapeutic drugs due to their effective biodegradability through the reduction of glutathione. Although the potential of ss-MONs in cancer theranostics has been studied, few researchers have systematically compared ss-MONs with MSNs with regard to endocytosis, drug release, cytotoxicity, and therapeutic effect. In this work, ss-MONs and MSNs with equal morphology and size were designed and used to payload doxorubicin hydrochloride (DOX) for liver cancer chemotherapy. The ss-MONs showed considerable degradability in the presence of glutathione and performed comparably to MSNs on biocompatibility measures, including cytotoxicity and endocytosis, as well as in drug-loading capacity. Notably, DOX-loaded ss-MONs exhibited higher intracellular drug release in cancer cells and better anticancer effects in comparison with DOX-loaded MSNs. Hence, the ss-MONs may be more desirable carriers for a highly efficient and safe treatment of cancer.

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Drug loaded and ethylcellulose coated mesoporous silica for controlled drug release prepared using a pilot scale fluid bed system

Cited by 30 publications

References 19 publications

Dual turn-on fluorescence signal-based controlled release system for real-time monitoring of drug release dynamics in living cells and tumor tissues

Dual turn-on fluorescence signal-based controlled release system for real-time monitoring of drug release dynamics in living cells and tumor tissues

Modified‐release oral pellets for duodenum delivery of doxycycline hyclate

A comparison of mesoporous silica nanoparticles and mesoporous organosilica nanoparticles as drug vehicles for cancer therapy

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