Evaluation of ordered mesoporous silica as a carrier for poorly soluble drugs: Influence of pressure on the structure and drug release

Vialpando, Monica; Aerts, Alexander; Persoons, Jeroen; Martens, Johan A.; Mooter, Guy Van den

doi:10.1002/jps.22535

Cited by 66 publications

(49 citation statements)

References 33 publications

(45 reference statements)

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“…Drug-loaded silica can be pressed into tablets without any pharmaceutical excipients by direct compression, [17][18][19] but the quality of the tablets is not ensured due to the poor compressibility. Finally, Limnelle et al 20 , Vialpando et al, 21 and Kiekens et al 22 have reported being able to compress drug-loaded silica with suitable excipients into tablets with acceptable quality.…”

Section: Introductionmentioning

confidence: 99%

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Wang¹,

Bao²,

Quan³

et al. 2012

IJN

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Background and methods:The aim of this study was to develop an immediate-release pellet formulation with improved drug dissolution and adsorption. Carbamazepine, a poorly watersoluble drug, was adsorbed into mesoporous silica (SBA-15-CBZ) via a wetness impregnation method and then processed by extrusion/spheronization into pellets. Physicochemical characterization of the preparation was carried out by scanning electron microscopy, transmission electron microscopy, nitrogen adsorption, small-angle and wide-angle x-ray diffraction, and differential scanning calorimetry. Flowability and wettability of the drug-loaded silica powder were evaluated by bulk and tapped density and by the angle of repose and contact angle, respectively. The drug-loaded silica powder was formulated into pellets to improve flowability. Results: With maximum drug loading in SBA-15 matrices determined to be 20% wt, in vitro release studies demonstrated that the carbamazepine dissolution rate was notably improved from both the SBA-15 powder and the corresponding pellets as compared with the bulk drug. Correspondingly, the oral bioavailability of SBA-15-CBZ pellets was increased considerably by 1.57-fold in dogs (P , 0.05) compared with fast-release commercial carbamazepine tablets. Conclusion: Immediate-release carbamazepine pellets prepared from drug-loaded silica provide a feasible approach for development of a rapidly acting oral formulation for this poorly water-soluble drug and with better absorption.

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Section: Introductionmentioning

confidence: 99%

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Wang¹,

Bao²,

Quan³

et al. 2012

IJN

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“…However, the crystallization process was inhibited by the small size of the pores. According to Vialpando et al 11 compared with the crystalline state, the amorphous drug is more soluble. Therefore, when the drug is loaded in MSNs, the drug solubility is significantly increased and the dissolution is also increased.…”

mentioning

confidence: 99%

Development of an oral push–pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles

Zhao¹,

Wu²,

Zhao³

et al. 2015

IJN

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In this study, mesoporous silica nanoparticles (MSNs) were used to prepare an oral push–pull osmotic pump. Fenofibrate, the selected model drug, was firstly loaded into the MSNs, followed by a suspending agent consisting of a drug layer of push–pull osmotic pump. Fenofibrate-loaded MSNs were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), nitrogen adsorption/desorption analysis, differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) analysis, and Fourier-transform infrared (FT-IR) spectroscopy. Polyethylene oxide of molecular weight (MW) 100,000 and polyethylene oxide of MW 6,000,000 were selected as the suspending agent and the expanding agent, respectively. Cellulose acetate was used as the semipermeable membrane, along with polyethylene glycol 6,000 to increase the flexibility and control the membrane permeability. The in vitro dissolution studies indicated that the osmotic pump tablet combined with MSNs was able to deliver fenofibrate in an approximately zero-order manner in 24 hours. A pharmacokinetic study showed that, although the maximum plasma concentration of the osmotic pump was lower than that of the reference formulation, the relative bioavailability was increased, indicating that the osmotic pump was more efficient than the reference tablets. Therefore, using MSNs as a carrier for poorly water-soluble drugs is an effective method for preparing osmotic pump tablets.

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“…It was in 2001 when SMMs were proposed for the first time as drug delivery systems [24]. Since then, SMMs have been widely reported as excellent matrices to load and locally release in a sustained fashion several kinds of drug molecules [25][26][27][28]30,32,33,[47][48][49]. Furthermore, SMMs present in vitro bioactive behaviour [16,50], since they are able to develop an apatite-like layer onto their surfaces when soaked into a simulated body fluid (SBF) [51].…”

Section: Bioactive Templated Glasses: a New Generation Of Nanostructumentioning

confidence: 99%

Structure and functionalization of mesoporous bioceramics for bone tissue regeneration and local drug delivery

Vallet‐Regí

Izquierdo‐Barba

Colilla

2012

Phil. Trans. R. Soc. A.

160

139

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This review article describes the importance of structure and functionalization in the performance of mesoporous silica bioceramics for bone tissue regeneration and local drug delivery purposes. Herein, we summarize the pivotal features of mesoporous bioactive glasses, also known as 'templated glasses' (TGs), which present chemical compositions similar to those of conventional bioactive sol-gel glasses and the added value of an ordered mesopore arrangement. An in-depth study concerning the possibility of tailoring the structural and textural characteristics of TGs at the nanometric scale and their influence on bioactive behaviour is discussed. The highly ordered mesoporous arrangement of cavities allows these materials to confine drugs to be subsequently released, acting as drug delivery devices. The functionalization of mesoporous silica walls has been revealed as the cornerstone in the performance of these materials as controlled release systems. The synergy between the improved bioactive behaviour and local sustained drug release capability of mesostructured materials makes them suitable to manufacture threedimensional macroporous scaffolds for bone tissue engineering. Finally, this review tackles the possibility of covalently grafting different osteoinductive agents to the scaffold surface that act as attracting signals for bone cells to promote the bone regeneration process.

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Evaluation of ordered mesoporous silica as a carrier for poorly soluble drugs: Influence of pressure on the structure and drug release

Cited by 66 publications

References 33 publications

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Development of an oral push–pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles

Structure and functionalization of mesoporous bioceramics for bone tissue regeneration and local drug delivery

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Evaluation of ordered mesoporous silica as a carrier for poorly soluble drugs: Influence of pressure on the structure and drug release

Cited by 66 publications

References 33 publications

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Development of an oral push&ndash;pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles

Structure and functionalization of mesoporous bioceramics for bone tissue regeneration and local drug delivery

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Development of an oral push–pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles