Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica

Speybroeck, Michiel Van; Mellaerts, Randy; Mols, Raf; Thi, Thao Do; Martens, Johan A.; Humbeeck, Jan Van; Annaert, Pieter; Mooter, Guy Van den; Augustijns, Patrick

doi:10.1016/j.ejps.2010.09.002

Cited by 184 publications

(98 citation statements)

References 36 publications

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“…13,14 That is because the angle of repose of drug-loaded silica powder is often more than 40 degrees, indicating poor flowability and leading to difficulty in packing the powder into capsules. Some researchers have put drug-loaded silica directly into capsules regardless of its poor flowability, 15 although Mellaerts et al 16 mixed drug-loaded silica with excipients to improve the flowability for capsule packing. 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.…”

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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“…They were originally developed for controlled drug release formulations (67)(68)(69) and their capability to enhance the release of poorly soluble drugs was discovered later (56,70,71). In recent studies, it was observed (72, 73) that drugs lose crystallinity when deposited on the surface of mesoporous silicates, which enhances their dissolution rate.…”

Section: Excipients For Liquisolid Systemsmentioning

confidence: 99%

“…In recent studies, it was observed (72, 73) that drugs lose crystallinity when deposited on the surface of mesoporous silicates, which enhances their dissolution rate. In comparison with non-porous materials, deposited molecules are not only absorbed onto the mesoporous silica surface but are also confined to pores (56).…”

Section: Excipients For Liquisolid Systemsmentioning

confidence: 99%

Liquisolid systems and aspects influencing their research and development

Vraníková¹,

Gajdziok²

2013

Acta Pharmaceutica

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“…A study was reported by Augustijns et al (25) on the relationship among the drug release rate, the rate of achieving supersaturation, and corresponding biopharmaceutical performance from mesoporous formulations of fenofibrate. As shown in Fig.…”

Section: In Vivo Study In Animal Modelsmentioning

confidence: 99%

Characterization of Supersaturatable Formulations for Improved Absorption of Poorly Soluble Drugs

Gao

Shi

2012

AAPS J

125

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Abstract. With the increasing number of poorly water-soluble compounds in contemporary drug discovery pipelines, the concept of supersaturation as an effective formulation approach for enhancing bioavailability is gaining momentum. This is intended to design the formulation to yield significantly high intraluminal concentrations of the drug than the thermodynamic equilibrium solubility through achieving supersaturation and thus to enhance the intestinal absorption. The major challenges faced by scientists developing supersaturatable formulations include controlling the rate and degree of supersaturation with the application of polymeric precipitation inhibitor and maintenance of post-administration supersaturation. This review is intended to cover publications on this topic since April 2009. Scientific publications associated with characterization of supersaturatable systems and related preclinical and clinical pharmacokinetics (PK) studies are reviewed. Specifically, this review will address issues related to assessing the performance of supersaturatable systems including: (1) Diversified approaches for developing supersaturatable formulations, (2) meaningful in vitro test methods to evaluate supersaturatable formulations, and (3) in vivo PK study cases which have demonstrated direct relevance between the supersaturation state and the exposure observed in animal models and human subjects.

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Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica

Cited by 184 publications

References 36 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

Liquisolid systems and aspects influencing their research and development

Characterization of Supersaturatable Formulations for Improved Absorption of Poorly Soluble Drugs

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