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

Zhao Z, Wu C, Zhao Y, Hao Y, Liu Y, Zhao W - Int J Nanomedicine (2015)

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Pharmacy School, Liaoning Medical University, Jinzhou, Liaoning Province, People's Republic of China.

ABSTRACT
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.

No MeSH data available.


DSC thermograms.Notes: The thermograms are shown for pure crystalline FF (a), the physical mixture of FF and the MSNs (b), and different ratio FF-MSNs: 1:1 (c), 1:2 (d), and 1:3 (e).Abbreviations: DSC, differential scanning calorimetry; FF, fenofibrate; FF-MSN, fenofibrate-loaded mesoporous silica nanoparticle; MSN, mesoporous silica nanoparticle.
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f3-ijn-10-1691: DSC thermograms.Notes: The thermograms are shown for pure crystalline FF (a), the physical mixture of FF and the MSNs (b), and different ratio FF-MSNs: 1:1 (c), 1:2 (d), and 1:3 (e).Abbreviations: DSC, differential scanning calorimetry; FF, fenofibrate; FF-MSN, fenofibrate-loaded mesoporous silica nanoparticle; MSN, mesoporous silica nanoparticle.

Mentions: The crystal properties were examined using DSC. Figure 3 shows the DSC thermograms of pure FF, physical mixtures of FF and MSNs, and different ratio FF-MSNs. A single sharp endothermic melting peak at 84.0°C was observed for both pure FF and physical mixtures of FF and MSNs; however, the FF endothermic peak disappeared completely at ratios of 1:2 and 1:3, indicating that FF existed in an amorphous state. However, when the ratio was 1:1, an FF endothermic peak was present, perhaps because the low percentage of the carrier resulted in incomplete loading of the drug into the pores, and a portion of the drug was attached to the surface of the MSNs.


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

Zhao Z, Wu C, Zhao Y, Hao Y, Liu Y, Zhao W - Int J Nanomedicine (2015)

DSC thermograms.Notes: The thermograms are shown for pure crystalline FF (a), the physical mixture of FF and the MSNs (b), and different ratio FF-MSNs: 1:1 (c), 1:2 (d), and 1:3 (e).Abbreviations: DSC, differential scanning calorimetry; FF, fenofibrate; FF-MSN, fenofibrate-loaded mesoporous silica nanoparticle; MSN, mesoporous silica nanoparticle.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4356664&req=5

f3-ijn-10-1691: DSC thermograms.Notes: The thermograms are shown for pure crystalline FF (a), the physical mixture of FF and the MSNs (b), and different ratio FF-MSNs: 1:1 (c), 1:2 (d), and 1:3 (e).Abbreviations: DSC, differential scanning calorimetry; FF, fenofibrate; FF-MSN, fenofibrate-loaded mesoporous silica nanoparticle; MSN, mesoporous silica nanoparticle.
Mentions: The crystal properties were examined using DSC. Figure 3 shows the DSC thermograms of pure FF, physical mixtures of FF and MSNs, and different ratio FF-MSNs. A single sharp endothermic melting peak at 84.0°C was observed for both pure FF and physical mixtures of FF and MSNs; however, the FF endothermic peak disappeared completely at ratios of 1:2 and 1:3, indicating that FF existed in an amorphous state. However, when the ratio was 1:1, an FF endothermic peak was present, perhaps because the low percentage of the carrier resulted in incomplete loading of the drug into the pores, and a portion of the drug was attached to the surface of the MSNs.

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Pharmacy School, Liaoning Medical University, Jinzhou, Liaoning Province, People's Republic of China.

ABSTRACT
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.

No MeSH data available.