Synthesis of the Cholesteryl Ester Prodrugs Cholesteryl Ibuprofen and Cholesteryl Flufenamate and their Formulation into Phospholipid Microemulsions

Murtha, John L.; Ando, Howard Y.

doi:10.1002/jps.2600830907

Cited by 36 publications

(16 citation statements)

References 22 publications

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“…As a result, the sustained and controlled release preparations of ibuprofen are developed widely, which includes extended-action tablets, modified-release capsules, delayed-release pellets, and sustained-release microspheres. [5][6][7][8][9] A modified release-capsule has long been on the market.…”

Section: Introductionmentioning

confidence: 99%

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Dian¹,

Yang²,

Li³

et al. 2013

IJN

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Abstract:In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P , 0.05). The ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment.

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Section: Introductionmentioning

confidence: 99%

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Dian¹,

Yang²,

Li³

et al. 2013

IJN

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“…Dissolution thus becomes the rate limiting step for absorption, and the quick release of ibuprofen in the gastrointestinal tract following oral administration is desirable. 1) Various formulations such as prodrugs, 2) inclusion complexes, 3) microcapsules, 4) etc. of ibuprofen were developed.…”

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confidence: 99%

Enhancement of Solubility, Dissolution and Bioavailability of Ibuprofen in Solid Dispersion Systems

et al. 2008

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To improve its solubility, dissolution, and bioavailability; Ibuprofen-polyethylene glycol 8000 (PEG 8000) solid dispersions (SDs) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for solubility, in-vitro release, and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C max , and a significant decrease in T max over pure ibuprofen. Preliminary results of this study suggested that the preparation of ibuprofen SDs using PEG 8000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution and bioavailability of ibuprofen.

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“…Dissolution thus becomes the rate-limiting step for absorption, and the quick release of ibuprofen in the gastrointestinal tract following oral administration is desirable (Laska et al 1986). Various formulations such as prodrugs (Murtha and Ando 1994), inclusion complexes (Ghorab and Adeyeye 2001), and microcapsules (Adeyeye and Price 1994), of ibuprofen were developed. However, the dissolution rate and the oral bioavailability of ibuprofen from these formulations differed widely; methods were time; consuming and costly; and some formulations were bulky with poor flow characteristics and handling difficulties.…”

mentioning

confidence: 99%

Preparation and Evaluation of Fast Dissolving Ibuprofen-Polyethylene Glycol 6000 Solid Dispersions

Newa¹,

Bhandari²,

Kim³

et al. 2008

Drug Delivery

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Synthesis of the Cholesteryl Ester Prodrugs Cholesteryl Ibuprofen and Cholesteryl Flufenamate and their Formulation into Phospholipid Microemulsions

Cited by 36 publications

References 22 publications

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Enhancement of Solubility, Dissolution and Bioavailability of Ibuprofen in Solid Dispersion Systems

Preparation and Evaluation of Fast Dissolving Ibuprofen-Polyethylene Glycol 6000 Solid Dispersions

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