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Development Of Megestrol Acetate Solid Dispersion Nanoparticles For Enhanced Oral Delivery By Using A Supercritical Antisolvent Process

Eun-sol Ha, J. Kim, I. Baek, Jin-Wook Yoo, Yunjin Jung, H. Moon, M. Kim
Published 2015 · Materials Science, Medicine

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In the present study, solid dispersion nanoparticles with a hydrophilic polymer and surfactant were developed using the supercritical antisolvent (SAS) process to improve the dissolution and oral absorption of megestrol acetate. The physicochemical properties of the megestrol acetate solid dispersion nanoparticles were characterized using scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction, and a particle-size analyzer. The dissolution and oral bioavailability of the nanoparticles were also evaluated in rats. The mean particle size of all solid dispersion nanoparticles that were prepared was <500 nm. Powder X-ray diffraction and differential scanning calorimetry measurements showed that megestrol acetate was present in an amorphous or molecular dispersion state within the solid dispersion nanoparticles. Hydroxypropylmethyl cellulose (HPMC) solid dispersion nanoparticles significantly increased the maximum dissolution when compared with polyvinylpyrrolidone K30 solid dispersion nanoparticles. The extent and rate of dissolution of megestrol acetate increased after the addition of a surfactant into the HPMC solid dispersion nanoparticles. The most effective surfactant was Ryoto sugar ester L1695, followed by D-α-tocopheryl polyethylene glycol 1000 succinate. In this study, the solid dispersion nanoparticles with a drug:HPMC:Ryoto sugar ester L1695 ratio of 1:2:1 showed >95% rapid dissolution within 30 minutes, in addition to good oral bioavailability, with approximately 4.0- and 5.5-fold higher area under the curve (0–24 hours) and maximum concentration, respectively, than raw megestrol acetate powder. These results suggest that the preparation of megestrol acetate solid dispersion nanoparticles using the supercritical antisolvent process is a promising approach to improve the dissolution and absorption properties of megestrol acetate.
This paper references
Improved oral absorption of dutasteride via Soluplus®-based supersaturable self-emulsifying drug delivery system (S-SEDDS).
D. Lee (2015)
Dissolution and oral absorption of pranlukast nanosuspensions stabilized by hydroxypropylmethyl cellulose.
I. Baek (2014)
Solid dispersion formulations of megestrol acetate with copovidone for enhanced dissolution and oral bioavailability
Soon Wook Hong (2011)
Effect of compaction pressure on the dissolution efficiency of some direct compression systems.
K. A. Khan (1972)
A comparative evaluation between utilizing SAS supercritical fluid technique and solvent evaporation method in preparation of Azithromycin solid dispersions for dissolution rate enhancement
E. Adeli (2014)
Characterization of Nanoparticles for Drug Delivery Applications
Z. Deng (2005)
Improvement in Quality‐of‐Life Measures and Stimulation of Weight Gain After Treatment with Megestrol Acetate Oral Suspension in Geriatric Cachexia: Results of a Double‐Blind, Placebo‐Controlled Study
Shing‐shing Yeh (2000)
Development and Therapy downloaded from by on 03-Apr-2017 For personal use only
Enhanced bioavailability of sirolimus via preparation of solid dispersion nanoparticles using a supercritical antisolvent process
M. Kim (2011)
Fabrication and evaluation of valsartan–polymer– surfactant composite nanoparticles by using the supercritical antisolvent process
M. Kim (2014)
Effect of physiochemical variables on phase solubility and dissolution behavior of indomethacin solid dispersion system
Mohanraj Palanisamy (2013)
Encapsulation and co-precipitation processes with supercritical fluids: Fundamentals and applications
M. J. Cocero (2009)
Encapsulation and coprecipitation processes with supercritical fluids: fundamentals and applications
Mj Cocero (2009)
Rapid and sensitive LC-MS/MS method for determination of megestrol acetate in human plasma: application to a human pharmacokinetic study.
Ji-Hyung Seo (2013)
Palliative treatment of cancer anorexia with oral suspension of megestrol acetate.
M. Tomíška (2003)
Nanonization of megestrol acetate by laser fragmentation in aqueous milieu.
Jean-Philippe Sylvestre (2011)
Improvement in quality-of-life measures and stimulation of weight gain after treatment with megestrol acetate oral suspension in geriatric cachexia: results of a double-blind, placebocontrolled study
Ss Yeh (2000)
Nanonization of Megestrol Acetate by Liquid Precipitation
Zhibing zhang (2009)
Preparation and evaluation of solid dispersion of atorvastatin calcium with Soluplus® by spray drying technique.
Eun-sol Ha (2014)
Soluplus®/TPGS-based solid dispersions prepared by hot-melt extrusion equipped with twin-screw systems for enhancing oral bioavailability of valsartan
J. Lee (2015)
Development and Therapy downloaded from by on 31-Mar-2017 For personal use only
Supersaturatable formulations for the enhanced oral absorption of sirolimus.
M. Kim (2013)
Drug Des Devel Ther
Nanocrystal technology, drug delivery and clinical applications
Jens-Uwe A. H. Junghanns (2008)
Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs
X. Yin (2015)
Nanoparticles of Poorly Water-Soluble Drugs Prepared by Supercritical Fluid Extraction of Emulsions
B. Shekunov (2005)
Combining in vitro and in silico methods for better prediction of surfactant effects on the absorption of poorly water soluble drugs-a fenofibrate case example.
R. Berthelsen (2014)
Influence of hydrophilic additives on the supersaturation and bioavailability of dutasteride-loaded hydroxypropyl-β-cyclodextrin nanostructures
M. Kim (2013)
Dissolution and bioavailability of lercanidipine-hydroxypropylmethyl cellulose nanoparticles with surfactant.
Eun-sol Ha (2015)
Formulation, Characterization, and in Vivo Evaluation of Celecoxib-PVP Solid Dispersion Nanoparticles Using Supercritical Antisolvent Process
Eun-sol Ha (2014)
Novel nanocrystal formulation of megestrol acetate has improved bioavailability compared with the conventional micronized formulation in the fasting state
K. Jang (2014)
Micellization and solubilization behavior of sucrose laurate, a new pharmaceutical excipient.
P. C. Lerk (1996)
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Figure 7 Correlation between in vitro dissolution efficiency and in vivo pharmacokinetic parameters. Notes: (A) aUc; (B) c max . Abbreviations: aUc, area under the concentration-time curve; c max
Enhanced bioavailability and anthelmintic efficacy of mebendazole in redispersible microparticles with low-substituted hydroxypropylcellulose
P. M. de la Torre-Iglesias (2014)
Enhanced dissolution of megestrol acetate microcrystals prepared by antisolvent precipitation process using hydrophilic additives.
Eunbi Cho (2010)

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Supercritical Antisolvent Process for Pharmaceutical Applications: A Review
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