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Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process.
Drug Des Devel Ther. 2015; 9:4269-77.DD

Abstract

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.

Authors+Show Affiliations

College of Pharmacy, Pusan National University, Yongin, South Korea.Dong-A ST Co Ltd, Yongin, South Korea.College of Pharmacy, Kyungsung University, Busan, South Korea.College of Pharmacy, Pusan National University, Yongin, South Korea.College of Pharmacy, Pusan National University, Yongin, South Korea.College of Pharmacy, Pusan National University, Yongin, South Korea.College of Pharmacy, Pusan National University, Yongin, South Korea.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26345723

Citation

Ha, Eun-Sol, et al. "Development of Megestrol Acetate Solid Dispersion Nanoparticles for Enhanced Oral Delivery By Using a Supercritical Antisolvent Process." Drug Design, Development and Therapy, vol. 9, 2015, pp. 4269-77.
Ha ES, Kim JS, Baek IH, et al. Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process. Drug Des Devel Ther. 2015;9:4269-77.
Ha, E. S., Kim, J. S., Baek, I. H., Yoo, J. W., Jung, Y., Moon, H. R., & Kim, M. S. (2015). Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process. Drug Design, Development and Therapy, 9, 4269-77. https://doi.org/10.2147/DDDT.S90706
Ha ES, et al. Development of Megestrol Acetate Solid Dispersion Nanoparticles for Enhanced Oral Delivery By Using a Supercritical Antisolvent Process. Drug Des Devel Ther. 2015;9:4269-77. PubMed PMID: 26345723.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process. AU - Ha,Eun-Sol, AU - Kim,Jeong-Soo, AU - Baek,In-Hwan, AU - Yoo,Jin-Wook, AU - Jung,Yunjin, AU - Moon,Hyung Ryong, AU - Kim,Min-Soo, Y1 - 2015/08/04/ PY - 2015/9/9/entrez PY - 2015/9/9/pubmed PY - 2016/6/4/medline KW - bioavailability KW - dissolution KW - megestrol acetate KW - supercritical technology SP - 4269 EP - 77 JF - Drug design, development and therapy JO - Drug Des Devel Ther VL - 9 N2 - 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. SN - 1177-8881 UR - https://www.unboundmedicine.com/medline/citation/26345723/Development_of_megestrol_acetate_solid_dispersion_nanoparticles_for_enhanced_oral_delivery_by_using_a_supercritical_antisolvent_process_ L2 - https://dx.doi.org/10.2147/DDDT.S90706 DB - PRIME DP - Unbound Medicine ER -