title: Design of a gelatin microparticle-containing self-microemulsifying formulation for enhanced oral bioavailability of dutasteride.
abstract: In this study, a gelatin microparticle-containing self-microemulsifying formulation (SMF) was developed using a spray-drying method to enhance the oral delivery of the poorly water-soluble therapeutic dutasteride. The effect of the amount of gelatin and the type and amount of hydrophilic additives, namely, Gelucire(®) 44/14, poloxamer 407, sodium lauryl sulfate, Soluplus(®), Solutol™ HS15, and D-α-tocopheryl polyethylene glycol 1000 succinate, on the droplet size, dissolution, and oral absorption of dutasteride from the SMF was investigated. Upon dispersion of the gelatin microparticle-containing SMF in water after spray-drying, the mean droplet size of the aqueous dispersion was in the range of 110-137 nm. The in vitro dissolution and recrystallization results showed that gelatin could be used as a solid carrier and recrystallization inhibitor for the SMF of dutasteride. Furthermore, combination of the gelatin microparticle-containing SMF and Soluplus enhanced the dissolution properties and oral absorption of dutasteride. The results of our study suggest that the gelatin microparticle-containing SMF in combination with Soluplus could be useful to enhance the oral absorption of dutasteride.
authors.affiliation: College of Pharmacy, Kyungsung University, Busan, Republic of Korea.
authors.forename: In-hwan
authors.initials: IH
authors.lastname: Baek
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Eun-Sol
authors.initials: ES
authors.lastname: Ha
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Jin-Wook
authors.initials: JW
authors.lastname: Yoo
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Yunjin
authors.initials: Y
authors.lastname: Jung
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
mesh_terms: D058891:5-alpha Reductase Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D000068538:Dutasteride / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D004655:Emulsions; D005079:Excipients / Q000737:chemistry; D005780:Gelatin / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D058891:5-alpha Reductase Inhibitors; D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D011145:Polyvinyls; C572167:polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; D011092:Polyethylene Glycols; D005780:Gelatin; D000068538:Dutasteride
keywords: bioavailability; dissolution; dutasteride; solubility