Formulation and optimization of raloxifene-loaded solid lipid nanoparticles to enhance oral bioavailability.
The main aim of this study was to improve the oral bioavailability of raloxifene (RXF), a selective estrogen receptor modulator, by incorporation into solid lipid nanoparticles (SLN). RXF-loaded SLN was prepared by homogenization-sonication technique and characterized through physicochemical, pharmacokinetic, and cytotoxicity studies. The optimized SLN formulation exhibited a spherical shape with average size around 140 nm, easing its transport across the lymphatic system. Augmentation in the profiles of C(max) (308%) and AUC (270%) indicated a significant enhancement in the rate and extent of bioavailability by SLN formulations compared to free drug. In vitro cytotoxicity study performed in NIH-3T3 cells revealed that RXF-SLN was cytocompatible, and SLN remained unchanged during the freeze-drying process. Furthermore, the optimized formulation was quite stable at room temperature for more than two months, exemplifying its superior performance. In conclusion, SLN provides a promising platform for the pronounced enhancement of RXF bioavailability.
Tuan Hiep
TH
Tran
Thiruganesh
T
Ramasamy
Hyuk Jun
HJ
Cho
Yong Il
YI
Kim
Bijay Kumar
BK
Poudel
Han-Gon
HG
Choi
Chul Soon
CS
Yong
Jong Oh
JO
Kim
D000284:Administration, Oral; D000818:Animals; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods; D004965:Estrogen Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry*; D046911:Macromolecular Substances / Q000737:chemistry; D008297:Male; D008422:Materials Testing; D008657:Metabolic Clearance Rate; D008968:Molecular Conformation; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D020849:Raloxifene Hydrochloride / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013499:Surface Properties
D004965:Estrogen Antagonists; D008055:Lipids; D046911:Macromolecular Substances; D053769:Nanocapsules; D020849:Raloxifene Hydrochloride