Poly (ε-caprolactone) nanocapsules for oral delivery of raloxifene: process optimization by hybrid design approach, in vitro and in vivo evaluation. (August 2014)

• Record Type: Journal Article
• Authors: Aditya, N.; Ravi, Punna Rao; Avula, Uday Sai Ranjan; Vats, Rahul
• Is Part Of: Journal of microencapsulation. Volume 31:Number 5(2014:Aug.)
• Page Start: 508
• Page End: 518
• Publication Date: 2014-08
• Subjects: Microencapsulation -- Periodicals; Controlled release technology -- Periodicals; 615.19
• DOI: 10.3109/02652048.2014.885603
• Languages: English
• ISSNs: 0265-2048

Abstract

<abstract> <title>Abstract</title> <p>Raloxifene HCl (RLX), a selective oestrogen receptor modulator, has low oral bioavailability (&lt;2%) in humans due to its poor aqueous solubility and extensive first-pass metabolism in gut. In this study, we optimised the method of preparation for poly (ε-caprolactone) (PCL) based nanocapsules of RLX by double emulsion method (w/o/w). A hybrid design approach, Plackett–Burman design followed by rotatable central composite design, was used to arrive at the optimised formulation. The optimised formulation was subjected to <italic>in vitro</italic> and <italic>in vivo</italic> evaluation. RLX loaded nanocapsules were spherical in shape with particle size less than 200 nm and high encapsulation efficiency (&gt;80%). RLX-loaded nanocapsules showed 2.1-fold increase in oral bioavailability compared to free RLX. IV pharmacokinetic studies indicated that RLX loaded into nanocapsule had significantly low clearance in comparison with free RLX. Designed nanocapsules showed promise as delivery systems to enhance oral bioavailability and in reducing clearance of raloxifene.</p> </abstract>