Oral Bioavailability Enhancement of Raloxifene with Nanostructured Lipid Carriers

Nanomaterials

Punna Rao Ravi¹  Shrinivas Malekar¹  Himanshu Kathuria¹  Aditya Murthy² 

[1] Department of Pharmacy, BITS-Pilani Hyderabad Campus, Hyderabad 500078, Telangana, India;Differentiated Formulations, Strides Pharma Science Ltd., R & D Centre, J.P. Nagar 2nd Phase, Bangalore 560083, Karnataka, India;

关键词: solid lipid nanoparticle;    nanostructured lipid carriers;    bioavailability;    glyceryl behenate;    raloxifene;    osteoporosis;   

DOI  :  10.3390/nano10061085

来源: DOAJ

【 摘 要 】

Raloxifene hydrochloride (RLX) shows poor bioavailability (<2%), high inter-patient variability and extensive gut metabolism (>90%). The objective of this study was to develop nanostructured lipid carriers (NLCs) for RLX to enhance its bioavailability. The NLC formulations were produced with glyceryl tribehenate and oleic acid. The particle characteristics, entrapment efficiency (EE), differential scanning calorimetry (DSC), in vitro drug release, oral bioavailability (in rats) and stability studies were performed. The optimized nanoparticles were 120 ± 3 nm in size with positive zeta potential (14.4 ± 0.5 mV); % EE was over 90% with the drug loading of 5%. The RLX exists in an amorphous form in the lipid matrix. The optimized RLX-NLC formulation showed sustained release in vitro. The RLX-NLC significantly (p < 0.05) enhanced oral bioavailability 3.19-fold as compared to RLX-free suspension in female Wistar rats. The RLX-NLC can potentially enhance the oral bioavailability of RLX. It can also improve the storage stability.

【 授权许可】

Unknown