Abstract
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.
Funder
University Grants Commission
Subject
General Materials Science,General Chemical Engineering
Reference50 articles.
1. Prevention and management of osteoporosis;World Health Organ Tech. Rep. Ser.,2003
2. An Atlas of Osteoporosis: The Encyclopedia of Visual Medicine Series;Francis;J. R. Soc. Med.,1993
3. Assessment of Osteoporosis at the Primary Health Care Level;Kanis,2008
4. An estimate of the worldwide prevalence and disability associated with osteoporotic fractures
5. Selective estrogen receptor modulators: mechanism of action and clinical experience. Focus on raloxifene
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