Lipid nanoparticles for oral delivery of raloxifene: Optimization, stability, in vivo evaluation and uptake mechanism

被引：115
作者：
Ravi, Punna Rao [1 ]
Aditya, N. [1 ]
Kathuria, Himanshu [1 ]
Malekar, Srinivas [1 ]
Vats, Rahul [1 ]
机构：
[1] BITS Pilani Hyderabad Campus, Dept Pharm, Hyderabad, Andhra Pradesh, India
来源：
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2014年 / 87卷 / 01期
关键词：
Raloxifene HCl; Solid lipid nanoparticle; Box-Bhenken design; Design of experiments; Everted gut sac; Lymphatic transport; Glyceryl behenate; BIODEGRADABLE POLYMERIC MICROSPHERES; INTESTINAL LYMPHATIC TRANSPORT; FLOW BLOCKING APPROACH; DRUG-DELIVERY; PHARMACOKINETICS; BIOAVAILABILITY; ABSORPTION; RELEASE; RATS; GLUCURONIDATION;
D O I：
10.1016/j.ejpb.2013.12.015
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Raloxifene HCI (RLX) shows low oral bioavailability (<2%) in humans due to poor aqueous solubility and extensive (>90%) metabolism in gut. Lipid nanoparticles (SLN) with glyceryl tribehenate were designed to enhance drug's oral bioavailability. Box-Bhenken design was used to optimize manufacturing conditions. Optimized SLN had particle size of 167 +/- 3 nm and high encapsulation efficiency (>92%). Oral bioavailability of RLX from SLN was improved by 3.24 folds compared to free RLX in female Wistar rats. Both clathrin and caveolae mediated endocytosis pathways were involved in the uptake of SLN. Lymphatic transport inhibitor, cycloheximide significantly reduced oral bioavailability of SLN. (C) 2014 Elsevier B.V. All rights reserved.
引用
收藏
页码：114 / 124
页数：11
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