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Enhanced Solubility, Oral Bioavailability and Anti-Osteoporotic Effects of Raloxifene Hcl in Ovariectomized Rats by Igepal Co-890 Nanomicelles Publisher Pubmed



Varshosaz J1 ; Ziaei V1 ; Minaiyan M2 ; Jahaniannajafabadi A3 ; Sayedtabatabaei L4
Authors
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Authors Affiliations
  1. 1. Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Research Center, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Department of Pharmacology, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  3. 3. Department of Pharmaceutical Biotechnology, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  4. 4. Pharmacy Students’ Research Committee, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Pharmaceutical Development and Technology Published:2019


Abstract

The purpose of the present study was to enhance the bioavailability and anti-osteoporotic effects of raloxifene HCl (RH) by increasing its solubility and inhibition of the p-glycoprotein pump using surfactant micelles of Igepal CO-890. The micelles were prepared by the direct method and their critical micellar concentration, drug dissolution rate, saturated solubility, drug loading and surface morphology were defined. The cytotoxicity of Igepal CO-890 and its ability to inhibit the p-glycoprotein pump were studied on Caco-2 cells. The pharmacokinetic parameters were analyzed by oral administration of a single dose of 15 mg/kg in Wistar rats. Anti-osteoporotic effects were studied by measuring the calcium, phosphorous, and uterus weight of rats after one month of oral administration of 6 mg/kg/day of RH in ovariectomized rats. Igepal CO-890 micelles enhanced the RH solubility by about two-fold. The FT-IR and DSC studies indicated no interaction between the drug and the surfactant. XRD spectrum showed an amorphous state of RH in the micelles. The p-glycoprotein pump was inhibited by Igepal CO-890 in Caco-2 cells comparable to verapamil. Micelles increased the uterine weight and decreased the serum calcium and phosphorus significantly compared to the untreated drug. Oral bioavailability of RH increased about four-fold by nanomicelles. © 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.
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