Title: Formulation, characterisation and comparison of different raloxifene hydrochloride loaded lipid-polymer hybrid nanoparticles

Authors: Syed Mahmood; Tan Cheh Phey; Lee Seow Kheng; Kee Poh Chen; Uttam Kumar Mandal

Addresses: Department of Pharmaceutical Engineering, Faculty of Chemical and Process Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia ' Department of Pharmaceutical Engineering, Faculty of Chemical and Process Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia ' Department of Pharmaceutical Engineering, Faculty of Chemical and Process Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia ' Department of Pharmaceutical Engineering, Faculty of Chemical and Process Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia ' Department of Pharmaceutical Sciences and Technology, Maharaja Ranjit Singh Punjab Technical University (MRSPTU), Bathinda 151001, India

Abstract: This study aims to formulate raloxifene loaded lipid-polymeric hybrid nanoparticles (LPHNPs) and the comparison of their properties. Three LPHNPs, each with phosphatidylcholine-lipid (PCL) as bilayer-forming-membrane with three different polymers like sodium alginate, chitosan and poly(lactic-co-glycolic-acid) were prepared by nanoprecipitation, solvent injection and emulsion solvent evaporation, respectively. Results showed that the prepared formulations were spherical-shaped with a heterogeneity. Surface morphology was viewed using a scanning electron microscopy (SEM). A high entrapment efficiency (>70%) with a sustained and pH dependent drug release profile for 24 h was observed and evaluated using mathematical kinetic modelling. Fourier transform infrared spectroscopy was used to confirm successful entrapment of raloxifene after evaluating the interaction and compatibility of the excipients used. Whereas, differential scanning calorimetry and X-ray diffraction revealed the transformation of raloxifene into an amorphous form. In conclusion, these hybrid nanoparticles provide a promising approach for oral delivery of raloxifene.

Keywords: raloxifene; lipid-polymeric hybrid nanoparticle; LPHNP; release study; pharmacokinetic release modelling.

DOI: 10.1504/IJNBM.2020.112224

International Journal of Nano and Biomaterials, 2020 Vol.9 No.3/4, pp.123 - 141

Received: 06 Dec 2019
Accepted: 06 May 2020

Published online: 05 Jan 2021 *

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