Title: Improving drug loading efficiency and delivery performance of micro- and nanoparticle preparations through optimising formulation variables

Authors: Chiao-Hsi Chiang; Hossein Hosseinkhani; Wen-Sheng Cheng; Cheng-Wei Chen; Chun-Hsiang Wang; Yi-Lei Lo

Addresses: School of Pharmacy, National Defense Medical Center, Taipei, Taiwan ' School of Pharmacy, National Defense Medical Center, Taipei, Taiwan; Graduate Institute of Biomedical Engineering, National Taiwan University of Science and Technology (Taiwan Tech), Taipei 10607, Taiwan ' School of Pharmacy, National Defense Medical Center, Taipei, Taiwan; Graduate Institute of Medical Sciences, National Defense Medical Center, Taipei, Taiwan ' ChenWei Biotechnology Co., Ltd., Taipei, Taiwan ' Weal-Chance Trading Co., Ltd., Taipei, Taiwan ' Division of Clinical Pharmacy, Sijhih Cathay General Hospital, New Taipei City, Taiwan

Abstract: In this report, we briefly introduce our recent studies related to drug delivery systems using biodegradable materials, PLGA, PLA or chitosan to prepare submicroparticles or microparticles for carrying vaccine, protein or small molecule drugs. These preparations were prepared by spray dried or solvent extraction methods. In addition, liposomal formulations containing various lipids and pegylated lipids were also investigated. Gene-loaded liposomal preparations were prepared and evaluated in ARPE19 (retinal pigment epithelium cell). These preparations were significantly internalised by ARPE19 and confirmed by confocal microscopy. Pegylated lipid linked with RGD peptide was synthesised for preparing siRNA delivery systems; these delivery systems could significantly enhance gene delivery and reduce the VEGF expression of ARPE19 for achieving anti-angiogenic effects. Another, poorly soluble compound was loaded in liposomal preparation which was further investigated in A549 (non-small cell lung cancer cell line). The preparation had higher cellular uptake to improve anti-cancer activity. Pegylated lipid with conjugated-ligand plays an important role to achieve efficient drug delivery. The strategy in preparing conjugated-ligand liposomal formulations can be a potential application for targeting delivery in cancer therapy or specific delivery to achieve therapeutic effects.

Keywords: drug delivery systems; chitosan; PLGA; PLA microparticles; pegylated liposomes; siRNA; vaccines; drug loading efficiency; nanoparticles; formulation variables; nanotechnology; biodegradable materials; gene delivery; cancer treatment; cancer therapy.

DOI: 10.1504/IJNT.2013.058125

International Journal of Nanotechnology, 2013 Vol.10 No.10/11, pp.996 - 1006

Available online: 08 Dec 2013 *

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