Inderscience Publishers

Improving drug loading efficiency and delivery performance of micro– and nanoparticle preparations through optimising formulation variables

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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

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