Abstract
BackgroundNanoparticles (NPs) play an important role in anticancer delivery systems. Surface modified NPs with hydrophilic polymers such as human serum albumin (HSA) have long half-life in the blood circulation system.MethodsThe method of modified nanoprecipitation was utilized for encapsulation of paclitaxel (PTX) in poly (lactic-co-glycolic acid) (PLGA). Para-maleimide benzoic hydrazide was conjugated to PLGA for the surface modifications of PLGA NPs, and then HSA was attached on the surface of prepared NPs by maleimide attachment to thiol groups (cysteines) of albumin. The application of HSA provides for the longer blood circulation of stealth NPs due to their escape from reticuloendothelial system (RES). Then the physicochemical properties of NPs like surface morphology, size, zeta potential, and in-vitro drug release were analyzed.ResultsThe particle size of NPs ranged from 170 to 190 nm and increased about 20–30 nm after HSA conjugation. The zeta potential was about -6 mV and it decreased further after HSA conjugation. The HSA conjugation in prepared NPs was proved by Fourier transform infrared (FT-IR) spectroscopy, faster degradation of HSA in Differential scanning calorimetry (DSC) characterization, and other evidences such as the increasing in size and the decreasing in zeta potential. The PTX released in a biphasic mode for all colloidal suspensions. A sustained release profile for approximately 33 days was detected after a burst effect of the loaded drug. The in vitro cytotoxicity evaluation also indicated that the HSA NPs are more cytotoxic than plain NPs.ConclusionsHSA decoration of PLGA NPs may be a suitable method for longer blood circulation of NPs.
Highlights
IntroductionSurface modified NPs with hydrophilic polymers such as human serum albumin (HSA) have long half-life in the blood circulation system
Nanoparticles (NPs) play an important role in anticancer delivery systems
Synthesis of polymer PLGA functionalized with maleimide group was synthesized and characterized. 1H-NMR and Fourier transform infrared (FT-IR) analysis was used for confirmation of the primary chemical structure of paramaleimido benzoic hydrazid (PMBH)–PLGA
Summary
Surface modified NPs with hydrophilic polymers such as human serum albumin (HSA) have long half-life in the blood circulation system. The interest on utilizing NPs formulated from biodegradable and biocompatible polymers such as the most commonly used PLGA are rising rapidly [6] These NPs are broadly studied as anticancer delivery systems since it has special characteristics such as controlled release and biocompatibility [6]. A new approach to evade the short half-life of the conventional drug and allow targeted delivery to tumor cells is drug targeting achieved by size engineering and surface modification [7,8]. Surface modification of particles with hydrophilic polymers like polyethylene glycol (PEG) and albumin leading to the development of long-circulating and stealth particles for delivery of anticancer drugs [13,14]. The NPs mount up in the interstitium which retards their uptake (EPR effect), unless those particles are degraded [16,17]
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