Multifunctional Poly Research Articles

Multifunctional poly(aspartic acid) nanoparticles containing iron oxide nanocrystals and doxorubicin for simultaneous cancer diagnosis and therapy

Multifunctional poly(aspartic acid) nanoparticles for simultaneous cancer diagnosis and therapy were developed. First, iron oxide nanocrystals were loaded in poly(aspartic acid) nanoparticles through an emulsion method using octadecyl grafted poly(aspartic acid). The influence of the organic solvent, used to disperse the hydrophobic iron oxide nanocrystals, on the size and loading efficiency of iron oxide nanocrystals loaded poly(aspartic acid) nanoparticles was investigated. Next, an anticancer drug, doxorubicin (DOX), was incorporated in the magnetic poly(aspartic acid) nanoparticles (MPAN). The presence of iron oxide nanocrystals in the poly(aspartic acid) nanoparticles and their size distribution were confirmed by transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), and dynamic light scattering (DLS), respectively. The drug release behavior was also observed for 3 days. From the results of T 2 weighted MR imaging and MTT assays, the DOX loaded MPAN showed high T 2 relaxivity coefficients and high cytotoxicity for cancer cells.

Synthesis, characterization and properties of multifunctional poly(arylene ether nitriles) (PEN)/CNTs/Fe3O4 nanocomposites

AbstractIn this study, a novel multifunctional poly(arylene ether nitriles)(PEN)/carbon nanotubes/Fe3O4 nanocomposite with high tensile strength, magnetic, and electrical properties was investigated. First, we synthesized the monodisperse Fe3O4 nanoparticles on the surface of the multiwalled carbon nanotubes and then the hybrid material was compounded with PEN through the solution‐casting method. The SEM and TEM images indicated that the monodisperse Fe3O4 nanoparticles, with the diameters of 70∼80 nm, were self‐assembled along CNTs via the covalent bond method, which was confirmed by FTIR and XRD. The results of tensile properties showed that the tensile strength and modulus reached their highest values at the CNTs/Fe3O4 loading content of 1 wt % and both were greatly enhanced after heat treatment. Electrical conductivity of the polymer was dramatically enhanced at the low loading level of CNTs/Fe3O4; the electrical percolation of was in the range of 5∼8 wt % of CNTs/Fe3O4. The magnetic study showed that the saturation magnetization (Ms) of PEN/CNTs/Fe3O4 nanocomposites increased with the increase of CNTs/Fe3O4 loading content, and the coercive force (Hc) of the nanocomposite was independent of the CNTs/Fe3O4 content. © 2011 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys, 2011

Encapsulation of 2-methoxyestradiol within multifunctional poly(amidoamine) dendrimers for targeted cancer therapy

We report here a general approach to using multifunctional poly(amidoamine) (PAMAM) dendrimer-based platform to encapsulate a potential anticancer drug for targeted cancer therapy. In this approach, amine-terminated generation 5 (G5) PAMAM dendrimers were sequentially modified with fluorescein isothiocyanate (FI) and folic acid (FA) via covalent conjugation, followed by an acetylation reaction to neutralize the remaining amines of the dendrimer surfaces. The synthesized multifunctional dendrimers (G5.NHAc-FI-FA) were then used to complex a potential anticancer drug, 2-methoxyestradiol (2-ME) for targeted delivery of the drugs to cancer cells overexpressing high-affinity folic acid receptors (FAR). We show that the formed G5.NHAc-FI-FA/2-ME complexes with each dendrimer encapsulating approximately 3.7 2-ME molecules are water soluble and stable. In vitro release studies show that 2-ME complexed with the multifunctional dendrimers can be released in a sustained manner. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay in conjunction with cell morphology observation demonstrates that the G5.NHAc-FI-FA/2-ME complexes can specifically target and display specific therapeutic efficacy to cancer cells overexpressing high-affinity FAR. Findings from this study suggest that multifunctional dendrimers may be used as a general drug carrier to encapsulate various cancer drugs for targeted therapy of different types of cancer.

Multifunctional poly(alkyl methacrylate) films for dental care

Towards the evaluation of non-permanent dental coatings for their capacity to impart dental-care benefits, thin films of a homologous series of comb-like poly(alkyl methacrylate)s (ethyl to octadecyl) have been deposited, from aqueous latex formulations, onto dentally relevant substrates. AFM studies have shown that the thickness (40–300 nm) and surface roughness (8–12 nm) of coherent polymer films are influenced by the degree of polymerization and by the length of the pendant chain. Of the polymers under consideration, poly(butyl methacrylate) formed a close-packed film that conferred to dental substrates a high degree of inhibition to acid-mediated erosion (about 27%), as evaluated by released-phosphate determinations. The potential utility of the coatings to act as anti-sensitivity barriers has been evaluated by determining the hydraulic conductance of coated bovine-dentine substrates; single treatments of dentine discs with poly(butyl methacrylate) or with poly(ethyl methacrylate) effected mean respective reductions in fluid flow of about 23% with respect to water-treated controls; repeated applications of the poly(butyl methacrylate) latex led to mean reductions in fluid flow of about 80%. Chromometric measurements have shown that pellicle-coated hydroxyapatite discs treated with poly(butyl methacrylate), poly(hexyl methacrylate) or poly(lauryl methacrylate) exhibit significant resistance to staining by food chromogens.

Liquid crystalline PEDOT derivatives exhibiting reversible anisotropic electrochromism and linearly and circularly polarized dichroism

The multifunctional poly(3,4-ethylenedioxythiophene) [PEDOT] derivatives that exhibit liquid crystallinity, reversible anisotropic electrochromism, and linearly and circularly polarized dichroism are developed. A series of copolymer-type liquid-crystalline PEDOT (LC PEDOT) derivatives are synthesized and evaluated in terms of optical and electrochromic properties. Two of the polymers are monosubstituted LC PEDOT derivatives with phenylcyclohexyl (PCH) or cyanobiphenyl (CB) mesogenic side chain moieties linked to the main chain via an ester bond. Four are disubstituted polymers bearing PCH or CB side chain moieties linked to the main chain via an ester or an ether bond. All of the polymers showed thermotropically nematic LC (N-LC) phases of an enantiotropic nature. Macroscopically aligned LC PEDOT derivatives were prepared by rubbing the polymer films in their N-LC phases, yielding linearly polarized fluorescence and anisotropic electrochromism. The morphologies of the polymer films reversibly changed between the neutral and oxidized states through electrochemical dedoping and doping procedures. The electrochromism between the neutral and oxidized states occurred in the parallel and perpendicular directions of the aligned polymer film, affording a novel anisotropic electrochromism. The chiral nematic LC (N*-LC) phases were also induced in the polymers by adding chiral binaphthyl derivatives as chiral inducer into the LC PEDOT derivatives. The polymer films with the induced N*-LC phase exhibited circular dichroism, implying the formation of an interchain helically π-stacked structure or intrachain helically twisted structure.

Targeted delivery of doxorubicin into cancer cells using a folic acid–dendrimer conjugate

We report here a general approach to using multifunctional poly(amidoamine) (PAMAM) dendrimer-based platform to encapsulate an anticancer drug doxorubicin (DOX) for targeted cancer therapy. In this approach, generation 5 (G5) PAMAM dendrimers modified with fluorescein isothiocyanate (FI) and folic acid (FA) via covalent conjugation, and with remaining terminal amines being acetylated (G5.NHAc-FI-FA) were used to complex DOX for targeted delivery of the drug to cancer cells overexpressing high-affinity folic acid receptors (FAR). We show that the formed G5.NHAc-FI-FA/DOX complexes with each dendrimer encapsulating approximately one DOX molecule are water soluble and stable. In vitro release studies show that DOX complexed with the multifunctional dendrimers can be released in a sustained manner. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell viability assay in conjunction with cell morphology observation demonstrates that the G5.NHAc-FI-FA/DOX complexes can specifically target and display specific therapeutic efficacy to cancer cells overexpressing high-affinity FAR. Findings from this study suggest that multifunctional dendrimers may be used as a general drug carrier to encapsulate various cancer drugs for targeting therapy of different types of cancer.

Synthesis and characterization of multifunctional poly(glycidyl methacrylate) microspheres and their use in cell separation

Multifunctional poly(glycidyl methacrylate) (PGMA) microspheres containing magnetic, fluorescent, and cancer cell-specific moieties were prepared in four steps: (i) preparation of parent PGMA microspheres by dispersion polymerization and their reaction with ethylenediamine to obtain amino groups, (ii) precipitation of iron ions (Fe 2+ and Fe 3+) to form Fe 3O 4 nanoparticles within the microspheres, (iii) consecutive reactions of folic acid with the amino groups on PGMA, and (iv) incorporation of fluorescein isothiocyanate into the microspheres. The microspheres were superparamagnetic, highly monodispersive, intensively fluorescent, and capable of recognizing and binding cancer cells that overexpress folic acid receptors. It was demonstrated that with these microspheres, HeLa cells could be captured from their suspension and easily moved in the direction of the externally applied magnetic field.

One-Pot Syntheses of Amphiphilic Centipede-like Brush Copolymers via Combination of Ring-Opening Polymerization and “Click” Chemistry

Amphiphilic centipede-like brush copolymers with biodegradable poly(e-caprolactone) and poly(ethyl ethylene phosphate) side segments were prepared by a one-pot syntheses strategy. The syntheses combined ring-opening polymerization of 2-ethoxy-2-oxo-1,3,2-dioxaphospholane through a “grafting from” strategy and “click” reaction with α-propargyl-ω-acetyl-poly(e-caprolactone) through a “grafting to” strategy, using multifunctional poly(tert-butyl methacrylate)-co-poly(2-hydroxy-3-azidopropyl methacrylate) that bears hydroxyl and azide groups from junction points. The reactions are controllable, and the structure of obtained centipede-like brush copolymer is well characterized. These brush copolymers are amphiphilic and self-assemble into spherical micellar structure in aqueous solution with critical aggregation concentration around 10−3 mg mL−1 and average diameters of 50−90 nm. Such micelles formed from centipede-like brush copolymers can be used as drug carriers for biomedical applications.

Interaction of the Vaccinia Virus RNA Polymerase-Associated 94-Kilodalton Protein with the Early Transcription Factor

A multisubunit RNA polymerase (RPO) encoded by vaccinia virus (VACV), in conjunction with specific factors, transcribes early, intermediate, and late viral genes. However, an additional virus-encoded polypeptide referred to as the RPO-associated protein of 94 kDa (RAP94) is tightly bound to the RPO for the transcription of early genes. Unlike the eight RPO core subunits, RAP94 is synthesized exclusively at late times after infection. Furthermore, RAP94 is necessary for the packaging of RPO and other components needed for early transcription in assembling virus particles. The direct association of RAP94 with NPH I, a DNA-dependent ATPase required for transcription termination, and the multifunctional poly(A) polymerase small subunit/2'-O-methyltransferase/elongation factor was previously demonstrated. That RAP94 provides a structural and functional link between the core RPO and the VACV early transcription factor (VETF) has been suspected but not previously demonstrated. Using VACV recombinants that constitutively or inducibly express VETF subunits and RAP94 with affinity tags, we showed that (i) VETF associates only with RPO containing RAP94 in vivo and in vitro, (ii) the association of RAP94 with VETF requires both subunits of the latter, (iii) neither viral DNA nor other virus-encoded late proteins are required for the interaction of RAP94 with VETF and core RPO subunits, (iv) different domains of RAP94 bind VETF and core subunits of RPO, and (v) NPH I and VETF bind independently and possibly simultaneously to the N-terminal region of RAP94. Thus, RAP94 provides the bridge between the RPO and proteins needed for transcription initiation, elongation, and termination.

Multifunctional Dendrimer-Modified Multiwalled Carbon Nanotubes: Synthesis, Characterization, and In Vitro Cancer Cell Targeting and Imaging

Carbon nanotubes hold great promise for their use as a platform in nanomedicine, especially in drug delivery, medical imaging, and cancer targeting and therapeutics. Herein, we present a facile approach to modifying carbon nanotubes with multifunctional poly(amidoamine) (PAMAM) dendrimers for cancer cell targeting and imaging. In this approach, fluorescein isothiocyanate (FI)- and folic acid (FA)-modified amine-terminated generation 5 (G5) PAMAM dendrimers (G5·NH(2)-FI-FA) were covalently linked to acid-treated multiwalled carbon nanotubes (MWCNTs), followed by acetylation of the remaining primary amine groups of the dendrimers. The resulting MWCNT/G5.NHAc-FI-FA composites are water-dispersible, stable, and biocompatible. In vitro flow cytometry and confocal microscopy data show that the formed MWCNT/G5·NHAc-FI-FA composites can specifically target to cancer cells overexpressing high-affinity folic acid receptors. The results of this study suggest that, through modification with multifunctional dendrimers, complex carbon nanotube-based materials can be fabricated, thereby providing many possibilities for various applications in biomedical sensing, diagnosis, and therapeutics.

Multifunctional Poly(N‐vinylcarbazole)‐Based Block Copolymers and their Nanofabrication and Photosensitizing Properties

The synthesis of poly(N-vinylcarbazole)-based block copolymers functionalized with rhenium diimine complexes or pendant terpyridine ligands is reported. The copolymers are synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization, and they exhibit interesting morphological properties as a result of the phase separation between different blocks. The rhenium complex polymer block may function as a photosensitizer, while the terpyridine-containing polymer block can be used as the template for nanofabrication by selective deposition of zinc complexes.

Synthesis of amphiphilic copolymer brushes possessing alternating poly(methyl methacrylate) and poly(N‐isopropylacrylamide) grafts via a combination of ATRP and click chemistry

AbstractWe report on the synthesis of well‐defined amphiphilic copolymer brushes possessing alternating poly(methyl methacrylate) and poly(N‐isopropylacrylamide) grafts, poly(PMMA‐alt‐PNIPAM), via a combination of atom transfer radical polymerization (ATRP) and click reaction (Scheme 1). Firstly, the alternating copolymerization of N‐[2‐(2‐bromoisobutyryloxy)ethyl]maleimide (BIBEMI) with 4‐vinylbenzyl azide (VBA) affords poly(BIBEMI‐alt‐VBA). Bearing bromine and azide moieties arranged in an alternating manner, multifunctional poly(BIBEMI‐alt‐VBA) is capable of initiating ATRP and participating in click reaction. The subsequent ATRP of methyl methacrylate (MMA) using poly(BIBEMI‐alt‐VBA) as the macroinitiator leads to poly(PMMA‐alt‐VBA) copolymer brush. Finally, amphiphilic poly(PMMA‐alt‐PNIPAM) copolymer brush bearing alternating PMMA and PNIPAM grafts is synthesized via the click reaction of poly(PMMA‐alt‐VBA) with an excess of alkynyl‐terminated PNIPAM (alkynyl‐PNIPAM). The click coupling efficiency of PNIPAM grafts is determined to be ∼80%. Differential scanning calorimetry (DSC) analysis of poly(PMMA‐alt‐PNIPAM) reveals two glass transition temperatures (Tg). In aqueous solution, poly(PMMA‐alt‐PNIPAM) supramolecularly self‐assembles into spherical micelles consisting of PMMA cores and thermoresponsive PNIPAM coronas, which were characterized via a combination of temperature‐dependent optical transmittance, micro‐differential scanning calorimetry (micro‐DSC), dynamic and static laser light scattering (LLS), and transmission electron microscopy (TEM). © 2009 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 47: 2608–2619, 2009

Development and In Vitro Characterization of Liposomes Coated with Thiolated Poly(Acrylic Acid) for Oral Drug Delivery

Mucoadhesive drug delivery systems offer promising opportunities for oral drug delivery. The aim of this study was to investigate the feasibility of preparing liposomes that are coated with the multifunctional polymer poly(acrylic acid)-cysteine (PAA-Cys). Cationic multilamellar vesicles (MLV) as well as cationic submicron-sized liposomes (ssLip) were prepared and coated with PAA-Cys. Size, zeta potential, amount of free thiol groups, aggregation behavior, drug-loading, and drug release of these novel carriers were evaluated. A switch of the initial positive zeta potential to a negative value after coating indicated the successful coating procedure. In both size ranges, MLV and ssLip, the amount of free thiol groups was comparable to that in a PAA-Cys solution of the same concentration. Drug loading of the hydrophilic marker fluorescence-isothiocyanate 4 kDa (FD4) was higher in PAA-Cys liposomes in comparison to noncoated liposomes, but lower in comparison to liposomes coated with unmodified poly(acrylic acid) (PAA). Only a minor ssLip or no increase MLV of the drug-loading was observed when using carboxyfluorescein (CF). These effects were attributed to interactions between the markers and the poly(acrylates). Coating of liposomes with PAA-Cys and PAA did not influence the release profile of FD4 and CF, whereas the release profile was affected by the molecular mass of the marker and the liposome size. In conclusion, the feasibility of coating liposomes with PAA-Cys was demonstrated, and it could be shown that this novel carrier system fulfills the basic requirements for an intended use in oral drug delivery.

Construction of well-defined multifunctional dendrimers using a trifunctional core

A simple synthetic strategy was developed for the synthesis of well-defined multifunctional poly(amide)-based dendrimers using a trifunctional core.

Experimental optimization of an in situ forming hydrogel for hemorrhage control

The fabrication of a novel in situ forming hydrogel composed of a multifunctional poly(ethylene glycol) (PEG) N-hydroxysuccinimide ester (NHS) and poly(allylamine hydrochloride) (PAA) was investigated. FTIR confirmed that PAA formed the hydrogel matrix (i.e., the formation of a PAA-like hydrogel). A factorial experiment was conducted to identify the key parameters that controlled gelation time, gel content, and swelling properties. The type of PEG (e.g., 4- and 6-arm) appeared to play a major role in determining all three performance parameters, with the greatest effect on gelation time. Other influencing factors include (a) the PEG concentration, which contributes to the gelation time and gel content; (b) pH of the buffer used for dissolving each polymer, which can affect the gelation time; and (c) PAA molecular weights, which contribute to the gel content and swelling. The concentration of PAA solution had no significant effects on hydrogel formation and properties within the investigated range, presumably due to negligible changes in the crosslinking density of the hydrogels. The PAA buffer pH influenced the gel content as well. Finally, thromboelastography was used to examine the effects of each polymer and their in situ gelation on blood coagulation in vitro. All individual polymers tested reduced clot strength, while the gelation of the polymers enhanced overall procoagulant effects. These results suggest that the biomaterial can be optimized to provide a combination of rapid gelation and swelling properties suitable for hemorrhage control and thus warrant further studies in animal bleeding models.

Preparation, Swelling, and Slow-Release Characteristics of Superabsorbent Composite Containing Sodium Humate

A series of multifunctional poly(acrylic acid-co-acrylamide)/Ca−montmorillonite/sodium humate superabsorbent composites with slow-release sodium humate were prepared by graft copolymerization reaction with partially neutralized acrylic acid (AA), acrylamide (AM), Ca−montmorillonite (Ca−MMT), and sodium humate (SH) in aqueous solution. The effects of SH and Ca−MMT contents on water absorbency were studied, and the highest water absorbency was obtained when the SH-to-MMT ratio was 3:2 (total amount of SH and Ca−MMT in the feed was fixed at 50 wt %). The swelling kinetics in distilled water and swelling behaviors in various pH solutions for the developed composites were systematically investigated. A two-stage release characteristic of SH in distilled water was observed, and the differences before and after SH release were characterized by FTIR, XRD, SEM, and TGA. With increasing SH and Ca−MMT contents, water absorbency differed, suggesting that SH was mainly chemically bonded with the polymer matrix, wherea...

Electrospinning of photocrosslinked and degradable fibrous scaffolds

Electrospun fibrous scaffolds are being developed for the engineering of numerous tissues. Advantages of electrospun scaffolds include the similarity in fiber diameter to elements of the native extracellular matrix and the ability to align fibers within the scaffold to control and direct cellular interactions and matrix deposition. To further expand the range of properties available in fibrous scaffolds, we developed a process to electrospin photocrosslinkable macromers from a library of multifunctional poly(beta-amino ester)s. In this study, we utilized one macromer (A6) from this library for initial examination of fibrous scaffold formation. A carrier polymer [poly(ethylene oxide) (PEO)] was used for fiber formation because of limitations in electrospinning A6 alone. Various ratios of A6 and PEO were successfully electrospun and influenced the scaffold fiber diameter and appearance. When electrospun with a photoinitiator and exposed to light, the macromers crosslinked rapidly to high double bond conversions and fibrous scaffolds displayed higher elastic moduli compared to uncrosslinked scaffolds. When these fibers were deposited onto a rotating mandrel and crosslinked, organized fibrous scaffolds were obtained, which possessed higher moduli (approximately 4-fold) in the fiber direction than perpendicular to the fiber direction, as well as higher moduli (approximately 12-fold) than that of nonaligned crosslinked scaffolds. With exposure to water, a significant mass loss and a decrease in mechanical properties were observed, correlating to a rapid initial loss of PEO which reached an equilibrium after 7 days. Overall, these results present a process that allows for formation of fibrous scaffolds from a wide variety of possible photocrosslinkable macromers, increasing the diversity and range of properties achievable in fibrous scaffolds for tissue regeneration.

New Syntheses of Branched, Multifunctional High-Molecular Weight Poly(ethylene glycol)s or (MultiPEG)s

A new set of branched high-molecular weight multifunctional poly(ethylene glycol) (MultiPEG) derivatives was obtained from smaller commercial diOH-PEGs (M.W. = 2000 and 6000 Da) which were selectively monoprotected, properly activated at the residual OH-functions and treated with 1,3-diamino-2-propanol and 2-amino-1,3-propandiol as polyfunctional linkers. They were purified by molecular exclusion chromatography or extensive dialysis and characterized by GPC and 1 H-NMR. The final polymeric derivatives are characterized by a higher number of terminal reacting moieties (up to 6 times) than that found in linear, commercial PEGs of same molecular size. This increased loading capability can be applied to improve their use as drug carriers and soluble synthetic supports.

Study on superabsorbent composites. XVIII. Preparation, characterization, and property evaluation of poly(acrylic acid‐co‐acrylamide)/organomontmorillonite/sodium humate superabsorbent composites

AbstractA series of novel multifunctional poly (acrylic acid‐co‐acrylamide) (PAA‐AM)/organomontmorillonite (O‐MMT)/sodium humate (SH) superabsorbent composites were synthesized by the graft copolymerization reaction of partially neutralized acrylic acid and acrylamide on O‐MMT micropowder and SH with N,N′‐methylene bisacrylamide as a crosslinker and ammonium persulfate as an initiator in an aqueous solution. The superabsorbent composites were characterized by means of Fourier transform infrared spectroscopy, X‐ray diffraction, scanning electron microscopy, and thermogravimetric analysis. The effect of the relative weight ratio of SH to O‐MMT on the water absorbency was studied, and the results indicated that the best water absorbency of 591 g/g in distilled water was obtained when an O‐MMT content of 20 wt % and an SH content of 30 wt % were incorporated. The superabsorbent composite possessed a good capacity for water retention; even after 30 days, 24.4 wt % of water could still be saved by the sand soil containing 1.0 wt % superabsorbent composite. The results from this study show that the water absorbency of a superabsorbent composite is improved by the simultaneous introduction of O‐MMT and SH into a PAA‐AM network in comparison with the incorporation of only O‐MMT or SH. Also, in comparison with PAA‐AM/MMT/SH, an appropriate amount of O‐MMT can benefit the developed composites with respect to their water absorbency, salt resistance, and capacity for water retention in sand soil. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008

Multifunctional poly( d, l-lactide- co-glycolide)/montmorillonite (PLGA/MMT) nanoparticles decorated by Trastuzumab for targeted chemotherapy of breast cancer

This paper continued our earlier work on the poly( d, l-lactide- co-glycolide)/montmorillonite nanoparticles (PLGA/MMT NPs), which were further decorated by human epidermal growth factor receptor-2 (HER2) antibody Trastuzumab for targeted breast cancer chemotherapy with paclitaxel as a model anticancer drug. Such a NP system is multifunctional, which formulates anticancer drugs with no harmful adjuvant, reduces the side effects of the formulated anticancer drug, promotes synergistic therapeutic effects, and achieves targeted delivery of the therapy. The paclitaxel-loaded PLGA/MMT NPs were prepared by a modified solvent extraction/evaporation technique, which were then decorated with Trastuzumab. The effects of the surface decoration on particle size and size distribution, surface morphology, drug encapsulation efficiency, as well as the drug release kinetics, were investigated. The NP formulation exhibited a biphasic drug release with a moderate initial burst followed by a sustained release profile. The surface decoration speeded the drug release. Surface chemistry analysis was conducted by X-ray photoelectron spectroscopy (XPS), which confirmed the presence of Trastuzumab on the NP surface. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis showed the stability of the antibody in the NP preparation process. Internalization of the coumarin-6-loaded PLGA/MMT NPs with or without the antibody decoration by both of Caco-2 colon adeno carcinoma cells and SK-BR-3 breast cancer cells was visualized by confocal laser scanning microscopy and quantitatively analyzed, which shows that the antibody decoration achieved significantly higher cellular uptake of the NPs. The results of in vitro cytotoxicity experiment on SK-BR-3 cells further proved the targeting effects of the antibody decoration. Judged by IC50 after 24 h culture, the therapeutic effects of the drug formulated in the NPs with surface decoration could be 12.74 times higher than that of the bare NPs and 13.11 times higher than Taxol ®.