Since the pioneering work dealing with the synthesis and physicochemical aspects of dendrimers, a predictable and tunable set of compositions for therapeutic, scaffolding and imaging systems has been reported. These are well documented, but many hot issues should be examined and reviewed. Herein, a review is given on dendritic nanopolymers and their applications that show promise in the field of regenerative medicine. This review begins

Supporting information AFM Studies. Alkanethiol materials. 1-adamantanethiol (AD) of 95% purity was purchased from Sigma-Aldrich (Missouri, USA) and was used as received. Ethanol solvent of 99.99% purity was purchased from Gold Shield Chemical Co. (California, USA) and served as the solvent for AD. Preparation of 1-adamantanethiol Self-Assembled Monolayers (SAM). The SAM preparation used in this study follows established procedures. 1, 2 Gold with 99,999% purity was purchased from Alfa Aesar (Massachusetts, USA) was deposited in a high-vacuum evaporator (Model DV502-A, Denton Vacuum, New Jersey, USA) at a base pressure below 2 x 10-7 Torr onto freshly cleaved mica substrates

Tripodal peptide analogues were designed on the basis of the phosphotyrosine binding pocket of the Src SH2 domain and assayed for their ability to bind to fluorescein-labeled phosphopeptides. Fluorescence polarization assays showed that a number of amphipathic linear peptide analogues (LPAs), such as LPA4, bind to fluorescein-labeled GpYEEI (F-GpYEEI). LPA4 was evaluated for potential application in cellular delivery of phosphopeptides. Fluorescence microimaging cellular uptake studies with fluorescein-attached LPA4 (F-LPA4) alone or with the mixture of LPA4 and F-GpYEEI in BT-20 cells showed dramatic increase of the fluorescence intensity in cytosol of cells, indicating that LPA4 can function as a delivery tool of F-GpYEEI across the cell membrane. Fluorescent flow cytometry studies showed the cellular uptake of F-LPA4 in an energy-independent pathway and confirmed the cellular uptake of F-GpYEEI in the presence of LPA4. These studies suggest that amphipathic tripodal peptide analo...

Dendrimers are highly customizable nanopolymers with qualities that make them ideal for drug delivery. The high binding affinity of biotin/avidin provides a useful approach to fluorescently label synthesized dendrimer-conjugates in cells and tissues. In addition, biotin may facilitate delivery of dendrimers through the blood-brain barrier (BBB) via carrier-mediated endocytosis. The purpose of this research was to: (1) measure toxicity using lactate dehydrogenase (LDH) assays of generation (G)4 biotinylated and non-biotinylated poly(amidoamine) (PAMAM) dendrimers in a co-culture model of the BBB, (2) determine distribution of dendrimers in the rat brain, kidney, and liver following systemic administration of dendrimers, and (3) conduct atomic force microscopy (AFM) on rat brain sections following systemic administration of dendrimers. LDH measurements showed that biotinylated dendrimers were toxic to cell co-culture after 48 h of treatment. Distribution studies showed evidence of biotinylated and non-biotinylated PAMAM

Dendritic nanomaterials are emerging as key building blocks for a variety of nanoscale materials and technologies. Poly(amidoamine) (PAMAM) dendrimers were the first class of dendritic nanomaterials to be commercialized. Despite numerous investigations, the environmental fate, transport, and toxicity of PAMAM dendrimers is still not well understood. As a first step toward the characterization of the environmental behavior of dendrimers in aquatic systems, we measured the octanol-water partition coefficients (logK ow ) of a homologous series of PAMAM dendrimers as a function of dendrimer generation (size), terminal group and core chemistry. We find that the logK ow of PAMAM dendrimers depend primarily on their size and terminal group chemistry. For G1-G5 PAMAM dendrimers with terminal NH 2 groups, the negative values of their logK ow indicate that they prefer to remain in the water phase. Conversely, the formation of stable emulsions at the octanol-water (O/ W) interface in the presence of G6-NH 2 and G8-NH 2 PAMAM dendrimers suggest they prefer to partition at the O/W interface. In all cases, published studies of the cytotoxicity of Gx-NH 2 PAMAM dendrimers show they strongly interact with the lipid bilayers of cells. These results suggest that the logK ow of a PAMAM dendrimer may not be a good predictor of its affinity with natural organic media such as the lipid bilayers of cell membranes. * Corresponding author phone: 626 395 2730; fax: 626 585 0918.

The aim of this publication is to present a general strategy to engineer more efficient photoluminescent dendritic molecules based on polyhedral oligomeric silsesquioxane (POSS) cores. A series of chromophores were grafted
on POSS cores to form dendritic molecules for which steric hindrance was used as a trigger to tune their photophysical properties. For fluorescence in the blue/near-UV spectral ranges, 4-vinylbiphenyl molecules were chosen as model chromophores to present a general approach based on stable chemistry and bulky groups grafted to the chromophores to enhance photoluminescence efficiency of the dendritic molecules.
Photoluminescence quantum yields as well as steady-state and time-resolved solution spectroscopy along with molecular dynamics investigation and electronic structure calculations on a family of new materials are reported. We highlight an apparent contrast between free chromophore and dendritic molecules photophysical properties and show that chromophores’ engineering and confinement around an inorganic core allows the design of more efficient photoluminescent dendritic molecules relevant to sensors and hybrid light-emitting diodes.

Ferrocenyl (Fc) dendrimers and polymers have attracted much attention owing to their multielectron redox properties and functions as biosensors, virus-like receptors, [4a] models of molecular batteries, [4b] and colorimetric sensors. Fcterminated dendrimers belong to the large family of redoxactive metallodendrimers that may eventually mimic related nanometer-sized biological processes and provide useful energy-relevant devices. In typical examples, Nishihara and co-workers have extensively studied the efficient electrodeposition of acylbiFc nanodevices in gold nanoparticles, and recently, the group of Reinhoudt and Ravoo elegantly demonstrated that small acylbiFc dendrimers form inclusion complexes with selfassembled monolayered b-cyclodextrin as "molecular printboards". Biferrocene itself can be incorporated without covalent bonding as a biferrocenium charge-transfer complex with the arylimino groups of Yamamotos arylazidomethine dendrimers. From these studies, it has become clear that the redox properties of the biFc derivatives, which include three easily accessible oxidation states, are much richer than those of the Fc group.

Nanotechnology has already started to significantly impact many industries and scientific fields including biotechnology, pharmaceutics, food technology and semiconductors. Nanotechnology-based tools and devices, including high-resolution imaging techniques, enable characterization and manipulation of materials at the nanolevel and further elucidate nanoscale phenomena and equip us with the ability to fabricate novel materials and structures. One of the most promising impacts of nanotechnology is in the area of nanotherapy. Employing nanosystems such as dendrimers, nanoliposomes, niosomes, nanotubes, emulsions and quantum dots, nanotherapy leads toward the concept of personalized medicine and the potential for early diagnoses coupled with efficient targeted therapy. The development of smart targeted nanocarriers that can deliver bioactives at a controlled rate directly to the designated cells and tissues will provide better efficacy and reduced side effects. Nanocarriers improve the solubility of bioactives and allow for the delivery of not only small-molecule drugs but also the delivery of nucleic acids and proteins. This review will focus on nanoscale bioactive delivery and targeting mechanisms and the role of high-resolution imaging techniques in the evaluation and development of nanocarriers. #

The attempt to decorate carbon nanotubes with organic molecules as a powerful means to form new functional materials has attracted broad attention in the scientific community. Here, we report the functionalization of single-walled carbon nanotubes (SWNTs) with zinc porphyrins (ZnP) using very mild conditions to afford a series of SWNTs-ZnP (1 and 2) electron donor-acceptor conjugates. Owing to the presence of either one or two ZnP, introduced via "click chemistry", different absorption cross sections were realized. Important in this context is that the covalent linkages between SWNT and ZnP were corroborated by monitoring the diagnostic signature of the nitrogen atoms as part of the formed triazole ring by X-ray photoelectron spectroscopy (XPS). The resulting SWNTs-ZnP 1 and 2 were fully characterized. This characterization was complemented by a full-fledged investigation of their electrochemical and photophysical properties. In particular, appreciably strong electronic coupling between the photo- and electroactive constituents (i.e., SWNT and ZnP) led to rapid excited-state deactivation of ZnP via charge transfer to the nanotubes. Here, the different absorption cross sections throughout the visible part of the solar spectrum turned out to be valuable in enhancing the overall light-harvesting features. Upon photoexcitation, for both SWNTs-ZnP 1 and 2, radical ion pair states (i.e., reduced SWNT and oxidized ZnP) are formed. The charge-separated states decay to regenerate the singlet ground state with lifetimes of 820 and 200 ps for 1 and 2, respectively.

Ficus carica Linn. (Moraceae) is commonly known as edible fig. The leaves, roots, fruits and latex of the plant are medicinally used in different diseases. The leaves are claimed to be effective in various inflammatory conditions like painful or swollen piles, insect sting and bites. However, there has been no report on anti-inflammatory and antioxidant activity of F. carica leaves. Therefore the aim of this study was to evaluate the anti-inflammatory and antioxidant activity of F. carica leaves. Our study validated the traditional claim with pharmacological data. Anti-inflammatory and antioxidant activity of the drug could be due to the presence of steroids and flavanoids, respectively, which are reported to be present in the drug. Furthermore, the anti-inflammatory activity of the drug could be due to its free radical scavenging activity. Further work is also required to isolate and characterise the active constituents responsible for the anti-inflammatory activities.

Dendrimers have attracted immense attention during the last decade due to their interesting properties both from a basic and an applied research viewpoint. Encapsulation of metal nanoparticles for catalysis, drug delivery and light harvesting are only some applications of dendrimers that are breaking new ground. A novel application of dendrimer technology is described in the present paper that relates to industrial water treatment. Industrial water systems often suffer from undesirable inorganic deposits. These can form either in the bulk or on metallic surfaces, such as heat exchangers or pipelines. Silica (SiO 2 ) scale formation and deposition is a major problem in high-silica-containing cooling waters. Scale prevention rather than removal is highly desired. In this paper, benchtop screening tests on various silica inhibition chemistries are reported, with emphasis on materials with a dendrimeric structure. Specifically, the inhibition properties of commercially available STARBURST  polyaminoamide (PAMAM) dendrimers generations 0.5, 1, 1.5, 2, and 2.5 are investigated in detail together with other commonly-used scale inhibitors. Experimental results show that inhibition efficiency largely depends on structural features of PAMAM dendrimers such as generation number and nature of the end groups. PAMAM dendrimers are effective inhibitors of silica scale growth at 40 ppm dosage levels. PAMAM dendrimers also act as silica nucleators, forming SiO 2 -PAMAM composites. This occurs because the SiO 2 formed by incomplete inhibition interacts with cationic PAMAM-1 and -2. The general scope of silica formation and inhibition in industrial waters is also discussed.

d e n t a l m a t e r i a l s 2 2 ( 2 0 0 6 ) 845-851 a v a i l a b l e a t w w w . s c i e n c e d i r e c t . c o m j o u r n a l h o m e p a g e : w w w . i n t l . e l s e v i e r h e a l t h . c o m / j o u r n a l s / d e m a Dental polymers Residual monomer High performance liquid chromatography Headspace-gas chromatography/mass spectrometry a b s t r a c t Objectives. The aim of this study was to analyze the residual monomer content of photopolymerized dendritic methacrylate copolymers and particulate filler composites. Headspacegas chromatography/mass spectrometry (HS-GC/MS) was compared with high performance liquid chromatography (HPLC). Methods. The resin mixtures consisted of a dendritic methacrylate monomer, methyl methacrylate and acetoacetoxyethyl methacrylate in varied proportions. In addition, one of the composites contained 1,4-butanediol dimethacrylate. Camphorquinone and 2-(N,Ndimethylamino)ethyl methacrylate were used as the light-activated initiator system. The content of residual methyl methacrylate and acetoacetoxyethyl methacrylate after 40 s photopolymerization were analyzed with HPLC and HS-GC/MS. Results. The content of residual methyl methacrylate decreased and residual acetoacetoxyethyl methacrylate increased with increasing concentration of acetoacetoxyethyl methacrylate in the resin mixture. The results with both methods had the same trend.

Nanotechnology could be defined as the technology that has allowed for the control, manipulation, study, and manufacture of structures and devices in the "nanometer" size range. These nano-sized objects, e.g., "nanoparticles", take on novel properties and functions that differ markedly from those seen from items made of identical materials. The small size, customized surface, improved solubility, and multi-functionality of nanoparticles will continue to open many doors and create new biomedical applications. Indeed, the novel properties of nanoparticles offer the ability to interact with complex cellular functions in new ways. This rapidly growing field requires crossdisciplinary research and provides opportunities to design and develop multifunctional devices that can target, diagnose, and treat devastating diseases such as cancer. This article presents an overview of nanotechnology for the biologist and discusses the attributes of our novel XPclad © nanoparticle formulation that has shown efficacy in treating solid tumors, for single dose vaccination, and oral delivery of therapeutic proteins.

Efficient drug delivery to the eye remains a challenging task for pharmaceutical scientists. Due to the various anatomical barriers and the clearance mechanisms prevailing in the eye, conventional drug delivery systems, such as eye drop solutions, suffer from low bioavailability. More invasive methods, such as intravitreal injections and implants, cause adverse effects in the eye. Recently, an increasing number of scientists have turned to nanomaterialbased drug delivery systems to address the challenges faced by conventional methods. This paper highlights recent applications of various nanomaterials, such as polymeric micelles, hydrogels, liposomes, niosomes, dendrimers, and cyclodextrins as ocular drug delivery systems to enhance the bioavailability of ocular therapeutic agents.

A number of new molecular entities (NMEs) selected for full-scale development based on their safety and pharmacological data suffer from undesirable physicochemical and biopharmaceutical properties, which lead to poor pharmacokinetics and distribution after in vivo administration. An optimization of the preformulation studies to develop a dosage form with proper drug delivery system to achieve desirable pharmacokinetic and toxicological properties can aid in the accelerated development of these NMEs into therapies. Nanoparticulate drug delivery systems show a promising approach to obtain desirable druglike properties by altering the biopharmaceutics and pharmacokinetics properties of the molecule. Apart from the advantages of enhancing potential for systemic administration, nanoparticulate drug delivery systems can also be used for site-specific delivery, thus alleviating unwanted toxicity due to nonspecific distribution, improve patient compliance, and provide favorable clinical outcomes. This review summarizes some of the parameters and approaches that can be used to evaluate nanoparticulate drug delivery systems in early stages of formulation development. ß

Nanotechnology is a field of research at the crossroads of biology, chemistry, physics, engineering, and medicine. Design of multifunctional nanoparticles capable of targeting cancer cells, delivering and releasing drugs in a regulated manner, and detecting cancer cells with enormous specificity and sensitivity are just some examples of the potential application of nanotechnology to oncological diseases. In this review we discuss the recent advances of cancer nanotechnology with particular attention to nanoparticle systems that are in clinical practice or in various stages of development for cancer imaging and therapy. Published by Elsevier Inc.

Los capítulos de este libro van encaminados a la creación de nuevas terapias y fármacos dirigidos frente a la infección por el VIH, basados en la nanomedicina, que juega un papel muy relevante en el cuidado de nuestra salud, a través de la generación de nuevos diagnósticos y detección rápida de enfermedad. La nanomedicina se agrupa en
nanodiagnóstico y nanoterapia, siendo su objetivo máxima curación con el mínimo daño secundario posible.

Central nervous system (CNS) diseases represent the largest and fastest-growing area of unmet medical need. Nanotechnology plays a unique instrumental role in the revolutionary development of brain-specific drug delivery, imaging, and diagnosis. With the aid of nanoparticles of high specificity and multifunctionality, such as dendrimers and quantum dots, therapeutics, imaging agents, and diagnostic molecules can be delivered to the brain across the blood-brain barrier (BBB), enabling considerable progress in the understanding, diagnosis, and treatment of CNS diseases. Nanoparticles used in the CNS for drug delivery, imaging, and diagnosis are reviewed, as well as their administration routes, toxicity, and routes to cross the BBB. Future directions and major challenges are outlined.

Recent advances in nanotechnology and nanobiotechnology have contributed to the development of nanomaterials, able to be used as drug carriers, probes, targets or cytostatic drugs by itself. Nanomedicine is now the leading area in nanotechnology where a large number and types of nanoparticles (NPs) has been developed and several are already in the clinical practice. Chemotherapy is one of the most widely used strategies to treat cancer. Most chemotherapeutic agents have poor solubility, low bioavailability, and are formulated with toxic solvents. NPs have been designed to overcome the lack of specificity of chemotherapeutic agents as well to improve circulation time in blood, taking advantages on tumor cells characteristics. In immunology, recent advances regarding the activation of the innate immune system artificially enhanced by NPs functionalized with immune-stimulators open a new window as novel methods in vaccines. Also, viruses and virus-like particles (VLPs) engineered to stimulate immune response against their similar virus or as molecular platforms for the presentation of foreign epitopes have been described. In this review we focused in the use of different types of NPs in oncology and immunology, pinpointing the main novelties regarding their development and use of nanotechnology in a broad array of applications, ranging from tumor diagnostics, immune-modulation up to cancer therapeutics.

Nanotechnology is an emerging field that covers a wide range of technologies which are presently under development in nanoscale. It plays a major role in the development of innovative methods to produce new products, to substitute existing production equipment and to reformulate new materials and chemicals with improved performance resulting in less consumption of energy and materials and reduced harm to the environment as well as environmental remediation. Although, reduced consumption of energy and materials benefits the environment, nanotechnology will give possibilities to remediate problems associated with the existing processes in a more sustainable way. Environmental applications of nanotechnology address the development of solutions to the existing environmental problems, preventive measures for future problems resulting from the interactions of energy and materials with the environment, and any possible risks that may be posed by nanotechnology itself. This article gives a comprehensive review on the ongoing research and development activities on environmental remediation by nanotechnology. First, the essential aspects of environmental problems are reviewed and then the application of nanotechnology to the compounds, which can serve as environmental cleaning, is described. Various environmental treatments and remediations using different types of nanostructured materials from air,

The development of DSM's Hybrane hyperbranched poly(ester amides) is described. The monomer (1) for the hyperbranched polyester is obtained from the reaction of a cyclic anhydride with diisopropanol amine, yielding a tertiairy amide with one COOH and two OH groups. Polycondensation takes place via an oxazolinium intermediate in bulk at relatively mild conditions in the absence of catalyst. The reaction has been scaled up to ton scale. By varying and combining anhydrides, and modification with several types of end groups, a large variety of structures with concomitant properties and industrial applications has been realized.

Dendrimers are unique biomaterials that are constructed by the stepwise addition of layers (generations) of polymer around a central core. They can be constructed with a range of molecular weights and have a polyfunctional surface that facilitates the attachment of drugs and pharmacokinetic modifiers such PEG or targeting moieties. These properties have led to considerable interest in the development of dendrimers for a range of biomedical applications. After subcutaneous administration, larger dendrimers in particular (N 8 nm), preferentially drain from the injection site into the peripheral lymphatic capillaries and therefore have potential as lymphatic imaging agents for magnetic resonance and optical fluorescence lymphangiography and as vectors for drug-targeting to lymphatic sites of disease progression. In general, lymphatic targeting of dendrimers is enhanced by increasing size although ultimately larger constructs may be incompletely absorbed from the injection site. Increasing hydrophilicity and reducing surface charge enhances drainage from subcutaneous injection sites, but the reverse is true of uptake into lymph nodes where charge and hydrophobicity promote retention. Larger hydrophilic dendrimers are also capable of extravasation from the systemic circulation, absorption into the lymphatic system and recirculation into the blood. Lymphatic recirculation may therefore be a characteristic of PEGylated dendrimers with long systemic circulation times.

We are grateful to CDT Oxford Ltd, the Engineering and Physical Sciences Research Council and the Scottish Funding Council for financial support. Dendrimers are now an important class of light-emitting material for use in organic light-emitting diodes (OLEDs). Dendrimers are branched macromolecules that consist of a core, one or more dendrons, and surface groups. The different parts of the macromolecule can be selected to give the desired optoelectronic and processing properties. The first light-emitting dendrimers were fluorescent but more recently highly efficient phosphorescent dendrimers have been developed. OLEDs containing light-emitting dendrimers have been reported to have external quantum efficiencies of up to 16 %. The solubility of the dendrimers opens the way for simple processing and a new class of flat-panel displays. In this Review we show how the structure of the light-emitting dendrimers controls key features such as intermolecular interactions and charge transport, which are important for all OLED materials. The advantages of the dendrimer architecture for phosphorescent emitters and the way the structure can be varied to enhance materials performance and device design are illustrated. REVIEW P. L. Burn et al./Light-Emitting Dendrimers for Displays 1676 www.advmat.de

Small interfering RNAs (siRNAs) mediate cleavage of specific, complementary mRNA sequences and thus regulate gene expression. Not surprisingly, their use for treatment of diseases that are rooted in aberrant gene expression, such as cancer, has become a paradigm that has gained wide interest. Here, we report the development of dendrimer-conjugated magnetofluorescent nanoworms that we call "dendriworms" as a modular platform for siRNA delivery in vivo. This platform maximizes endosomal escape to robustly produce protein target knockdown in vivo, and is tolerated well in mouse brain. We demonstrate that siRNA-carrying dendriworms can be readily internalized by cells and enable endosomal escape across a wide range of loading doses, whereas dendrimers or nanoworms alone are inefficient. Further, we show that dendriworms carrying siRNA against the epidermal growth factor receptor (EGFR) reduce protein levels of EGFR in human glioblastoma cells by 70؊80%, 2.5-fold more efficiently than commercial cationic lipids. Dendriworms were well-tolerated after 7-days of convection-enhanced delivery to the mouse brain and in an EGFR-driven transgenic model of glioblastoma, anti-EGFR dendriworms led to specific and significant suppression of EGFR expression. Collectively, these data establish dendriworms as a multimodal platform that enables fluorescent tracking of siRNA delivery in vivo, cellular entry, endosomal escape, and knockdown of target proteins.

Dendrimers have unique molecular architectures and properties that make them attractive materials for the development of nanomedicines. Key properties such as defined architecture and a high ratio of multivalent surface moieties to molecular volume also make these nanoscaled materials highly interesting for the development of synthetic (non-viral) vectors for therapeutic nucleic acids. Rational development of such vectors requires the link to be made between dendrimer structure and the morphology and physicochemistry of the respective nucleic acid complexes and, furthermore, to the biological performance of these systems at the cellular and systemic level. The review focuses on the current understanding of the role of dendrimers in those aspects of synthetic vector development. Dendrimer-based transfection agents have become routine tools for many molecular and cell biologists but therapeutic delivery of nucleic acids remains a challenge. D

A nonavalent glycodendrimer bearing terminal R-D-mannopyranoside units has been synthesized with a convergent approach. Terminal trivalent mannoside dendrons bearing p-halophenyl ethers were prepared by glycosylation of pentaerythritol derivatives having three 2-hydroxyethyl ether substituents. Two efficient routes were developed for the synthesis of the pentaerythritol-based core , which has three terminal propargyl ethers. Conditions were found under which the triple Sonogashira coupling reaction of the dendron and the tri-O-propargyl ether (17) proceeded efficiently. The product was deprotected and it and precursors were fully characterized by NMR spectroscopy and FT-ICR mass spectrometry.

Dendrimer pharmacokinetics: the effect of size, structure and surface characteristics on ADME properties Dendrimers show increasing promise as drug-delivery vectors and can be generated with a wide range of scaffold structures, sizes and surface functionalities. To this point, the majority of studies of dendrimerbased drug-delivery systems have detailed pharmacodynamic outcomes, or have followed the pharmacokinetics of a solubilized or conjugated drug. By contrast, detailed commentary on the in vivo fate of the dendrimer carrier is less evident, even though the pharmacokinetics of the carrier will likely dictate both pharmacodynamic and toxicokinetic outcomes. In the current article, the influence of size, structure and surface functionality on the absorption, distribution, metabolism and elimination (ADME) properties of dendrimers have been examined and the implications of these findings for delivery system design are discussed.

C atalysis by palladium derivatives is now one of the most important tools in organic synthesis. Whether researchers design palladium nanoparticles (NPs) or nanoparticles occur as palladium complexes decompose, these structures can serve as central precatalysts in common carbonÀcarbon bond formation. Palladium NPs are also valuable alternatives to molecular catalysts because they do not require costly and toxic ligands.

Amphiphilic polymers are particularly useful for drug delivery because of their ability to self-assemble into discrete aggregates. While this behavior has been studied in depth for simple linear block copolymer amphiphiles, recent advances in synthetic methodologies have provided efficient routes to amphiphilic polymers with more complex architecture, including dendrimers, hyperbranched polymers, star polymers, and cyclic polymers. These architectures can impart unique advantages, such as increased stability, on their micellar aggregates. Herein the different strategies for preparing these complex amphiphiles are described, and the application of their assemblies towards drug delivery are summarized.

We report a new use of acetylated dendrimer-entrapped gold nanoparticles (Au DENPs) for in vitro and in vivo computed tomography (CT) imaging of cancer cells. In this study, Au DENPs prepared using amineterminated generation 5 poly(amidoamine) dendrimers were subjected to an acetylation reaction to neutralize the positive surface potential. The acetylated Au DENPs were used for both in vitro and in vivo CT imaging of a human lung adencarcinoma cell line (SPC-A1 cells). Micro-CT images show that SPC-A1 cells can be detected under X-ray after incubation with the acetylated Au DENPs in vitro and the xenograft tumor model can be imaged after both intratumoral and intraperitoneal administration of the particles. Transmission electron microscopy data further confirm that the acetylated Au DENPs are able to be uptaken dominantly in the lysosomes of the cells. Combined morphological observation of cells after hematoxylin and eosin staining, MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay of cell viability, and flow cytometric analysis of cell cycle show that the acetylated Au DENPs do not appreciably affect the cell morphology, viability, and cell cycle, indicating their good biocompatibility at the given concentration range. Findings from this study suggest that the developed acetylated Au DENPs have a great potential to be used for CT imaging of cancer cells.

The delivery of biologically active agents to the desired site in the body and intracellular organelles is still a big challenge despite efforts made for more than five decades. With the elaboration of synthetic methodologies to branched and hyperbranched macromolecules such as miktoarm stars and dendrimers, the focus has shifted to nanocarriers able to release and direct drug molecules to a desired location in a controlled manner. We present here recent developments in the field of targeted drug delivery with a focus on two specific macromolecular nanocarriers, dendrimers and miktoarm stars, and provide examples of these nanocarriers tested in different biological systems. A particular attraction of miktoarm stars is their versatility in achieving superior drug loading within their self-assembled structures. Advantages of dendrimers over linear polymers are that the former provide a platform for development of multivalent and multifunctional nanoconjugates, in addition to their ability to accommodate a large number of molecules inside, or at their surfaces.

In this paper we report synthesis and characterization of new and modified citric acid dendrimers as biocompatible compound with -cyclodextrine ( -CD). Then obtained compounds were applied as the drug-delivery systems in utilization of suitable size molecule such as naltrexone. Common spectroscopic methods have been used for the characterization the structure of synthesized dendrimers. The controlled release of naltrexone as the guest molecule with these biodegradable dendrimers were investigated in different pH. Release and loading capacity of the abovementioned compounds were investigated using UV spectroscopy method. Diameter of nanocarriers was determined with applying dynamic light scattering (DLS) experiments, and it was found that the diameter size of the particles are between 50 and 70 nm for different nanocarrier systems having drug molecules as encapsulated in the cavity of CDs or dendrimers. The release of the guest molecules from nanocarriers was evaluated at biological pH 1, 7.4 and 10.

A range of dendritic molecules was made using the monodentate SEMI-ESPHOS phosphine oxide ligand, which was derivatised with a series of functional groups including bromide, vinyl, allyl and terminal alkyne. Several methods to attach the resulting precursors onto octavinylsilsesquioxane (OVS), ranging from hydrosilylation, Suzuki, Heck, Grubbs or Sonogashira coupling reactions, have been investigated. Cross-metathesis of SEMI-ESPHOS oxide dendrons containing vinyl end groups with OVS catalyzed by Grubbs’ catalyst was proven to be effective in the formation of precursors for dendritic molecules based on OVS.

Dendrimers are well-defined, versatile polymeric architecture with properties resembling biomolecules. Dendritic polymers emerged as outstanding carrier in modern medicine system because of its derivatisable branched architecture and flexibility in modifying it in numerous ways. Dendritic scaffold has been found to be suitable carrier for a variety of drugs including anticancer, anti-viral, anti-bacterial, antitubercular etc., with capacity to improve solubility and bioavailability of poorly soluble drugs. In spite of extensive applicability in pharmaceutical field, the use of dendrimers in biological system is constrained because of inherent toxicity associated with them. This toxicity is attributed to the interaction of surface cationic charge of dendrimers with negatively charged biological membranes in vivo. Interaction of dendrimers with biological membranes results in membrane disruption via nanohole formation, membrane thinning and erosion. Dendrimer toxicity in biological system is generally characterized by hemolytic toxicity, cytotoxicity and hematological toxicity. To minimize this toxicity two strategies have been utilized; first, designing and synthesis of biocompatible dendrimers; and second, masking of peripheral charge of dendrimers by surface engineering. Biocompatible dendrimers can be synthesized by employing biodegradable core and branching units or utilizing intermediates of various metabolic pathways. Dendrimer biocompatibility has been evaluated in vitro and in vivo for efficient presentation of biological performance. Surface engineering masks the cationic charge of dendrimer surface either by neutralization of charge, for example PEGylation, acetylation, carbohydrate and peptide conjugation; or by introducing negative charge such as half generation dendrimers. Neutral and negatively charged dendrimers do not interact with biological environment and hence are compatible for clinical applications as elucidated by various studies examined in this review. Chemical modification of the surface is an important strategy to overcome the toxicity problems associated with the dendrimers. The present review emphasizes on the approaches available to overcome the cationic toxicity inherently associated with the dendrimers.