The document discusses drug delivery, summarizing several key topics in the field. It provides an overview of the importance of drug delivery and some of the challenges like biological barriers and pharmacokinetic issues. It then highlights several recent research articles on targeted drug delivery using various nanoparticle carriers and formulations to overcome barriers and more effectively deliver drugs to specific sites.

1. Drug Delivery
The importance of drug delivery to chemists, medicinal and otherwise, has increased
since the advent of integrated drug discovery processes. Physicochemical and
biological barriers, pathways for drug delivery, formulation, pharmacokinetic and
pharmacodynamic issues, metabolism, and cell culture models used in studying drug
delivery are just some of the topics that make drug delivery an exciting field for
researchers.
Find all articles on drug delivery in Wiley Online Library...
Recent Articles
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Targeted Drug Delivery: Liposome-Loaded Cell Backpacks (Adv. Healthcare Mater. 18/2015)
Cellular backpacks are circular 7μm-wide polymer patches that can be adhered to the surface of
living cells. The image shows backpacks containing liposomes loaded with the anticancer drug
doxorubicin (red) attached to the surface of living monocytes. More details are provided on page
2832 by M.F. Rubner and co-workers.
[Frontispiece]
Roberta Polak, Rosanna M. Lim, Marisa M. Beppu, Ronaldo N. M. Pitombo, Robert E. Cohen,
Michael F. Rubner
Adv. Healthcare Mater., December 28, 2015, DOI: 10.1002/adhm.201570104. Read article
A Divalent PAMAM-Based Matrix Metalloproteinase/Carbonic Anhydrase Inhibitor for the Treatment of Dry Eye
Syndrome
It’s all in the delivery: The inhibitor shown here is a nanomolar, dendron-based
divalent sulfonamide that can bind gelatinase (MMP-9), the most important MMP on
the ocular surface, and the transmembrane human carbonic anhydrase XII, present
in eyes and considered an antiglaucoma target. In an animal model of a dry eye, no
evidence of corneal desiccation was observed in eyes treated with our inhibitor.
[Full Paper]
B. Richichi, V. Baldoneschi, S. Burgalassi, M. Fragai, D. Vullo, A. Akdemir, E.
Dragoni, A. Louka, M. Mamusa, D. Monti, D. Berti, E. Novellino, G. De Rosa, C. T.
Supuran, C. Nativi
Chem. Eur. J., December 22, 2015, DOI: 10.1002/chem.201504355. Read article.
Controlled Multi-functionalization Facilitates Targeted Delivery of Nanoparticles to Cancer Cells
Through the barricades: Controlled multi-functionalization of nanoparticles with

2. a cytotoxic drug, a glycan ligand for the cell surface receptor CD22, and an
imaging moiety led to a remarkable 60-fold enhancement in cytotoxicity of CD22
(+) lymphoma cells compared to non-targeted nanoparticles.
[Full Paper]
Manish S. Hudlikar, Xiuru Li, Ivan A. Gagarinov, Nagesh Kolishetti, Margreet A.
Wolfert, Geert-Jan Boons
Chem. Eur. J., December 18, 2015, DOI: 10.1002/chem.201503999. Read article.
Ruthenium-Containing Block Copolymer Assemblies: Red-Light-Responsive Metallopolymers with Tunable
Nanostructures for Enhanced Cellular Uptake and Anticancer Phototherapy
Self-assembled nanostructures of red-light-responsive Ru(II)-containing block
copolymers are used for anticancer photo​therapy. The Ru complexes in the block
copolymers are photocleavable and anticancer agents. Red light releases the Ru
complexes and generates singlet oxygen in cancer cells. A moderate irradiation dose,
which prevents photodamage, is sufficient to inhibit the growth of cancer cells.
[Full Paper]
Wen Sun, Maria Parowatkin, Werner Steffen, Hans-Jürgen Butt, Volker Mailänder, Si Wu
Adv. Healthcare Mater., December 17, 2015, DOI: 10.1002/adhm.201500827. Read
article
Glutathione Bioresponsive Cyclodextrin Nanosponges
Cyclodextrin-based nanosponges: A
new one-step synthetic route for the
production of glutathione (GSH)-
responsive nanosponges was reported.
The system can encapsulate the
anticancer drug doxorubicin and release it
as a function of external GSH
concentration. In vitro and in vivo studies
showed an increase in effectiveness of
anticancer drugs encapsulated within the
nanosponge (see figure).
[Communication]
Francesco Trotta, Fabrizio Caldera, Chiara Dianzani, Monica Argenziano, Giuseppina Barrera, Roberta Cavalli
ChemPlusChem, December 15, 2015, DOI: 10.1002/cplu.201500531. Read article
Coordination Polymers Derived from Non-Steroidal Anti-Inflammatory Drugs for Cell Imaging and Drug Delivery
Coordinated functions: A series of MnII-based coordination polymers were derived
from different non-steroidal anti-inflammatory drugs (NSAIDs), which showed
excellent cell imaging, in vitro anti-inflammatory and drug delivery properties (see
figure).
[Full Paper]
Mithun Paul, Parthasarathi Dastidar
Chem. Eur. J., December 11, 2015, DOI: 10.1002/chem.201503706. Read article.
Near-Infrared Light-Triggered Intracellular Delivery of Anticancer Drugs Using Porous Silicon Nanoparticles
Conjugated with IR820 Dyes
Porous silicon nanoparticles conjugated with IR820 dyes trigger excellent intracellular drug release with near-infrared
laser irradiation.
[Full Paper]
Bing Xia, Bin Wang, Zhenyu Chen, Qi Zhang, Jisen Shi

3. Adv. Mater. Interfaces, December 10, 2015, DOI: 10.1002/admi.201500715. Read article
Selective Killing of Breast Cancer Cells by Doxorubicin-Loaded Fluorescent Gold Nanoclusters: Confocal
Microscopy and FRET
Licence to kill: This study shows the real-time release (delivery) of the anticancer
drug doxorubicin from gold nanoclusters (AuNCs) carrier inside cancer and noncancer
cells. The use of doxorubicin-loaded AuNCs leads to the selective killing of breast
cancer cells (MCF7), significantly increases the survival rate of noncancer breast cells
(MCF10A), and shows strong potential as a breast cancer cell specific therapeutic
material with minimal side effects.
[Article]
Shyamtanu Chattoraj, Asif Amin, Batakrishna Jana, Saswat Mohapatra, Surajit
Ghosh, Kankan Bhattacharyya
ChemPhysChem, December 04, 2015, DOI: 10.1002/cphc.201500982. Read article
Liposome-Loaded Cell Backpacks
Liposomes loaded with doxorubicin are successfully embedded into cell
backpacks with retention of their structure. Liposome-loaded backpacks are attached
to the surface of living monocytes, which remain viable over timescales relevant to usual
drug delivery schemes. An interesting observation suggests a potential new use of cell
backpacks as vectors for the direct targeting of cancer cells.
[Full Paper]
Roberta Polak, Rosanna M. Lim, Marisa M. Beppu, Ronaldo N. M. Pitombo, Robert E. Cohen, Michael F. Rubner
Adv. Healthcare Mater., November 30, 2015, DOI: 10.1002/adhm.201500604. Read article
Photoinduced Dynamics and Toxicity of a Cancer Drug in Proximity of Inorganic Nanoparticles under Visible
Light
Given the green light: Rose bengal in conjugation with zinc oxide nanoparticles
(ZnO NPs) enhances the generation of reactive oxygen species (ROS) upon
green-light irradiation in comparison with the free drug. Detailed spectroscopic
investigations were performed and the in vitro toxicity of the nanohybrid was
confirmed using various cell lines.
[Article]
Siddhi Chaudhuri, Samim Sardar, Damayanti Bagchi, Shreyasi Dutta, Sushanta
Debnath, Partha Saha, Peter Lemmens, Samir Kumar Pal
ChemPhysChem, November 26, 2015, DOI: 10.1002/cphc.201500905. Read
article
Gelatin-Assisted Synthesis of Vaterite Nanoparticles with Higher Surface Area and Porosity as Anticancer Drug
Containers In Vitro
Holey vaterite nanoparticles! Porous vaterite nanoparticles (VNs) fabricated with gelatin assistance displayed high
surface area and improved stability in aqueous solution. Their application as doxorubicin containers and their therapeutic
efficacy against cancer cells were investigated in vitro. The vaterite nanoparticles

4. prove to be excellent containers for anticancer drugs after modification by folic acid.
[Full Paper]
Anhe Wang, Yang Yang, Xiaoming Zhang, Xingcen Liu, Wei Cui, Junbai Li
ChemPlusChem, November 24, 2015, DOI: 10.1002/cplu.201500515. Read article
An Apoferritin-based Drug Delivery System for the Tyrosine Kinase Inhibitor Gefitinib
Anticancer drug Gefitinib encapsulated within human heavy chain apoferritin by
diffusion allows pH-controlled sustained release of cargo. The combination of increased
cellular uptake, and potent and enhanced antitumor activity against the HER2
overexpressing SKBR3 cell line compared to Gefitinib alone, makes it a promising carrier
for delivery of drugs to tumor sites.
[Communication]
Anchala I. Kuruppu, Lei Zhang, Hilary Collins, Lyudmila Turyanska, Neil R. Thomas,
Tracey D. Bradshaw
Adv. Healthcare Mater., November 23, 2015, DOI: 10.1002/adhm.201500389. Read
article
Polydopamine-Functionalized Superparamagnetic Magnetite Nanocrystal Clusters – Rapid Magnetic Response
and Efficient Antitumor Drug Carriers
Magnetite nanocrystal clusters (MNCs) are fabricated by a self-assembly strategy,
the surface of the MNCs is functionalized with polydopamine (PDOPA), and the
antitumor drug epirubicin is attached onto the surface. The achieved
MNC@PDOPA exhibits superparamagnetic characteristics, improved
magnetization behavior under external magnetic field, well-controlled loading, and
pH-responsive properties.
[Full Paper]
Shaokun Song, Wanting Zhu, Chao Long, Yang Zhang, Shun Chen, Lijie Dong
Eur. J. Inorg. Chem., November 18, 2015, DOI: 10.1002/ejic.201500912. Read
article.
Biomedical Applications of Functionalized ZnO Nanomaterials: from Biosensors to Bioimaging
Recent developments for ZnO nanostructures are presented, highlighting great
potential for biomedical applications such as biosensing, tissue regeneration, bioimaging,
and drug delivery.
[Review]
Ping Zhu, Zhengyang Weng, Xia Li, Xiangmei Liu, Shuilin Wu, K. W. K. Yeung, Xianbao
Wang, Zhenduo Cui, Xianjin Yang, Paul. K. Chu
Adv. Mater. Interfaces, October 29, 2015, DOI: 10.1002/admi.201500494. Read article
Versatile Protein Nanogels Prepared by In Situ Polymerization
The in situ polymerized nanogels with encapsulated proteins have great promises
for storage and release of cargos in a spatial, temporal, and dosage-controlled manner.
The preparation method and stimuli-responsive properties of the protein nanogels are
listed and explained herein.
[Talents & Trends]
Yanqi Ye, Jicheng Yu, Zhen Gu
Macromol. Chem. Phys., October 27, 2015, DOI: 10.1002/macp.201500296. Read article
Dermal Patch with Integrated Flexible Heater for on Demand Drug Delivery
A wearable drug delivery system based on a hydrogel sheet containing thermo​responsive drug carriers
interfaced with a flexible heater is engineered for topical applications. The platform maintains a conformal contact

5. with skin and enables on demand and tunable drug delivery by controlling the hydrogel
temperature. The release rates of various molecules with different sizes are studied. The
system paves the way toward engineering smart wound dressings.
[Full Paper]
Sara Bagherifard, Ali Tamayol, Pooria Mostafalu, Mohsen Akbari, Mattia Comotto, Nasim
Annabi, Masoumeh Ghaderi, Sameer Sonkusale, Mehmet R. Dokmeci, Ali
Khademhosseini
Adv. Healthcare Mater., October 26, 2015, DOI: 10.1002/adhm.201500357. Read article
Pentafluorophenyl Ester-based Polymersomes as Nanosized Drug-Delivery Vehicles
The formation of polymersomes from HPMA-related amphiphilic blockcopolymers
is presented. These polymers are prepared via activated ester chemistry, which allows
efficient and facile modification. The vesicles formed from them exhibit high
encapsulation efficiencies for hydrophilic cargo via dual centrifugation. Furthermore, they
prove to be biocompatible, which makes them promising candidates as nanosized drug
carriers.
[Communication]
Martin Scherer, Karl Fischer, Frank Depoix, Thomas Fritz, Raphael Thiermann, Kristin Mohr, Rudolf Zentel
Macromol. Rapid Commun., October 19, 2015, DOI: 10.1002/marc.201500444. Read article
Thermo/pH Dual Responsive Mixed-Shell Polymeric Micelles Based on the Complementary Multiple Hydrogen
Bonds for Drug Delivery
Join the DOX: Thermo/pH dual responsive mixed-shell polymeric micelles based
on the complementary multiple hydrogen bonds are synthesized. The collapsed
poly(N-vinylcaprolactam) (PNVCL) shell could form hydrophobic domains on the
poly(ɛ-caprolactone) (PCL) core and the corona formed by the water soluble
methoxy poly(ethylene glycol) (MPEG) chains was embedded into the PNVCL shell
and acted as a channel and a protective barrier against aggregation of the micelles.
[Full Paper]
Qiuhua Wu, Xiuping Tang, Xue Liu, Yu Hou, He Li, Chen Yang, Jie Yi, Ximing
Song, Guolin Zhang
Chem. Asian J., October 15, 2015, DOI: 10.1002/asia.201500847. Read article
Photomediated Reactive Oxygen Species-Generable Nanoparticles for Triggered Release and Endo/Lysosomal
Escape of Drug upon Attenuated Single Light Irradiation
Photomediated reactive oxygen species (ROS)-generable nanoparticles (SRNs)
incorporated with ROS-generator and scavenger in a single delivery platform is
developed. Under attenuated single light irradiation, doxorubicin loaded SRNs (D-SRNs)
synergistically exhibit simultaneous triggered drug release and endo/lysosomal escape
as well as photodynamic therapy for highly efficient cancer treatment.
[Full Paper]
Eun Ha Seo, Chung-Sung Lee, Kun Na
Adv. Healthcare Mater., October 09, 2015, DOI: 10.1002/adhm.201500622. Read article
Grafting of ZnS:Mn-Doped Nanocrystals and an Anticancer Drug onto Graphene Oxide for Delivery and Cell
Labeling
New inroads in theranostics: The grafting of fluorescent ZnS:Mn-doped nanocrystals and
the anticancer drug doxorubicin onto graphene oxide can be used for cell labeling and drug
delivery applications. The nanocomposite particles exhibit drug entrapment efficiency of
100% and cancer cell killing efficiency of 85%. The particles label the perinuclear region of
HeLa cells with yellow fluorescence (see figure).
[Full Paper]
Sanghamitra Dinda, Mitali Kakran, Jialiu Zeng, Thankiah Sudhaharan, Sohail Ahmed,
Debajyoti Das, Subramanian Tamil Selvan
ChemPlusChem, September 01, 2015, DOI: 10.1002/cplu.201500349. Read article

6. Dual Release Carriers for Cochlear Delivery
The fabrication of a carrier system capable of selectively encapsulating two therapeutics,
piribedil and glial cell derived neurotrophic factor, in select compartments, and the programming
of their independent release rates is investigated. The characterization of these particles, the
release of each therapeutic, and the persistence of the particles within Guinea pig cochlea are
assessed.
[Communication]
Sahar Rahmani, Astin M. Ross, Tae-Hong Park, Hakan Durmaz, Acacia F. Dishman, Diane M.
Prieskorn, Nathan Jones, Richard A. Altschuler, Joerg Lahann
Adv. Healthcare Mater., July 14, 2015, DOI: 10.1002/adhm.201500141. Read article
© Wiley-VCH 2015.