Delivery of drugs into the cellular cytoplasm of target cells represents a major hurdle in treating various diseases. This challenge can be addressed by encapsulation of drugs onto or within nanoparticles, which can then be targeted to diseased cells. Here, needle-shaped particles are shown to exhibit substantially higher cytoplasmic delivery of drugs such as siRNA compared to their spherical counterparts. Furthermore, these needles are designed to lose their sharp tips over time and can render themselves ineffective over time, thereby offering control over their duration of activity and toxicity. Such polymer nanoneedles open new avenues for delivering drug molecules directly into the cytoplasm with low toxicity.
"Cylindrical-shape PLGA nanoparticles have been used for the delivery of docetaxel to mice bearing a human ovarian carcinoma SKOV-3 flank xenograft (Chu et al., 2013). Needle shaped nanoparticles has been used for the delivery of siRNA in the cytoplasm (Kolhar et al., 2011). A number of specialized techniques were investigated for the design of nanoparticles of varying geometric shapes. "
"Finally, based on the troublesome nature of the fluorescein label, a more quantitative/absolute approach to studying the shape effect on nanoparticle uptake with nanomedical prospects and the efficiency of different particles in cargo delivery could constitute a more correlative approach. To date, this has been successfully measured in the extent of causing cytotoxicity upon delivery of the chemotherapeutic agent camptothecin or paclitaxel
 or the efficacy of GFP knockdown
 upon siRNA delivery, and similar approaches will also be pursued in our ongoing and future studies. "
[Show abstract][Hide abstract] ABSTRACT: In nanomedicine, physicochemical properties of the nanocarrier affect the nanoparticle's pharmacokinetics and biodistribution, which are also decisive for the passive targeting and nonspecific cellular uptake of nanoparticles. Size and surface charge are, consequently, two main determining factors in nanomedicine applications. Another important parameter which has received much less attention is the morphology (shape) of the nanocarrier. In order to investigate the morphology effect on the extent of cellular internalization, two similarly sized but differently shaped, rod-like and spherical, mesoporous silica nanoparticles were synthesized, characterized and functionalized to yield different surface charges. The uptake in two different cancer cell lines was investigated as a function of particle shape, coating (organic modification), surface charge and dose. According to the presented results, particle morphology is a decisive property regardless of both the different surface charges and doses tested, whereby rod-like particles internalized more efficiently in both cell lines. At lower doses, whereby the shape-induced advantage is less dominant, however, charge-induced effects can be used to fine-tune the cellular uptake as a prospectively "secondary" uptake regulator for tight dose-control in nanoparticle-based drug formulations.
Nanoscale Research Letters 07/2012; 7(1):358. DOI:10.1186/1556-276X-7-358 · 2.78 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Osteoporosis represents a major public health burden especially considering the aging populations worldwide. Drug targeting will be important to better meet these challenges and direct the full therapeutic potential of therapeutics to their intended site of action. This review has been organized in modules, such that scientists working in the field can easily gain specific insight in the field of bone targeting for the drug class they are interested in. We review currently approved and emerging treatment options for osteoporosis and discuss these in light of the benefit these would gain from advanced targeting. In addition, established targeting strategies are reviewed and novel opportunities as well as promising areas are presented along with pharmaceutical strategies how to render novel composites consisting of a drug and a targeting moiety responsive to bone-specific or disease-specific environmental stimuli. Successful implementation of these principles into drug development programs for osteoporosis will substantially contribute to the clinical success of anti-catabolic and anabolic drugs of the future.
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