PH-sensitive vesicles, polymeric micelles, and nanospheres prepared with polycarboxylates

Polymeric micelles for nano-scale drug delivery

Anti-CD22 Antibody Targeting of pH-responsive Micelles Enhances Small Interfering RNA Delivery and Gene Silencing in Lymphoma Cells

Bioavailability of the colloidal particles is of great concern. It is because about 40% of the newly discovered colloidal agents are poorly water soluble and thus poorly bioavailable. Various colloidal technologies have been adopted to enhance the bioavailability of such drugs. In this review, advanced colloidal technologies are discussed to understand the mechanism of bioavailability enhancement of drugs, coding latest references from the literature. Additionally, advantages and disadvantages of the concerned colloidal technologies are discussed to understand the potential usage of each process. All these colloidal technologies effectively enhance the bioavailability of poorly bioavailable drugs, either by protecting them from the environment of the gastrointestinal or by prolonging their intended therapeutic effect. Furthermore, complexation of the drug molecule with potential carries, particle size reduction to nanoscale, co-crystallization and self-emulsifying drug delivery system are also discussed which not only enhance the bioavailability but also reduce the potential toxicities of the loaded drugs. It is therefore important to understand the vital colloidal technologies with their recent advancements, potential applications and future challenges, which is discussed in this review. Finally, this article concludes that the advanced colloidal technologies, including freeze-dried liposome, solid lipid nanoparticle, polymeric nanoparticle (polymeric micelles), dendrimers and solid emulsifying drug delivery systems, have the potential to achieve improved bioavailability and targeted drug delivery.

Revolutionizing drug delivery: The power of stimulus-responsive nanoscale systems

This paper describes a flexible model that can be used to simulate laser-based photoactivation of drug delivery systems. It considers Gaussian beams for the excitation while the heat diffusion equation is solved by use of the finite element method. As an example, a typical liposome geometry in the focal volume of a laser beam is simulated and the results are compared with experimental data obtained in the literature, showing a good agreement. The model has potential in the design of drug delivery systems as it can be a starting point for the development of new kinds of micro- and nano-scale drug delivery systems.

IntroductionWith all of the developments on infectious diseases, tuberculosis (TB) remains a cause of death among people. One of the most promising assembly techniques in nano-technology is “scaffolded DNA origami” to design and construct a nano-scale drug delivery system. Because of the global health problems of tuberculosis, the development of potent new anti-tuberculosis drug delivery system without cross-resistance with known anti-mycobacterial agents is urgently needed. The aim of this study was to design a nano-scale drug delivery system for TB treatment using the DNA origami methodMethodsIn this study, we presented an experimental research on a DNA drug delivery system for treating Tuberculosis. TEM images were visualized with an FEI Tecnai T12 BioTWIN at 120 kV. The model was designed by caDNAno software and computational prediction of the 3D solution shape and its flexibility was calculated with a CanDo server.ResultsSynthesizing the product was imaged using transmission electron microscopy after negative-staining by uranyl formate.ConclusionWe constructed a multilayer 3D DNA nanostructure system by designing square lattice geometry with the scaffolded-DNA-origami method. With changes in the lock and key sequences, we recommend that this system be used for other infectious diseases to target the pathogenic bacteria.

: Polymer micelles are nanoscale drug delivery systems that have the potential to improve breast tumor treatment. Micelles can increase the half-life and solubility of drugs, as is the case with beta-lapachone (beta-lap), a novel anticancer agent which is bioactivated by the enzyme NQO1, found overexpressed in tumors. They can also be fitted with tumor-specific ligands, and can be tracked in vivo through incorporation of an imaging moiety. The ultimate goal of the study was to develop beta-lap PEG-PLA micelles as novel nanotherapeutics for the treatment of breast tumors. Quantum dots (QD) were incorporated into micelles for purposes of image trackability. Micelles were characterized using 1H-NMR, TEM, and DLS. The in vitro and in vivo antitumor efficacy of the micelles was also examined. Beta-lap micelles were found to be small in size, and showed adequate cell-killing potential in vitro. In vivo studies showed that the micelles suppressed tumor growth for ~2 months, with minimal toxicity. QDs were successfully incorporated into micelles, yielding micelles of small size that retained fluorescence. Cell lines treated in vitro with the QD-micelles demonstrated slow and continuous uptake of micelles, found accumulated in the cytoplasm. Future studies involve the addition of a cRGD ligand to the surface of micelles to increase cellular uptake and yield multifunctional micelles.

Polymeric micelles, originating from the self-assembly of amphiphilic block copolymers, presenting a lipophilic core and hydrophilic shell, are widely used as nanoscale drug-delivery systems. In the present study, the functional nanosized FTY720-loaded polymeric micelles (NP@FTY720) were constructed via covalent attachment of the terminal carboxy group of poly(ethylene glycol) (PEG) with FTY720 through an amide bond linker. FTY720 was embedded into the PEG core, which ensures high stability of the nanoparticle and significantly reduces nonspecific protein adsorption. The micellar system was characterized by good stability in a neutral environment and effective drug release in the lysosomal environment within cells. This enables NP@FTY720 to promote microglial M1 to M2 polarization in H2O2-induced BV2 microglia without apparent toxicity in vitro. Importantly, NP@FTY720 through intravenous administration accumulated at hemorrhagic sites and responsively released therapeutic FTY720 to exert neuroprotective roles following ICH in mice, which was involved in microglial M2 polarization and inflammation reduction. Taken in concert, our results suggest that the self-assembled FTY720-loaded polymeric micelles may represent a promising nanoformulation for intracerebral hemorrhage (ICH) treatment.

To reduce premature drug release while ensuring burst intracellular drug release of solid lipid nanoparticle-based drug delivery system with clathrin modification

Luteolin (Lu) is a naturally occurring flavonoid compound with a diverse array of pharmacological activities, including anti-tumor, anti-inflammatory, antibacterial, and neuroprotective properties. However, the therapeutic efficacy and clinical application of Lu are significantly hindered by inherent limitations, such as poor water solubility, short half-life, low bioavailability, and potential off-target toxicity. Recent studies have demonstrated that the utilization of nanocarriers presents a promising strategy to enhance the solubility of Lu, prolong its circulation time, and improve its targeting ability. Despite numerous reviews over the past few decades having focused on the source, pharmacological activities, and molecular mechanisms of Lu, there exists a conspicuous gap in the literature regarding a comprehensive review of Lu-loaded nanoformulations and their applications. To address this gap, we present an exhaustive overview of the advancements and applications of nano-scale drug delivery systems specifically designed for Lu. These platforms encompass micelles, nanocarrier-based systems, emulsified drug delivery systems, and vesicular drug delivery systems. We provide detailed insights into the synthetic materials, preparation methods, physicochemical properties, and significant outcomes associated with these nanoformulations. This systematic review will be particularly valuable to researchers seeking novel avenues in the field of nano-delivery strategies and exploring the potential clinical applications of Lu.

Polymeric mixed micelles as nanomedicines: Achievements and perspectives

Advancements of nanoscale drug formulations for combination treatment of colorectal cancer.

Psoriasis is a typical dermal condition that has been anticipated since prehistoric times when it was mistakenly implicit in being a variant of leprosy. It is an atypical organ-specific autoimmune disorder, which is triggered by the activation of T-cells and/or B-cells. Until now, the pathophysiology of this disease is not completely explicated and still, many research investigations are ongoing. Different approaches have been investigated to treat this dreadful skin disease using various anti-psoriatic drugs of different modes of action through smart drug-delivery systems. Nevertheless, there is no ideal therapy for a complete cure of psoriasis owing to the dearth of an ideal drug-delivery system for anti-psoriatic drugs. The conventional pharmacotherapy approaches for the treatment of psoriasis demand various classes of anti-psoriatic drugs with optimum benefit/risk ratio and insignificant untoward effects. The advancement in nanoscale drug delivery had a great impact on the establishment of a nanomedicine-based therapy for better management of psoriasis in recent times. Nanodrug carriers are exploited to design and develop nanomedicine-based therapy for psoriasis. It has a promising future in the improvement of the therapeutic efficacy of conventional anti-psoriatic drugs. The present manuscript aims to discuss the pathophysiology, conventional pharmacotherapy, and contemporary research in the area of nanoscale topical drug delivery systems for better management of psoriasis including the significance of targeted pharmacotherapy in psoriasis.

The emergence of nanoscale drug delivery systems provides new opportunities for targeting the delivery of chemotherapeutic drugs and has achieved excellent results. In recent years, with the rise in the concept of intelligent drug delivery systems, the design and preparation of carriers have become more and more complicated, which is not conducive to clinical transformation. Researchers are gradually focused on biomimetic nanoscale drug delivery systems, trying to combine the physicochemical properties of nanoscale carriers with the natural biological functions of endogenous substances, so as to boost tumor targeting delivery. In this article, we first classify and introduce biomimetic nanoscale drug delivery systems, and then emphasize their unique biological functions. The biomimetic nanoscale drug delivery systems have the advantages of simple preparation, powerful functions, and low immunogenicity, having a good application prospect.

Paclitaxel (PTX) is usual for the treatment of a variety of malignancies, however, its applications are greatly limited due to its poor water solubility. Over the past years, there has been a considerable research interest in the area of nanoscale drug delivery systems (DDSs) as carrier for PTX due to their solubilization, safety, targeting and controlled release. There are many different types and shapes of nanoscale DDSs that have been prepared to deliver PTX, including nanoliposome, lipid nanoemulsion, nanosuspension, nanocapsule, nanofiber, nanotube, nanopolymersome, micelle and nanoparticle (NP). Nanoscale DDSs can be based on lipids, proteins, polysaccharides, polymers or other materials. The recent strategic developments of PTX formulation have been discussed with emphasis on lipid-, polymer- and protein-based nanoscale DDSs. Here we focus on the comparative analysis of the preparation, morphology, solubilization, targeting, penetrability, controllability and efficacy profile of various PTX-loaded nanoscale DDSs, which were reported in the different researches. Meanwhile the advantages and disadvantages are also discussed for each type of DDS. Furthermore, the current review embodies an in-depth discussion of human serum albumin (HSA) NP formulation, which showed significantly great efficacy and low toxicity. All the information obtained in this review might shed light on designing new and better nanoscale PTX formulations for potential anticancer applications in the clinic.