Versatile Nanoparticulate Systems as a Prosperous Platform for Targeted Nose-Brain Drug Delivery.

The intranasal route has proven to be a reliable and promising route for delivering therapeutics to the central nervous system (CNS), averting the blood-brain barrier (BBB) and avoiding extensive first-pass metabolism of some drugs, with minimal systemic exposure. This is considered to be the main problem associated with other routes of drug delivery such as oral, parenteral, and transdermal, among other administration methods. The intranasal route maximizes drug bioavailability, particularly those susceptible to enzymatic degradation such as peptides and proteins. This review will stipulate an overview of the intranasal route as a channel for drug delivery, including its benefits and drawbacks, as well as different mechanisms of CNS drug targeting using nanoparticulate drug delivery systems devices; it also focuses on pharmaceutical dosage forms such as drops, sprays, or gels via the nasal route comprising different polymers, absorption promoters, CNS ligands, and permeation enhancers.

"Review of strategic methods for encapsulating essential oils into chitosan nanosystems and their applications".

Essential oils (EOs) are hydrophobic, concentrated extracts of botanical origin containing diverse bioactive molecules that have been used for their biomedical properties. On the other hand, the volatility, toxicity, and hydrophobicity limited their use in their pure form. Therefore, nano-encapsulation of EOs in a biodegradable polymeric platform showed a solution. Chitosan (CS) is a biodegradable polymer that has been intensively used for EOs encapsulation. Various approaches such as homogenization, probe sonication, electrospinning, and 3D printing have been utilized to integrate EOs in CS polymer. Different CS-based platforms were investigated for EOs encapsulation such as nanoparticles (NPs), nanofibers, films, nanoemulsions, 3D printed composites, and hydrogels. Biological applications of encapsulating EOs in CS include antioxidant, antimicrobial, and anticancer functions. This review explores the principles for nanoencapsulation strategies, and the available technologies are also reviewed, in addition to an in-depth overview of the current research and application of nano-encapsulated EOs.

The potential of carbon-based nanomaterials in hepatitis C virus treatment: a review of carbon nanotubes, dendrimers and fullerenes.

HCV, hepatitis C virus, is a virus that causes damage to the liver. Both chronic infection or lack of treatment increase morbidity except if it is an acute infection, as the body clears the virus without any intervention. Also, the virus has many genotypes, and until now, there has yet to be a single treatment capable of affecting and treating all these genotypes at once. This review will discuss the main and most used old treatments, IFN-a, PEG IFN-a, Ribavirin, Celgosvir, and sofosbuvir alone and with the combination of other drugs and their drawbacks. They should be given in combination to improve the effect on the virus compared with being administrated independently, as in the case of sofosbuvir. For these reasons, the need for new treatments and diagnostic tools arises, and the rule of nanotechnology comes here. The role of carbon nanotubes, dendrimers, and fullerenes will be discussed. CNTs, carbon nanotubes, are one-dimensional structures composed of a cylindrical sheet of graphite and are mainly used for diagnostic purposes against HCV. Dendrimers, three-dimensional highly branched structures, are macromolecules that provide better drug delivery and treatment options due to their unique structure that can be modified, producing versatile types; each has unique properties. Fullerenes which are cage like structures derived and closely related to CNTs, and composed of carbon atoms that can be substituted by other atoms which in return open unlimited usage for these carbon based materials. Fullerenes rule is unique since it has two mechanisms that prevent the virus from binding and acting on the virus-replicating enzyme. However, their charge needs to be determined; otherwise, it will lead to cytotoxicity. Lastly, no review has been done on the role of nanotechnology against HCV yet.

Antibacterial and antioxidant properties of Cichorium intybus extract embedded in chitosan nanocomposite nanofibers.

Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) bacteria acquired serious bacterial resistance against antibiotics. Untreated dangerous infections can cause death. We proposed nanofibers (NFs) of Polyvinyl alcohol (PVA)/Chitosan (CS) nanocomposite embedded with Chicory root extract (CRE) as a safe solution. We determined the best extraction solvent and drying method, 70 % ethanol and freeze-drying, respectively. We investigated the optimal electrospinner parameters for a smooth PVA/CS NFs. Finally, we discovered PVA/CS/CRE-50 mg (F4) to be the most effective antibacterial and antioxidant CRE concentration. Interestingly, it was found that ethanolic extract had the highest yield % at 24.7 % with Total Phenolic Contents (TPC) of 4 mg Gallic Acid Equivalent (GAE)/1 g, 80 % antioxidant activity at 25 mg with an IC50 of 4.15 mg/mL and a Minimum Bactericidal Concentration (MBC) of 100 mg against S. aureus and 25 mg against E. coli. Remarkably, F4 NFs had an IC50 33.32 mg/mL, Entrapment Efficiency 64.89 %, Loading Capacity 4.41 %, obeying Noyes-Whitney release model. F4 had an MBC of 2 mg with both bacterial strains, which proved to be potent antibacterial material that surpasses the pure extract 50 times. F4 has also shown an extraordinary antioxidant activity that exceeds PVA/CS NF activity 23 times.

Green tea essential oil encapsulated chitosan nanoparticles-based radiopharmaceutical as a new trend for solid tumor theranosis.

The existing study is embarked on investigating the antineoplastic activity of green tea essential oil (GTO) as a natural product. In this regard, GTO was encapsulated in cationic chitosan, nitrogenous-polysaccharide derived by partial deacetylation of chitin, nanoparticles (CS NPs) with entrapment efficiency (EE%) of 81.4 ± 5.7% and a mean particle-size of 30.7 ± 1.13 nm. Moreover, the cytotoxic effect of CS/GTO NPs was evaluated versus human liver (HepG-2), breast (MCF-7) and colon (HCT-116) cancer cell-lines and exhibited a positive impact when compared to bare CS NPs by 3, 2.3 and 1.7 fold for the three cell lines, respectively. More interestingly, CS/GTO NPs were complexed with technethium-99m (99mTc) radionuclide. With a view to achieve a successful radiolabeling process, different parameters were optimized resulting in a radiolabeling efficiency (RE%) of 93.4 ± 1.2%. Radiopharmacokinetics of the radiolabeled NPs in healthy mice demonstrated a reticuloendothelial system (RES) evading and long blood circulation time up to 4 h. On the other hand, the biodistribution profile in solid tumor models showed 20.3 ± 2.1% localization and cancer cell targeting within just 30 min. On the whole, the reported results encourage the potential use of CS/GTO NPs as a side effect-free anticancer agent and its 99mTc-analogue as a novel CS/GTO NPs-based diagnostic-radiopharmaceutical for cancer.

Applying Box-Behnken Design for Formulation and Optimization of PLGA-Coffee Nanoparticles and Detecting Enhanced Antioxidant and Anticancer Activities.

In an attempt to prove biological activity enhancement upon particle size reduction to the nanoscale, coffee (Cf) was chosen to be formulated into poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) using the single emulsion-solvent evaporation (SE-SE) method via Box-Behnken Design (BBD) to study the impact of certain process and formulation parameters on the particle size and size homogeneity, surface stability and encapsulation efficiency (EE%). The coffee-loaded PLGA (PLGA-Cf) NPs were characterized by different methods to aid in selecting the optimum formulation conditions. The desirable physicochemical characteristics involved small particle sizes with an average of 318.60 ± 5.65 nm, uniformly distributed within a narrow range (PDI of 0.074 ± 0.015), with considerable stability (Zeta Potential of -20.50 ± 0.52 mV) and the highest EE% (85.92 ± 4.01%). The antioxidant and anticancer activities of plain PLGA NPs, pure Cf and the optimum PLGA-Cf NPs, were evaluated using 2,2-Diphenyl-1-picryl-hydrazyl (DPPH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays, respectively. As a result of nano-encapsulation, antioxidant activity was enhanced by 26.5%. Encapsulated Cf showed higher anticancer potency than pure Cf against different cancerous cell lines with an increase of 86.78%, 78.17%, 85.84% and 84.84% against MCF-7, A-549, HeLa and HepG-2, respectively. The in vitro release followed the Weibull release model with slow and biphasic release profile in both tested pH media, 7.4 and 5.5.

Essential oil loaded pectin/chitosan nanoparticles preparation and optimization via Box-Behnken design against MCF-7 breast cancer cell lines.

In the continuous search for effective cancer treatments, we here report a novel anticancer nanoparticulate system composed of jasmine oil (JO), an essential oil with proven anticancer activity and pectin/chitosan composite nanoparticles (Pec/CS NPs) as encapsulating materials to overcome JO's solubility and sensitivity problems using a green ionotropic gelation method. Pec/CS/JO NPs were formulated using Box-Behnken design (BBD) to estimate the interactions and effects of studied formulation variables on particle size, zeta potential and encapsulation efficiency to develop an optimized Pec/CS nanoformulation. The nano-encapsulation system preserved the consistency of total phenolic contents in JO and amended its thermal stability by 1.64 fold. The antioxidant potency of JO was enhanced after encapsulation by 96.28%. Consequently, the cytotoxic activity of bare Pec/CS NPs, pure JO and encapsulated JO in Pec/CS NPs against (MCF-7) breast cancer cells and (L-929) normal cells was evaluated using MTT assay. Encapsulated JO was more potent than pure JO with ≈13 fold improvement in anticancer activity, whereas the cell viability of normal cells wasn't affected but was rather enhanced when treated with Pec/CS NPs.

Comparative study of encapsulated peppermint and green tea essential oils in chitosan nanoparticles: Encapsulation, thermal stability, in-vitro release, antioxidant and antibacterial activities.

Essential oils (EOs) such as Peppermint oil (PO) and Green Tea oil (GTO) have extensively been reported for their nutritional and biomedical properties. To overcome the sensitivity of EOs to the environmental conditions, nano-encapsulation has emerged as a method to address this limitation. In this work, PO and GTO were encapsulated in chitosan nanoparticles (CS NPs) following emulsification/ionic gelation method. The nano-encapsulated PO (CS/PO NPs) and GTO (CS/GTO NPs) were fully characterized by various methods. Spherical NPs with an average size range of 20-60 nm were revealed by TEM for both systems. The loading capacity reached 22.2% and 23.1%, for PO and GTO, respectively, and the in-vitro release followed a Fickian behavior in different buffer systems. The TGA thermograms of both nano-encapsulated EOs showed an increase in the temperature of maximum degradation rate up to 350 °C. The nano-encapsulation maintained the stability of the total phenolic contents in both EOs, improved the antioxidant activity by ~2 and 2.4-fold for PO and GTO respectively. Surprisingly, the antibacterial activity of CS/GTO NPs was more potent than CS/PO NPs and especially against Staphylococcus aureus with ~9.4 folds improvement compared to pure GTO, and ~4.7 fold against Escherichia coli.