The emerging science of nanotechnology sparked a research attention in its potential benefits in comparison to the conventional materials used. Oral products prepared via nanoparticles (NPs) have garnered great interest worldwide. They are used commonly to incorporate nutrients and provide antimicrobial activity. Formulation into NPs can offer opportunities for targeted drug delivery, improve drug stability in the harsh environment of the gastrointestinal (GI) tract, increase drug solubility and bioavailability, and provide sustained release in the GI tract. However, some issues like the management of toxicity and safe handling of NPs are still debated and should be well concerned before their application in oral preparations. This article will help the reader to understand safety issues of NPs in oral drug delivery and provides some recommendations to the use of NPs in the drug industry.

Bortezomib (BTZ) as an anticancer drug has been used through the injection pathway. Two types of Cyclodextrin nanosponges (CDNSs) were synthesized and studied by DLS, TEM, FTIR, and DSC instruments...

Lipid-based nano-drug delivery systems (LBNDDSs) have gained widespread attention in oral drug delivery due to their tunable and versatile properties such as biocompatibility and biodegradability, ...

Purpose: Intestinal drug absorption is one of the main factors that govern the fraction of oral dose absorbed (F_a) of drugs. It is reported that oral absorption of BTZ can be restricted by its low intestinal permeability. In this study, we aimed to evaluate the impact of self-nanoemulsifying drug delivery systems (SNEDDS) on the intestinal absorption and F_a of BTZ. Methods: Intestinal permeability studies were conducted using in situ single-pass intestinal perfusion (SPIP) technique in rats. Human intestinal absorption (P_{eff (Human)}) and F_a values of BTZ and BTZ-SNEDDS were predicted based on SPIP data. Results: Based on the obtained data, P_{eff (rat)} values of (3.36 ± 0.5) × 10⁻⁵ and (8.9 ± 3) × 10⁻⁵ cm/sec (mean ± SEM) were calculated for BTZ and BTZ-SNEDDS, respectively. Meanwhile, P_{eff (human)} values of (7 × 10⁻⁵) and (68 × 10⁻⁵) cm/sec were predicted for BTZ and BTZ-SNEDDS, respectively. Besides, F_{a (human)} values of 72.5% and 97% were estimated for BTZ and BTZ-SNEDDS, respectively. Conclusions: According to the obtained data, it is concluded that SNEDDS can be considered as a promising drug delivery system to improve the intestinal absorption and F_a values of BTZ.

MRNA technology has demonstrated potential for use as an effective cancer immunotherapy. However, inefficient in vivo mRNA delivery and the requirements for immune co-stimulation present major hurdles to achieving anti-tumour therapeutic efficacy. Therefore, we used a cationic hyper-branched cyclodextrin-based polymer to increase mRNA delivery in both in vitro and in vivo melanoma cancer. We found that the transfection efficacy of the mRNA-EGFP-loaded Ppoly system was significantly higher than that of lipofectamine and free mRNA in both 2D and 3D melanoma cancer cells; also, this delivery system did not show cytotoxicity. In addition, the biodistribution results revealed time-dependent and significantly higher mEGFP expression in complexes with Ppoly compared to free mRNA. We then checked the anti-tumour effect of intratumourally injected free mRNA–OVA, a foreign antigen, and loaded Ppoly; the results showed a considerable decrease in both tumour size and weight in the group treated with OVA-mRNA in loaded Ppoly compared to other formulations with an efficient adaptive immune response by dramatically increasing most leukocyte subtypes and OVA-specific CD8+ T cells in both the spleen and tumour tissues. Collectively, our findings suggest that the local delivery of cationic cyclodextrin-based polymer complexes containing foreign mRNA antigens might be a good and reliable concept for cancer immunotherapy.

In this article, we used monolayer two dimensional (2D) and 3D multicellular spheroid models to improve our understanding of the gene delivery process of a new modified cationic hyper-branched cyclodextrin-based polymer (Ppoly)-loaded plasmid encoding Enhanced Green Fluorescent Protein (EGFP). A comparison between the cytotoxicity effect and transfection efficiency of the plasmid DNA (pDNA)-loaded Ppoly system in 2D and 3D spheroid cells determined that the transfection efficiency and cytotoxicity of Ppoly–pDNA nanocomplexes were lower in 3D spheroids than in 2D monolayer cells. Furthermore, histopathology visualization of Ppoly–pDNA complex cellular uptake in 3D spheroids demonstrated that Ppoly penetrated into the inner layers. This study indicated that the Ppoly, as a non-viral gene delivery system in complex with pDNA, is hemocompatible, non-toxic, high in encapsulation efficiency, and has good transfection efficiency in both 2D and 3D cell cultures compared to free pDNA and lipofectamine (as the control).