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Scientific research has focused its attention on finding an alternative route to systemic oral and parenteral administration, to overcome their usual drawbacks, such as hepatic first-pass which decreases drug bioavailability after oral administration, off-target effects, low patient compliance and low speed of onset of the pharmacological action in first-aid cases. Innovative drug delivery systems (DDS), mainly based on polymer and lipid biocompatible materials, have given a great prompt in this direction in the last years. The intranasal (IN) route of administration is a valid non-invasive alternative. It is highly suitable for self-administration, the drug quickly reaches the bloodstream, largely avoiding the first pass effect, and can also reach directly the brain bypassing BBB. Association of IN route with DDS can thus become a winning strategy for the controlled delivery of drugs, especially when a very quick effect is desired or needed. This review aims at analyzing the scientific literature regarding IN-DDS and their different ways of administration (systemic, topical, pulmonary, nose-to-brain). In particular, attention was devoted to polymer- and lipid-based micro- and nanocarriers, being the topic of most published articles in the last decade, but the whole plethora of colloidal DDS investigated in recent years for IN administration was presented.

Nowadays, a combinatorial drug delivery system that simultaneously transports two or more drugs to the targeted site in a human body, also recognized as a dual-drugs delivery system, represents a promising strategy to overcome drug resistance. Solid lipid nanoparticles loaded with clotrimazole (CLZ) and alphalipolic acid (ALA), considered as an effective agent in the reduction of reactive oxygen species, can enhance anti-infective immunity being proposed as a non-toxic and mainly non-allergic dual-drugs delivery system. In this study, uncoated and cationic CLZ-ALA-loaded SLN were prepared and compared. Suspensions with a narrow size distribution of particles of mean size below 150 nm were obtained, having slight negative or highly positive zeta potential values, due to the presence of the cationic lipid, which also increased nanoparticles stability, as confirmed by Turbiscan® results. Calorimetric studies confirmed the rationale of separately delivering the two drugs in a dual-delivery system. Furthermore, they confirmed the formation of SLN, without significant variation in presence of the cationic lipid. In vitro release studies showed a prolonged drug release without the occurrence of any burst effect. In vitro studies performed on 25 strains of Candida albicans showed the antimicrobial drug activity was not altered when it was loaded into lipid nanoparticles. The study has proved the successfully encapsulation of CLZ and ALA in solid lipid nanoparticles that may represent a promising strategy to combine ALA protective effect in the treatment with CLZ., Competing Interests: Declaration of Competing Interest The authors declare no conflict of interest., (Copyright © 2020 The Authors. Published by Elsevier B.V. All rights reserved.)

The nasal route has received a great deal of attention as a convenient and reliable method for the brain target on administration of drugs. When drugs are loaded into nanoparticles (NPs) the interaction with mucosa transports directly into the brain, skipping the blood-brain barrier and achieving rapid cerebrospinal fluid levels. Poly-lactic acid (PLA), poly-lactic-co-glycolic acid (PLGA), and chitosan (CS) were chosen to prepare NPs. After optimization of CS nanocarriers, our goal was to evaluate the different type of NPs uptake into olfactory ensheathing cells (OECs). We then correlated obtained biological data to zeta potential measurements of cells treated with NPs. Rodhamine-loaded NPs were used to study the uptake of OECs carried out by confocal microscopy at different times (1, 2, and 4 h). Our results showed that uptake of rodhamine-NPs by OECs was time dependent and it was influenced by the carrier charge. Confocal imaging of OECs demonstrated that NPPLGA showed a higher increase in uptake compared with NPPLA and NPCS after 1 h and it increased at 2-4 h. Zeta potential values of treated cells were more amplified with respect to untreated cells. The highest values were showed by unloaded NPPLGA, confirming microscopy data., (© 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.)

Introduction: Idebenone (IDE) is an antioxidant compound, structurally related to coenzyme Q10. Its therapeutic potential is growing in different application areas, as demonstrated by the number of experimental works and patents produced in very recent years., Areas Covered: Cyclodextrin inclusion complexes, liposomes, microemulsions, prodrugs, polymeric and lipid nanoparticles have been explored to achieve different goals, such as topical administration, brain targeting or increasing the bioavailability of this highly lipophilic drug. This review summarizes the results of works published in the last 20 years for the delivery and targeting of this drug., Expert Opinion: A direct comparison of the different carrier systems is not easy and could not even be significant, due to the large variables existing among them. However, the different forms of delivery can help increase idebenone solubility, stability and biochemical activity. Further studies will be developed in order to improve the controlled release and targeting of idebenone.

Poly(3-hydroxybutyrate-co-epsilon-caprolactone) copolymers and poly(3-hydroxybutyrate-co-3-hydroxyvalerate-co-epsilon-caprolactone) terpolymers were used by a solvent deposition technique to prepare either micro- or nanoparticles. In particular, the synthesis and analytical characterization of the terpolymers were described.On the basis of copolymer composition and properties, either micro- or nanoparticles were obtained; nanoparticle size was below 500 nm for the suspensions obtained from P(HB-co-CL) copolymers, and even smaller (200-300 nm) for those obtained using terpolymers. Particle size showed only a limited tendency to increase during storage, suggesting a good chemical and physical stability in the short-term storage at room temperature. Some copolymers produced hetero-dispersed microparticles under the same conditions, with a mean size between 10 and 30 microm. These systems showed a tendency to aggregate upon storage at room temperature.The nanoparticles showed a negative surface charge (around -20 mV for those prepared using an UltraTurrax and about -5 mV for those prepared by magnetic stirring). After storage at 4 degrees C the surface charge tend to decrease and these changes have been explained in terms of a partial hydrolysis of the polymeric matrix in aqueous suspension, which led to a change of chemical composition at the surface of the particles.The fluorescent probes calcein and Oil Red O were encapsulated in these systems as models of a hydrophilic and lipophilic drug molecule, respectively. Encapsulation efficiency and in vitro release profiles were studied to evaluate the effect of copolymer properties, such as molecular weight and composition, on their behaviour as potential materials to prepare controlled drug delivery carriers. Calcein was generally better encapsulated (up to 100%) than Oil Red O (10-30%); however, the zeta-potential measurement and in vitro release experiments suggested that a large amount of calcein was adsorbed onto the particle surface and was rapidly released within the first minutes of the test. Conversely, the lipophilic probe was dispersed within the polymeric matrix and its release profile from the nanoparticles was characterized by a considerable lag time (up to 8 h), followed by a slow and almost linear release.As a general trend, we observed that the composition and crystallinity of the tested polymers affected the type and size of obtained systems (micro- or nanoparticles), whereas the molecular weight mainly influenced the probes encapsulation and release.

In this work, positively charged nanocapsules have been developed for potential ocular delivery exploiting the deposition of PLA onto the droplet surface of a W/O nanoemulsion prepared by the reversed procedure of the PIT method. PLA in combination with different amounts of various oils and surfactants have been studied in order to select the best formulation for polymeric nanocapsule preparation. The traditional visual observation together with the Turbiscan ® technology were exploited in order to identify the best combination of polymer/oil for nanocapsule preparation. Two different primary surfactants (Span ® 60 and Span ® 80) have been tested to select their influence on the field of existence of the nanoemulsion by the construction of the pseudoternary phase diagrams. Cationic hybrid NC have been prepared by the addition of a coating layer of DDAB. The physico-chemical and morphological properties of all the prepared nanocapsules have been evaluated and compared by PCS, DSC and AFM. Therefore, positively charged nanocapsules can be easily prepared by a simple eco-friendly technique that exploits biocompatible materials avoiding a large input of mechanical energy as a potential ocular delivery systems for hydrophilic compounds or gene materials. [ABSTRACT FROM AUTHOR]