OCTAVIO DIEZ SALES

University of Valencia | UV · Department of Pharmacy and Pharmaceutical Technology

Introduction: Borderline medical devices are products in a "gray area", this means due to their characteristics, they could belong to different "legal products". In addition, regulation is a controversial topic and may change depending on the country which may put public health at risk and distort the market. Areas covered: This article analyzes...

The aims of this study were to evaluate the feasibility of a nortriptyline (NT) formulation for transdermal administration and to assess the usefulness of an estimated kinetic parameter (kout) using the in vitro infinite dose technique to predict in vivo plasma levels when used in combination with pharmacokinetic parameters. To do so, a simple one-...

Objective: To compare the measures taken by the European Union, Switzerland and the United Kingdom to ensure the continuity of the medical devices market, complying with the requirements of Regulation 2017/745. Method: To carry out this work, a review was made of the official websites of the European Commission, the Spanish Agency for Medicines...

In the present study, canthaxanthin was produced by biofermentation from Dietzia natronolimnaea HS-1 (D. natronolimnaea) and was loaded in phospholipid vesicles prepared with natural component using an easy and low dissipative method. Indeed, glycerosomes, hyalurosomes, and glycerohyalurosomes were prepared by direct hydration of both phosphatidylc...

Pistacia lentiscus L. is a sclerophyllous shrub capable of growing under harsh climatic conditions especially in the Mediterranean Basin. Different products can be obtained from this plant, such as essential oil, mastic gum or even fixed oil. The last is well known for its flavor which is mainly exploited in the food industry. Additionally, it has...

Aim: Collagen-enriched transfersomes, glycerosomes and glytransfersomes were specifically tailored for skin delivery of oleuropein. Methods: Vesicles were prepared by direct sonication and their main physicochemical and technological properties were measured. Biocompatibility, protective effect and promotion of the healing of a wounded cell monolay...

Objective: The objective of this article is to review the quality equirements and recommended uses of the different types of face masks with a view to helping optimize their use and facilitating identification of nonconforming products. Method: A literature search was conducted in PubMed, the Spanish Official State Gazette and Eudralex. The webs...

This article is focused on evaluating the rheological properties of tomato ketchup. The purpose of the paper was to show the importance of knowledge about the rheological properties of ketchup and to find new more adequate equations of the temperature-viscosity dependence. All measurements were performed under the same temperature conditions at app...

This work aimed at developing a mouthwash based on liposomes loading Citrus limon var. pompia essential oil or citral to treat oropharyngeal diseases. Vesicles were prepared by dispersing phosphatidylcholine and pompia essential oil or citral at increasing amounts (12, 25 and 50 mg/mL) in water. Transparent vesicle dispersions were obtained by dire...

Aim: The moisturizing properties of glycerol, the penetration enhancing capability of propylene glycol and the bioadhesive properties of mucin were combined to improve the carrier capabilities of transfersomes and the efficacy of mangiferin in the treatment of skin lesions. Materials & methods: Mangiferin was incorporated in transfersomes and glyco...

Hair loss affects a large number of people worldwide and it has a negative impact on the quality of life. Despite the availability of different drugs for the treatment of hair disorders, therapeutic options are still limited and scarcely effective. An innovative strategy to improve the efficacy of alopecia treatment is presented in this work. Finas...

Mangiferin, a natural compound isolated from Mangifera indica L, was incorporated in glycerosomes, ethosomes and alternatively in glycerol-ethanol phospholipid vesicles (glycethosomes). Actually, only glycethosomes were able to stably incorporate the mangiferin that was loaded at increasing concentrations (2, 4, 6, 8 mg/mL). The morphology, size di...

A new class of biocompatible and scalable phospholipid vesicles was developed, aiming at improving the efficacy of baicalin on the skin. Phosphatidylcholine and baicalin (a natural polyphenol) were hydrated in two steps with a mixture of ethanol, glycerol, and propylene glycol at different ratios, and a low amount of water (4%). Hence, water was al...

In this paper mangiferin nanoemulsions were developed using hyaluronic acid of different molecular weight, in absence or presence of Transcutol-P. An extensive study was carried out on the physico-chemical properties of nanoemulsions. Nanosizer and transmission electron microscopy showed oil droplets average size 296 nm with monodisperses distribut...

Periodontal diseases are inflammatory disorders caused primarily by dental plaque microorganisms that even may need surgery to remove damaged tissue. Adhesive biocompatible films may be an adequate form in order to improve drug retention or prevent microbial infections by covering the surgical site. In recent years, much attention has been focused...

The present study aimed at developing a new vesicular formulation capable of promoting the protective effect of ascorbic acid and tocopherol against intestinal oxidative stress damage, and their efficacy in intestinal wound healing upon oral administration. A pH-dependent copolymer (Eudragit® L100), a water-soluble prebiotic fibre (Nutriose® FM06),...

0.5–1% of the world's population is affected by vitiligo, a disease characterized by a gradual depigmentation of the skin. Baicalin and berberine are natural compounds with beneficial activities, such as antioxidant, anti-inflammatory and proliferative effects. These polyphenols could be useful for the treatment of vitiligo symptoms, and their effi...

Aiming at improving the protective effects of baicalin on the skin, new highly-biocompatible penetration enhancer containing vesicles (PEVs) were developed by modifying the base formulation of transfersomes with sorbitol, thus obtaining sorbitol-PEVs. An extensive evaluation of the physico-chemical features of both transfersomes and sorbitol-PEVs w...

Transfersomes were prepared by using different polysorbates (i.e., Tween 20, 40, 60 and 80) and loaded with tocopherol acetate, a naturally-occurring phenolic compound with antioxidant activity. The vesicles showed unilamellar morphology, small size (∼85 nm), low polydispersity index (≤0.27), and high entrapment efficiency, which increased as a fun...

Malnutrition is a common feature of chronic and acute diseases, often associated with a poor prognosis, including worsening of clinical outcome, owing, among other factors, to dysfunction of the most internal organs and systems affecting the absorption, metabolism and elimination of drugs and nutrients. Taurine is involved in numerous biological pr...

This chapter reviews alternative methods recommended for animal testing in various toxicological areas. An alternative model to achieve complete animal replacement for acute toxicity testing is not possible. Skin corrosion/irritation alternative methods have been validated and accepted. For eye irritation testing, no single method is able to replac...

Nutriosomes, new phospholipid nanovesicles specifically designed for intestinal protection were developed by simultaneously loading a water-soluble dextrine (Nutriose® FM06) and a natural antioxidant (curcumin). Nutriosomes were easily fabricated in a one-step, organic solvent-free procedure. The stability and the delivery performances of the vesic...

Ultradeformable liposomes were formulated using naringin (NA), a flavanone glycoside, at different concentrations (3, 6 and 9mg/mL). Nanovesicles were small size (∼100nm), regardless of the NA concentration used, and monodisperse (PI<0.30). All formulations showed a high entrapment efficiency (∼88%) and a highly negative zeta potential (around -30m...

Gellan nanohydrogel and phospholipid vesicles were combined to incorporate baicalin in new self-assembling core-shell gellan-transfersomes obtained by an easy, scalable method. The vesicles were small in size (~107nm) and monodispersed (P.I. ≤ 0.24), forming a viscous system (~ 24mPa/s) as compared to transfersomes (~ 1.6mPa/s), as confirmed by rhe...

Dentifrices are semi-solid products which are designed to clean the teeth and provide a fresh and pleasant breath. The attributes that initially attract consumers in the purchase of the toothpaste are: advertising and promotion, the design of its container and aroma given off when being used. But there are others that are also important: the rheolo...

Resveratrol and gallic acid, a lipophilic and a hydrophilic phenol, were co-loaded in innovative, biocompatible nanovesicles conceived for ensuring the protection of the skin from oxidative- and inflammatory-related affections. The basic vesicles, liposomes and glycerosomes, were produced by a simple, one-step method involving the dispersion of pho...

In this work, diclofenac was encapsulated, as sodium salt, in glycerosomes containing 10, 20 or 30% of glycerol in the water phase with the aim to ameliorate its topical efficacy. Taking into account previous findings, glycerosome formulation was modified, in terms of economic suitability, using a cheap and commercially available mixture of hydroge...

This work was aimed at finding an innovative vesicle-type formulation able to improve the bioavailability of curcumin upon oral administration. To this purpose, phospholipid, Eudragit® S100 and hyaluronan sodium salt were combined to obtain eudragit-hyaluronan immobilized vesicles using an easy and environmentally-friendly method. For the first tim...

The topical efficacy of baicalin, a natural flavonoid isolated from Scutellaria baicalensis Georgi, which has several beneficial properties, such as antioxidative, antiviral, anti-inflammatory and antiproliferative, is hindered by its poor aqueous solubility and low skin permeability. Therefore, its incorporation into appropriate phospholipid vesic...

New biocarriers, named santosomes, were formulated using Santolina insularis essential oil and hydrogenated phosphatidylcholine. They were modified by adding propylene glycol, a hydrophylic penetration enhancer, and loaded with phycocyanin, a protein found in cyanobacteria, which possesses antioxidant and antiinflammatory properties. The essential...

Liquorice extract, obtained by percolation in ethanol of Glycyrrhiza glabra L. roots, was incorporated in liposomes and hyalurosomes, new phospholipid-sodium hyaluronate vesicles, and their protective effect against oxidative stress skin damages was probed. As a comparison, raw glycyrrhizin was also tested. All the vesicles were small in size (≤100...

In this study, the effects of ethanol and/or diclofenac on vesicle bilayer structure have been studied. Liposomes with hydrogenated soy phosphatidylcholine, cholesterol and two different concentrations of diclofenac sodium (5 and 10 mg/ml) were obtained. In addition, ethanol was mixed in the water phase at different concentrations (5, 10 and 20 % v...

Polymers such as Hyaluronic acid (HA), Polyethylene glycol-400 (PEG-400) and Xanthan Gum (XG) are promising in drug delivery applicationsbecause of their biomedical and pharmaceutical potential applications. In HA 2%-PEG 400 systems, the effect of pH and PEG-400 concentration were evaluated. The viscosity of HA-PEG 400 formulations slightly increas...

Biocompatible quercetin nanovesicles were developed by coating polyethylene glycol-containing vesicles with chitosan and nutriose, aimed at targeting the colon. Uncoated and coated vesicles were prepared using hydrogenated soy phosphatidylcholine and quercetin, a potent natural anti-inflammatory and antioxidant drug. Physicochemical characterizatio...

Context: Quercetin (QUE) is a flavonoid with antioxidant/anti-inflammatory properties, poorly absorbed when orally administered. Objectives: To prepare chitosan/xanthan gum microparticles to increase QUE oral bioavailability and optimize its release in the colon. Materials and methods: Chitosan/xanthan gum hydrogel embedding QUE was spray-drie...

Purpose To develop quercetin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), and to investigate their efficacy on TPA-induced skin inflammation. Methods Vesicles were made from a mixture of phospholipids, quercetin and polyethylene glycol 400 (PEG), specifically added to increase drug solubility a...

Rheological creep and recovery tests have been applied at different assay times to xanthan gum hydrogels a several concentrations. The Burger model has been successfully applied to fit the creep data and to analyze results. Increasing the xanthan gum concentration also increases the elastic and viscous components without changing the molecular dist...

To develop quercetin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), and to investigate their efficacy on TPA-induced skin inflammation. Vesicles were made from a mixture of phospholipids, quercetin and polyethylene glycol 400 (PEG), specifically added to increase drug solubility and penetration t...

In the present work biocompatible quercetin and curcumin nanovesicles were developed as a novel approach to prevent and restore skin tissue defects on chronic cutaneous pathologies. Stable and suitable quercetin- and curcumin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), were prepared. Vesicles...

This study focuses on the extraction and isolation of a natural anti-inflammatory phycocyanin and its nanoformulation in innovative and efficient vesicular carriers able to improve its delivery to the skin. C-phycocyanin was successfully isolated from a commercial dry extract (AfaMax) of blue-green Klamath algae. Protein extraction and purity were...

Abstract The aim of this study was to evaluate the passive and iontophoretic permeation of triclosan in human skin using a triclosan solution and triclosan-loaded cationic nanospheres in order to determine which of the two strategies is more effective in allowing the deposition of triclosan within the skin. Triclosan-loaded nanospheres were prepar...

In this work we studied various nanoformulations of resveratrol in phospholipid vesicles. Conventional phophatidylcholine liposomes were prepared and characterized in parallel with PEVs (Penetration Enhancer-containing Vesicles) obtained by adding one of eight selected amphiphilic penetration enhancers (PEs; 0.2% w/v; HLB range 1-16) to the composi...

The purpose of this study was to develop a new delivery system capable of improving bioavailability and controlling release of hydrophilic drugs. Metformin-loaded liposomes were prepared and to improve their stability surface was coated with chitosan cross-linked with the biocompatible β-glycerolphosphate. X-ray diffraction, differential scanning c...

The aim of this study was to prepare diclofenac/hydroxypropylmethylcellulose (HPMC) and diclofenac-loaded nanoparticles/HPMC films as potential systems for ocular delivery. Two different concentration of the polymer were used: 1.5 and 2.0% w/v. Chitosan-hyaluronic acid nanoparticles were prepared by the ionotropic gelation technique. Nanoparticles...

The effects of lipid concentration and composition on the physicochemical properties, aerosol performance and in vitro toxicity activity of several rifampicin-loaded liposomes were investigated. To this purpose, six liposome formulations containing different amounts of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine, with and witho...

The effects of lipid concentration and composition on the physicochemical properties, aerosol performance and in vitro toxicity activity of several rifampicin-loaded liposomes were investigated. To this purpose, six liposome formulations containing different amounts of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine, with and witho...

Liquid toothpastes, commonly called "2 in 1", are sold as a mixture of dentifrice and mouthwash. These products were launched for the first time in 1992, trying to combine both the cosmetic effects of the toothpaste and the pharmacological activity of an oral rinse. Their texture, less solid than regular toothpastes, facilitates reaching dental spa...

The aim of this study was to evaluate the passive and iontophoretic permeation of triclosan in human skin using a triclosan solution and triclosan-loaded cationic nanospheres in order to determine which of the two strategies is more effective in allowing the deposition of triclosan within the skin. Triclosan-loaded nanospheres were prepared by the...

The objective of this study was to prepare NS-chitosan microparticles for the delivery of 5-aminosalicylic acid (5-ASA) to the colon. Microparticles can spread out over a large area of colon allowing a more effective local efficacy of 5-ASA. N-Succinyl-chitosan was chosen as carrier system because of its excellent pharmaceutical properties in colon...

5-Aminosalicylic acid (5-ASA) loaded N-Succinyl-chitosan (SucCH) microparticle and freeze-dried system were prepared as potential delivery systems to the colon. Physicochemical characterization and in vitro release and swelling studies were previously assessed and showed that the two formulations appeared to be good candidates to deliver the drug t...

In vitro study on N-succinyl chitosan and chitosan (control) matrices for selective colon delivery of 5-aminosalicylic acid is described. Matrices containing β-cyclodextrin were also prepared. As shown by DSC analyses, the drug was successfully loaded into the matrices reaching up to 95% entrapment efficiency. Swelling and drug release were studied...

The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH–XG-microcomplexes were prepared in aqueous lactic acid at different chitosan–xanthan gum perce...

A simple, sensitive and specific high-performance liquid chromatography method has been developed for the determination of nortriptyline (NT) in plasma samples. The assay involved derivatization with 9H-fluoren-9-ylmethyl chloroformate (Fmoc-Cl) and isocratic reversed-phase (C(18)) chromatography with fluorescence detection. The developed method re...

The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH-XG-microcomplexes were prepared in aqueous lactic acid at different chitosan-xanthan gum perce...

The aim of this study was to prepare and characterize both physically and biopharmaceutically, a nortriptyline hydrochloride (NTP-HCl) patch formulated in chitosan. 16 g of each chitosan patch formulation (I, II and III, see Table 1 ) was poured onto rectangular glass plates (64 cm²) at a height of 1 mm and dried for 24 h at room temperature. In or...

Rheological creep and recovery tests have been applied at different assay times to xanthan gum hydrogels at several concentrations. The Burger model has been successfully applied to fit the creep data and to analyze results. Increasing the xanthan gum concentration also increases the elastic and viscous components without changing the molecular dis...

IntroductionAlthough it has been used orally, the variability in its absorption and the risk of causing vomiting has lead to a push towards the intravenous use of busulfan. This study looks at the stability of 60 mg of busulfan, in fixed volumes of 250 mL (0.24 mg/mL) and 500 mL (0.12 mg/mL) of physiological saline and different conservation condit...

Introducción: Aunque se ha utilizado por vía oral, la variabilidad en su absorción y el riesgo de que se produzcan vómitos, ha impulsado la utilización intravenosa de busulfán. En el presente trabajo se estudiará la estabilidad de 60 mg de busulfán, en volúmenes fijos de 250 ml (0,24 mg/ml) y 500 ml (0,12 mg/ml) de suero fisiológico y diferentes co...