Efficacy of memantine prodrug microemulsion in a Preclinical model of tendinopathy.

Tendinopathy is a complex musculoskeletal pathology characterized by pain and dysfunction in the tendon. Tendinopathy management includes pharmacological treatments, which, however, have numerous side effects and low efficacy. New pharmacological approaches are essential to overcome these drawbacks.

Plant Resin Delivery by Nanovectors as an Emerging Approach to Boost Solubility, Permeability and Bioavailability.

Resins are complex mixtures of natural constituents containing non-volatile and volatile terpenes, in combination with gums and polyphenols, used since ancient times for their medicinal properties. Current research has evidenced their therapeutic value with a plethora of activities. The main limits of resins and their constituents for their clinical use are low water solubility, poor stability and bioavailability.

Environmentally Friendly Microemulsions of Essential Oils of and to Protect Crops against .

Essential oils (EOs) are reported to be natural pesticides, but their use to protect crops is very limited due to EOs' high instability and great volatility. Nanovectors represent a very smart alternative, and in this study, EOs from (AEO) and (SEO) were formulated into microemulsions and tested against . The EOs were extracted by steam distillation and analyzed by GC-MS.

Combination of Nanodelivery Systems and Constituents Derived from Novel Foods: A Comprehensive Review.

Novel Food is a new category of food, regulated by the European Union Directive No. 2015/2283. This latter norm defines a food as "Novel" if it was not used "for human consumption to a significant degree within the Union before the date of entry into force of that regulation, namely 15 May 1997".

Escinosome thermosensitive gel optimizes efficacy of CAI-CORM in a rat model of rheumatoid arthritis.

Rheumatoid arthritis is among the most common disabling diseases associated with chronic inflammation. The efficacy of the current therapeutic strategies is limited; therefore, new pharmacological agents and formulation approaches are urgently needed. In this work, we developed a thermosensitive gel incorporating escinosomes, innovative nanovesicles made of escin, stabilized with 10% of tween 20 and loaded with a Carbonic Anhydrase Inhibitor (CAI) bearing a Carbon Monoxide Releasing Moiety (CORM) (i.

Promising Nanocarriers to Enhance Solubility and Bioavailability of Cannabidiol for a Plethora of Therapeutic Opportunities.

In recent years, the interest in cannabidiol (CBD) has increased because of the lack of psychoactive properties. However, CBD has low solubility and bioavailability, variable pharmacokinetics profiles, poor stability, and a pronounced presystemic metabolism. CBD nanoformulations include nanosuspensions, polymeric micelles and nanoparticles, hybrid nanoparticles jelled in cross-linked chitosan, and numerous nanosized lipid formulations, including nanostructured lipid carriers, vesicles, SNEEDS, nanoemulsions, and microemulsions.

Escinosomes: Safe and Successful Nanovesicles to Deliver Andrographolide by a Subcutaneous Route in a Mice Model of Oxaliplatin-Induced Neuropathy.

Andrographolide (AG) is a natural diterpene lactone endowed with considerable therapeutic potential for treating numerous diseases, including neurological disorders, but its low aqueous solubility and scarce bioavailability limit its clinical use. To overcome this problem, AG was encapsulated in escinosomes, special nanovesicles made of escin (ESN), a natural saponin, and phosphatidylcholine. Escinosomes loaded with AG had an average size of 164.

Development and Evaluation of Khellin-loaded Microemulgel for Dermatological Applications.

Microemulsions are optically nanosized emulsions, isotropic and thermodynamically stable. They represent versatile drug delivery systems with high potential because they can be administered regardless of route. In the present study, we report on the formulation of a microemulsion made with glycerol (2.

Nanostructured Lipid Carriers Can Enhance Oral Absorption of Khellin, a Natural Pleiotropic Molecule.

A novel formulation based on nanostructured lipid carriers (NLCs) was developed to increase solubility and intestinal absorption of khellin. K-NLCs were prepared with stearic acid, hempseed oil, Brij S20, and Labrafil M 1944 CS, using the emulsification-ultrasonication method. Developed nanoparticles were chemically and physically characterized by liquid chromatography, light scattering techniques, and electron microscopy.

The Anti-Arthritic Efficacy of Khellin Loaded in Ascorbyl Decanoate Nanovesicles after an Intra-Articular Administration.

Osteoarthritis is the most widespread joint-affecting disease. The management of persistent pain remains inadequate and demands new therapeutic strategies. In this study, we explored the pain relieving and protective properties of a single intra-articular (i.

Development and optimisation of biopharmaceutical properties of a new microemulgel of cannabidiol for locally-acting dermatological delivery.

Cannabidiol (CBD) is a pleiotropic phytocannabinoid, recently investigated to treat many skin diseases. This study aimed to develop a CBD-loaded O/A microemulsion (CBD-ME) formulated as microemulgel (CBD-MEgel), suitable for local administration. The developed CBD-ME consisted of Solutol HS 15 (20%, surfactant), Transcutol P (9%, cosolvent), isopropyl myristate (5%, oil phase), water (66%) and 1% w/w CBD.

Nanovesicles Loaded with and Essential Oils and Their Activity against Food-Borne Pathogens and Spoilage Microorganisms.

Food poisoning is a common cause of illness and death in developing countries. Essential oils (EOs) could be effective and safe natural preservatives to prevent and control bacterial contamination of foods. However, their high sensitivity and strong flavor limit their application and biological effectiveness.

Hydroxyethyl cellulose hydrogel for skin delivery of khellin loaded in ascosomes: Characterization, in vitro/in vivo performance and acute toxicity.

Aim of this work was to prepare and characterize a hydroxyethyl cellulose hydrogel loaded with ascosomes, nanovesicles based on phosphatidylcholine plus ascorbyl octanoate (ASC8) or ascorbyl decanoate (ASC1), and khellin (2 mg/mL), for topical use. ASC10 vesicles were selected for the hydrogel formulation because of the best biopharmaceutical characteristics, namely size of 115 nm, PDI of 0.26, ζ-potential of -40.

Development of Nanoliposomes Loaded with Carbon Dioxide (Saw Palmetto) Extract.

Liposomes represent, among the nanocarriers, the most useful ones for dermatological use, and their composition, charge, size strongly influence their performance in topical drug delivery systems, with possible accumulation of the loaded drugs in the hair follicles. Recently, a saw palmetto carbon dioxide (CO₂) extract has been reported useful for the treatment of hair loss because of the inhibition of 5-reductase enzyme, responsible of the conversion of testosterone to the most potent androgen, the 5-dihydrotestosterone. In this work, the formation of nano-sized liposomes and the encapsulation efficiency of saw palmetto CO₂ extract were investigated by light scattering techniques, microscopy and HPLC.

Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression.

The MDR phenomenon has become a major obstacle in the treatment of cancers, and among the strategies to reverse it, the inhibition of P-gp function and expression is essential to increase for effective anticancer drugs. In the present paper, the co-delivery of berberine chloride and tariquidar loaded nanoliposomes was investigated with the aim of enhancing solubility and improving desired effects for the antineoplastic drug and the P-gp inhibitor. Developed nanoliposomes were loaded with the electron-dense enzyme horseradish peroxidase, and analyzed by TEM to investigate their ability to enter in both K562 and K562/DOXO cell lines.

Hydroxypropyl methylcellulose hydrogel of berberine chloride-loaded escinosomes: Dermal absorption and biocompatibility.

Aim of this work was to prepare and characterize new nanocarrier-loaded hydrogel formulations for topical application, using hydroxypropyl methylcellulose (HMPC) and special nanovesicles, the escinosomes. The combination of the two technological strategies, nanocarriers and hydrogels, was selected to circumvent some drawbacks of nanovesicles and develop stable and efficient skin-delivery platforms. HPMC is a derivative of cellulose with a wide range of physicochemical properties, forming suitable hydrogel for dermatological applications.

Formulation of a Phenol-Rich Extract from Unripe Olives ( L.) in Microemulsion to Improve Its Solubility and Intestinal Permeability.

The beneficial properties of phenolic compounds from L. are well-known. An olive extract (OE) was prepared from unripe olives (Moraiolo cultivar).

Glycerosome of L. Essential Oil for Effective Anti-HSV Type 1.

Essential oils are complex mixtures of strongly active compounds, very volatile and sensitive to light, oxygen, moisture and temperature. Loading inside nanocarriers can be a strategy to increase their stability and successfully use them in therapy. In the present study, a commercial L.

Development and Percutaneous Permeation Study of Escinosomes, Escin-Based Nanovesicles Loaded with Berberine Chloride.

Escin is a natural saponin, clinically used for the anti-edematous and anti-inflammatory effects. The aim of the study was to explore the possibility of converting escin into vesicle bilayer-forming component. The hyaluronidase inhibition activity of escin was evaluated after its formulation in escinosomes.

Nanocarriers: A Successful Tool to Increase Solubility, Stability and Optimise Bioefficacy of Natural Constituents.

Natural products are fascinating molecules in drug discovery for their exciting structure variability and also for their interaction with various targets. Drugs multi-targeting effect represents a more realistic approach to develop successful medications for many diseases. However, besides a large number of successful in vitro and in vivo studies, most of the clinical trials fail.