Supercritical fluid (SCF)-assisted preparation of cyclodextrin-based poly(pseudo)rotaxanes for transdermal purposes.

This study aims to investigate the effect of the preparation of solid dispersions using supercritical CO (scCO) on the physicochemical properties and the performance of supramolecular gels based on polymer-cyclodextrin (CD) interactions (named poly(pseudo)rotaxanes, PPR) envisaging a transdermal administration. Solid dispersions containing Soluplus, the antihypertensive drug carvedilol (CAR), and CD (αCD or HPβCD) were prepared and characterized by HPLC, XRPD, FTIR, and DSC. PPRs prepared from solid dispersions (SCF gels) and the corresponding physical mixtures (PM gels) were analyzed regarding rheology, morphology, in vitro drug diffusion, and ex vivo drug skin permeation.

Development of Lipid Polymer Hybrid Drug Delivery Systems Prepared by Hot-Melt Extrusion.

This study sought to develop polymer-lipid hybrid solid dispersions containing the poorly soluble drug lopinavir (LPV) by hot-melt extrusion (HME). Hence, the lipid and polymeric adjuvants were selected based on miscibility and compatibility studies. Film casting was used to assess the miscibility, whereas thermal, spectroscopic, and chromatographic analyses were employed to evaluate drug-excipient compatibility.

Cyclodextrin inclusion complex of a multi-component natural product by hot-melt extrusion.

This study aimed to investigate whether hot-melt extrusion (HME) processing can promote molecular encapsulation of a multi-component natural product composed of volatile and pungent hydrophobic substances (ginger oleoresin (OR)) with cyclodextrins. 6-Gingerol and 6-shogaol, the biomarkers of ginger OR, were quantified by HPLC. Phase-solubility studies were performed using β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) for ginger OR complexation.

Iontophoresis application for drug delivery in high resistivity membranes: nails and teeth.

Iontophoresis has been vastly explored to improve drug permeation, mainly for transdermal delivery. Despite the skin's electrical resistance and barrier properties, it has a relatively high aqueous content and is permeable to many drugs. In contrast, nails and teeth are accessible structures for target drug delivery but possess low water content compared to the skin and impose significant barriers to drug permeation.

Combination of lipid nanoparticles and iontophoresis for enhanced lopinavir skin permeation: Impact of electric current on lipid dynamics.

Nanostructured lipid carriers (NLC)-loaded with lopinavir (LPV) were developed for its iontophoretic transdermal delivery. Electronic paramagnetic resonance (EPR) spectroscopy of fatty acid spin labels and differential scanning calorimetry (DSC) were applied to investigate the lipid dynamic behavior of NLC before and after the electrical current. In vitro release and permeation studies, with and without anodic and cathodic iontophoresis were also performed.

Effects of Formulation and Manufacturing Process on Drug Release from Solid Self-emulsifying Drug Delivery Systems Prepared by High Shear Mixing.

This study sought to investigate the influence of formulation and process factors of the high shear mixing (HSM) on the properties of solid self-emulsifying drug delivery systems (S-SEDDS) containing the model drug carvedilol (CAR). Firstly, liquid SEDDS (L-SEDDS) were prepared by mixing castor oil with different proportions of surfactant (Solutol or Kolliphor RH40) and cosolvent (Transcutol or PEG400). A miscible L-SEDDS with high drug solubility (124.

Inorganic pellets containing microsclerotia of Metarhizium anisopliae: a new technological platform for the biological control of the cattle tick Rhipicephalus microplus.

This study was sought to devise pellets containing inorganic materials and microsclerotia of Metarhizium anisopliae strain IP 119 for biological control of Rhipicephalus microplus, the most economically important tick in Brazilian cattle industry. In addition, we evaluated the storage stability of the pellets, their tolerance to ultraviolet radiation (UV-B), and efficacy against ticks under laboratory conditions. Fungal microsclerotia were produced by liquid culture fermentation and mixed with pre-selected inorganic matrices: vermiculite powder, diatomaceous earth, and colloidal silicon dioxide (78:20:2, w/w/w).

Enhanced Skin Permeation of Punicalagin after Topical Application of Pluronic Micelles or Vesicles Loaded with Lafoensia pacari Extract.

Punicalagin, the principal ellagitannin of leaves, has proven antioxidant activity, and standardized extracts of can be topically used for skin aging management. We hypothesized that Pluronic nanomicelles or vesicles could solubilize sufficiently large amounts of the standardized extracts of and provide chemical stability to punicalagin. The standardized extracts of were obtained with an optimized extraction procedure, and the antioxidant activity was characterized.

Enhanced nail delivery of voriconazole-loaded nanomicelles by thioglycolic acid pretreatment: A study of protein dynamics and disulfide bond rupture.

This work aimed to select an effective penetration enhancer (PE) for nail pretreatment, develop voriconazole (VOR)-loaded nanomicelles, and evaluate their ability to deliver VOR to the nail. A complete analysis of nail protein dynamics, bond rupture, and microstructure was performed. Alternative methods as electron paramagnetic resonance (EPR) and the Ellman's reagent (DTNB) assay were also evaluated.

Development of carvedilol-loaded lipid nanoparticles with compatible lipids and enhanced skin permeation in different skin models.

The study aimed to develop lipid nanoparticles using excipients compatible with carvedilol (CARV) for enhanced transdermal drug delivery. Nanostructured lipid carriers (NLC) were successfully obtained and fully characterised. Franz diffusion cells were used for release and permeation studies in the porcine epidermis (EP) and full-thickness rat skin.

Thymol-Loaded Biogenic Silica Nanoparticles in an Aquatic Environment: The Impact of Particle Aggregation on Ecotoxicity.

Thymol, a monoterpene phenol, is used as a natural biocide. To circumvent its chemical instability, we propose use of thymol-loaded biogenic silica nanoparticles (BSiO #THY NPs); however, the toxicity of this system for aquatic organisms is unknown. Thus, the present study aimed to evaluate the toxicogenetic effects induced by thymol, BSiO NP, and BSiO #THY on Artemia salina and zebrafish (Danio rerio) early life stages.

Cyclodextrin-based poly(pseudo)rotaxanes for transdermal delivery of carvedilol.

This work aimed to design supramolecular gels combining Soluplus or Solutol and alfa- and hydroxypropyl-β-cyclodextrin (α-CD, HPβ-CD) for carvedilol (CAR) transdermal delivery. Poly(pseudo)rotaxane formation (appearance, SEM, H NMR), drug solubilization, rheological properties and in vitro release were investigated. CAR-CD complexes were prepared in situ or by spray drying.

Removal of azo dye using Fenton and Fenton-like processes: Evaluation of process factors by Box-Behnken design and ecotoxicity tests.

The conventional treatment of textile effluents is usually inefficient in removing azo dyes and can even generate more toxic products than the original dyes. The aim of the present study was to optimize the process factors in the degradation of Disperse Red 343 by Fenton and Fenton-like processes, as well as to investigate the ecotoxicity of the samples treated under optimized conditions. A Box-Behnken design integrated with the desirability function was used to optimize dye degradation, the amount of residual HO [HO], and the ecotoxicity of the treated samples (lettuce seed, Artemia salina, and zebrafish in their early-life stages).

A Novel Polymer-Lipid Hybrid Nanoparticle for the Improvement of Topotecan Hydrochloride Physicochemical Properties.

Background: Topotecan (TPT) is a water-soluble derivate of camptothecin, which undergoes ring-opening hydrolysis in neutral solutions, leading to stability loss and poor cellular uptake. Lipid nanoencapsulation can improve TPT stability, and polymer-lipid hybrid nanoparticles (PLN) are interesting alternatives to improve TPT nanoencapsulation.

Objective: This study seeks to prepare complexes between the cationic TPT and the negatively charged dextran sulfate (DS) with a view of improving drug loading, chemical stability and release control.

SLN- and NLC-encapsulating antifungal agents: skin drug delivery and their unexplored potential for treating onychomycosis.

Background: Lipid nanoparticles have been extensively studied for drug delivery of antifungal drugs, especially for dermatophytosis treatments. They can accumulate in skin appendages and release drugs in a controlled manner and also increase skin moisture, due to the formation of an occlusive film. Since moisture heavily influences nail and skin permeability, these systems seem to pose great potential for antifungal drug delivery.

Voriconazole-loaded nanostructured lipid carriers (NLC) for drug delivery in deeper regions of the nail plate.

Voriconazole-loaded nanostructured lipid carriers (VOR-NLC) were developed and drug penetration evaluated in porcine hooves in vitro. Synergistic effect of urea (Ur), selected among other known chemical enhancers according to hoof hydration potential, was also evaluated. VOR-NLC presented a high encapsulation efficiency (74.

Topotecan-loaded lipid nanoparticles as a viable tool for the topical treatment of skin cancers.

Objectives: This work aimed to evaluate semisolid formulations containing topotecan (TPT) loaded nanostructured lipid carriers (NLC) for topical treatment of skin cancers, as TPT is effective against a variety of tumours. A formulation which increases TPT skin permeation would be extremely desirable.

Methods: TPT-NLC were prepared and incorporated in hydrogels with hydroxyethyl cellulose and chitosan (TPT-NLC-HEC and TPT-NLC-Ch, respectively).

Development of a High-Performance Liquid Chromatographic Method for Asiaticoside Quantification in Different Skin Layers after Topical Application of a Centella asiatica Extract.

The topical application of extract has been commonly used for many different purposes but especially for cosmetic use in the treatment of gynoid lipodystrophy. Asiaticoside, the most active component in this extract, is responsible for its therapeutic activities. However, little is known to date about asiaticoside skin penetration.

Improved tacrolimus skin permeation by co-encapsulation with clobetasol in lipid nanoparticles: Study of drug effects in lipid matrix by electron paramagnetic resonance.

Combined therapy with corticosteroids and immunosuppressant-loaded nanostructured lipid carriers (NLC) could be useful in the treatment of skin diseases. To circumvent NLC loading capacity problems, loaded drugs should have different physicochemical characteristics, such as tacrolimus (TAC) and clobetasol (CLO). Therefore, in the present study, TAC and CLO were encapsulated in NLC (TAC-NLC, CLO-NLC and TAC+CLO-NLC), coated or otherwise with chitosan.

Mucoadhesive Properties of Thiolated Pectin-Based Pellets Prepared by Extrusion-Spheronization Technique.

The aim of this study was to develop mucoadhesive pellets on a thiolated pectin base using the extrusion-spheronization technique. Thiolation of pectin was performed by esterification with thioglycolic acid. The molecular weight and thiol group content of the pectins were determined.

Compacted Multiparticulate Systems for Colon-Specific Delivery of Ketoprofen.

Pellet-containing tablets for colon-specific drug delivery present higher targeting efficiency and lower costs when compared with monolithic tablets and pellet-filled capsules, respectively. In this study, pellets containing ketoprofen were coated with different acrylic polymers and submitted to compaction. The influence of formulation and process factors on film integrity was then evaluated.

Chemical and physical strategies in onychomycosis topical treatment: A review.

Onychomycosis is a fungal infection of the fingernails or toenails caused by dermatophytes, nondermatophytes, moulds, and yeasts. This condition affects around 10-30% people worldwide, negatively influencing patients' quality of life, with severe outcomes in some cases. Since the nail unit acts as a barrier to exogenous substances, its physiological features hampers drug penetration, turning the onychomycosis treatment a challenge.

Clobetasol-loaded nanostructured lipid carriers for epidermal targeting.

Objectives: The aim of this study was to investigate in vitro the epidermal targeting potential of clobetasol propionate-loaded nanostructured lipid carriers (CP-NLC) when compared to that of chitosan-coated (CP-NLC-C).

Methods: CP-NLC were prepared by microemulsion method and characterized by dynamic light scattering, transmission electron microscopy, in vitro release and permeation studies. To verify epidermal targeting, permeation studies were performed in two sets of experiments.

Liposomal voriconazole (VOR) formulation for improved ocular delivery.

Treating infectious eye diseases topically requires a drug delivery system capable of overcoming the eye's defense mechanisms, which efficiently reduce the drug residence time right after its administration, therefore reducing absorption. In order to try to surpass such administration issues and improve life quality for patients with fungal keratitis, liposomal voriconazol (VOR) formulations were prepared. Formulations were composed of soy phosphatidylcholine (PC) containing or not 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) and cholesterol.