A Patent Review on the Use of Cyclodextrin Inclusion Complexes to Enhance Physicochemical and Pharmacological Properties in Antidepressant Drugs.

Major depressive disorder is considered one of the most common and prevalent diseases worldwide, affecting children, adults, and the elderly. Currently, several antidepressant drugs are available on the market, but the low adherence of patients due to the slow therapeutic response is a problem to be solved. In this way, cyclodextrins become an alternative to circumvent the limitations and improve the physicochemical and pharmacological properties of this class of drugs.

Polymeric Nanocapsules Containing Ozonated Oil and Terbinafine Hydrochloride as a Potential Treatment Against Dermatophytes.

Terbinafine hydrochloride is a synthetic allylamine whose mechanism of action consists of inhibiting the enzyme squalene epoxidase that participates in the first stage of ergosterol synthesis, interfering with fungal membrane function. Ozonated oils are used for topical application of ozone, producing reactive oxygen species that cause cellular damage in microorganisms, therefore being an alternative treatment for acute and chronic skin infections. This study aimed to develop and characterize Eudragit RS100 nanocapsules, obtained by interfacial deposition of preformed polymer method, containing 0.

Carvacrol-loaded nanoemulsions produced with a natural emulsifier for lettuce sanitization.

Carvacrol is an antimicrobial agent that shows potential for eliminating microorganisms in vegetables, increasing food safety. However, intense odor and low water solubility of carvacrol are limiting factors for its application for fresh vegetables sanitization, which can be overcome by nanotechnology. Two different nanoemulsions containing carvacrol (11 mg/mL) were developed by probe sonication: carvacrol-saponin nanoemulsion (CNS) and carvacrol-polysorbate 80 nanoemulsion (CNP).

Development of a Clioquinol Nanocarrier as a New, Promising Option for the Treatment of Dermatomycosis.

Dermatomycosis is a common fungal infection, and its treatment is limited by few antifungal agents. Clioquinol (CQ) is an antiparasitic agent that has been studied for new uses, such as antifungal and antiviral applications. CQ was incorporated into a lipid-based nanocarrier as a new, promising option for dermatomycosis.

Nanoemulsion Containing Kojic Dipalmitate and Rosehip Oil: A Promising Formulation to Treat Melasma.

Melasma is a hard-to-treat hyperpigmentation disorder. Combined incorporation of kojic dipalmitate (KDP), the esterified form of kojic acid, and rosehip oil, an oil with antioxidant and skin-regenerating properties, into nanocarrier systems appears to be a suitable strategy to develop high-performance formulations. A high-energy method (Ultra-Turrax) was used to develop nanoemulsions containing up to 2 mg/mL KDP, 5% rosehip oil, and 7.

Lamivudine and Zidovudine-Loaded Nanostructures: Green Chemistry Preparation for Pediatric Oral Administration.

Here, we report on the development of lipid-based nanostructures containing zidovudine (1 mg/mL) and lamivudine (0.5 mg/mL) for oral administration in the pediatric population, eliminating the use of organic solvents, which is in accordance with green chemistry principles. The formulations were obtained by ultrasonication using monoolein (MN) or phytantriol (PN), which presented narrow size distributions with similar mean particle sizes (~150 nm) determined by laser diffraction.

Nanotechnology-based alternatives for the topical delivery of immunosuppressive agents in psoriasis.

Psoriasis is a recurring, immune-mediated dermatological disorder. Many therapeutic agents are available for the treatment of psoriasis, including immunosuppressants and biologic treatments with immunosuppressant action. The employment of nanotechnology allows drug tailoring to achieve dermal targeting, improve efficacy and minimize undesirable effects.

Biological activities and safety data of kojic acid and its derivatives: A review.

Kojic acid presents a variety of applications for human use, especially as a depigmenting agent. Its derivatives are also proposed in order to prevent chemical degradation, prevent adverse effects and improve efficacy. The aim of this study was to peer review the current scientific literature concerning the biological activities and safety data of kojic acid or its derivatives, aiming at human use and trying to elucidate the action mechanisms.

Evaluation of an Efficient and Skin-Adherent Semisolid Sunscreen Nanoformulation.

Introduction: Sunscreens are substances applied on the skin surface to protect the skin from the harmful effects of UV light. Nanoparticles can increase the retention time of the sunscreen on the skin surface and its efficacy, by acting as physical barriers. The present investigation aimed to evaluate the influence of the chitosan coating of benzophenone-3-loaded lipid-core nanocapsules (CH-LCN) on the skin adhesion and photoprotective effect of the sunscreen.

Dermatopharmacokinetic and pharmacodynamic evaluation of a novel nanostructured formulation containing capsaicinoids for treating neuropathic pain.

The in vivo skin penetration by dermal microdialysis and the pharmacological efficacy of a chitosan hydrogel containing capsaicinoids-loaded nanocapsules (CHNC) was evaluated in this study. Such gel has previously been proven to control capsaicinoids release and decrease the drugs side effects in humans. The nanocapsules containing capsaicinoids had an average size around 150 nm, with a low polydispersity index, positive zeta potential, and high encapsulation efficiency of the drugs.

The use of electronic tongue and sensory panel on taste evaluation of pediatric medicines: a systematic review.

The palatability of medications is an essential factor for children's adherence to drug treatment. Several methods for drug taste assessment have been developed. The aim of this review is to explore the literature reports of the main methods for the evaluation of medicines taste, named electronic tongue (e-tongue, ) and human sensory panel.

Improved sensory properties of a nanostructured ritonavir suspension with a pediatric administration perspective.

The pediatric adherence to antiretroviral therapy is critical to therapeutic success. Ritonavir, a protease inhibitor drug, is commercially available as an oral solution containing a high amount of ethanol and propylene glycol, contraindicated in children younger than 4 years. Moreover, this medicine presents a bitter taste, which is limiting for the adherence to treatment.

Simultaneous nanoencapsulation of lipoic acid and resveratrol with improved antioxidant properties for the skin.

Cutaneous aging is intimately related to redox imbalance, which is mainly caused by ultraviolet radiation exposure. The aim of the present investigation was to develop lipid-core nanocapsules for the co-nanoencapsulation of resveratrol and lipoic acid aiming to improve the chemical stability and photostability of the compounds, as well as their antioxidant properties. Lipid-core nanocapsules were developed and characterized according to their mean size, size distribution, zeta potential, pH value, drug content, encapsulation efficiency, release profile, stability under storage, photostability and skin permeation profile.

Rapid and sensitive LC-MS/MS method for simultaneous quantification of capsaicin and dihydrocapsaicin in microdialysis samples following dermal application.

A bioanalytical LC-MS/MS method was developed and validated for the simultaneous quantification of capsaicin (CAPS) and dihydrocapsaicin (D-CAPS) in dermal microdialysis samples from rats. Capsaicinoids were separated by using a C18 column, with a mobile phase of water and acetonitrile, both with 0.1% of formic acid, eluted as a gradient.

The use of chitosan as cationic coating or gel vehicle for polymeric nanocapsules: Increasing penetration and adhesion of imiquimod in vaginal tissue.

The human papillomavirus (HPV) infection, which is strongly related to cervical cancer, can be reduced by the topical application of imiquimod. Some strategies have been used to increase the adhesion and penetration of drugs through the vaginal mucosa. Two of them are the development of mucoadhesive semisolid formulations and the development of polymeric nanocarriers.

Nanoencapsulation of Rose-Hip Oil Prevents Oil Oxidation and Allows Obtainment of Gel and Film Topical Formulations.

The rose-hip oil holds skin regenerating properties with applications in the dermatological and cosmetic area. Its nanoencapsulation might favor the oil stability and its incorporation into hydrophilic formulations, besides increasing the contact with the skin and prolonging its effect. The aim of the present investigation was to develop suitable rose-hip-oil-loaded nanocapsules, to verify the nanocapsule effect on the UV-induced oxidation of the oil and to obtain topical formulations by the incorporation of the nanocapsules into chitosan gel and film.

Co-encapsulation of imiquimod and copaiba oil in novel nanostructured systems: promising formulations against skin carcinoma.

In this study, two types of cutaneous-directed nanoparticles are proposed for the co-encapsulation of imiquimod (a drug approved for the treatment of basal cell carcinoma) and copaiba oil (oil that exhibits anti-proliferative properties). Nanostructured copaiba capsules (NCCImq) were prepared using the interfacial deposition method, and nanostructured Brazilian lipids (NBLImq) were prepared by high-pressure homogenization. The formulations exhibited average diameter, zeta potential, pH and drug content of approximately 200nm, -12mV, 6 and 1mgmL(-1), respectively.

Applying the sensory analysis in the development of chitosan hydrogel containing polymeric nanocapsules for cutaneous use.

This work aimed to develop a chitosan hydrogel containing polymeric nanocapsules with optimized sensory properties, linking the advantages of the nanocarriers, such as controlled release and protection of the substances, to the chitosan properties, such as bioadherence, cicatrizing effect, and antimicrobial activity. Sixty untrained volunteers evaluated the sensory properties of chitosan hydrogels compared to hydroxyethyl cellulose gels (Phase I) and to optimized chitosan gels (Phase II). The volunteers' preference between formulations was also evaluated.

Improving drug biological effects by encapsulation into polymeric nanocapsules.

This review is based on selected reports from 2004 to 2014 and provides a comprehensive and updated overview of the state of the art related to the drug delivery advantages of polymeric nanocapsules, which are a specific type of polymeric nanoparticles used for improvement of biological effects. Special attention is given to the application of nanocapsules to increase the chemical and photostability of drugs, to modulate the interaction with cells and tissues, to reduce adverse effects of drugs, and to increase the drug efficiency and/or bioavailability. Moreover, this review covers in vitro and in vivo studies, highlighting interesting examples of drugs from several therapeutic classes for which efficacy is improved by encapsulation in different types of nanocapsules, especially in lipid-core nanocapsules.

Structural analysis of chitosan hydrogels containing polymeric nanocapsules.

The incorporation of different concentrations of polymeric nanocapsule suspensions into chitosan hydrogels is proposed, in order to study the structure of a formulation with the properties of great tissue adhesion and controlled release of the nanoencapsulated drugs, represented here by capsaicinoids. The gels presented acceptable acid pH values and the nanoparticles were visually observed in the system. A transition from the micrometer to the nanometer scales suggested that the nanocapsules are initially agglomerated in the hydrogel.

Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery.

The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit RS 100 and Eudragit S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations.

Labeling the oily core of nanocapsules and lipid-core nanocapsules with a triglyceride conjugated to a fluorescent dye as a strategy to particle tracking in biological studies.

The synthesis of novel fluorescent materials represents a very important step to obtain labeled nanoformulations in order to evaluate their biological behavior. The strategy of conjugating a fluorescent dye with triacylglycerol allows that either particles differing regarding supramolecular structure, i.e.

Combined effect of polymeric nanocapsules and chitosan hydrogel on the increase of capsaicinoids adhesion to the skin surface.

This work explored the effect of the encapsulation in polymeric nanocapsules, as well as of the incorporation of such nanoparticles in a chitosan hydrogel, on the skin adhesion and skin penetration/permeation of capsaicinoids (capsaicin and dihydrocapsaicin), which are used as topical analgesic to treat chronic pain. The skin experiments were performed using a modified (drug adhesion and drug diffusion) and a normal Franz diffusion cell (drug diffusion) with porcine skin as membrane. The AUC0-h of the washability profile (% washed away vs.