Development of biopolymer films loaded with fluconazole and thymol for resistant vaginal candidiasis.

Vulvovaginal candidiasis (VVC) is an opportunistic infection caused by a fungus of the Candida genus, affecting approximately 75 % of women during their lifetime. Fungal resistance cases and adverse effects have been the main challenges of oral therapies. In this study, the topical application of thin films containing fluconazole (FLU) and thymol (THY) was proposed to overcome these problems.

Development of ophthalmic nanoemulsions of β-caryophyllene for the treatment of Acanthamoeba keratitis.

Although rare, amoebic keratitis (AK) is a disease caused by Acanthamoeba spp. that can lead to blindness. The drugs currently available for its treatment are very toxic, which has motivated the investigation for more effective and safe therapeutic options.

Revisiting the Effect of Aging on the Transport of Molecules through the Skin.

Both intrinsic and extrinsic aging lead to a series of morphological changes in the skin including the flattening of the dermal-epidermal junction, increased stratum corneum dryness, reduction in sebaceous gland activity and enzyme activity as well as atrophy of blood vessels. In this study, the impact of these changes on the transport of molecules through the skin was revised. The increase in the number of transdermal formulations on the market in recent decades and life expectancy represent the main reasons for an in-depth discussion of this topic.

The rheology of injectable hyaluronic acid hydrogels used as facial fillers: A review.

Injectable hyaluronic acid (HA) hydrogels have been popularized in facial aesthetics as they provide a long-lasting effect, low risk of complications, allergenicity tests are not required before application and can be easily removed by the action of hyaluronidases. On the other hand, the development of these systems requires in-depth studies of chemical mechanisms involved in hydrogel formation. Ideal dermal fillers should temporarily fluidize during extrusion through the needle and quickly recover their original shape after application.

Nanoemulsions and nanocapsules loaded with Melaleuca alternifolia essential oil for sepsis treatment.

Sepsis represents a complex clinical syndrome that results from a harmful host response to infection. The infections most associated with sepsis are pneumonia, intra-abdominal infection, and urinary tract infection. Tea tree oil (TTO) has shown high antibacterial activity; however, it exhibits low aqueous solubility and high volatility, which have motivated its nanoencapsulation.

Effect of invasome composition on membrane fluidity, vesicle stability and skin interactions.

Invasomes have been widely exploited to enhance the percutaneous permeation of drugs. On the other hand, few studies have been dedicated to evaluating how their composition impacts the interaction with the skin, vesicle rigidity and stability, which was the focus of this investigation. Light scattering and spectroscopic techniques were considered for vesicle characterization.

Drug-excipient compatibility studies in formulation development: A case study with benznidazole and monoglycerides.

Monoglycerides (MGs) such as glycerol monolaurate (GML) and glycerol monostearate (GMS) have been used as excipients in oral formulations because of their emulsifying effect as well as their ability to inhibit the precipitation and intestinal efflux of drugs. Excipient-drug compatibility studies, however, have been underexplored. In this study, benznidazole (BNZ) was selected as a drug model due to the difficulty in improving its solubility and because of the potential impact on public health (it is the only drug currently used to treat Chagas disease).

A Comparative Analysis of Biological and Synthetic Skin Models for Drug Transport Studies.

Ethical restrictions as well as practical or economic issues related to use of animal and human skin has been the main reason the growth in the number of investigations with alternative models. Reconstructed skin models, for example, have been useful to evaluate the in vitro toxicity of compounds; however, these models usually overestimate the amount of drug permeated due to impaired barrier properties. In this review, the performance of synthetic and biological skin models in transport studies was compared by considering two compounds with different physicochemical properties.

An update of nano-based drug delivery systems for cannabinoids: Biopharmaceutical aspects & therapeutic applications.

Nanotechnology has been widely used to improve stability, efficacy, release control and biopharmaceutical aspects of natural and synthetic cannabinoids. In this review, the main types of cannabinoid-based nanoparticles (NPs) reported so far are addressed, taking into account the advantages and disadvantages of each system. Formulation, preclinical and clinical studies performed with colloidal carriers were individually analyzed.

Advanced Solid Formulations For Vulvovaginal Candidiasis.

Vulvovaginal candidiasis (VVC) is an opportunistic and endogenous infection caused by a fungus of the Candida genus, which can cause pruritus, dysuria, vulvar edema, fissures and maceration of the vulva. The treatment of vaginal candidiasis is carried out mainly by antifungal agents of azole and polyene classes; however, fungal resistance cases have been often observed. For this reason, new therapeutic agents such as essential oils, probiotics and antimicrobial peptides are being investigated, which can be combined with conventional drugs.

Effect of Vehicle Composition on the Preparation of Different Types of Dapsone Crystals for Topical Drug Delivery.

Topical formulations composed of API-pure crystals have been increasingly studied, especially in regards to the impact of particle size in penetration efficiency. Less attention, however, has been devoted to the solid-state properties of drugs delivered to the skin. In this study, we address the effect of formulation composition on the crystal form existing in topical products.

A New Saquinavir Mesylate-Sodium Decyl Sulfate Salt Discovered by Serendipity during an Anomalous Dissolution Test.

Purpose: To understand the anomalous behavior of Saquinavir Mesylate (SQVM) in sodium decyl sulfate (SDS) medium during a dissolution test through a crystallographic analysis of the crystal obtained. As a result, it will be possible to elucidate its crystal structure and carry out a complete solid-state characterization of the API.

Methods: The solid form obtained was characterized by a structural analysis through X-ray single crystal and powder diffraction.

Phenolic profile and in vitro anti-inflammatory activity of Mimosa scabrella Bentham honeydew honey in RAW 264.7 murine macrophages.

The anti-inflammatory activity is mainly attributed to the phenolic compounds. Once the geographical location affects the phenolic content of honeys, a relationship between the collection spot and the anti-inflammatory effect of bracatinga (Mimosa scabrella Bentham) honeydew honeys was hypothesized. The inhibitory effect of 14 honey samples on NOx, TNF-α, IL-6, IL-12p70, MCP-1, INF-γ, and IL-10 in RAW 264.

How to define the experimental conditions of skin permeation assays for drugs presenting biopharmaceutical limitations? The experience with testosterone.

Cutaneous permeation assays are crucial to attest the performance or bioequivalence of topical or transdermal products. Although the official guidelines (e.g.

In vitro anti-inflammatory properties of honey flavonoids: A review.

Honey is a natural ready-to-eat product rich in flavonoids, which is known by the wound healing properties due to both antibacterial and antioxidant activity. Flavonoids mitigate inflammatory processes, and thus it could currently support studies of anti-inflammatory potential of honeys. In this review, in vitro anti-inflammatory properties of flavonoids found in honey were prioritized.

Thermosensitive hydrogels for vaginal delivery of secnidazole as an approach to overcome the systemic side-effects of oral preparations.

Secnidazole (SEC) has been suggested as an alternative agent against Trichomonas vaginalis to overcome the adverse effects, antimicrobial resistance problems and poor adherence to the currently available therapy. Once no topical formulation may be found in the market until now, SEC was incorporated in thermosensitive bioadhesive systems to extend the contact time in the mucosa and to avoid a systemic drug disposition. Formulations containing 20% poloxamer 407, 1% poloxamer 188 and 1 or 2.

Development and characterization of thermopressed polyvinyl alcohol films for buccal delivery of benznidazole.

Given that oral preparations of benznidazole (BZN) have demonstrated limited efficacy in the treatment of Chagas' disease due to pharmacokinetic or toxicological problems, the development of buccal polymeric films was purposed in this study. These systems ensure high patient acceptability and direct access to the systemic circulation, improving drug bioavailability and toxicological profile. Polymer films were prepared through a thermopressing method by mixing BZN and polyvinyl alcohol (PVAL).

Emerging Technologies to Target Drug Delivery to the Skin - the Role of Crystals and Carrier-Based Systems in the Case Study of Dapsone.

Dapsone (DAP) is a long-established molecule that remains a promising therapeutic agent for various diseases mainly because it combines antimicrobial and anti-inflammatory activities. Its oral application, however, is limited by the dose-dependent hematological side effects that may rise from systemic exposure. As an alternative to overcome this limitation, the administration of DAP to the skin has witnessed prominent interest in the past 20 years, particularly when applied to the treatment of dermatological disorders.

Transbuccal Delivery of Isoniazid: Ex Vivo Permeability and Drug-Surfactant Interaction Studies.

The oral administration of isoniazid (INH) may lead to discontinuation of tuberculosis treatment due to drug-related hepatotoxicity events, and thus, the transbuccal delivery of this drug was investigated, for the first time, as an alternative administration route. Ex vivo permeability assays were performed in Franz-type diffusion chambers, applying INH alone and in combination with sodium dodecyl sulfate (SDS) and sodium taurocholate (ST). After confirming the formation of micelle structures by dynamic light scattering analysis, UV-visible spectroscopy and zeta potential analyses were used to investigate drug-micelle interactions.

Transbuccal delivery of metal complexes of isoniazid as an alternative to overcome antimicrobial resistance problems.

In isolated isoniazid (INH)-resistant strains, deletion or mutations in thekatGgene have been identified, which result in loss of catalase-peroxidase activity. This enzyme plays a key role in the activation of this prodrug. As an alternative, the coordination of the INH to metal complexes has been purposed to activate it regardless of enzyme functionality.

Development of curcumin-loaded chitosan/pluronic membranes for wound healing applications.

The emergence of new materials with improved antibacterial, anti-inflammatory and healing properties compared to conventional wound dressings has both social and economic appeal. In this study, novel chitosan-based (CTS) membranes containing curcumin (CUR) incorporated in Pluronic (PLU) copolymers were developed and characterized to obtain suitable properties for applications as a wound healing dressing. The mechanical, thermal, swelling, wettability, release and permeation properties were evaluated by DSC, TGA, water contact angle measurements, FTIR, fluorescence and microscopic techniques.

Investigation of phenolic compounds, antioxidant and anti-inflammatory activities in stingless bee honey (Meliponinae).

The objective of this study was to investigate and quantify the composition phenolic, reducing capacity, the free radical scavenging activity, as well as, the anti-inflammatory effect evaluated against lipopolysaccharides-stimulated RAW264.7 macrophages through modulation of inflammatory mediators, in eight stingless bee honey types (Meliponinae) from southern Brazil. Stingless bee honey did not show to be cytotoxic at the tested concentrations (1-100 µM) and also reduced nitric oxide and the secretion of the pro-inflammatory cytokine in the inflamed macrophages.

Transbuccal delivery of benznidazole associated with monoterpenes: permeation studies and mechanistic insights.

Benznidazole (BZN) represents the only drug currently available for the treatment of Chagas disease in most endemic countries. When administered orally, high doses are required due to its extensive hepatic metabolism and its toxicity represents the main reason for treatment withdrawals. Because of these complications, transbuccal administration of BZN was investigated.

Intestinal permeability enhancement of benzopyran HP1-loaded nanoemulsions.

The benzopyran HP1, a compound isolated from Hypericum polyanthemum, has demonstrated significant opioid-mediated antinociceptive activity after its oral administration. Despite the pharmacological potential, the poor aqueous solubility limits the oral absorption of this compound. For this reason, HP1 has been alternatively incorporated in lipid-based drug delivery systems.

Vasorelaxant effect of standardized extract of Cecropia glaziovii Snethl encapsulated in PLGA microparticles: In vitro activity, formulation development and release studies.

In this study, the standardized dry extract of C. glaziovii (SDE) provided a significant vasorelaxant effect after contractions induced by phenylephrine in rat aortic rings in an endothelium-dependent manner, confirming that endothelial factors are needed to stimulate this response. A vasorelaxation close to that of acetylcholine was achieved, justifying the development of new formulations for this plant material.