Topical administration of dapsone can be an alternative route for treatment of leprosy and can also provide new therapeutic applications for an established drug. However, the physicochemical ...properties of dapsone make it difficult to incorporate into conventional formulations. The current study was directed toward developing a stable nanoemulsion that contains dapsone which can be adapted for topical use.
Nanoemulsions were prepared using isopropyl myristate or n-methyl-pyrrolidone as the oil phase, and characterized according to their mean droplet size, conductivity, refractive index, pH, drug content, and stability. The in vitro release of dapsone and its ability to permeate the epidermis were also evaluated.
Physicochemical characterization demonstrated that nanosystems were formed, which had a uniform droplet distribution and a pH compatible with the skin surface. Use of n-methyl-pyrrolidone provided a greater nanoemulsion region and higher solubilization of dapsone, and increased the in vitro release rate when compared with a nanoemulsion prepared using isopropyl myristate. However, use of isopropyl myristate promoted an increase in in vitro epidermal permeation that followed the Higuchi model. This demonstrates the ability of a nanosystem to influence permeation of dapsone through the skin barrier. Furthermore, the nanoemulsions developed and evaluated here had ideal physicochemical stability over a 3-month period.
Incorporation of dapsone into a nanoemulsion may be a promising system for enabling topical delivery of dapsone, while minimizing skin permeation, for the treatment of acne. The method developed here used isopropyl myristate as the oil phase, and promoted permeation of dapsone through the skin barrier for the treatment of leprosy upon use of n-methyl-pyrrolidone as the oil phase.
The oil of babassu tree nuts (Orbignya speciosa) is a potential alternative for treatment and prophylaxis of benign prostatic hyperplasia. Improved results can be obtained by drug vectorization to ...the hyperplastic tissue. The main objective of this work was the preparation and characterization of poly(lactic-co-glycolic acid) (PLGA) nanoparticle and clay nanosystems containing babassu oil (BBS). BBS was extracted from the kernels of babassu tree nuts and characterized by gas chromatography-mass spectrometry as well as 1H and 13C nuclear magnetic resonance. BBS-clay nanosystems were obtained by adding polyvinylpyrrolidone, Viscogel B8®, and BBS at a 2:1:1 mass ratio and characterized by X-ray diffraction, thermogravimetric analysis, infrared spectroscopy, and laser diffraction. The PLGA-BBS nanoparticles were prepared by the precipitation-solvent evaporation method. Mean diameter, polydispersity, zeta potential, and scanning electron microscopic images of the nanosystems were analyzed. Thermogravimetric analysis showed successful formation of the nanocomposite. PLGA nanoparticles containing BBS were obtained, with a suitable size that was confirmed by scanning electron microscopy. Both nanostructured systems showed active incorporation yields exceeding 90%. The two systems obtained represent a new and potentially efficient therapy for benign prostatic hyperplasia.
•A chromatographic method with UV detection was developed to assay β-caryophyllene and α-humulene in copaiba oleoresin.•The RP-HPLC method was adequate to assay products containing copaiba without ...the sample preparation step.•Box-Behnken design was successfully utilized in the optimization of a new chromatographic method.
The sesquiterpene isomers, β-Cariofileno (CAR) and α-Humuleno (HUM) are the primary constituents of the copaiba oleoresin species. These natural products are primarily used by the Amazonian population and marketed as phytotherapies and cosmetics. The aim of this study was to develop and validate a method that simultaneously assays the isomers present in copaiba oleoresins by high performance liquid chromatography using the Box-Behnken design. After preliminary studies, the reverse phase chromatographic system was selected using a cyano column and a mobile phase consisting of acetonitrile and phosphate buffer. The Box-Behnken design was applied at three levels and with four independent variables: flow rate (X1), gradient slope time (X2), proportion of organic compounds at the end of the gradient (X3) and at the beginning of the gradient (X4). Also, the responses of the dependent variables: CAR retention time (Y1) and the resolution between the CAR and HUM peaks (Y2) was assessed. The mathematical model obtained from the regression results was satisfactory (R2>0.98, n=27) and showed a quadratic relationship where the effects of interactions between the variables, was observed by response surface graphs. The simultaneous optimization method was used to establish the best compromise of the resolution between the CAR and HUM isomers while adjusting the retention time of CAR. This method was successfully optimized by BBD obtaining chromatographic peaks with good symmetry, resolution and separation efficiency. The validation of the developed method confirmed its specificity, precision, accuracy and linearity in the range of 5.0–11.0 and 0.4–1.0μg/mL for CAR and HUM, respectively, and is considered suitable for routine applications which assure quality control.
The intramuscular administration of the injectable suspension betamethasone sodium phosphate (BSP) and betamethasone dipropionate (BD) has immediate therapeutic activity due to solubilized BSP and ...prolonged activity resulting from the slow release of BD micro-crystals. The purpose of this study was to develop and validate a dissolution method for BD in intramuscular injectable suspensions with detection by high-performance liquid chromatography (HPLC) method. Five commercial products presented a distribution of particle sizes, ranging between 7.43 and 40.25 μm as measured by laser diffraction. It was also found that particle sizes differed between batches of the same product. The different products were tested using the paddle apparatus, with stirring speeds of 25 and 50 rpm in 300 mL of phosphate buffer; simulated body fluid, muscle fluid, and synovial fluid were used as biorelevant dissolution media at 37 ± 0.5°C. It was verified that not only does average particle size affect the dissolution rate, but also the mode and the polydispersity index of the particles. Discriminatory power was obtained using the
in vitro
dissolution method with 0.1 M sodium phosphate buffer pH 7.4 containing 0.1% sodium lauryl sulfate and a stirring speed of 50 rpm. The HPLC-method is linear, precise, selective, and accurate for the quantification of BSP and BD in dissolution profile testing. This dissolution method can be utilized as a method to control the quality of these injectable suspensions.
Copaiba oleoresin (CPO), obtained from Copaifera landgroffii, is described as active to a large number of diseases and more recently in the endometriosis treatment. In this work, ...poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing CPO were obtained using the design of experiments (DOE) as a tool to optimize the production process. The nanoparticles optimized by means of DOE presented an activity in relation to the cellular viability of endometrial cells. The DOE showed that higher amounts of CPO combined with higher surfactant concentrations resulted in better encapsulation efficiency and size distribution along with good stability after freeze drying. The encapsulation efficiency was over 80% for all produced nanoparticles, which also presented sizes below 300 nm and spherical shape. A decrease in viability of endometrial stromal cells from ectopic endometrium of patients with endometriosis and from eutopic endometriotic lesions was demonstrated after 48 h of incubation with the CPO nanoparticles. The nanoparticles without CPO were not able to alter the cell viability of the same cells, indicating that this material was not cytotoxic to the tested cells and suggesting that the effect was specific to CPO. The results indicate that the use of CPO nanoparticles may represent a promising alternative for the treatment of endometriosis.
Objectives
The hormonal treatment for endometriosis frequently fails to completely eradicate endometriotic implants. A new therapeutic treatment is needed. This study investigates the in‐vitro effect ...of Copaifera langsdorffii oil‐resin on human eutopic and ectopic endometrium stromal cell cultures (EuESCs and EctESCs).
Methods
A nanocomposite system containing the copaiba oil‐resin (NanoCOR) was developed and acute toxicity test was performed. Endometrial stromal cells (ESCs) from non‐endometriotics controls (CESCs), EuESCs and EctESCs were isolated and treated with different concentrations of NanoCOR, at different time intervals to evaluate its effect on cell morphology, proliferation, viability, necrosis and apoptosis induction.
Key findings
When treated with 50 μg/ml of NanoCOR, the morphology of EctESCs changed, as the actin microfilaments were disorganized, disassembled or disrupted. Moreover, at 24 h of treatment with NanoCOR, the EctESCs viability was inhibited, and a significant number of these cells underwent apoptosis. In EuESCs, these effects were observed only at 48 h. Finally, the treatment of EctESCs with NanoCOR increased the lactate dehydrogenase release into the extracellular medium more than in EuESCs.
Conclusions
Our data indicate that NanoCOR has a greater impact on the behaviour of human endometriotic stromal cells than on the eutopic endometrium stromal cells, supporting the idea that NanoCOR should be further investigated as a novel and valuable alternative to treat endometriosis.
Apresentamos uma proposta de efetuar experimentos ao ar livre com objetos e situações cotidianas. O trabalho, realizado por um grupo de graduandos em Física, tem o intuito de propor práticas ...interdisciplinares ao ar livre que proporcionem a possibilidade da interlocução entre as disciplinas de Física e Educação Física, no Ensino Médio. Encenamos situações com o potencial para servir de experimentos que demonstrem conceitos de mecânica clássica, utilizamos a câmera do telefone celular para gravar as cenas e usamos o software Tracker para extrair e analisar os vídeos. Resgatamos o experimento clássico de demonstração da inércia, realizado por Galileu Galilei, com o uso de uma motocicleta e o lançamento vertical de uma bola, além disso, analisamos o lançamento oblíquo por meio do arremesso ao cesto na quadra basquete, também verificamos o movimento superamortecido de uma bola de tênis quicando no solo e conferimos a trajetória representada pela braquistócrona com o uso de uma marca feita no pneu de uma bicicleta em movimento. Todas as cenas selecionadas se mostraram adequadas para utilização na proposta interdisciplinar.
In this work, newly developed nanocomposites based upon lamellar silicates are evaluated to determine their potential in controlling endometriosis. The preparation of the new nanocarriers is ...detailed, properties characterized and in vitro pharmacological evaluation performed. The nanocomposites in this study were obtained from the reaction of copaiba oil-resin (COPA) with the polymer polyvinylpyrrolidone (PVP K-30). COPA was selected due to its antiinflammatory and anticancer activities along with the organophilic derivatives of sodium montmorillonite, Viscogel B8, S7 and S4. The results indicated that it was feasible to obtain a good yield of a COPA nanocomposite using a simple process. Intercalation was confirmed by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). In vitro release experiments demonstrated that COPA was released from the nanocomposite in a delayed fashion. Whereas, in vitro pharmacological studies showed a reduction in viability and proliferation of endometriotic cell cultures upon COPA nanocomposite treatment, suggesting that the system developed here can be a promising alternative therapy for the oral treatment of endometriosis.
•Nanocomposite containing copaiba oil-resin can be obtained with good yield by intercalation in solution method.•The copaiba oil-resin is released from the nanocomposite following Higuchi's model in a delayed release.•The nanocomposites containing copaiba reduced the viability and proliferative capacity of the endometriotic cell cultures.
Inclusions of lidocaine hydrochloride in cyclodextrins were prepared to obtain stable complexes compatible for association with chlorhexidine in a new gel formulation for use in urogenital ...applications. Two cyclodextrins, β-cyclodextrin and methyl-β-cyclodextrin, were used for encapsulating lidocaine hydrochloride through solubilization and kneading techniques. The lidocaine-cyclodextrin complexes were characterized by ultraviolet spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The results revealed that the techniques generated good yields of inclusion products that maintained the functional properties of lidocaine. In addition, the inclusion products obtained improved the compatibility of lidocaine hydrochloride with chlorhexidine in solution and a gel formulation. The gel formulation displayed desirable rheological and physicochemical properties. The results presented here are the first description of the inclusion of lidocaine with cyclodextrins, which improves compatibility with chlorhexidine in formulations for simultaneous delivery.
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