Cristiane Franco Codevilla

Validation of an SEC‐HPLC Method for the Analysis of rhG‐CSF in Pharmaceutical Formulations

Abstract Granulocyte colony‐stimulating factor (G‐CSF) is a hematopoietic cytokine produced by recombinant DNA technology and used clinically to treat neutropenia. An isocratic high performance liquid chromatography procedure was developed for the assay of filgrastim in pharmaceutical formulations. HPLC separation was carried out by size‐exclusion chromatography on a TSK gel G2000 SW column (60 cm × 7.5 mm I.D.). The mobile phase was composed of phosphoric acid (pH 2.5; 0.1 M), run at a flow rate of 1.0 mL min−1 and with UV detection at 214 nm. Method validation investigated parameters such as the range, linearity (r 2 = 0.9998), precision, accuracy, and robustness; the method yielded good results with a quantitation limit of 45 µg mL−1 and a detection limit of 12 µg mL−1. The results demonstrate the validity of the SEC‐HPLC method for the analysis of filgrastim.

Development and validation of a stability-indication LC-UV method for determination of daptomycin injectable form and kinetic study in alkaline medium

An isocratic liquid chromatography method (LC-UV) was developed and validated to determine daptomycin in injectable form. The method was carried out in a Waters XBridge C18 column (250 mm × 4.6 mm, 5 μm). The mobile phase was composed of methanol–acetonitrile–buffer (pH 2.2) (40 : 30 : 30 v/v/v) at a flow rate of 1.0 mL−1, using photodiode array (PDA) detection at 223 nm. The retention time obtained for daptomycin was 6.1 min and the method was linear in the range of 10 to 50 μg mL−1 (r = 0.9999). Forced degradation studies were performed to verify the specificity and stability-indicating capability of the method. The degradation kinetics under alkaline conditions were also evaluated. The method showed suitable accuracy (99.17%) and precision (RSD 0.59%) A two level full factorial design was used to determine the method robustness. The proposed method was applied for the analysis of daptomycin injectable form, contributing to the improvement of the quality control of this pharmaceutical product.

Transferrin-Conjugated Nanocarriers as Active-Targeted Drug Delivery Platforms for Cancer Therapy

A lot of effort has been devoted to achieving active targeting for cancer therapy in order to reach the right cells. Hence, increasingly it is being realized that active-targeted nanocarriers notably reduce off-target effects, mainly because of targeted localization in tumors and active cellular uptake. In this context, by taking advantage of the overexpression of transferrin receptors on the surface of tumor cells, transferrin-conjugated nanodevices have been designed, in hope that the biomarker grafting would help to maximize the therapeutic benefit and to minimize the side effects. Notably, active targeting nanoparticles have shown improved therapeutic performances in different tumor models as compared to their passive targeting counterparts. In this review, current development of nano-based devices conjugated with transferrin for active tumor-targeting drug delivery are highlighted and discussed. The main objective of this review is to provide a summary of the vast types of nanomaterials that have been used to deliver different chemotherapeutics into tumor cells, and to ultimately evaluate the progression on the strategies for cancer therapy in view of the future research.

Nanoestruturas contendo compostos bioativos extraídos de plantas

Many natural compounds, extracted from fruits and vegetables, have promising potential for maintaining and promoting health as well as preventing and treating some diseases. In the food industry, the use of plant extracts, as an alternative to chemical or synthetic antioxidants and antimicrobials to combat the foodborne pathogens, inhibiting lipid oxidation and thus extending the shelf life is an increasing trend. However, most of bioactive compounds present in these extracts such as polyphenols, carotenoids, alkaloids, among others, have low water solubility, stability and bioavailability. In this sense, nanotechnology is an innovative approach that has potential applications in nutraceutical research, since it improves these characteristics, besides enhance their absorption, protect them from premature degradation in the body and prolong their circulation time. There are different nanostructured systems that can be used in foods such as liposome, polymeric nanoparticles, lipid solid nanoparticles and nanoemulsions. This work presents a review of the main nanostructured systems used for association of different plant extracts and some technological applications.

Validação de método por cromatografia líquida de alta eficiência para determinação da lamivudina e zidovudina em comprimidos

An HPLC method was validated to assay lamivudine and zidovudine combined in tablets. The chromatographic separation was carried out using methanol and acetate buffer pH 6.5 (50:50 v/v) and a RP-18 column, as mobile and stationary phase, respectively. The UV detection was at 270 nm. The method was linear in the range of 24 - 36 µg/mL (lamivudine) and 48 - 72 µg/mL (zidovudine). The recovery (accuracy) ranged from 101.35% to 103.04% and the precision (repeatability and intermediate precision) was less than 2%. The method can be also applied to the quantification of these drugs in the dissolution test of tablets containing both drugs.

Biological potency evaluation and characterization of rhG-CSF in pharmaceutical products

The identification of rhG-CSF was carried out in pharmaceutical preparations by non-reducing polyacrylamide gel electrophoresis and western blotting with specific antibodies, showing a single band in the 19 kDa region. The potency was assessed by the neutropenia mouse bioassay giving values between 88.4 and 122.4% of the stated potency. The precision index expressed by weight was between 141 and 432 for the independent assays. Batch-to-batch, the samples met the requirements for the safety test and bacterial endotoxins test. The biological and immunological results showed the quality of the products in clinical use and the specifications established contribute to assuring the safety and efficacy of biological medicines.

Incorporação da curcumina em sistemas nanoestruturados: Revisão

A curcumina e um composto polifenolico extraido do rizoma de Curcuma longa Linn com diversas propriedades farmacologicas, como anti-inflamatorio, antioxidante, anticarcinogenico, antimicrobiano, hepatoprotetor, hipoglicemiante, entre outras, sendo interessante o desenvolvimento de produtos contendo curcumina, os quais trarao beneficios a saude. A curcumina pode ser empregada como um aditivo natural em substituicao aos sinteticos, como corantes, antioxidantes e antimicrobianos, e tambem em funcao de suas propriedades farmacologicas. Entretanto, a sua incorporacao em alimentos funcionais ou sua utilizacao como suplemento alimentar e dificultada pela baixa solubilidade em agua, susceptibilidade a condicoes alcalinas, luz, calor e oxidacao. A nanotecnologia e uma area emergente para melhorar a baixa solubilidade, estabilidade e biodisponibilidade da curcumina. Varios tipos de nanoparticulas tem sido encontrados como sendo adequados para a encapsulacao de curcumina. Este artigo revisa os sistemas nanoestruturados contendo curcumina, como nanoparticulas polimericas, nanoparticulas lipidicas solidas, lipossomas e nanoemulsoes. Alem das tecnicas de nanoencapsulacao e caracteristicas fisico-quimicas destes carreadores.

MICROENCAPSULATION OF BIOACTIVE COMPOUNDS BY EXTRUSION METHOD

The development of functional foods by adding bioactive faces many hurdles in the production of new foods. Microencapsulation is a useful tool to facilitate the protection of these compounds in foods, in particular, probiotics, vitamins, minerals, fatty acids, etc. Various microencapsulation methods have been used in order to improve the use of these ingredients promoting the successful delivery of these bioactive substances in the gastrointestinal tract. Among the microencapsulation techniques bioactive compounds, extrusion has been employed to obtain microparticles. In this review we will discuss topics regarding bioactive compounds and how to improve its stability through microencapsulation, emphasizing the method and studies on the extrusion technique.

Encapsulação de compostos bioativos por coacervação complexa

The bioactive compounds are chemicals found in plants and are widely known for bringing health benefits, so it can be designated as functional foods. However, they are sensitive to various factors found in the environment that are exposed primarily to tratogastrointestinal and, moreover, are lipophilic, therefore, have low solubility in aqueous media. In this sense, the encapsulation of these compounds is an alternative protection, and the provision of such compounds in suitable amounts. The complex coacervation microencapsulation is a technique commonly used for such compounds, besides having front advantages to other techniques such as the use of biopolymers, no use of toxic agents, among others. Currently, there are a lot of research in this direction, which will be presented in this paper. Thus, the present review aims to present the main bioactive compounds studied and encapsulated as well as the parameters for complex coacervation technique.

Emulsificação/gelificação iônica interna: Alternativa para microencapsulação de compostos bioativos

The application of bioactive compounds in food have attracted the interest of the industry due to potential health benefits to humans. However, the efficiency depends on the stability, bioactivity and bioavailability of these active ingredients in the food matrix. The unpleasant taste and instability limit the application of these compounds. The use of encapsulated bioactive instead of free compounds can effectively alleviate these problems. The encapsulation technology being used in many different active compounds is the emulsification/internal ionic gelation, which is an important alternative for improving the stability and application in food.