A Critical Review of Properties and Analytical Methods for the Determination of Docetaxel in Biological and Pharmaceutical Matrices.

Docetaxel (DTX) is an antineoplastic agent of the second generation of the taxoid family. It is a semi-synthetic drug prepared from a precursor extracted of the plant Taxus baccata. The commercial formulation of DTX, Taxotere®, employs the surfactant polysorbate 80, due to the low water solubility of the drug, causing several side effects. Therefore, there is a need to develop delivery systems to reduce the side effects of DTX. In addition, this drug has been qualitative and quantitatively analyzed in pharmaceutical formulations and biological samples. Thus, several techniques and analytical methods have been reported with the aim of optimizing the analytical signal, increasing sensitivity, selectivity and reducing the effects of interference. Herein, we highlight immunoassay, capillary electrophoresis and chromatographic methods. This review presents a summary of physicochemical and pharmacokinetics properties, mechanisms of action, drug delivery systems and analytical methods used in quantification of DTX in diverse matrices such as blood, plasma, oral fluid, urine, carcinoma cells, pharmaceutical formulations and delivery systems.

Immunoliposomes: A review on functionalization strategies and targets for drug delivery.

Nanoparticles, especially liposomes, have gained prominence in the field of drug delivery for the treatment of human diseases, particularly cancer; they provide several advantages, including controlled drug release, protection of the drug against degradation, improved pharmacokinetics, long circulation, and passive targeting to tumors and inflammatory sites due to the enhanced permeability and retention effect. The functionalization of liposomes with monoclonal antibodies or antibody fragments to generate immunoliposomes has emerged as a promising strategy for targeted delivery to and uptake by cells overexpressing the antigens to these antibodies, with a consequent reduction in side effects. In this review, we address functionalization strategies for the non-covalent and covalent attachment of monoclonal antibodies and their fragments to liposomal surfaces. The main reaction occurs between the sulfhydryl groups of thiolated antibodies and maleimide-containing liposomes. Furthermore, we explore the main targeting possibilities with these ligands for the treatment of a variety of pathologies, including HER2- and EGFR-positive cancers, inflammatory and cardiovascular diseases, infectious diseases, and autoimmune and neurodegenerative diseases, which have not previously been reviewed together. Overall, many studies have shown selective delivery of immunoliposomes to target cells, with promising in vivo results, particularly for cancer treatment. Although clinical trials have been conducted, immunoliposomes have not yet received clinical approval. However, immunoliposomes are promising formulations that are expected to become available for therapeutic use after clinical trials prove their safety and efficacy, and after scaling issues are resolved.

Anti-inflammatory, antioxidant and anti-Mycobacterium tuberculosis activity of viridiflorol: The major constituent of Allophylus edulis (A. St.-Hil., A. Juss. & Cambess.) Radlk.

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Allophylus edulis (A. St.-Hil., A. Juss. & Cambess.) Radlk. (Sapindaceae) are traditionally used as a natural anti-inflammatory agent; however, there are no scientific studies demonstrating its activity essential oil. The content of essential oil in A. edulis may be the chemical basis to explain its ethnobotanical uses, since infusions of this plant are used to treat inflammation in the traditional medicine in Brazil. AIM OF THE STUDY: This study evaluated the anti-inflammatory, antioxidant and anti-mycobacterial activities of the essential oil (EOAE) and viridiflorol, its main compound. MATERIAL AND METHODS: Essential oil from fresh leaves of A. edulis (EOAE) was obtained by hydrodistillation in a Clevenger-type apparatus. Forty-one compounds, accounting for 99.10% of the oil, were identified by gas chromatography-mass spectrometry (GC-MS). The major constituent of the oil was viridiflorol (30.88%). Additionally, the essential oil and viridiflorol were evaluated using an in vitro test against Mycobacterium tuberculosis and in 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. Both EOAE (30 and 100mg/kg) and viridiflorol (3 and 30mg/kg) by oral administration were assayed in carrageenan-induced mice paw oedema and pleurisy using subcutaneous injection of dexamethasone (0.5mg/kg) as the positive control. RESULTS: EOAE and viridiflorol displayed moderate in vitro activity in the M. tuberculosis assay. In all tests, EOAE and viridiflorol showed moderate antioxidant activity compared with reference standards. Both EOAE and viridiflorol showed significant inhibition in the carrageenan-induced mice paw oedema via oral administration of the oil (30 and 100mg/kg), compound (3 and 30mg/kg), and subcutaneous injection of dexamethasone (0.5mg/kg, reference drug). Also EOAE and viridiflorol significantly inhibited carrageenan (Cg) induced pleurisy, reducing the migration of total leucocytes in mice by 62±5% (30mg/kg of oil), 35±8% (100mg/kg of oil), 71±5% (3mg/kg of viridiflorol) and 57±3% (30mg/kg of viridiflorol). CONCLUSION: For the first time, the results from this work corroborate the literature, showing that A. edulis can be used as a natural anti-inflammatory agent. Moreover, both EOAE and viridiflorol exhibited biological activities, such as anti-mycobacterial, anti-inflammatory and antioxidant activity.

Potencial alelopático de Tropaeolum majus L. na germinação e crescimento inicial de plântulas de picão-preto / Allelophaty potential of Tropaeolum majus L on picão-preto seeds germination and initial seedling growth

Objetivou-se com este estudo avaliar o potencial alelopático de extratos metanólicos de folhas, flores e raízes de capuchinha (Tropaeolum majus L.) sobre a germinação de sementes e o crescimento inicial de plântulas de picão-preto. O extrato metanólico com melhor potencial de inibição foi submetido a particionamento, resultando nas frações hexânica, clorofórmica, acetato de etila e hidrometanólica e posterior caracterização pelo espectro de absorção na região do infravermelho (IV). O efeito alelopático foi avaliado sobre as sementes de picão-preto, as quais foram distribuídas sobre papel germitest umedecido com 2mL dos extratos e mantidas em germinador do tipo B.O.D. regulado a temperatura de 25°C e luz branca constante, sendo que as sementes imersas diretamente em água constituíram o tratamento controle. A avaliação da qualidade da semente foi realizada pelos testes de germinação e vigor (primeira contagem e comprimento de raiz primária e de hipocótilo das plântulas), em delineamento inteiramente ao acaso. O potencial alelopático das folhas de capuchinha foi maior em relação às demais partes da planta sobre a germinação das sementes, comprimento de hipocótilo e de raiz das plântulas de picão-preto. Estes efeitos podem estar associados à presença de grupos químicos polares, pois à medida que se aumentou a polaridade dos solventes detectou-se maior efeito inibitório sobre a germinação e o crescimento inicial de plântulas de picão-preto.

This research aimed to evaluate the metanolic extracts allelopathic potential from leaves, flowers and roots of capuchinha (Tropaeolum majus L.) on picão-preto seeds germination and initial seedling growth. The best inhibitor metanolic extract was fractioned, in hexanic, cloroformic, etil acetate and hidrometanolic fractions and it was characterized through absorption spectrum using mid-infrared. To evaluate the allelopathic effect of metanolic extracts and the fractions aftereffect; it was used picão-preto seeds distributed on 2ml extracts moistured paper maintained in B.O.D. germinator at 25°C and white constant light. Seeds sowed directly in water moistured germitest paper constituted the control. The allelopathic potential extracts were evaluated through the first count, final germination percentage, seedlings primary root and hypocotyl length (cm). The experiment was carried out DIC with three replications of 25 seeds. The capuchinha leaves showed allelopathic potential on picão-preto seeds germination, hypocotyl and seedlings primary root length. It was suggested that such effects are associated to the presence of polar chemical groups because the increase in the solvents polarity detected the major picão-preto germination and seedlings growth inhibition effect.