Preparation of PEGylated graphene oxide nanoparticles loaded with oridonin and its inhibitory effects on human colon cancer / 中草药

Objective To prepare PEGylated graphene oxide nanoparticles (GO-PEG-NPs) loaded with oridonin (ORI) and investigate its inhibitory effect on human colon cancer. Methods 4-armed PEG was grafted onto GO via an amidation process and GO-PEG was characterized by IR and TGA. Then, ORI, a widely used cancer chemotherapy drug, was absorbed onto GO-PEG via blending. The encapsulation efficiency and drug loading ratio were measured by UV. The cytotoxicity of ORI-GO-PEG, GO-PEG, and free ORI on SW620 and HT29 human colon cancer cells were evaluated using MTT assay. In vivo anti-tumor activity of ORI-GO-PEG-NPs were evaluated in mice bearing SW620 tumor. Results IR and TGA data indicated that 4-armed PEG was successfully coupled with GO and UV data showed that the encapsulation efficiency and drug loading ratio were 95.81% and 48.92%, respectively. Moreover, ORI-GO-PEG-NPs showed good stability in physiological condition. The results of cytotoxicity test indicated that compared to free ORI, the ORI-GO-PEG-NPs exhibited higher cytotoxicity in SW620 and HT29 cells. Meanwhile, it was confirmed that ORI-GO-PEG- NPs could significantly inhibit the growth of SW620 tumor in vivo compared with ORI. Conclusion The obtained ORI-GO-PEG-NPs displayed excellent drug-loading capacity and better tumor inhibitory effect. These results provided the experimental basis for development of anticancer drug delivery system.

Physico-chemical and structural characterization of mucilage isolated from seeds of Diospyros melonoxylon Roxb

Mucilage was isolated from the seeds of Diospyros melonoxylon Roxb., a plant growing naturally in the forests of India. Various physico-chemical methods like particle analysis, scanning electron microscopy, differential scanning calorimetry, differential thermal analysis, thermogravimetry analysis, molecular weight by gel permeation chromatography, rheometry, elemental analysis, x-ray diffraction spectrometry, zeta potential, fourier transform infrared spectroscopy, 1D(1H and 13C) (NMR) have been employed to characterize this gum in the present study. Particle analyses suggest that mucilage had particle size in nanometer. SEM analysis suggested that the mucilage had irregular particle size. The glass transition temperature of the gum observed was 78 °C and 74 °C by DSC and DTA respectively. The Thermogravimetry analysis suggested that mucilage had good thermal stability with two stage decomposition. The molecular weight of mucilage was determined to be 8760, by gel permeation chromatography, while the viscosity of mucilage was observed to be 219.1 cP. The XRD pattern of the mucilage indicated a complete amorphous nature. Elemental analysis of the gum revealed specific contents of carbon, hydrogen, nitrogen and sulfur. The major functional groups identified from FT-IR spectrum include 3441 cm-1 (-OH), 1632 cm-1 (-COO-), 1414 cm-1 (-COO-) and 1219 cm-1 (-CH3CO). Analysis of mucilage by paper chromatography and 1D NMR indicated the presence of sugars.

Mucilagem foi isolada de sementes de Diospyros melanoxylon Roxb, uma planta que cresce naturalmente nas florestas da Índia. Vários métodos físico-químicos, como análise de partículas, microscopia electrônica, calorimetria diferencial de varredura, análise térmica diferencial, análise termogravimétrica, massa molecular por cromatografia de permeação em gel, viscosidade, análise elementar, espectrometria de difração de raios-x, potencial zeta, espectroscopia no infravermelho com transformada de Fourier, 1D (1H e 13C) (NMR) foram utilizados no presente estudo para caracterizar essa goma. A análise de partículas sugere que a mucilagem tem tamanho de partícula em nm. A análise SEM sugere que a mucilagem tem tamanho de partícula irregular. Observou-se temperatura de transição vítrea da goma de 78 °C e 74 °C por DSC e DTA, respectivamente. A análise termogravimétrica sugeriu que a mucilagem possuía boa estabilidade térmica, com duas fases de decomposição. A massa molecular da mucilagem foi 8760, por meio de cromatografia de permeação em gel, enquanto que a viscosidade foi 219,1 cP. O padrão de DRX da mucilagem indicou natureza completamente amorfa. Os principais grupos funcionais identificados a partir do espectro de FT-IR foram: 3441 cm-1 (-OH), 1632 cm-1 (-COO-), 1414 cm-1 (-COO-) e 1.219 cm-1 (CH3CO-). As análises de mucilagem por cromatografia em papel e 1D RMN indicaram a presença de açúcares.

Estudios organolépticos, fisicoquímicos, microbiológicos e interacción con excipientes farmacéuticos de un extracto purificado de cera de Apis mellifera / Organoleptic, physicochemical and microbiological studies and its interaction with pharmaceutical excipients of a purified extract from Apis mellifera wax

El D-002, ingrediente activo antioxidante extraído de la cera de abejas Apis mellifera, fue caracterizado desde el punto de vista físicoquímico, de igual forma se analizó su interacción con excipientes de interés farmacéutico. El D-002 es un polvo fluido inodoro de color blanco a crema, con pérdidas por secado £ 1 por ciento; es insoluble en agua y etanol, y muy ligeramente soluble en otros disolventes orgánicos. Su composición, determinada por cromatografía de gases, fue: 1-tetracosanol (6-15 por ciento), 1-hexacosanol (7-20 por ciento), 1-octacosanol (12-20 por ciento), 1-triacontanol (25-35 por ciento) 1-dotriacontanol (18-25 por ciento) y 1-tetratriacontanol (£ 7,5 por ciento), para una pureza ³ 85 por ciento. Fue estable durante 5 años en la zona climática IV y su análisis por calorimetría diferencial de barrido mostró 2 transiciones de fusión a 59,0 y 81,1 ºC sin descomposición, una alta estabilidad térmica hasta 200 ºC, así como la ausencia de interacciones con lactosa, almidón, croscarmelosa sódica, polivinil pirrolidona, celulosa microcristalina y estearato de magnesio, lo que posibilita el empleo de estos excipientes en la formulación de las tabletas

The D002, an antioxidant active ingredient extracted from the Apis mellifera bees wax was characterized from the physicochemical point of view analyzing its interaction with excipients of pharmaceutical interest. The D-002 is a creamy white odourless fluid powder with losses by £ 1 percent dry; it is water and ethanol insoluble and very slightly soluble in other organic solvents. Its composition, determined by gas chromatography was: 1-tetracosanol (6-15 percent), 1-hexacosanol (7-20 percent), 1-octacosanol (12-20 percent), 1-triacontanol (25-35 percent, 1-dotriacontanol (18-25 percent) and 1-tetratriacontaol (£ 7,5 percent) for ³ 85 percent of purity. It remained stable during 5 years in the IV climatic zone and its analysis by differential scanning calorimetry showed 2 fusion transitions at 59,0 and 81,1 ºC. without decomposition, a high thermal stability up to 200 ºC, as well as a lack of interactions with lactose, starch, sodium croscarmelosa, polyvinylpyrrolidone, microcrystalline cellulose, and magnesium stearate allowing the use of these excipients in tablets formula