Understanding the Integrity of Coating for Taste-Masked Granules – Before and After Tablet Compression

Raman microscopy was used to visualize the integrity of a barrier membrane coating at the various stage of chewable tablets development. The effect of substrate morphology and particle characteristics was found to be important in maintaining the integrity of the coating throughout the process of chewable tablets manufacture. Furthermore, the observations from the Raman image analysis provide an understanding of the factors affecting drug release

Impact of dispersion time interval and particle size on release profiles of propranolol HCl and carbamazepines from microparticle blends system

The objective of this study was to investigate the effect of dispersion time interval (DTI) on physicochemical properties of drug following the incorporation of propranolol HCl (Pro) and carbamazepine (CBZ) within ethyl cellulose (EC) microparticle blends using solvent evaporation method. The first Pro emulsion and second CBZ oil phase were dispersed in an external aqueous phase, with DTI of 0 and 60 min. The morphology of microparticle blends were characterized by SEM. The particle size mean of the emulsion droplets/hardened microparticles were monitored by FBRM. Encapsulation efficiency (EE) and in vitro drug release were also investigated. The resulting microparticle blends were spherical and formed two populations. The particle size mean of microparticle blends ranged from 113.27 µm to 122.42 µm. The EE was 77.28% to 78.64% for Pro and 96.48% to 98.64% for CBZ. FBRM studies showed that the size of microparticle blend prepared as W/O/W (Pro) and O/W (CBZ) system with DTI of 60 min and stirring time 4 h were larger than those prepared with DTI of 0 min. In vitro drug release studies after 28 days that revealed the CBZ release (58.72%) was faster than Pro release (43.16%). Investigation on surface morphology by SEM showed that the second drug CBZ which added as the oil phase in the W/O/W emulsion system had blocked the pores on the surface Pro microparticles prepared from the first primary emulsion, therefore affecting the drug release. This blocking effects of second drug (CBZ) on first emulsion microparticles (Pro) depended on the DTI. This phenomenon is only applicable if the first primary emulsion is W/O/W system

PREPARATION AND CHARACTERIZATION OF POLY(Є-CAPROLACTONE) MICROPARTICLE BLENDS CONTAINING PROPRANOLOL HCl AND CARBAMAZEPINE

The purpose of this study was to investigate physicochemical properties of poly(є- caprolactone) microparticle blends containing drugs with different solubilities (Propranolol HCl [Pro] and carbamazepine [CBZ]). Microparticle blends were formulated with W/O/W emulsion for Pro and O/W emulsion for CBZ. The Pro emulsion (W/O) and CBZ oil phase (O) were dispersed in an external aqueous phase (W), with dispersion time interval (DTI) of 0 and 60 min. Morphology of microparticle blends were characterized by scanning electron microscopy (SEM). Particle size mean of emulsion droplets/hardened microparticles were monitored by focused beam reflectance measurement (FBRM). Encapsulation efficiency (EE) and in vitro drug release in phosphate buffer (pH 7.4) were also investigated. The results showed that the resulting microparticle blends obtained by solvent evaporation method were spherical and having two populations. FBRM data showed that the size of microparticle blends prepared with DTI 60 min and stirring time 4 h was larger than those with DTI 0 min. The encapsulation efficiency were 62.05% to 66.38% for Pro and 70.56% to 73.85% for CBZ in microparticle blends. Drug release in phosphate buffer after 28 days showed that the Pro release (33%) was slower than CBZ release (60%) from microparticle blends with DTI 60 min. This phenomenon was attributed to the interaction of oil phase (CBZ) with hard particles from primary emulsion (Pro), whereby the oil phase had blocked and coated pores on the surface of hard particle from primary emulsion

Drug distribution in nanostructured lipid particles

The targeted design of nanoparticles for efficient drug loading and defined release profiles is even after 25 years of research on lipid-based nanoparticles still no routine procedure. It requires detailed knowledge about the interaction of the drug with the lipid compounds and about its localisation and distribution in the nanoparticle. We present here an investigation on nano-sized lipid particles (NLP) composed of Gelucire and Witepsol as solid lipids, and Capryol as liquid lipid, loaded with Dexamethasone, a glucocorticoid used in topical treatment of inflammatory dermal diseases. The interactions of Dexamethasone, which was spin-labelled by 3-(Carboxy)-2,2,5,5-tetramethyl-1-pyrrolidinyloxy (DxPCA), with its microenvironment are monitored by EPR spectroscopy at 94 GHz at low temperatures. The mobility of the spin-labelled drug was probed by X-band EPR at room temperature. In order to relate the magnetic and dynamic parameters deduced from EPR to the local environment of the spin probe in the NLP, investigations of DxPCA in the individual lipid compounds were carried out. The magnetic parameters reflecting the polarity of DxPCA’s environment as well as the parameters describing the mobility of the drug reveal that in the case of colloidal dispersions of the lipids and also the NLP DxPCA is attached to the surface of the nanoparticles. Although the lipophilic drug is almost exclusively associated with the NLP in aqueous solution, dilution experiments show, that it can be easily released from the nanoparticle

Nanocrystals for Improved Drug Delivery of Dexamethasone in Skin Investigated by EPR Spectroscopy

Nanocrystals represent an improvement over the traditional nanocarriers for dermal application, providing the advantages of 100% drug loading, a large surface area, increased adhesion, and the potential for hair follicle targeting. To investigate their advantage for drug delivery, compared to a base cream formulation, dexamethasone (Dx), a synthetic glucocorticoid frequently used for the treatment of inflammatory skin diseases, was covalently linked with the paramagnetic probe 3-(carboxy)-2,2,5,5-tetramethyl-1-pyrrolidinyloxy (PCA) to DxPCA. To investigate the penetration efficiency between these two vehicles, electron paramagnetic resonance (EPR) spectroscopy was used, which allows the quantification of a spin-labeled drug in different skin layers and the monitoring of the drug release. The penetration behavior in excised healthy and barrier-disrupted porcine skin was monitored by EPR, and subsequently analyzed using a numerical diffusion model. As a result, diffusion constants and free energy values in the different layers of the skin were identified for both formulations. Dx-nanocrystals showed a significantly increased drug amount that penetrated into viable epidermis and dermis of intact (factor 3) and barrier-disrupted skin (factor 2.1) compared to the base cream formulation. Furthermore, the observed fast delivery of the spin-labeled drug into the skin (80% DxPCA within 30 min) and a successive release from the aggregate unit into the viable tissue makes these nanocrystals very attractive for clinical applications

Priprava, in vitro i in vivo evaluacija bioadhezivnih mikrosfera s algino-pektinom: ispitivanje utjecaja polimera pomoću multiple poredbene analize

Ionotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigated in vitro for possible sustained drug release and their use in vivo as a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunett\u27s multiple comparison analyis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.U radu je opisana priprava algino-pektinskih bioadhezivnih mikrosfera protuupalnog lijeka aceklofenaka metodom ionotropnog geliranja. In vitro je ispitivana mogućnost postupnog oslobađanja ljekovite tvari iz mikrosfera te mogućnost upotrebe mikrosfera kao gastroprotektivnog sustava za isporuku aceklofenaka in vivo. Ispitivan je utjecaj koncentracije polimera i omjera polimera i lijeka na svojstva mikrosfera. Mikrosfere su bile bioahezivne i sadržavale su veliki udio lijeka. Oslobađanje aceklofenaka iz alginatnih mikrosfera bilo je brže, a iz mikrosfera s algino-pektinom usporeno. Dunnetova multipla analiza ukazuje na značajnu razliku u postotku inhibicije edema šape kada se usporede optimizirana formulacija i čista ljekovita tvar. Može se zaključiti da su bioadhezivne mikrosfere s algino-pektinom povoljne za usporeno oslobađanje aceklofenaka te da pružaju umjerenu zaštitu sluznice želuca

The Effect of Temozolomide/Poly(lactide-co-glycolide) (PLGA)/Nano-Hydroxyapatite Microspheres on Glioma U87 Cells Behavior

In this study, we investigated the effects of temozolomide (TMZ)/Poly (lactide-co-glycolide)(PLGA)/nano-hydroxyapatite microspheres on the behavior of U87 glioma cells. The microspheres were fabricated by the “Solid/Water/Oil” method, and they were characterized by using X-Ray diffraction, scanning electron microscopy and differential scanning calorimetry. The proliferation, apoptosis and invasion of glioma cells were evaluated by MTT, flow cytometry assay and Transwell assay. The presence of the key invasive gene, αVβ3 integrin, was detected by the RT-PCR and Western blot method. It was found that the temozolomide/PLGA/nano-hydroxyapatite microspheres have a significantly diminished initial burst of drug release, compared to the TMZ laden PLGA microspheres. Our results suggest they can significantly inhibit the proliferation and invasion of glioma cells, and induce their apoptosis. Additionally, αVβ3 integrin was also reduced by the microspheres. These data suggest that by inhibiting the biological behavior of glioma cells in vitro, the newly designed temozolomide/PLGA/nano-hydroxyapatite microspheres, as controlled drug release carriers, have promising potential in treating glioma

Microencapsulation of Flavors in Carnauba Wax

The subject of this study is the development of flavor wax formulations aimed for food and feed products. The melt dispersion technique was applied for the encapsulation of ethyl vanillin in wax microcapsules. The surface morphology of microparticles was investigated using scanning electron microscope (SEM), while the loading content was determined by HPLC measurements. This study shows that the decomposition process under heating proceeds in several steps: vanilla evaporation occurs at around 200 °C, while matrix degradation starts at 250 °C and progresses with maxima at around 360, 440 and 520 °C. The results indicate that carnauba wax is an attractive material for use as a matrix for encapsulation of flavours in order to improve their functionality and stability in products

New biomaterial based on cotton with incorporated biomolecules

The aim of this study was to investigate a method of embedding l-cysteine (l-cys), an antimicrobial agent, between layers of chitosan (CH) and sodium alginate (ALG) onto cotton samples obtained via a layer-by-layer electrostatic deposition technique via several embedding methods. The results show that the best way to incorporate l-cys into the layers was the one that used the property of gelling ALG. To monitor the l-cys embedding into the CH/ALG multilayer film, different methods were used: energy-dispersive X-ray spectrometry analysis to assess the presence of sulfur on the sample, Ellman's reagent method to analyze l-cys release from the sample, and attenuated total reflectance (ATR) Fourier transform infrared spectroscopy (FTIR) to compare the ATR–FTIR spectra of the pure l-cys and l-cys embedded in the CH/ALG multilayer film to study the interaction between the l-cys and the CH/ALG multilayer films. Functionalized CH/ALG cotton samples were also investigated for their antibacterial properties toward Staphylococcus aureus andKlebsiella pneumonia with the Japanese Industrial Standard method JIS L 1902:2002, and the results show an enhancement of the antibacterial effect due to the presence of l-cys.The authors thank Fundação para a Ciência e Tecnologia for the funding granted concerning the project PTDC/EBB-BIO/113671/ 2009 (FCOMP-01-0124-FEDER-014752). Also, they thank Fundo Europeu de Desenvolvimento Regional through COMPETE—Programa Operacional Factores de Competitividade for cofunding