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Solid Lipid Nanoparticles (solid + lipid_nanoparticle)
Selected AbstractsSolid lipid nanoparticles (SLN) as carriers for the topical delivery of econazole nitrate: in-vitro characterization, ex-vivo and in-vivo studiesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2007Vanna Sanna Solid lipid nanoparticles (SLN) designed for topical administration of econazole nitrate (ECN), were prepared by o/w high-shear homogenization method using different ratios of lipid and drug (5:1 and 10:1). SLN were characterized in terms of particle size, morphology, encapsulation efficiency and crystalline structure. After incorporation of SLN into hydrogels, rheological measurements were performed, and ex-vivo drug permeation tests were carried out using porcine stratum corneum (SC). In-vivo study of percutaneous absorption of ECN as a function of application time and composition of gels was carried out by tape-stripping technique. Penetration tests of the drug from a conventional gel were performed as comparison. High-shear homogenization method resulted in a good technique for preparation of ECN-loaded SLN. Particles had a mean diameter of about 150 nm and a regular shape and smooth surface. The encapsulation efficiency values were about 100%. Ex-vivo tests showed that SLN were able to control the drug release through the SC; the release rate depended upon the lipid content on the nanoparticles. In-vivo studies demonstrated that SLN promoted a rapid penetration of ECN through the SC after 1 h and improved the diffusion of the drug in the deeper skin layers after 3 h of application compared with the reference gel. [source] Tocopheryl acetate disposition in porcine and human skin when administered using lipid nanocarriersJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2010Mojgan Moddaresi Abstract Objectives Assessing the delivery of a drug into the skin when it has been formulated within a nanocarrier is a complex process that does not conform to the conventions of traditional semi-solid formulations. The aim of this study was to gain a fundamental understanding of drug disposition in both human and porcine skin when applied using a lipidic nanocarrier. Methods A model system was generated by loading tocopheryl acetate into a well-characterised solid lipid nanoparticle and formulating this system as a traditional aqueous hyaluronic acid gel. Franz diffusion cells fitted with a silicone or nylon membrane were used to assess drug and particle transport independently whilst human and pig skin were employed to determine skin delivery. Key findings The tocopheryl acetate, when loaded into the solid lipid nanoparticles, did not release from the particle. However, 1.65 ± 0.90% of an infinite dose of tocopheryl acetate penetrated into the stratum corneum of pig skin when delivered using a nanoparticle-containing gel. Conclusions These results suggest that hydration of the stratum corneum in pig skin could lead to the opening of hydrophilic pores big enough for 50 nm-sized particles to pass into the superficial layers of the skin, a phenomenon that was not repeated in human skin. [source] Cosmetic features and applications of lipid nanoparticles (SLN®, NLC®)INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 3 2008E. B. Souto Synopsis A detailed review of the literature is presented in attempts to emphasize several advantages of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for cosmetic applications. Examples of several actives are given and the main features of the solid core of SLN and NLC for topical delivery of cosmetics are discussed. Lipid nanoparticles have been more and more explored in pharmaceutical technology, showing superior advantages for topical purposes over conventional colloidal carriers. Résumé Un examen détaillé de la littérature est présenté dans les tentatives de souligner les plusieurs avantages des nanoparticule lipidique solide (SLN) et lipidique nanostructurés (NLC) pour applications cosmétiques. Exemples de plusieurs substances actives sont données et les caractéristiques principales du noyau plein de SLN et de NLC pour la libération topique des produits de beauté sont discutées. Les nanoparticles lipides ont été de plus en plus explorées en technologie pharmaceutique, montrant des avantages supérieurs pour les porteurs colloïdaux conventionnels pour administration topique de buts. [source] Comparison of ciprofloxacin hydrochloride-loaded protein, lipid, and chitosan nanoparticles for drug deliveryJOURNAL OF BIOMEDICAL MATERIALS RESEARCH, Issue 1 2008Dharmendra Jain Abstract The aim of the present study was to develop single dose delivery systems based on nanotechnology for prolonged antibiotic release in a controlled manner. Five different drug,carrier ratios of ciprofloxacin hydrochloride-loaded nanoparticles of albumin, gelatin, chitosan (CS), and lipid [solid lipid nanoparticles (SLNs)] were prepared and characterized. Average particle size was found to be in the range of 73 ± 2 to 98 ± 44 nm for SLNs, 140 ± 7 to 175 ± 24 nm for albumin nanoparticles, 143 ± 18 to 184 ± 27 nm for gelatin nanoparticles, and 247 ± 48 to 322 ± 52 nm for CS nanoparticles. A drug-to-carrier ratio of 0.5:1 was preferred for CS nanoparticles having zeta potential of >20 mV and drug encapsulation of 35.01% ± 2.66%. Similarly, 0.6:1 ratio was preferred for albumin nanoparticles with zeta potential >16 mV and drug encapsulation 48.20% ± 3.01%. Zeta potentials of gelatin nanoparticles loaded with ciprofloxacin suggested that they were unstable and prone to flocculation. SLN with 0.25:1 drug carrier ratio showed 38.71% ± 2.38% drug entrapment and ,28 ± 1 mV surface charge. All the nanoparticles showed sustained drug release avoiding "burst effect" of the free drugs for up to 120 h for albumin nanoparticles, 96 h for CS and gelatin nanoparticles, and 80 h for SLNs. The drug release profiles followed Higuchi model. Results suggest that CS nanoparticles and SLNs can act as promising carriers for sustained ciprofloxacin release in infective conditions. © 2007 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2008 [source] Pharmacokinetics and tissue distribution of idarubicin-loaded solid lipid nanoparticles after duodenal administration to ratsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 5 2002Gian Paolo Zara Abstract Idarubicin-loaded solid lipid nanoparticles (IDA-SLN) and idarubicin in solution were prepared and the two formulations were administered to rats, either by the duodenal route or intravenously (iv). The aim of this research was to study whether the bioavailability of idarubicin can be improved by administering IDA-SLN duodenally to rats. Idarubicin and its main metabolite idarubicinol were determined in plasma and tissues by reversed-phase high-performance liquid chromatography. The pharmacokinetic parameters of idarubicin found after duodenal administration of the two formulations were different: area under the curve of concentration versus time (AUC) and elimination half-life were ,21 times and 30 times, respectively, higher after IDA-SLN administration than after the solution administration. Tissue distribution also differed: idarubicin and idarubicinol concentrations were lower in heart, lung, spleen, and kidneys after IDA-SLN administration than after solution administration. The drug and its metabolite were detected in the brain only after IDA-SLN administration, indicating that SLN were able to pass the blood,brain barrier. After iv IDA-SLN administration, the AUC of idarubicin was lower than after duodenal administration of the same formulation. Duodenal administration of IDA-SLN modifies the pharmacokinetics and tissue distribution of idarubicin. The IDA-SLN act as a prolonged release system for the drug. © 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:1324,1333, 2002 [source] Tocopheryl acetate disposition in porcine and human skin when administered using lipid nanocarriersJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2010Mojgan Moddaresi Abstract Objectives Assessing the delivery of a drug into the skin when it has been formulated within a nanocarrier is a complex process that does not conform to the conventions of traditional semi-solid formulations. The aim of this study was to gain a fundamental understanding of drug disposition in both human and porcine skin when applied using a lipidic nanocarrier. Methods A model system was generated by loading tocopheryl acetate into a well-characterised solid lipid nanoparticle and formulating this system as a traditional aqueous hyaluronic acid gel. Franz diffusion cells fitted with a silicone or nylon membrane were used to assess drug and particle transport independently whilst human and pig skin were employed to determine skin delivery. Key findings The tocopheryl acetate, when loaded into the solid lipid nanoparticles, did not release from the particle. However, 1.65 ± 0.90% of an infinite dose of tocopheryl acetate penetrated into the stratum corneum of pig skin when delivered using a nanoparticle-containing gel. Conclusions These results suggest that hydration of the stratum corneum in pig skin could lead to the opening of hydrophilic pores big enough for 50 nm-sized particles to pass into the superficial layers of the skin, a phenomenon that was not repeated in human skin. [source] Melatonin delivery in solid lipid nanoparticles: prevention of cyclosporine A induced cardiac damageJOURNAL OF PINEAL RESEARCH, Issue 3 2009Rita Rezzani Abstract:, Melatonin is a potent antioxidant molecule with a capacity to protect tissues from damage caused by oxidative stress. It reduces cyclosporine A (CsA)-induced cardiotoxicity; this improvement required melatonin's binding to its membrane receptors. This experimental study examined whether melatonin is a useful tool for counteracting CsA-induced apoptosis in the heart of rats. We investigated melatonin's antiapoptotic efficacy in protecting the heart and tested whether this effect was totally dependent on its binding to membrane receptors or also involved radical scavenging. In some animals, solid lipid nanoparticles (SLN) as a melatonin delivery system were used. In one group of rats, melatonin (1 mg/kg/day i.p.) was given concurrently with CsA (15 mg/kg/day s.c.; CsA-MT) for 21 days. In other animals, melatonin loaded in SLN was injected with CsA (CsA-MTSLN). Oxidative stress in heart tissue was estimated using the evaluation of lipid peroxidation and the expression of the isoform of inducible nitric oxide (iNOS). The antiapoptotic effect of melatonin was evaluated using TUNEL staining and Bcl-2 protein family expression. CsA administration produced morphological and biochemical changes in the heart of rats, while melatonin reversed the changes. In particular, since the antiapoptotic melatonin's efficacy is mainly observed when it is loaded in SLN, we suggest that MT1/MT2 pathway is not sufficient for apoptosis antagonism and the additional intracellular effects may be required. Finally, we show that, (i) melatonin significantly reduces CsA cardiotoxicity acting also on apoptotic processes, and (ii) the reduction in CsA-induced cardiotoxicity is mediated mainly by its antioxidant effect. [source] Hydrogenated castor oil nanoparticles as carriers for the subcutaneous administration of tilmicosin: in vitro and in vivo studiesJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 2 2009C. HAN Tilmicosin-loaded solid lipid nanoparticles (SLN) were prepared with hydrogenated castor oil (HCO) by o/w emulsion,solvent evaporation technique. The nanoparticle diameters, surface charges, drug loadings and encapsulation efficiencies of different formulations were 90,230 nm, ,6.5,,12.5 mV, 40.3,59.2% and 5.7,11.7% (w/w), respectively. In vitro release studies of the tilmicosin-loaded nanoparticles showed a sustained release and the released tilmicosin had the same antibacterial activity as that of the free drug. Pharmacokinetics study after subcutaneous administration to Balb/c mice demonstrated that a single dose of tilmicosin-loaded nanoparticles resulted in sustained serum drug levels (>0.1 ,g/mL) for 8 days, as compared with only 5 h for the same amount of tilmicosin phosphate solution. The time to maximum concentration (Tmax), half-life of absorption (T½ ab) and half-life of elimination (T½ el) of tilmicosin-loaded nanoparticles were much longer than those of tilmicosin phosphate solution. Tissue section showed that drug-loaded nanoparticles caused no inflammation at the injection site. Cytotoxicity study in cell culture and acute toxicity test in mice demonstrated that the nanoparticles had little or no toxicity. The results of this exploratory study suggest that the HCO,SLN could be a useful system for the delivery of tilmicosin by subcutaneous administration. [source] Novel Sample Preparation Method of Polymer Emulsion for SEM ObservationMICROSCOPY RESEARCH AND TECHNIQUE, Issue 10 2007Jing Xu Abstract The aim of this study was to design a simple and reliable method for obtaining the detailed information about the average size, size distribution, and the surface morphology of particles with variation of the sample preparation of a polymer emulsion. In this work, the characteristic features of the particles of rosin size with high viscosity were first described by scanning electron microscopy (SEM). The morphologies of polymer emulsion of solid lipid nanoparticles and of the microspheres were observed. The advantage of the method is that not only the true size and shape of emulsion particles can be shown, but the problem of high-viscosity emulsion that prevents there study with SEM is solved. Using this new method, the micromorphology and size distribution of the emulsion particles with different viscosities have been clearly observed. Microsc. Res. Tech., 2007. © 2007 Wiley-Liss, Inc. [source] | ||||||||||