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Abstract: Long chain lipid (LCL) based tamoxifen loaded nanostructured lipid carriers (Tmx-NLCs) meant to target intestinal lymphatic systems (ILSs) was developed and characterized previously. The aim of the present work was to evaluate in vitro efficacy of developed Tmx-NLC against breast cancer cell lines and to confirm the hypothesis of targeting ILS after single dose oral administration. In vitro anticancer activity of Tmx-NLC was assessed in human estrogen receptor expressing breast cancer cell lines viz. MCF-7 and ZR-75-1. The study revealed relatively improved activity for Tmx-NLC compared to free Tmx against MCF-7 cells. However, the activity was compromised against ZR-75-1 cells which could be attributed to its up regulation of MUC1 gene. Confocal and flow cytometric analysis revealed remarkable intracellular uptake of Tmx-NLC and its localization in nuclear and perinuclear region of cells. Tmx-NLC exhibited distinctly different pharmacokinetic profile compared to Tamoxifen suspension (Tmx-susp) and exhibited an increment in the bioavailability by 2.71-fold and prolonged the T 1/2 by 7.10-fold. Moreover, detectable drug concentration in mesenteric lymph nodes justifies our hypothesis of targeting ILS and explains the major uptake of Tmx to occur via lymphatic system. [Copyright &y& Elsevier]

Abstract: The main objective of this study was to evaluate the potential of Quercetin-loaded nanostructured lipid carriers (QT-NLCs) as a topical delivery system. QT-NLCs were prepared by the method of emulsion evaporation–solidification at low temperature. The average entrapment efficiency and drug loading of the optimized QT-NLCs were 89.95±0.16% and 3.05±0.01%, respectively. Under the transmission electron microscope, the nanoparticles were spherically shaped. The average particle size was 215.2nm, the zeta potential was −20.10±1.22mV and pH value of QT-NLCs system was 4.65. Topical delivery of QT in the form of NLCs was investigated in vitro and in vivo. The results showed that QT-NLCs could promote the permeation of QT, increase the amount of QT retention in epidermis and dermis, and enhance the effect of anti-oxidation and anti-inflammation exerted by QT. Then the mechanism of NLCs for facilitating drug penetration was further investigated through histological sections. In conclusion, NLCs could be a promising vehicle for topical delivery of QT. [Copyright &y& Elsevier]

Abstract: Itraconazole-loaded NLC for pulmonary application were developed. In Precirol ATO 5 and oleic acid Itraconazole had the highest solubility. The solid lipid and the oil were mixable in a ratio 9:1 possessing a melting point above body temperature. 0.4% Itraconazole was dissolved in this lipid blend. Eumulgin SLM 20 was the stabilizer with the highest affinity to the lipid blend used as particle matrix. 2.5% Eumulgin SLM 20 was sufficient to obtain NLC with a narrow particle size distribution and sufficient stability. The tonicity of the formulation was adjusted with glycerol. Sterility was obtained by autoclaving. Neither the addition of glycerol nor autoclaving had an influence on the particle size and the zeta potential of Itraconazole-loaded NLC. SEM images showed spherical particles confirming the particle size measured by light scattering techniques. An entrapment efficiency of 98.78% was achieved. Burst release of Itraconazole from the developed carrier system was found. Itraconazole-loaded NLC possessed good storage stability. Nebulizing Itraconazole-loaded NLC with a jet stream and an ultrasonic nebulizer had no influence on the particle size and the entrapment efficiency of Itraconazole in the particle matrix, being a precondition for pulmonary application. [Copyright &y& Elsevier]

Abstract: The objective of the present study was to formulate and characterize Acitretin loaded Nanostructured Lipid Carriers (ActNLCs), to understand in vitro drug release and clinically evaluate the role of the developed gel in the topical treatment of psoriasis. ActNLCs were prepared by solvent diffusion technique using 32 full factorial design. The mean diameter and surface morphology of ActNLC was evaluated. ActNLCs were lyophilized and crystallinity of NLC was characterized by Differential Scanning Calorimtery (DSC) and powder X-Ray Diffraction (XRD). The NLCs were incorporated in 1% w/w Carbopol 934 P gel base and in vitro skin deposition studies in Human Cadaver Skin and double-blind clinical studies in psoriatic patients were conducted. The optimized ActNLCs were spherical in shape, with average particle size of 223(±8.92)nm, zeta potential of −26.4 (±0.86) mV and EE of 63.0(±1.54)%. DSC and XRD data confirmed the formation of NLCs. Significantly higher deposition of Acitretin was found in human cadaver skin from ActNLC gel (81.38 ±1.23%) as compared to Act plain gel (47.28±1.02%). Clinical studies demonstrated significant improvement in therapeutic response and reduction in local side effects with ActNLCs loaded gel indicated its effectiveness in the topical treatment of Psoriasis. [ABSTRACT FROM AUTHOR]