1.Nanoemulsions of thymol and eugenol co-emulsified by lauric arginate and lecithin.
Ma Q1, Davidson PM1, Zhong Q2. Food Chem. 2016 Sep 1;206:167-73. doi: 10.1016/j.foodchem.2016.03.065. Epub 2016 Mar 19.
Lauric arginate (LAE) is a cationic surfactant with excellent antimicrobial activities. To incorporate essential oil components (EOCs) in aqueous systems, properties of EOC nanoemulsions prepared with a LAE and lecithin mixture were studied. The LAE-lecithin mixture resulted in stable translucent nanoemulsions of thymol and eugenol with spherical droplets smaller than 100nm, contrasting with the turbid emulsions prepared with individual emulsifiers. Zeta-potential data suggested the formation of LAE-lecithin complexes probably through hydrophobic interaction. Negligible difference was observed for antimicrobial activities of nanoemulsions and LAE in tryptic soy broth. In 2% reduced fat milk, nanoemulsions showed similar antilisterial activities compared to free LAE in inhibiting Listeria monocytogenes, but was less effective against Escherichia coli O157:H7 than free LAE, which was correlated with the availability of LAE as observed in release kinetics.
2.Topical Ketoprofen Nanogel: Artificial Neural Network Optimization, Clustered Bootstrap Validation, and In Vivo Activity Evaluation Based on Longitudinal Dose Response Modeling.
Elkomy MH1, El Menshawe SF1, Eid HM1, Ali AM1,2. Drug Deliv. 2016 Apr 11:1-42. [Epub ahead of print]
OBJECTIVES: This work aimed at investigating the potential of solid lipid nanoparticles (SLN) as carriers for topical delivery of Ketoprofen (KP); evaluating a novel technique incorporating Artificial Neural Network (ANN) and clustered bootstrap for optimization of KP loaded SLN (KP-SLN); and demonstrating a longitudinal dose response (LDR) modeling-based approach to compare the activity of topical non-steroidal anti-inflammatory drug formulations.
3.Advantage of the Dissolution/Permeation System for Estimating Oral Absorption of Drug Candidates in the Drug Discovery Stage.
Miyaji Y1, Fujii Y1, Takeyama S1, Kawai Y1, Kataoka M2, Takahashi M1, Yamashita S2. Mol Pharm. 2016 Apr 13. [Epub ahead of print]
In order to increase the success rate in the development of oral drugs, an in vitro method, which can accurately estimate human oral absorption of a large variety of compounds from solid formulations, is required in the drug discovery stage. A dissolution/permeation (D/P) system is an in vitro system that simultaneously evaluates dissolution and permeation processes of drugs administered orally. In this study, we have investigated the advantages of a D/P system for use in the provisional estimation of human oral absorption of a drug (absorbed fraction, Fa) by applying it in its solid state. The D/P system mounted with a Madin-Darby canine kidney (MDCK) II cell monolayer was used to simultaneously evaluate the dissolved and the permeated amounts (% of dose) of 48 marketed drugs. Slightly modified, fasted-state simulated intestinal fluid (FaSSIFmod, 8 mL) was used as the apical medium of the D/P system. Each test drug was applied to the apical side of the D/P system as a suspension at one-hundredth of the clinical dose.
4.Formulation and evaluation of voriconazole ophthalmic solid lipid nanoparticles in situ gel.
Pandurangan DK1, Bodagala P1, Palanirajan VK2, Govindaraj S3. Int J Pharm Investig. 2016 Jan-Mar;6(1):56-62. doi: 10.4103/2230-973X.176488.
In the present investigation, solid lipid nanoparticles (SLNs)-loaded in situ gel with voriconazole drug was formulated. Further, the formulation was characterized for pH, gelling capacity, entrapment efficiency, in vitro drug release, drug content, and viscosity. Voriconazole is an antifungal drug used to treat various infections caused by yeast or other types of fungi. Film hydration technique was used to prepared SLNs from lecithin and cholesterol. Based on the entrapment efficiency 67.2-97.3% and drug release, the optimized formulation NF1 of SLNs was incorporated into in situ gels. The in situ gels were prepared using viscosity-enhancing polymers such as Carbopol and (hydroxypropyl)methyl cellulose (HPMC). Formulated SLN in situ gel formulations were characterized, which showed pH 4.9-7.1, drug content 65.69-96.3%, and viscosity (100 rpm) 120-620 cps. From the characterizations given above, F6 was optimized and evaluated for microbial assay and ocular irritation studies.
