Preparation and characterization of drug-loaded polymer-lipid hybrid nanoparticles with tunable surface hydrophobicity / 药学学报

The surface hydrophobicity of nanoparticles plays an important role in drug delivery process. The aim of this study was to verify the feasibility of using self-assembly method to prepare drug-loaded nanoparticles with tunable surface hydrophobicity. Here, Soluplus was selected as the polymeric carrier to prepare panobinostat (PNB) loaded micelles. Three different monoglycerides, glycerly monooleate (GMO), glycerly linoleate (GML) and glycerly linolenate (GMLO), were used to modify the surface of PNB-Soluplus micelles to prepare polymer-lipid hybrid nanoparticles (PLHNs). The effect of monoglyceride type and amount on the physico-chemical properties of PNB-loaded PLHNs was investigated, and the surface hydrophobicity of PLHNs was characterized by Rose Bengal (RB) binding method and mucin particle method. The results suggested that compared with the PNB-Soluplus micelles (particle size 77.97 ± 0.78 nm, zeta potential 0.44 ± 0.29 mV, entrapment efficiency 99.45% ± 1.47%, the RB binding constant (K) value 0.008 ± 0.002, the increased particle size after mixing with mucin particles 7.90 ± 1.41 nm), surface hydrophobicity of the PLHNs increased significantly when modified by GMO, GML, GMLO, with K values of 0.055 ± 0.010, 0.050 ± 0.011 and 0.058 ± 0.008, respectively. The increased particle sizes after mixing with mucin particles were 17.37 ± 4.48 nm, 22.60 ± 2.10 nm and 25.13 ± 3.89 nm, respectively. Among them, the physico-chemical properties of the GMLO modified PNB-loaded PLHNs (particle size 81.60 ± 4.52 nm, zeta potential 0.77 ± 0.03 mV, entrapment efficiency 99.59% ± 0.20%) kept constant, thus GMLO was selected to further investigate the effect of GMLO mass ratio (1%-3%) to Soluplus on the properties of the nanoparticles. While no statistical significant difference in particle size, zeta potential, entrapment efficiency or in vitro release behavior was found when GMLO ratio increased, the surface lipophilicity of the PLHNs, as characterized by K values and the increased particle sizes after mixing with mucin particles, increased almost linearly with the increase of GMLO amount. In conclusion, we demonstrated that drug-loaded PLHNs based on Soluplus and GMLO can be prepared by self-assembly method, and the surface hydrophobicity was tunable by modifying the mass ratio of GMLO to Soluplus. This approach could be used for related basic science research aiming to elucidate the effect of surface hydrophobicity on in vivo behavior of drug-loaded system.

Draft genome sequence of a caprolactam degrader bacterium: Pseudomonas taiwanensis strain SJ9

Abstract Pseudomonas taiwanensis strain SJ9 is a caprolactam degrader, isolated from industrial wastewater in South Korea and considered to have the potential for caprolactam bioremediation. The genome of this strain is approximately 6.2 Mb (G + C content, 61.75%) with 6,010 protein-coding sequences (CDS), of which 46% are assigned to recognized functional genes. This draft genome of strain SJ9 will provide insights into the genetic basis of its caprolactam-degradation ability.

Estudos sobre a toxicologia da ε - caprolactama: [revisão] / Studies on the toxicology of ε - caprolactam: [review]

A ε-caprolactama (CAP) é um monômero precursor de polímeros denominados nylon 6. Esses polímeros destinam-se à produção de tapetes, vestuário e materiais plásticos tais como equipamentos, sistemas e componentes automotivos, conectores, além de embalagens plásticas. Resíduos de CAP podem migrar de embalagens plásticas de nylon 6 para os alimentos. Diante disso, foi de interesse realizar uma revisão dos efeitos relativos à exposição à CAP e o seu impacto sobre a saúde humana. Estudos epidemiológicos indicam a possibilidade da CAP causar inflamações oculares e cutâneas, além de irritações no sistema respiratório. Pode ocorrer ainda hipotensão, taquicardia, palpitações, rinorréia, ressecamento nasal, efeitos geniturinários e sobre a reprodução como distúrbios nas funções menstrual e ovariana, e complicações no parto; além de problemas neurológicos e hematológicos. Estudos com animais são consistentes com tais relatos. Os estudos de genotoxicidade in vitro e in vivo por via oral e intraperitoneal mostram em sua grande maioria, resultados negativos, bem como ausência de efeitos carcinogênicos em ratos e camundongos e sobre o desenvolvimento e reprodução em ratos e coelhos.

ε -Caprolactam (CAP) is a precursor monomer of nylon 6 polymers. Nylon 6 is used in the manufacture of carpets, clothes and plastic materials, such as equipment, systems and automotive components, connectors and plastic packaging. CAP residues can migrate from nylon 6 plastic packaging to foods. Given this fact, this review was realized concerning the effects of CAP exposure and its impact on human health. Epidemiological studies indicate that CAP could cause ocular, cutaneous and respiratory irritations, as well as hypotension, tachycardia, palpitations, rhinorrhea, nose dryness, neurological and blood problems, and genitourinary and reproductive effects, such as alterations in ovarian-menstrual functions and pregnancy/birth complications. Animal studies are consistent with such reports; however, the majority of in vitro and in vivo genotoxicity studies by oral and intraperitoneal routes show negative results, including the absence of carcinogenicity in rats and mice and developmental and reproductive effects in rats and rabbits.

Two Cases of Convulsion Associated With Caprolactam / 대한산업의학회지

Two young men were seen with nausea, vomiting, dermatitis, seizure after two-four days of occupational exposure to caprolactam, a nylon fiber precursor. There were no significant results in laboratory test, brain CT, EEG except leukocytosis, hyperglycemia. Caprolactam has been shown to induce convulsive disorder in experimental animal studios and Tuma et al (1981) described that one worker acutely exposed to caprolactam developed generalized tonic-clonic seizure with leukocytosis. The coincidence of typical skin lesion with otherwise unexplained generalized tonic-clonic seizure in those young man strongly suggests that caprolactam was causal agent.