RESUMEN
Simvastatin (Sim) is a widely known drug in the treatment of hyperlipidemia, which has attracted so much attention in bone regeneration due to its potential osteoanabolic effect. However, repurposing of Sim in bone regeneration will require suitable delivery systems that can negate undesirable off-target/side effects. In this study, we have investigated a new lipid nanoparticle (NP) platform that was fabricated using a binary blend of emulsifying wax (Ewax) and glyceryl monooleate (GMO). Using the binary matrix materials, NPs loaded with Sim (0-500 µg/mL) were prepared and showed an average particle size of about 150 nm. NP size stability was dependent on Sim concentration loaded in NPs. The suitability of NPs prepared with the binary matrix materials in Sim delivery for potential application in bone regeneration was supported by biocompatibility in pre-osteoclastic and pre-osteoblastic cells. Additional data demonstrated that biofunctional Sim was released from NPs that facilitated differentiation of osteoblasts (cells that form bones) while inhibiting differentiation of osteoclasts (cells that resorb bones). The overall work demonstrated the preparation of NPs from Ewax/GMO blends and characterization to ascertain potential suitability in Sim delivery for bone regeneration. Additional studies on osteoblast and osteoclast functions are warranted to fully evaluate the efficacy of Sim-loaded Ewax/GMO NPs using in-vitro and in-vivo approaches.
Asunto(s)
Regeneración Ósea/efectos de los fármacos , Sistemas de Liberación de Medicamentos/métodos , Emulsionantes/síntesis química , Glicéridos/síntesis química , Nanopartículas/química , Simvastatina/síntesis química , Animales , Regeneración Ósea/fisiología , Evaluación Preclínica de Medicamentos/métodos , Reposicionamiento de Medicamentos/métodos , Emulsionantes/administración & dosificación , Glicéridos/administración & dosificación , Ratones , Nanopartículas/administración & dosificación , Osteoblastos/efectos de los fármacos , Osteoblastos/fisiología , Células RAW 264.7 , Simvastatina/administración & dosificación , Ceras/síntesis química , Ceras/farmacologíaRESUMEN
A simple method for incorporating amine groups in hydrogenated castor oil (HCO) to produce wax for beeswax or carnauba wax substitution in packaging and coating was developed. From the conversion rate of the products, HCO was reacted with ethanolamine at 150°C for 5 h, and the molar ratio of HCO and ethanolamine was 1:4. The hardness of the final product was seven times higher than that of beeswax, the cohesiveness of the final product was 1.3 times higher than that of beeswax and approximately one half of that of carnauba wax, and the melting point of the final product is 98°C. The Fourier transform Infrared spectroscopy showed that the amide groups were incorporated to form the amide products. In coating application, the results showed that the force of the final product coating cardboard was higher than that of beeswax and paraffin wax and less than that of carnauba wax. After 24 h soaking, the compression forces were decreased. HCO fatty acid wax can be an alternative wax for carnauba wax and beeswax in coating applications.
Asunto(s)
Amidas/síntesis química , Aceite de Ricino/análogos & derivados , Fenómenos Químicos , Técnicas de Química Sintética/métodos , Etanolamina/química , Ceras/síntesis química , Aceite de Ricino/química , Calor , Hidrogenación , Espectroscopía Infrarroja por Transformada de Fourier , Factores de TiempoRESUMEN
Condensation product of fatty acids and fatty alcohols is termed as wax esters. A series of fatty acids and fatty alcohols both saturated & unsaturated ranging from C 12 to C 22 were synthesised using p-TSA as a catalyst. Carbonyl functionality was confirmed by infrared spectrophotometer. Wax esters were used as friction modifier additives at 1%, 3%, 5% in 150N and 500N commercial petroleum base stocks. These base stocks were characterized by tribological properties like wear scar, weld load and coefficient of friction. All the tribological properties were better for saturated products than the unsaturated ones.
Asunto(s)
Ésteres/química , Fricción , Petróleo , Ceras/química , Ésteres/síntesis química , Ceras/síntesis químicaRESUMEN
Cetyl myristoleate (CM) was reported by Diehl and May [J Pharm Sci 83 (1994) 296] to block inflammation and prevent adjuvant-induced arthritis in rats. To verify this earlier work, we have synthesized pure CM and tested its anti-arthritic properties in a collagen-induced arthritis model in DBA/1LacJ mice. Multiple intraperitoneal injections of CM in 450 and 900 mg kg(-1) doses resulted in a significantly lower incidence of disease and caused a modest but significant diminution in clinical signs in those mice that developed arthritis. CM administered in daily oral doses of 20 mg kg(-1) also reduced the incidence of arthritis and caused a small reduction in the clinical signs in mice that developed arthritis. Although the protective effect of CM in collagen-induced arthritis observed in the present study was less dramatic than that reported earlier, our results confirm the anti-arthritic properties of pure CM.
Asunto(s)
Artritis Experimental/tratamiento farmacológico , Modelos Animales de Enfermedad , Ceras/síntesis química , Ceras/uso terapéutico , Animales , Artritis Experimental/patología , Evaluación Preclínica de Medicamentos/métodos , Femenino , Ratones , Ratones Endogámicos DBARESUMEN
Cetyl myristoleate was isolated from National Institutes of Health, general purpose, Swiss albino mice that were immune to the polyarthritis induced in rats with Freund's adjuvant. This substance, or material synthesized from cetyl alcohol and myristoleic acid, afforded good protection against adjuvant-induced arthritic states in rats. In limited comparisons, cetyl oleate, also found in Swiss albino mice, gave lesser protection, whereas cetyl myristate and cetyl elaidate, the trans-isomer of cetyl oleate, appeared to be virtually ineffective. Dosage of the protective compound as well as the site of injection of Freund's adjuvant was important.