Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, in vitro and in vivo Assessment

ObjectiveThe aim of this study was to investigate the in vitro and in vivo performance of self-nanoemulsifying drug delivery systems (SNEDDSs) of talinolol (TAL), a poorly water-soluble drug.MethodsSelf-nanoemulsifying drug delivery systems of TAL were prepared using various oils, non-ionic surfactants and/or water-soluble co-solvents and assessed visually/by droplet size measurement. Equilibrium solubility of TAL in the anhydrous and diluted SNEDDS was conducted to achieve the maximum drug loading. The in vitro dissolution experiments and human red blood cells (RBCs) toxicity test, ex vivo gut permeation studies, and bioavailability of SNEDDS in rats were studied to compare the representative formulations with marketed product Cordanum® 50 mg and raw drug.ResultsThe results from the characterization and solubility studies showed that SNEDDS formulations were stable with lower droplet sizes and higher TAL solubility. From the dissolution studies, it was found that the developed SNEDDS provided significantly higher rate of TAL release (>97% in 2.0 h) compared to raw TAL and marketed product Cordanum®. The RBC lysis test suggested negligible toxicity of the formulation to the cells. The ex vivo permeability assessment and in vivo pharmacokinetics study of a selected SNEDDS formulation (F6) showed about four-fold increase in permeability and 1.58-fold enhanced oral bioavailability of TAL in comparison to pure drug, respectively.ConclusionTalinolol loaded SNEDDS formulations could be a potential oral pharmaceutical product with high drug-loading capacity, improved drug dissolution, increased gut permeation, reduced/no human RBC toxicity, and enhanced oral bioavailability

Association of COPD with osteoporosis in male smokers: A case control study in a tertiary medical college hospital in Bangladesh

OBJECTIVES: Chronic obstructive pulmonary disease (COPD) may increase the risk of osteoporosis and resulting fractures can contribute to disability and mortality of patients. We intended to evaluate the frequency of osteoporosis in male smokers with and without COPD and study whether any correlation existed between osteoporosis and COPD. MATERIALS AND METHODS: This case-control study was carried out in the Department of Medicine, Sylhet M.A.G. Osmani Medical College Hospital, Sylhet, Bangladesh between July 2013 and June 2015. Seventy four male smokers with COPD and 66 age-matched male smokers without COPD were enrolled. All individuals underwent Bone Mass Densitometry (BMD) by Dual-Energy X-Ray Absorptiometry (DEXA). RESULTS: COPD and non-COPD groups did not differ regarding age and smoking pack-years. Osteoporosis at femoral neck (48.6% versus 16.7%; p< 0.001) and lumbar spine (68.9% versus 37.9%; p< 0.01) was significantly higher in COPD compared to controls. Osteopenia did not differ significantly. Patients with COPD were 4.5 times more likely to develop osteoporosis than controls after adjusting age, smoking-pack years and BMI (adjusted OR = 4.5; 95% CI = 1.8–11.5). CONCLUSIONS: Osteoporosis is more frequent in male smokers with COPD compared to smokers without COPD. COPD is a risk factor of osteoporosis independent of age, smoking and BMI