Preparation and characterization of nanocochelate by using phosphatidylcholine as lipid carrier for enhancement of permeability and bioavailability of rosuvastatin.

OBJECTIVE: Rosuvastatin (ROS) is a class of antihyperlipidemic agents belonging to the class of statins with poor permeability, which results in low oral bioavailability, i.e. 20%. The objective of the present study was to improve the permeability and bioavailability of ROS by developing nanocochelates using naturally biocompatible phosphatidylcholine, a type of lipid which is used as Ca2+ cations for the calcification process. SIGNIFICANCE: For the loaded ROS, the trapping method was used to build nanocochelates to boost the intestinal permeability of phosphatidylcholine and divalent choline is a calcium chloride cationic solution. METHODS: Nine different formulations have been produced and with varying lipid and cationic solution concentrations. The formulation of nanocochelates characterized by scanning electron microscopy, particle size, and zeta potential. Permeability studies have been conducted to determine the permeability improvement property of nanocochelates. The pharmacokinetic study was performed in Wistar albino rats to determine the bioavailability enhancement potential of nanocochlelates. RESULTS: The concentration of optimum lipid, calcium chloride was found to be 80 mg, 200 uL respectively which improve permeability by 3.44 times as compared to the marketed formulation. The in-vitro drug release over a prolonged period i.e.12 h. Which was substantially better than the traditional formulation of tablets. Nearly five fold enhancement in bioavailability was observed in case of optimized formulation as compared to the marketed formulation (p < 0.05). CONCLUSION: The findings suggest that the use of natural lipid carrier by nanocochelates of Rosuvastatin was promising drug delivery approach.

Bone density in pediatric Crohn's disease: A cross-sectional observation from South India.

BACKGROUND: Crohn's disease (CD) frequently manifests in the second and third decades of life. Malnutrition and corticosteroid therapy may affect bone mineralization and delay bone growth. Our aim was to study bone mineral density and factors associated low bone mineral density (BMD) in pediatric CD. METHODS: A cross-sectional observational study in children with CD (aged 5 to <18 years) was done. Demographic and treatment details were noted. Vitamin D levels <20 ng/mL were considered as deficiency. Bone mineral density was evaluated with dual-energy X-ray absorptiometry (DEXA) scan and Z score of <-2 SD was considered as low BMD. Data was analyzed descriptively. RESULTS: In 30 cases with CD enrolled over 1 year, mean age of the patients was 13.8±3.0 years. Age of onset and diagnosis was 11.4±3.2 years and 13.4±2.8 years, respectively. 73.3% were in the underweight category. All cases received azathioprine whereas 86.7% were receiving corticosteroids. Vitamin D deficiency was seen in 86.7% cases. A low BMD was evident in 70% children. Overall, low BMI (p=0.005) and vitamin D deficiency (p=0.005) were associated with low BMD. However, no association between severity grade of vitamin D deficiency and low BMD was found. Treatment with corticosteroid was associated with low BMD in 76.9% cases (p=0.069). CONCLUSION: Low BMD was frequent in children with CD and was associated with low BMI and vitamin D deficiency.