Author(s): Tiziana M.G. Pecora, Teresa Musumeci, Lucrezia Musumeci, Massimo Fresta, Rosario Pignatello.
Background: Microencapsulation of natural antioxidants in polymeric systems represents a possible strategy for improving the oral bioavailability of compounds that are otherwise poorly soluble.
Objective: α-lipoic acid (ALA) was microencapsulated with polymethacrylate polymers (blends at various ratios of Eudragit® RS100 and RL100 resins).
Method: Microspheres were produced by solvent displacement of an ethanol cosolution of ALA and polymers; the microsuspensions were then freeze-dried, using trehalose as a cryoprotector. Microspheres were characterized in the solid state for micromeritic properties and drug loading, as well as by infrared spectroscopy, powder X-ray diffractometry and differential scanning calorimetry. The antioxidant activity of free and encapsulated ALA was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay.
Results: In vitro release studies, performed in simulated gastric (pH 1.2) and intestinal fluid (pH 6.8), showed that, depending on polymer composition and drug-to-polymer ratio, ALA release can be slowed down, compared to the dissolution pattern of the free drug. Solid-state characterization confirmed the chemical stability of ALA in the microspheres, suggesting that ALA did not develop strong interactions with the polymer and was present in an amorphous or a disordered-crystalline state within the polymer network. As indicated by the DPPH assay, the microencapsulation of ALA in Eudragit® Retard matrices did not alter its antioxidant activity.
Conclusion: ALA was effectively encapsulated in Eudragit® Retard matrices, showing a chemical stability up to 6 months at room conditions and at 40°C. Moreover, since the drug maintained its antioxidant activity in vitro, the potential application of these microparticulate systems for oral administration would deserve further studies.
Read more here: http://www.eurekaselect.com/135836/article
Current Pharmaceutical Design 22, Issue 46
Current Drug Targets 18, Issue 3
Current Topics in Medicinal Chemistry 17, Issue 8
Current Medicinal Chemistry 24, Issue 2
Letters in Drug Design & Discovery 14, Issue 3
Current Computer Aided-Drug Design 13, Issue 1
Current Organic Chemistry 21, Issue 6
Protein & Peptide Letters 24, Issue 3
Medicinal Chemistry 13, Issue 2
For every newcomer to the world, family and friends instantly begin to speculate who the baby will be like – mother or father! This speculation has proved unanswerable for the reason that one can never guess the outcome. Sometimes the children tend to inherit the father’s traits and sometimes the mother’s.
Recently researchers from University of Utah dug into the science behind inheriting genes and discovered that it is a rather complicated matter. It had been thought that newborn cells equally inherit traits from the genes of both the parents. Contrary to this idea, the cells show partiality at a very early stage of development, and tend to silence one gene providing dominance to the other. This may happen that later the silenced genes emerge as well but they remain recessive. Their study on mice and other specimen showed this phenomenon visibly. Especially the brain cells were found depicting this nature in abundance.
This study has the potential to find the roots of many inherited diseases that mar the lives of people and then their off-springs.
ARTICLE BY DISEASE ON “CARDIOLOGY”
Many clinically important differences exist between beta blockers. B1-selectivity is of clinical interest because at clinically used doses, b1- selective agents block cardiac b-receptors while having minor effects on bronchial and vascular b-receptors. Beta-adrenergic blocking agents significantly decrease the frequency and duration of angina pectoris, instead the prognostic benefit of beta-blockers in stable angina has been extrapolated from studies of post myocardial infarction but has not yet been documented without left ventricular disfunction or previous myocardial infarction. Organic nitrates are among the oldest drugs, but they still remain a widely used adjuvant in the treatment of symptomatic coronary artery disease. While their efficacy in relieving angina pectoris symptoms in acute settings and in preventing angina before physical or emotional stress is undisputed, the chronic use of nitrates has been associated with potentially important side effects such as tolerance and endothelial dysfunction. B-blockers are the firstline anti-anginal therapy in stable stable angina patients without contraindications, while nitrates are the secondline anti-anginal therapy. Despite 150 years of clinical practice, they remain fascinating drugs, which in a chronic setting still deserve investigation. This review evaluated pharmacotherapy and indications of Beta-blockers and nitrates in stable angina.
Read more: http://www.eurekaselect.com/node/127075/article
Mini-Reviews in Medicinal Chemistry 17, Issue 4
Cardiovascular & Hematological Agents in Medicinal Chemistry 14, Issue 2
Current Medical Imaging Reviews 13, Issue 1
Current Pharmaceutical Design 22, Issue 45
Current Psychiatry Reviews 12, Issue 4
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Current Hypertension Reviews 12, Issue 3
Adolescent Psychiatry 6, Issue 2
Current Drug Metabolism 18, Issue 1
Current HIV Research 15, Issue 1