and full-text of published articles. The journal is devoted to the promotion of health sciences and related disciplines (including medicine, pharmacy, nursing, biotechnology, cell and molecular biology, and related engineering fields). It seeks particularly (but not exclusively) to encourage multidisciplinary research and collaboration among scientists, the industry and the healthcare professionals. It will also provide an international forum for the communication and evaluation of data, methods and findings in health sciences and related disciplines. The journal welcomes original research papers, reviews and case reports on current topics of special interest and relevance. All manuscripts will be subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication) will be published without delay. The maximum length of manuscripts should normally be 10,000 words (20 single-spaced typewritten pages) for review, 6,000 words for research articles, 3,000 for technical notes, case reports, commentaries and short communications.
Ordered mixtures consist of adhering fine particles of a hydrophobic drug to the surface of larger particles of a water soluble carrier substance (1). Carrier particles dissolve in the presence of water, whereby adherent particles of the pharmaceutical substance disperse throughout the liquid. This eliminates the inherent tendency of hydrophobic drug particles to collect into not-readily dissolvable and dispersible aggregate. Literature reveals that various water soluble excipients such as lactose, mannitol, sorbitol and sodium chloride have been extensively used in preparation of ordered mixtures (1-3).Gliclazide is 1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea with molecular mass of 323.41 (PubChem Database; http://pubchem. ncbi.nlm.nih.gov). Gliclazide is used for the treatment of type II non-insulin dependent The poorly water soluble antidiabetic drug gliclazide was selected to study the effect of excipients on dissolution rate enhancement. Ordered mixtures of micronized gliclazide with lactose, mannitol, sorbitol, maltitol and sodium chloride were prepared by manual shaking of glass vials containing the drug and excipient(s). Different water soluble excipients, addition of surfactant and superdisintegrant, drug concentration and carrier particle size influenced the dissolution rate of the drug. Dissolution rate studies of the prepared ordered mixtures revealed an increase in drug dissolution with all water soluble excipients. The order of dissolution rate improvement for gliclazide was mannitol > lactose > maltitol > sorbitol > sodium chloride. Composite granules of the particle size range 355-710 mm were superior in increasing the drug dissolution rate from ordered mixtures. Reducing the carrier particle size decreased the dissolution rate of the drug as well as the increase in drug concentration. Kinetic modeling of drug release data fitted best the Hixson--Crowell model, which indicates that all the ordered mixture formulations followed the cube root law fairly well.
The objectives of this investigation were to prepare microspheres of the anti-diabetic drug, metformin hydrochloride, using ethyl cellulose as the polymer and evaluate the encapsulation efficiency and release characteristics in vitro and in vivo; utilizing different microencapsulation techniques. Different proportions of polymer were used to obtain varying drug-polymer ratios. Physical properties, loading efficiency and dissolution rate were dependent on the method chosen for preparation and also on the drug-to-polymer ratio. The addition of surfactant during emulsification and petroleum ether in non-solvent addition process affected release of drug and also size distribution of microspheres. To investigate the type of mechanism that occurs, dissolution data were plotted according to different kinetic models. In vitro release studies show first order and Higuchi model release characteristics being exhibited. All the results were treated statistically to validate the findings. Significant differences in percentage yield, entrapment efficiency and sustaining capacity were seen with microspheres prepared by two different methods. In vivo studies in normal and hyperglycemic mice show faster glucose reduction with microspheres prepared by the evaporation method, whereas the release sustaining effect was more pronounced with microspheres prepared by the non-solvent addition method.
Utilization of osmotic pressure as a driving force for delivery of pharmaceutical agents in a controlled pattern for a prolonged period of time is a well-established fact. The concept of osmotic drug delivery was first introduced by Theeuwes (1). The simplest design of an osmotic drug delivery system consists of an osmotically active core surrounded by a semipermeable membrane, with one or more delivery orifices through which the drug is delivered in a controlled fashion. Various modifications of the basic design of osmotic pump have been reported (2) and reviewed (3,4).One such modification is the utilization of asymmetric membrane coating for osmotic drug delivery. The walls of an asymmetric membrane capsule are prepared by the phase inversion technique. As the name suggests, the membrane is asymmetric in nature, i.e., it has a relatively thin dense region supported on a thicker porous region (5). An asymmetric membrane capsule of cellulose acetate for osmotic delivery of flurbiprofen has been developed and influence of osmogents and solubilizing agent on in vitro drug release were evaluated. The capsule membrane was prepared by the phase inversion technique. To ensure the osmotic delivery of drug, two approaches were adopted: (i) the drug was encapsulated with osmogents like sodium chloride and mannitol to increase the osmotic pressure of the core, and (ii) the drug was encapsulated with sodium lauryl sulfate in the core of the formulation to increase the solubility and thus its osmotic pressure. Scanning electron microscopy of the membrane confirmed its porous, dense asymmetric nature. Dye test revealed in situ pore formation. The in vitro release study showed that as the proportion of osmogent and solubilizing agent was increased the release rate also increased. A good correlation was observed between the zero-order rate constant and the amount of the osmogent and solubilizing agent used.
Aim: The present study was expected to explore the molecular interaction of five oxidative stress (OS) associated target receptors with Alpha-Pinene and its antioxidant validation for the effective treatment of Parkinson’s disease (PD). Background: Oxidative stress (OS) via multitudinous cascades is considered to be the leading attribute to dopaminergic cell degeneration in PD. Furthermore, it is also well-linked to other mechanisms involved in the neurodegeneration process, like dysfunction of mitochondria, neuroinflammation and excitotoxicity due to NO. Objective: The present investigation was to establish a molecular association of OS-associated target receptors with the bioactive compound alpha-pinene and how this molecular interaction empowers the mitigation of PD. Material and Method: Five different molecular targets namely Peroxisome Proliferator-Activated Receptor- Gamma (PPARγ), Liver-X receptor beta (LXR- β), Human Monoamine Oxidase-B (MAO-B), Human Nuclear receptor related-1 protein (Nurr1) and Human Lipoprotein-associated phospholipase A2 (Lp-PLA2) were obtained from RCSB-PDB, which has some leading association in the inhibition of the OS-induced neurodegeneration. Molecular interactions were stuffed by the simulation molecular docking software. Antioxidant activity was validated by in-vitro models as per standardized procedures against 2,2- diphenyl-1- picrylhydrazyl (DPPH), 2,2'-azinobis-(3-ethylbenzothiazoline -6-sulfonic acid) (ABTS), Ferric ion (Fe3+), Hydroxyl (•OH), nitric oxide (•NO), Peroxynitrite (ONOO-) and Hypochlorous acid (HOCl). Result: Our results indicated that alpha-pinene can interact with all the five different target receptors at the active binding site of receptors. Alpha-pinene was found to show better interaction with MAO-B, Nurr1 and PPARγ with binding energy of -5.50, -4.52 and -5.25, respectively as compared to the native ligand. Furthermore, the interaction of alpha-pinene with LXR-β and Lp-PLA2 was also significant with binding energy of -5.6 and -5.12, respectively. It also capable of neutralizing all the different free radicals under consideration with significant IC50 values against HOCl and •NO. Conclusion: It might be concluded that alpha-pinene could act as a potential inhibitor and scavenger of OS which could act on the multiple target receptors under consideration.
The release of poorly water-soluble drug, flurbiprofen, through asymmetric membrane capsule of cellulose acetate containing different pore forming agents like glycerol, polyethylene glycol 400, and dibutyl phthalate, in presence of sodium lauryl sulfate was investigated. The asymmetric membrane was fabricated in the shape of capsule body and cap by phase inversion technique. The type of pore forming agent incorporated had a marked influence on the porosity of the asymmetric membrane. However flurbiprofen due to its poor solubility was unable to create enough osmotic pressure and hence less than 10% of drug was released from all the systems with out SLS. However when the study was conducted with SLS, a maximum release of 72% was observed from the capsule with 70% glycerol. The release rates were found to increase with the increase in the concentration of pore forming agent and the amount of SLS encapsulated.
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