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Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation


Active ingredients in pharmaceuticals differ by their physico-chemical properties and their bioavailability therefore varies. The most frequently used and most convenient way of administration of medicines is oral, however many drugs are little soluble in water. Thus they are not sufficiently effective and suitable for such administration. For this reason a system of lipid based formulations (LBF) was developed. Series of formulations were prepared and tested in water and biorelevant media. On the basis of selection criteria, there were selected formulations with the best emulsification potential, good dispersion in the environment and physical stability. Samples of structurally different drugs included in the Class II of the Biopharmaceutics classification system (BCS) were obtained, namely Griseofulvin, Glibenclamide, Carbamazepine, Haloperidol, Itraconazol, Triclosan, Praziquantel and Rifaximin, for testing of maximal saturation in formulations prepared from commercially available excipients. Methods were developed for preparation of formulations, observation of emulsification and its description, determination of maximum solubility of drug samples in the respective formulation and subsequent analysis. Saturation of formulations with drugs showed that formulations 80 % XA and 20 % Xh, 35 % XF and 65 % Xh were best able to dissolve the drugs which supports the hypothesis that it is desirable to identify limited series of formulations which could be generally applied for this purpose.

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Spinal Cord Injuries in Dogs Part II: Standards of Care, Prognosis and New Perspectives


Severe spinal cord injuries (SCI), causing physical handicaps and accompanied by many serious complications, remains one of the most challenging problems in both, human and veterinary health care practices. The central nervous system in mammals does not regenerate, so the neurological deficits in a dog following SCI persists for the rest of its life and the affected animals display an image of permanent suffering. Diagnostics are based on: neurological examination, plain x-rays of vertebral column, x-rays of the vertebral column following intrathecal administration of a water-soluble contrast medium (myelography), x-rays of the vertebral column following epidural administration of a contrast medium (epidurography), computed tomography (CT) and/or magnetic resonance imaging (MRI). Currently, only limited therapeutic measures are available for the dogs with SCIs. They include: the administration of methylprednisolone sodium succinate (MPSS) during the acute stage; early spinal cord decompression; stabilisation of vertebral fractures or luxations; prevention and treatment of complications, and expert rehabilitation. Together with the progress in the understanding of pathophysiologic events occurring after SCI, different therapeutic strategies have been instituted, including the local delivery of MPSS, the utilisation of novel pharmacological agents, hypothermia, and stem/precursor cell transplantation have all been tested in the experimental models and preclinical trials with promising results. The aim of this review is the presentation of the generally accepted methods of diagnostics and management of dogs with SCIs, as well as to discuss new therapeutic modalities. The research strategy involved a PubMed, Medline (Ovid), Embase (Ovid) and ISI Web of Science literature search from January 2001 to December 2017 using the term “spinal cord injury”, in the English language literature; also references from selected papers were scanned and relevant articles included.

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