<?xml version="1.0" encoding="utf-8"?>
<export-example>
  <doc>
    <id>12464</id>
    <completedYear/>
    <publishedYear>2006</publishedYear>
    <thesisYearAccepted/>
    <language>eng</language>
    <pageFirst>82</pageFirst>
    <pageLast>89</pageLast>
    <pageNumber/>
    <edition/>
    <issue>1</issue>
    <volume>317</volume>
    <type>article</type>
    <publisherName>Elsevier</publisherName>
    <publisherPlace>Amsterdam</publisherPlace>
    <creatingCorporation/>
    <contributingCorporation/>
    <belongsToBibliography>1</belongsToBibliography>
    <completedDate>--</completedDate>
    <publishedDate>--</publishedDate>
    <thesisDateAccepted>--</thesisDateAccepted>
    <title language="eng">Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN®) versus drug nanocrystals</title>
    <abstract language="eng">For the development of an optimized oral formulation for cyclosporine A, 2% of this drug has been formulated in solid lipid nanoparticles (SLN, mean size 157 nm) and as nanocrystals (mean size 962 nm). The encapsulation rate of SLN was found to be 96.1%. Nanocrystals are composed of 100% of drug. For the assessment of the pharmacokinetic parameters the developed formulations have been administered via oral route to three young pigs. Comparison studies with a commercial Sandimmun Neoral/Optoral® used as reference have been performed. The blood profiles observed after oral administration of the commercial microemulsion Sandimmun® revealed a fast absorption of drug leading to the observation of a plasma peak above 1000 ng/ml within the first 2 h. For drug nanocrystals most of the blood concentrations were in the range between 30 and 70 ng/ml over a period of 14 h. These values were very low, showing huge differences between the measuring time points and between the tested animals. On the contrary, administration of cyclosporine-loaded SLN led to a mean plasma profile with almost similarly low variations in comparison to the reference microemulsion, however with no initial blood peak as observed with the Sandimmun Neoral/Optoral®. Comparing the area under the curves (AUC) obtained with the tested animals it could be stated that the SLN formulation avoids side effects by lacking blood concentrations higher than 1000 ng/ml. In this study it has been proved that using SLN as a drug carrier for oral administration of cyclosporine A a low variation in bioavailability of the drug and simultaneously avoiding the plasma peak typical of the first Sandimmun® formulation can be achieved.</abstract>
    <parentTitle language="eng">International journal of pharmaceutics</parentTitle>
    <identifier type="old">14189</identifier>
    <identifier type="doi">10.1016/j.ijpharm.2006.02.045</identifier>
    <identifier type="issn">0378-5173</identifier>
    <identifier type="issn">1873-3476</identifier>
    <enrichment key="bibliotheksstandort">Sonderstandort: Publica-Schrank</enrichment>
    <enrichment key="date_peer_review">22.06.2006</enrichment>
    <author>R.H. Müller</author>
    <author>S. Runge</author>
    <author>V. Ravelli</author>
    <author>W. Mehnert</author>
    <author>Andreas Thünemann</author>
    <author>E.B. Souto</author>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Solid lipid nanoparticles</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>SLN</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Drug nanocrystals</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Sandimmun Neoral/Optoral</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Oral administration</value>
    </subject>
    <collection role="literaturgattung" number="">Verlagsliteratur</collection>
    <collection role="fulltextaccess" number="">Physisches Exemplar in der Bibliothek der BAM vorhanden ("Hardcopy Access")</collection>
  </doc>
  <doc>
    <id>17534</id>
    <completedYear/>
    <publishedYear>2008</publishedYear>
    <thesisYearAccepted/>
    <language>eng</language>
    <pageFirst>535</pageFirst>
    <pageLast>544</pageLast>
    <pageNumber/>
    <edition/>
    <issue>3</issue>
    <volume>68</volume>
    <type>article</type>
    <publisherName>Elsevier</publisherName>
    <publisherPlace>Amsterdam</publisherPlace>
    <creatingCorporation>Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik</creatingCorporation>
    <contributingCorporation/>
    <belongsToBibliography>1</belongsToBibliography>
    <completedDate>--</completedDate>
    <publishedDate>--</publishedDate>
    <thesisDateAccepted>--</thesisDateAccepted>
    <title language="eng">Cyclosporine-loaded solid lipid nanoparticles (SLN): Drug-lipid physicochemical interactions and characterization of drug incorporation</title>
    <abstract language="eng">Solid lipid nanoparticles (SLN) were produced loaded with cyclosporine A in order to develop an improved oral formulation. In this study, the particles were characterized with regard to the structure of the lipid particle matrix, being a determining factor for mode of drug incorporation and drug release. Differential scanning calorimetry (DSC) and wide-angle X-ray scattering (WAXS) measurements were employed for the analysis of the polymorphic modifications and mode of drug incorporation. Particles were produced using Imwitor®900 as lipid matrix (the suspension consisted of 10% particles, 8% Imwitor®900, 2% cyclosporine A), 2.5% Tagat S, 0.5% sodium cholate and 87% water. DSC and WAXS were used to analyse bulk lipid, bulk drug, drug incorporated in the bulk and unloaded and drug-loaded SLN dispersions. The processing of the bulk lipid into nanoparticles was accompanied by a polymorphic transformation from the ß to the α-modification. After production, the drug-free SLN dispersions converted back to ß-modification, while the drug-loaded SLN stayed primarily in α-modification. After incorporation of cyclosporine A into SLN, the peptide lost its crystalline character. Based on WAXS data, it could be concluded that cyclosporine is molecularly dispersed in between the fatty acid chains of the liquid-crystalline α-modification fraction of the loaded SLN.</abstract>
    <parentTitle language="eng">European journal of pharmaceutics and biopharmaceutics</parentTitle>
    <identifier type="old">19601</identifier>
    <identifier type="doi">10.1016/j.ejpb.2007.07.006</identifier>
    <identifier type="issn">0939-6411</identifier>
    <identifier type="issn">1873-3441</identifier>
    <enrichment key="bibliotheksstandort">Sonderstandort: Publica-Schrank</enrichment>
    <enrichment key="date_peer_review">05.06.2008</enrichment>
    <author>R.H. Müller</author>
    <author>S.A. Runge</author>
    <author>V. Ravelli</author>
    <author>Andreas Thünemann</author>
    <author>W. Mehnert</author>
    <author>E.B. Souto</author>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Solid lipid nanoparticles</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Cyclosporine A</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Characterization</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Oral bioavailability</value>
    </subject>
    <subject>
      <language>eng</language>
      <type>uncontrolled</type>
      <value>Lipid polymorphism</value>
    </subject>
    <collection role="literaturgattung" number="">Verlagsliteratur</collection>
    <collection role="fulltextaccess" number="">Physisches Exemplar in der Bibliothek der BAM vorhanden ("Hardcopy Access")</collection>
  </doc>
</export-example>
