1 Ocak 2022 Dergi makalesi Açık Erişim

Oktay, Ayse Nur; Polli, James E.

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/261647</identifier>
  <creators>
    <creator>
      <creatorName>Oktay, Ayse Nur</creatorName>
      <givenName>Ayse Nur</givenName>
      <familyName>Oktay</familyName>
    </creator>
    <creator>
      <creatorName>Polli, James E.</creatorName>
      <givenName>James E.</givenName>
      <familyName>Polli</familyName>
      <affiliation>Univ Maryland, Dept Pharmaceut Sci, 20 Penn St, Baltimore, MD 21201 USA</affiliation>
    </creator>
  </creators>
  <titles>
    <title>Comparison Of A Single Pharmaceutical Surfactant Versus Intestinal Biorelevant Media For Etravirine Dissolution: Role And Impact Of Micelle Diffusivity</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2022</publicationYear>
  <dates>
    <date dateType="Issued">2022-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/261647</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1016/j.ijpharm.2022.122015</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://www.opendefinition.org/licenses/cc-by">Creative Commons Attribution</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">Etravirine is an antiviral whose oral absorption is limited by low solubility/dissolution. The objective was to predict and compare etravirine's surfactant-mediated dissolution into polyoxyethylene-10 lauryl ether (POE) and FeSSIF-V2, including the contribution of slow micelle diffusivity. Dynamic light scattering (DLS) was used to measure the size and diffusivity values of drug-loaded micelles. In vitro intrinsic dissolution into surfactant media were predicted using a model for surfactant-mediated dissolution. Compared to maleic buffer, POE and FeSSIF-V2 increased etravirine solubility 232-fold and 8.97-fold, respectively. From DLS, micelle diffusivity of drug-loaded POE micelle and FeSSIF-V2 mixed-micelle was 5.15x10(-7) cm(2)/s and 5.76x10(-8) cm(2)/s, respectively. Observed and predicted dissolution enhancement into POE were 50.7 and 31.3, and 1.26 and 1.24 into FeSSIF-V2, respectively. Hence, there was high dissolution enhancement into POE, although the observed enhancement was only 21.9% of the observed solubility enhancement, reflecting the attenuating impact of the large and slowly diffusing drug-loaded POE micelles. Meanwhile, there was minimal dissolution enhancement into FeSSIF-V2, and the observed enhancement was only 14.0% of the observed solubility enhancement, reflecting the even slower diffusing drug-loaded FeSSIF-V2 mixed-micelles compared to drug-loaded POE micelles. Results are considered in light of designing a single pharmaceutical surfactant system for dissolution that mimics a FeSSIF-V2 system.</description>
  </descriptions>
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