INTESTINAL ABSORPTION OF EPROSARTAN MESYLATE FROM SELF EMULSIFYING SYSTEM AND CYCLODEXTRIN COMPLEX
Authors: Quader Mohammed M. Abdol , Osman Mohamed A. , El Maghraby Gamal M. 
Published: February 2017

<p class="MsoNormal" style="margin-top: 6.0pt; margin-right: 0in; margin-bottom: 6.0pt; margin-left: 0in; text-align: justify; line-height: 97%;"><strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">Objective: </span></strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">The aim of this work was to determine the intestinal membrane transport parameters of eprosartan mesylate (EM) and to investigate self-nano emulsifying drug delivery systems (SNEDDS) and inclusion complexation with hydroxypropyl </span><span style="font-size: 8.0pt; line-height: 97%; font-family: Symbol;">b </span><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">cyclodextrin (HP</span><span style="font-size: 8.0pt; line-height: 97%; font-family: Symbol;">b</span><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">CD) for enhanced intestinal absorption of eprosartan mesylate. </span></p><p class="MsoNormal" style="margin-top: 6.0pt; margin-right: 0in; margin-bottom: 6.0pt; margin-left: 0in; text-align: justify; line-height: 97%;"><strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">Methods: </span></strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">The intestinal absorption was monitored using the in situ rabbit intestinal perfusion technique. SNEDDS was developed using labrafil, Lauroglycol with a tween in the presence of ethanol. Inclusion complexation was achieved by construction of phase solubility diagram in the presence of HP</span><span style="font-size: 8.0pt; line-height: 97%; font-family: Symbol;">b</span><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">CD. The prepared complex was evaluated using Fourier Transform Infrared Spectroscopy (FTIR) and differential scanning calorimetry (DSC). </span></p><p class="MsoNormal" style="margin-top: 6.0pt; margin-right: 0in; margin-bottom: 6.0pt; margin-left: 0in; text-align: justify; line-height: 97%;"><strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">Results: </span></strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">The drug was found to be poorly absorbed from the jejuno-ileum and the colon with the absorption being mainly through paracellular pathway. An inclusion complex was developed between the drug and HPβCD. Perfusion of the drug in the nanoemulsion formulation or as an inclusion complex resulted in a significant increase in the intestinal absorption of the drug compared with the control<strong>.</strong></span></p><p class="MsoNormal" style="margin-top: 6.0pt; margin-right: 0in; margin-bottom: 6.0pt; margin-left: 0in; text-align: justify; line-height: 97%;"><strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">Conclusion: </span></strong><span style="font-size: 8.0pt; line-height: 97%; font-family: 'Cambria','serif';">SNEDDS and inclusion complexation are promising strategies for enhanced intestinal absorption of eprosartan mesylate.</span></p><p><!--[if gte vml 1]><v:shapetype id="_x0000_t32" coordsize="21600,21600" o:spt="32"

o:oned="t" path="m,l21600,21600e" filled="f">

<v:path arrowok="t" fillok="f" o:connecttype="none"/>

<o:lock v:ext="edit" shapetype="t"/>

</v:shapetype><v:shape id="_x0000_s1026" type="#_x0000_t32" style='position:absolute;

margin-left:.55pt;margin-top:12.95pt;width:7in;height:0;z-index:251664384'

o:connectortype="straight" strokeweight="2.5pt">

<v:shadow color="#868686"/>

</v:shape><![endif]--><!--[if !vml]--><span style="mso-ignore: vglayout; position: absolute; z-index: 251664384; margin-left: -1px; margin-top: 15px; width: 676px; height: 4px;"><br /></span></p>