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J Microencapsul. 2013;30(2):161-72. doi: 10.3109/02652048.2012.714408. Epub 2012 Aug 15.

In situ absorption and relative bioavailability studies of zaleplon loaded self-nanoemulsifying powders.

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1
Department of Pharmaceutics, St. Peter's Institute of Pharmaceutical Sciences, Hanamkonda, Warangal, Andhra Pradesh, India.

Abstract

Self-nanoemulsifying drug delivery systems (SNEDDSs) offer potential as suitable carriers for improved oral delivery of poorly soluble and low bioavailable drugs. To derive self-nanoemulsifying powders (SNEPs), the optimized Z-SNEDDS formulation was adsorbed onto different carriers and based on micromeritics the formulation loaded onto neusilin US2 (SNEP-N) was selected for further characterization. The solid-state characterization (scanning electron microscopy, differential scanning calorimetry and powder X-ray diffraction) studies unravel the transformation of native crystalline state to amorphous and/or molecular state. The higher predictive effective permeability coefficient and fraction absorbed in humans extrapolated from in situ single-pass intestinal absorption study data in rats provide an insight on the potential of SNEPs for augment in absorption across gastrointestinal barrier. Overall a 3.5-fold enhancement in the extent of absorption of zaleplon from SNEP-N formulation proves the feasibility of SNEPs formulation for improved oral delivery of zaleplon.

PMID:
22894164
DOI:
10.3109/02652048.2012.714408
[Indexed for MEDLINE]
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