In situ absorption and relative bioavailability studies of zaleplon loaded self-nanoemulsifying powders.
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.
Department of Pharmaceutics, St. Peter's Institute of Pharmaceutical Sciences, Hanamkonda, Warangal, Andhra Pradesh, India.
Karthik Y
KY
Janga
Raju
R
Jukanti
Sharath
S
Sunkavalli
Ashok
A
Velpula
Suresh
S
Bandari
Prabhakar
P
Kandadi
Prabhakar Reddy
PR
Veerareddy
D000081:Acetamides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000284:Administration, Oral; D017607:Aluminum Compounds; D000538:Aluminum Silicates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems; D004655:Emulsions; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D008274:Magnesium / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D017616:Magnesium Compounds; D008297:Male; D010316:Particle Size; D011743:Pyrimidines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D017640:Silicates
D000081:Acetamides; D017607:Aluminum Compounds; D000538:Aluminum Silicates; D000927:Anticonvulsants; D004655:Emulsions; D017616:Magnesium Compounds; D011743:Pyrimidines; D017640:Silicates; C033065:aluminum magnesium silicate; D008274:Magnesium; C085665:zaleplon