In situabsorption and relative bioavailability studies of zaleplon loaded self-nanoemulsifying powders

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.

Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability

“…Improvement in AVA bioavailability relies heavily upon the improvement in its aqueous solubility. One of the approaches applied to improve drug aqueous solubility is achieved through the utilization of self-nanoemulsifying drug delivery systems (SNEDDS) (4)(5)(6)(7)(8)(9). SNEDDS disperse in aqueous media as fine emulsion with globules in the nanosize range, so the drug remains in solution, consequently overcoming one of the main barriers for drug absorption, the dissolution step (10)(11)(12)(13)(14).…”

Self-microemulsifying drug delivery system (SMEDDS) – challenges and road ahead

“…can be filled into capsule shells. This prevents physical incompatibility of liquid SMEDDS with the capsule shell (Janga et al, 2012;Kallakunta et al, 2012). Tablets.…”

A Review of Novel Formulation Strategies to Enhance Oral Delivery of Zaleplon

“…Janga et al [17] formulated proliposomes for enhanced oral bioavailability of zaleplon and also investigated the role of surface charge on the enhancement of zaleplon bioavailability. Hydrogenated soyphosphatidylcholine and cholesterol in varying ratios were used to formulate the proliposomes, and the finalized formulation was tailored with dicetyl phosphate to obtain negative charge vesicles and stearylamine to attain positive charged vesicles, respectively.…”