Influence of the preparation procedure and chitosan type on physicochemical properties and release behavior of alginate-chitosan microparticles.
BACKGROUND
The potential for use of chitosan-treated alginate microparticles as a vehicle for oral phenytoin delivery has not been thoroughly exploited.


OBJECTIVE
We studied the influence of preparation procedure and chitosan type on physicochemical properties and release behavior of alginate-chitosan microparticles.


METHODS
The total number of 24 microparticles formulations prepared by varying contents of calcium gelling ions and varying contents and type of chitosan was examined. As an additional variable, two different hardening times (1 and 24 hours) were employed. Possible interactions of components, surface morphology of microparticles as well as release profile of phenytoin were studied.


RESULTS
Both series of formulations with regard to hardening times, irrespective of the chitosan type and/or concentration employed appeared to be highly loaded with the model drug (above 90%). The drug release studies showed that the kinetics of phenytoin cannot be straightforwardly predicted based on the molecular weight of chitosan alone. On the other hand, prolonging the hardening time from 1 to 24 hours had significantly improved phenytoin kinetics, and gave rise to a formulation with the liberation half-time of about 2.5 hours.


CONCLUSIONS
This study showed that the latter formulation is eligible for further modifications aimed at improving the regularity of phenytoin absorption.
DCP Hemigal, Leskovac, Serbia.
Nebojsa D
ND
Cekić
Jela R
JR
Milić
Snezana D
SD
Savić
Miroslav M
MM
Savić
Zarko
Z
Jović
Rolf
R
Daniels
D000464:Alginates / Q000737:chemistry*; D000927:Anticonvulsants / Q000008:administration & dosage / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D005746:Gastric Emptying; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010316:Particle Size; D010672:Phenytoin / Q000008:administration & dosage / Q000493:pharmacokinetics
D000464:Alginates; D000927:Anticonvulsants; D005079:Excipients; D010672:Phenytoin; D048271:Chitosan