Comparison of different zeolite framework types as carriers for the oral delivery of the poorly soluble drug indomethacin.

Abstract:

:Microporous zeolites of distinct framework types, textural properties and crystal morphologies namely BEA, ZSM and NaX, have been employed as carriers to assess their effect on modulating the dissolution behavior of a BCS II model drug (indomethacin). Preparation of the loaded carriers via the incipient wetness method induced significant drug amorphization for the BEA and NaX samples, as well as high drug payloads. The stability of the amorphous drug content was retained after stressing test evaluation of the porous carriers. The dissolution profile of loaded indomethacin was evaluated in simulated gastric fluid (pH 1.2) and simulated intestinal fluids FaSSIF (fasted) and FeSSIF (fed state) conditions and was found to be dependent on the aluminosilicate ratio of the zeolites and the degree of crystalline drug content. The feasibility of the zeolitic particles as oral drug delivery systems was appraised with cytocompatibility and cellular toxicity studies in Caco-2 cultures in a time- and dose-dependent manner by means of the MTT assay and flow cytometry analysis, respectively. Intracellular accumulation of the zeolite particles was observed with no apparent cytotoxic effects at the lower concentrations tested, rendering such microporous zeolites pertinent candidates in oral drug delivery applications.

journal_name

Int J Pharm

authors

Karavasili C,Amanatiadou EP,Kontogiannidou E,Eleftheriadis GK,Bouropoulos N,Pavlidou E,Kontopoulou I,Vizirianakis IS,Fatouros DG

doi

10.1016/j.ijpharm.2017.05.061

subject

Has Abstract

pub_date

2017-08-07 00:00:00

pages

76-87

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(17)30484-2

journal_volume

528

pub_type

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