Preparation and Characterization of Theophylline-Chitosan Beads as an  Aapproach to Colon Delivery

Mohammad Reza Avadi; Amir Hossein Ghassemi; Assal Mir Mohammad Sadeghi; Mohammad Erfan; Azim Akbarzadeh; Hamid Reza Moghimi; Morteza Rafiee-Tehrani

doi:10.22037/ijpr.2010.579

IJ Pharmaceutical Research

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https://doi.org/10.22037/ijpr.2010.579

Preparation and Characterization of Theophylline-Chitosan Beads as an Aapproach to Colon Delivery

Author(s):

Mohammad Reza Avadi^{1, 2},

Amir Hossein Ghassemi³,

Assal Mir Mohammad Sadeghi²,

Mohammad Erfan¹,

Azim Akbarzadeh⁴,

Hamid Reza Moghimi⁵,

Morteza Rafiee-Tehrani^3,*

1School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services, Tehran, Iran

2Hakim Pharmaceutical Company, Tehran, Iran

3School of Pharmacy, Tehran University of Medical Sciences and Health Services, Tehran, Iran

4Pasteur Institute of Iran, Tehran, Iran

5School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services, Tehran, Iran. bHakim Pharmaceutical Company, Tehran, Iran

IJ Pharmaceutical Research:Vol. 3, issue 2; 73-80

Published online:Nov 20, 2010

Article type:Research Article

Received:Mar 01, 2004

Accepted:Jun 01, 2004

How to Cite:Mohammad Reza AvadiAmir Hossein GhassemiAssal Mir Mohammad SadeghiMohammad ErfanAzim AkbarzadehHamid Reza MoghimiMorteza Rafiee-Tehraniet al.Preparation and Characterization of Theophylline-Chitosan Beads as an Aapproach to Colon Delivery.Iran J Pharm Res.3(2):e128185.https://doi.org/10.22037/ijpr.2010.579.

Abstract

Chitosan with excellent biodegradable and biocompatible characteristics has received attention as an oral drug delivery vehicle for controlled-release formulations. In this study an enteric-coated capsule containing theophylline-chitosan beads based on 2³ factorial designs was prepared as a colon drug delivery system. The theophylline-chitosan gel beads were formulated by adding the drug-containing solution of chitosan into tripolyphosphate solutions, dropwise. The obtained beads were washed with water and freeze-dried before filling into the capsules. Eudragit^® S100 was then used to enteric-coat the prepared capsules. Drug entrapment efficiency and the effects of different variables including: bead morphology, swelling behavior of the beads and the release behavior of the system on these parameters were investigated. Results showed that the highest and lowest swelling ratio is obtained at pH 4.5 and 7.2, respectively. These studies have shown that chitosan concentration and drug polymer weight ratio significantly affect the drug entrapment. Decreasing the drug solubility in external phase caused a significant increase in drug loading. External phase saturation with theophylline and tripolyphosphate, as well as decreasing temperature, have increased drug loading. Furthermore, the lowering of temperature had a significant effect on bead's hardness. The release of theophylline from freeze-dried beads filled in enteric-coated capsules was also investigated. Release of theophylline was prolonged with saturation of both drug and tripolyphosphate in the external phase. Results showed that the release of theophylline from chitosan beads is possibly due to more than one mechanism, possibly dissolution, diffusion and relaxation of the polymer chains.

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Author(s):

Mohammad Reza Avadi:[PubMed][Scholar]
Amir Hossein Ghassemi:[PubMed][Scholar]
Assal Mir Mohammad Sadeghi:[PubMed][Scholar]
Mohammad Erfan:[PubMed][Scholar]
Azim Akbarzadeh:[PubMed][Scholar]
Hamid Reza Moghimi:[PubMed][Scholar]
Morteza Rafiee-Tehrani:[PubMed][Scholar]