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Intercalated theophylline-smectite hybrid for pH-mediated delivery

Trivedi, Vivek, Nandi, Uttom, Maniruzzaman, Mohammed, Coleman, Nichola (2018) Intercalated theophylline-smectite hybrid for pH-mediated delivery. Drug Delivery and Translational Research, 8 . pp. 1781-1789. ISSN 2190-393X. (doi:10.1007/s13346-018-0478-8)

Abstract

On the basis of their large specific surface areas, high adsorption and cation exchange capacities, swelling potential and low toxicity, natural smectite clays are attractive substrates for the gastric protection of neutral and cationic drugs. Theophylline is an amphoteric xanthine derivative that is widely used as a bronchodilator in the treatment of asthma and chronic obstructive pulmonary disease. This study considers the in vitro uptake and release characteristics of the binary theophylline-smectite system. The cationic form of theophylline was readily ion exchanged into smectite clay at pH 1.2 with a maximum uptake of 67 ± 2 mg g−1. Characterisation of the drug-clay hybrid system by powder X-ray diffraction analysis, Fourier transform infrared spectroscopy, differential scanning calorimetry and scanning electron microscopy confirmed that the theophylline had been exclusively intercalated into the clay system in an amorphous form. The drug remained bound within the clay under simulated gastric conditions at pH 1.2; and the prolonged release of approximately 40% of the drug was observed in simulated intestinal fluid at pH 6.8 and 7.4 within a 2-h timeframe. The incomplete reversibility of the intercalation process was attributed to chemisorption of the drug within the clay lattice. These findings indicate that smectite clay is a potentially suitable vehicle for the safe passage of theophylline into the duodenum. Protection from absorption in the stomach and subsequent prolonged release in the small intestine are advantageous in reducing fluctuations in serum concentration which may impact therapeutic effect and toxicity.

Item Type: Article
DOI/Identification number: 10.1007/s13346-018-0478-8
Uncontrolled keywords: Smectite, Montmorillonite, Theophylline, Intercalation, Drug release
Subjects: R Medicine > RS Pharmacy and materia medica
Divisions: Central Services > Universities at Medway
Faculties > Sciences > Medway School of Pharmacy
Depositing User: Vivek Trivedi
Date Deposited: 24 Apr 2019 10:08 UTC
Last Modified: 15 Jan 2020 12:31 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/73602 (The current URI for this page, for reference purposes)
Trivedi, Vivek: https://orcid.org/0000-0001-9304-9214
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