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Formulation and statistical optimization of a novel crosslinked polymeric anti-tuberculosis drug delivery system
Lisa Claire du Toit1, Viness Pillay, Michael Paul Danckwerts
1Department of Pharmacy and Pharmacology, University of the Witwatersrand, 7 York Road, Parktown 2193, South Africa.
Journal of Pharmaceutical Sciences
|September 21, 2007
Summary
This study developed a novel multiparticulate system for tuberculosis treatment, improving drug delivery and bioavailability. The optimized formulation ensures segregated gastrointestinal delivery of rifampicin and isoniazid.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Tuberculosis treatment faces challenges with co-administered drugs like rifampicin (RIF) and isoniazid (INH), impacting RIF bioavailability.
- Developing advanced drug delivery systems is crucial for enhancing therapeutic efficacy and patient compliance.
Purpose of the Study:
- To formulate a reconstitutable multiparticulate anti-tuberculosis drug delivery system for segregated gastrointestinal delivery of RIF and INH.
- To optimize enterosphere formulation using response surface methodology for improved drug entrapment and controlled release.
Main Methods:
- Ionotropically crosslinked polymeric enterospheres were developed for isoniazid (INH) delivery.
- A 3(4) Box-Behnken statistical design optimized formulation variables like electrolyte concentration, reaction time, drying temperature, and plasticizer concentration.
- Drug entrapment efficiency (DEE) and mean dissolution time (MDT) were evaluated using complexometric and UV spectrophotometric methods.
Main Results:
- Optimized enterospheres demonstrated high drug entrapment efficiency (up to 99.77%) and controlled drug release.
- Zinc sulfate concentration and plasticizer significantly impacted DEE and MDT.
- High drying temperatures (>42.5°C) improved DEE, and a dry dispersible system incorporating RIF and INH was successfully developed.
Conclusions:
- The developed multiparticulate system facilitates segregated gastrointestinal delivery of RIF and INH, addressing bioavailability issues.
- The formulation and optimization approach using response surface methodology proved effective for creating advanced anti-tuberculosis drug delivery systems.
- This system offers a promising strategy for enhanced tuberculosis treatment through improved drug administration and efficacy.
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