Hollow microspheres for gastroretentive floating- pulsatile drug delivery: preparation and in vitro evaluation.

Abstract

PURPOSE:

A multiparticular floating-pulsatile drug delivery system was developed for time and site specific drug release of piroxicam. A blend of floating and pulsatile principles of drug delivery system would have the advantage that a drug can be released in the upper GI tract after a definite time period.

METHODS:

Hollow microspheres were prepared by the emulsion solvent diffusion method using Eudragit S as an enteric acrylic polymer with piroxicam at various polymer/drug ratios in a mixture of dichloromethane and ethanol. Developed formulations were evaluated for yield, encapsulation efficiency, particle size, shape, apparent density, buoyancy studies and dissolution studies.

RESULTS:

The obtained microballoons were spherical with no major surface irregularity and mean particle size ranging from 250 to 380 for different batches. Formulations show a slight amount of relaese ranging from 0.7 to 11% in acidic medium (SGF) with complete release of drug in simulated intestinal fluid (SIF) in less than 3 h. Encapsulation efficiency of different formulations varied from 90 to 98%. The optimum loading amount of drug in the particles was found to impart suitable floatable properties to the microballoons. With increasing polymer/drug ratio, buancy of the microballoons increases accompanied by simultaneous reduction of apparent particle density.

CONCLUSION:

A pulsatile release of piroxicam was demonstrated by a simple drug delivery system which could be useful in chronopharmacotherapy of rheumatoid arthritis.

• Authors: Maryam Maghsoodi, Elham Hemati, Bahram Qadermazi, Zahra Yari
• Journal: Advanced pharmaceutical bulletin (Adv Pharm Bull) Vol. 1 Issue 2 Pg. 55-61 ( 2011) ISSN: 2228-5881 [Print] Iran
• PMID: 24312757 (Publication Type: Journal Article)