Preparation and characterization of azathioprine microspheres for colon specific delivery

Abstract

The objective of the present study is to develop colon targeted drug delivery system using dextrin (polysaccharide) as a carrier for Azathioprine. Microspheres containing azathioprine, dextrin and various excipients were prepared by solvent evaporation technique. The prepared microsphere were evaluated by different methods parameters like particle size, drug entrapment efficiency, percentage yield, shape and surface morphology and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric, intestinal fluid and simulated colonic fluid. In dextrin based microspheres, dextrin as a carrier was found to be suitable for targeting of Azathioprine for local action in the site of colon. Dextrin microspheres released 95-99% of azathioprine in simulated colonic fluid with 4% human fecal matter solution. The results of in-vitro studies of the azathioprine microspheres indicate that for colon targeting dextrin are suitable carriers to deliver the drug specifically in the colonic region. Dextrin based azathoprine microspheres showed no significance change in particle size and % residual upon storage at 5 ± 3ºC, 25 ± 2ºC/60 ± 5% RH (room temperature) and 40 ± 2ºC/75 ±5%RH humidity for three months.
 Keywords: azathioprine, microsphere, dextrin, colon specific drug delivery.

Coating Processes of Pharmaceutical Applicability: A Glimpse

“…The chemical deposition processes is either gas-phase deposition processes or vapourphase deposition processes 4,16 . Thermo-mechanical deposition process realises embedding & layering of CoM particles thru strong mechanical force and/or impaction force accompanied by generated heat 3,[12][13][14] .…”

“…These comprises group of processes that realises coating thru use of impaction force and/or thermal energy or by application of ambient shearing stress 3,6,12,16 . Herein applied ambient mechanical/ impaction force accompanied with generated heat realises embedding and layering of CMPs onto substrate surface 3,13,14 . In some exempla, coating of substrates realises thru deformation of CoM along with embedding of them onto substrate surface 1,3 .…”

“…Later on issues/ concerns like regulatory concern, residual VOS, environmental safety & concerns, safety of operator, and cost had been providing momentum for springing-up, improving, and perfecting aqueous film-coating, as preferred alternative 5,6,[8][9][10][11][12] . Aqueous film-coating processes are in most instances are aqueous dispersions based systems 5,13 . Said dispersion comprises low level of film former & large quantity of water 5,14 .…”

“…Said dispersion comprises low level of film former & large quantity of water 5,14 . They are thus energy and time consuming reasoning from evaporating large quantity of water 5,[13][14][15] .…”

Advances in Polysaccharide-Based Oral Colon-Targeted Delivery Systems: The Journey So Far and the Road Ahead

“…Dextrin acts as a carrier that prevents the drug release in the upper GIT and releases more amount of the drug specifically in the colon. The in-vitro dissolution study revealed that 95-99% of azathioprine was released in the colonic fluid and produced local action [ 57 ].…”