Development and Evaluation of Mucoadhesive Microcapsules of Rosiglitazone

Singh C., Agarwal K., Nema R.K. and Jain A. K.

Abstract: Mucoadhesive microcapsules of rosiglitazone were prepared using sodium alginate as a shell forming polymer and Carbapol 940, HPMC, Sodium CMC as mucoadhesive polymer for the potential use of treating acute and chronic diabetes mellitus (Type II diabetes). Large spherical microcapsules with a coat consisting of alginate and a mucoadhesive polymer could be prepared by orifice-ionic gelation process. The microcapsules exhibited good mucoadhesive properties in an in-vitro test. Rosiglitazone release from these mucoadhesive microcapsules was slow and extended over longer periods of time and depending on the composition of the coat. Drug release was diffusion controlled and followed zero-order kinetic.

Rosiglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycemic control by improving insulin sensitivity while reducing circulating insulin levels. Rosiglitazone is a highly selective and potent agonist for the peroxisome proliferator-activated receptor-gamma (PPARg). In humans, PPAR receptors are found in key target tissues for insulin action such as adipose tissue, skeletal muscle and liver. Activation of PPARg nuclear receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In addition, PPARg-responsive genes also participate in the regulation of fatty acid metabolism.
Microencapsulation has been accepted as a process to achieve controlled release and drug targeting. Mucoadhesion has been a topic of interest in the design of drug delivery system to prolong the residence time of the dosage form at the site of application or the absorption and to facilitate intimate contact dosage form with the underlying absorption surface to improve and enhance the bioavailability of drugs. Therefore control release (CR) products are needed for Rosiglitazone, to improve duration of action and patient compliance.
Material and methods
Rosiglitazone was supplied by Sun Pharma limited, India as a gift sample, sodium carboxy methylcellulose (sodium CMC) was kindly provided by Stadmed Private LTD. (Kolkata, India), Hydroxypropylmethylcellulose (HPMC) was a gift sample from Colorcon Asia PVT, LTD.(Verna, India). All other ingredients used were of analytical grade and used as provided. Spectrophotometeric studies carried out by using double beam UV spectrophotometer, Pharmaspac 1700, Shimadzu, Japan.
Preparation of mucoadhesive microcapsules
Microcapsules are prepared by orifice- ionic gelation method. Sodium alginate and mucoadhesive polymer are dissolved in purified water to form a homogenous polymer solution. The active substance, Rosiglitazone is added to polymer solution and mixed thoroughly with a stirrer to form a viscous dispersion with different polymer and different concentration (Table-1). The resulting dispersion is then added manually drop wise into CaCl2 (10% w/v) solution through a syringe with a needle of size no. 18. The added droplets are related in the CaCl2 solution for 15 min to complete the curing reactions and to produce spherical rigid microcapsule. The microcapsules are collected by decantation, and the product thus separated, washed repeatedly with water and dried at 45˚C for 12 hrs. 


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